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Current Insights on Lipid-Based Nanosystems 2023
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Current Insights on Lipid-Based Nanosystems 2023

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (31 July 2023) | Viewed by 30602

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Prof. Dr. Ana Catarina Silva

E-Mail Website
Guest Editor
1. UCIBIO, REQUIMTE, Laboratory of Pharmaceutical Technology/Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
2. Associate Laboratory i4HB - Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
3. FP-I3ID (Instituto de Investigação, Inovação e Desenvolvimento), FP-BHS (Biomedical and Health Sciences Research Unit), Faculty of Health Sciences, University Fernando Pessoa, 4249-004 Porto, Portugal
Interests: nasal and cutaneous drug delivery; nose-to-brain delivery; lipid nanoparticles; biopharmaceuticals; biological medicines; advanced therapy medicinal products (ATMPs)
Special Issues, Collections and Topics in MDPI journals
Dr. João Nuno Moreira

E-Mail Website
Guest Editor
1. CNC—Center for Neurosciences and Cell Biology, Center for Innovative Biomedicine and Biotechnology (CIBB), Faculty of Medicine (Polo 1), University of Coimbra, Rua Larga, 3004-504 Coimbra, Portugal
2. Pólo das Ciências da Saúde, Faculty of Pharmacy, CIBB, Univ. Coimbra—University of Coimbra, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal
Interests: cancer; liposomes; drug targeting; translational research
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. José Manuel Sousa Lobo

E-Mail Website1 Website2
Guest Editor
UCIBIO, REQUIMTE, Laboratory of Pharmaceutical Technology, Centre of Research in Pharmaceutical Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal
Interests: pharmaceutical technology; biopharmacy; pharmacokinetics; pharmaceutical nanotechnology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues, 

Lipid-based nanosystems, including solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), cationic lipid nanoparticles, nanoemulsions, and liposomes, have been extensively studied to improve drug delivery through different administration routes. The main advantages linked to these systems are the ability to protect, transport, and control the release of lipophilic and hydrophilic molecules (either small molecular weight or macromolecules), the use of generally recognized as safe (GRAS) excipients that minimize the toxicity of the formulations, and the possibility to modulate pharmacokinetics and enable site-specific delivery of encapsulated payloads. In addition, the versatility of lipid-based nanosystems has been further demonstrated through the delivery of vaccines, protection of cosmetic actives, or improvement of moisturizing properties of cosmetic formulations. 

Currently, lipid-based nanosystems are well established, and there are already different commercially approved formulations for different human disorders. This success has actually paved the way to diversifying the pipeline of development, upon addressing unmet medical needs for several indications, such as cancer, neurological disorders, and autoimmune, genetic, and infectious diseases. 

This Special Issue aims to update readers on the latest research on lipid-based nanosystems, both at the preclinical and clinical levels. Submissions of original unpublished research work and review manuscripts are welcome.

Dr. Ana Catarina Silva
Dr. João Nuno Moreira
Prof. Dr. José Manuel Sousa Lobo
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • solid lipid nanoparticles
  • nanostructured lipid carriers
  • cationic lipid nanoparticles
  • liposomes
  • nanoemulsions

Published Papers (17 papers)

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Editorial

Jump to: Research, Review

4 pages, 226 KiB  
Editorial
Current Insights on Lipid-Based Nanosystems 2023
by Ana Catarina Silva, João Nuno Moreira and José Manuel Sousa Lobo
Pharmaceuticals 2023, 16(12), 1700; https://doi.org/10.3390/ph16121700 - 08 Dec 2023
Viewed by 702
Abstract
Among the different types of nanosystems that have been investigated for therapeutic use, lipid-based ones are the most explored, as they have advantages over non-lipid nanosystems, especially for improving the transport and efficacy of drugs through different routes of administration, such as ocular, [...] Read more.
Among the different types of nanosystems that have been investigated for therapeutic use, lipid-based ones are the most explored, as they have advantages over non-lipid nanosystems, especially for improving the transport and efficacy of drugs through different routes of administration, such as ocular, cutaneous, intranasal, and intravenous [...] Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)

Research

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14 pages, 3038 KiB  
Article
Development of Gefitinib-Loaded Solid Lipid Nanoparticles for the Treatment of Breast Cancer: Physicochemical Evaluation, Stability, and Anticancer Activity in Breast Cancer (MCF-7) Cells
by Ibrahim A. Aljuffali, Md. Khalid Anwer, Mohammed Muqtader Ahmed, Ahmed Alalaiwe, Mohammed F. Aldawsari, Farhat Fatima and Shahid Jamil
Pharmaceuticals 2023, 16(11), 1549; https://doi.org/10.3390/ph16111549 - 02 Nov 2023
Cited by 2 | Viewed by 1056
Abstract
In the current study, the toxic effects of gefitinib-loaded solid lipid nanoparticles (GFT-loaded SLNs) upon human breast cancer cell lines (MCF-7) were investigated. GFT-loaded SLNs were prepared through a single emulsification–evaporation technique using glyceryl tristearate (Dynasan™ 114) along with lipoid® 90H (lipid [...] Read more.
In the current study, the toxic effects of gefitinib-loaded solid lipid nanoparticles (GFT-loaded SLNs) upon human breast cancer cell lines (MCF-7) were investigated. GFT-loaded SLNs were prepared through a single emulsification–evaporation technique using glyceryl tristearate (Dynasan™ 114) along with lipoid® 90H (lipid surfactant) and Kolliphore® 188 (water-soluble surfactant). Four formulae were developed by varying the weight of the lipoid™ 90H (100–250 mg), and the GFT-loaded SLN (F4) formulation was optimized in terms of particle size (472 ± 7.5 nm), PDI (0.249), ZP (−15.2 ± 2.3), and EE (83.18 ± 4.7%). The optimized formulation was further subjected for in vitro release, stability studies, and MTT assay against MCF-7 cell lines. GFT from SLNs exhibited sustained release of the drug for 48 h, and release kinetics followed the Korsmeyer–Peppas model, which indicates the mechanism of drug release by swelling and/or erosion from a lipid matrix. When pure GFT and GFT–SLNs were exposed to MCF-7 cells, the activities of p53 (3.4 and 3.7 times), caspase-3 (5.61 and 7.7 times), and caspase-9 (1.48 and 1.69 times) were enhanced, respectively, over those in control cells. The results suggest that GFT-loaded SLNs (F4) may represent a promising therapeutic alternative for breast cancer. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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16 pages, 2888 KiB  
Article
Pharmacokinetics and Anti-Tumor Efficacy of PEGylated Liposomes Co-Loaded with Cisplatin and Mifepristone
by Karen Ocaña-Arakachi, Julio Martínez-Herculano, Rafael Jurado, Monserrat Llaguno-Munive and Patricia Garcia-Lopez
Pharmaceuticals 2023, 16(10), 1337; https://doi.org/10.3390/ph16101337 - 22 Sep 2023
Cited by 2 | Viewed by 943
Abstract
Although cisplatin is an effective chemotherapy drug used against many types of cancer, it has poor bioavailability, produces severe adverse effects, and frequently leads to tumor resistance. Consequently, more effective formulations are needed. The co-administration of cisplatin with mifepristone, which counters an efflux [...] Read more.
Although cisplatin is an effective chemotherapy drug used against many types of cancer, it has poor bioavailability, produces severe adverse effects, and frequently leads to tumor resistance. Consequently, more effective formulations are needed. The co-administration of cisplatin with mifepristone, which counters an efflux pump drug-resistance mechanism in tumor cells, has shown important synergism, but without resolving the problem of poor bioavailability. Specificity to tumor tissue and bioavailability have been improved by co-encapsulating cisplatin and mifepristone in a liposomal formulation (L-Cis/MF), which needs further research to complete pre-clinical requirements. The aim of this current contribution was to conduct a pharmacokinetic study of cisplatin and mifepristone in male Wistar rats after administration of L-Cis/MF and the conventional (unencapsulated) formulation. Additionally, the capacity of L-Cis/MF to reduce tumor growth in male nude mice was evaluated following the implantation of xenografts of non-small-cell lung cancer. The better pharmacokinetics (higher plasma concentration) of cisplatin and mifepristone when injected in the liposomal versus the conventional formulation correlated with greater efficacy in controlling tumor growth. Future research on L-Cis/MF will characterize its molecular mechanisms and apply it to other types of cancer affected by the synergism of cisplatin and mifepristone. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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14 pages, 3781 KiB  
Article
Enhanced Antidepressant Activity of Nanostructured Lipid Carriers Containing Levosulpiride in Behavioral Despair Tests in Mice
by Sadia Tabassam Arif, Muhammad Ayub Khan, Shahiq uz Zaman, Hafiz Shoaib Sarwar, Abida Raza, Muhammad Sarfraz, Yousef A. Bin Jardan, Muhammad Umair Amin and Muhammad Farhan Sohail
Pharmaceuticals 2023, 16(9), 1220; https://doi.org/10.3390/ph16091220 - 29 Aug 2023
Viewed by 891
Abstract
The potential of levosulpiride-loaded nanostructured lipid carriers (LSP-NLCs) for enhanced antidepressant and anxiolytic effects was evaluated in the current study. A forced swim test (FST) and tail suspension test (TST) were carried out to determine the antidepressant effect whereas anxiolytic activity was investigated [...] Read more.
The potential of levosulpiride-loaded nanostructured lipid carriers (LSP-NLCs) for enhanced antidepressant and anxiolytic effects was evaluated in the current study. A forced swim test (FST) and tail suspension test (TST) were carried out to determine the antidepressant effect whereas anxiolytic activity was investigated using light–dark box and open field tests. Behavioral changes were evaluated in lipopolysaccharide-induced depressed animals. The access of LSP to the brain to produce therapeutic effects was estimated qualitatively by using fluorescently labeled LSP-NLCs. The distribution of LSP-NLCs was analyzed using ex vivo imaging of major organs after oral and intraperitoneal administration. Acute toxicity studies were carried out to assess the safety of LSP-NLCs in vivo. An improved antidepressant effect of LSP-NLCs on LPS-induced depression showed an increase in swimming time (237 ± 51 s) and struggling time (226 ± 15 s) with a reduction in floating (123 ± 51 s) and immobility time (134 ± 15 s) in FST and TST. The anxiolytic activity in the light–dark box and open field tests exhibited superiority over LSP dispersion. Near-infrared images of fluorescently labeled LSP-NLCs demonstrated the presence of coumarin dye in the brain after 1 h of administration. An acute toxicity study revealed no significant changes in organ-to-body weight ratio, serum biochemistry or tissue histology of major organs. It can be concluded that nanostructured lipid carriers can efficiently deliver LSP to the brain for improved therapeutic efficacy. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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14 pages, 2599 KiB  
Article
Formulation and Evaluation of Plumbagin-Loaded Niosomes for an Antidiabetic Study: Optimization and In Vitro Evaluation
by Rama Tyagi, Ayesha Waheed, Neeraj Kumar, Abdul Ahad, Yousef A. Bin Jardan, Mohd. Mujeeb, Ashok Kumar, Tanveer Naved and Swati Madan
Pharmaceuticals 2023, 16(8), 1169; https://doi.org/10.3390/ph16081169 - 17 Aug 2023
Viewed by 993
Abstract
Diabetes treatment requires focused administration with quality systemic circulation to determine the optimal therapeutic window. Intestinal distribution through oral administration with nanoformulation provides several benefits. Therefore, the purpose of this study is to create plumbagin enclosed within niosomes using the quality by design [...] Read more.
Diabetes treatment requires focused administration with quality systemic circulation to determine the optimal therapeutic window. Intestinal distribution through oral administration with nanoformulation provides several benefits. Therefore, the purpose of this study is to create plumbagin enclosed within niosomes using the quality by design (QbD) strategy for efficient penetration and increased bioavailability. The formulation and optimization of plumbagin-loaded niosomes (P-Ns-Opt) involved the use of a Box–Behnken Design. The particle size (PDI) and entrapment efficiency of the optimized P-Ns-Opt were 133.6 nm, 0.150, and 75.6%, respectively. TEM, DSC, and FTIR were used to analyze the morphology and compatibility of the optimized P-Ns-Opt. Studies conducted in vitro revealed a controlled release system. P-Ns-Opt’s antioxidant activity, α-amylase, and α-glucosidase were evaluated, and the results revealed a dose-dependent efficacy with 60.68 ± 0.02%,90.69 ± 2.9%, and 88.43 ± 0.89%, respectively. In summary, the created P-Ns-Opt demonstrate remarkable potential for antidiabetic activity by inhibiting oxygen radicals, α-amylase, and α-glucosidase enzymes and are, therefore, a promising drug delivery nanocarrier in the management and treatment of diabetes. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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17 pages, 7543 KiB  
Article
Mannose-Functionalized Isoniazid-Loaded Nanostructured Lipid Carriers for Pulmonary Delivery: In Vitro Prospects and In Vivo Therapeutic Efficacy Assessment
by Shaveta Ahalwat, Dinesh Chandra Bhatt, Surbhi Rohilla, Vikas Jogpal, Kirti Sharma, Tarun Virmani, Girish Kumar, Abdulsalam Alhalmi, Ali S. Alqahtani, Omar M. Noman and Marwan Almoiliqy
Pharmaceuticals 2023, 16(8), 1108; https://doi.org/10.3390/ph16081108 - 04 Aug 2023
Cited by 5 | Viewed by 1305
Abstract
Resistance to isoniazid (INH) is common and increases the possibility of acquiring multidrug-resistant tuberculosis. For this study, isoniazid-loaded nanostructured lipid carriers (INH-NLCs) were developed and effectively functionalized with mannose (Man) to enhance the residence time of the drug within the lungs via specific [...] Read more.
Resistance to isoniazid (INH) is common and increases the possibility of acquiring multidrug-resistant tuberculosis. For this study, isoniazid-loaded nanostructured lipid carriers (INH-NLCs) were developed and effectively functionalized with mannose (Man) to enhance the residence time of the drug within the lungs via specific delivery and increase the therapeutic efficacy of the formulation. The mannose-functionalized isoniazid-loaded nanostructured lipid carrier (Man-INH-NLC) formulation was evaluated with respect to various formulation parameters, namely, encapsulation efficiency (EE), drug loading (DL), average particle size (PS), zeta potential (ZP), polydispersity index (PDI), in vitro drug release (DR), and release kinetics. The in vitro inhalation behavior of the developed formulation after nebulization was investigated using an Andersen cascade impactor via the estimation of the mass median aerosolized diameter (MMAD) and geometric aerodynamic diameter (GAD) and subsequently found to be suitable for effective lung delivery. An in vivo pharmacokinetic study was carried out in a guinea pig animal model, and it was demonstrated that Man-INH-NLC has a longer residence time in the lungs with improved pharmacokinetics when compared with unfunctionalized INH-NLC, indicating the enhanced therapeutic efficacy of the Man-INH-NLC formulation. Histopathological analysis led us to determine that the extent of tissue damage was more severe in the case of the pure drug solution of isoniazid compared to the Man-INH-NLC formulation after nebulization. Thus, the nebulization of Man-INH-NLC was found to be safe, forming a sound basis for enhancing the therapeutic efficacy of the drug for improved management in the treatment of pulmonary tuberculosis. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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16 pages, 2649 KiB  
Article
Enhancing Oral Bioavailability and Brain Biodistribution of Perillyl Alcohol Using Nanostructured Lipid Carriers
by Samila Horst Peczek, Ana Paula Santos Tartari, Isabella Camargo Zittlau, Camila Diedrich, Christiane Schineider Machado and Rubiana Mara Mainardes
Pharmaceuticals 2023, 16(8), 1055; https://doi.org/10.3390/ph16081055 - 25 Jul 2023
Cited by 3 | Viewed by 1048
Abstract
Perillyl alcohol (POH), a bioactive monoterpenoid derived from limonene, shows promise as an antitumor agent for brain tumor treatment. However, its limited oral bioavailability and inadequate brain distribution hinder its efficacy. To address these challenges, this study developed nanostructured lipid carriers (NLCs) loaded [...] Read more.
Perillyl alcohol (POH), a bioactive monoterpenoid derived from limonene, shows promise as an antitumor agent for brain tumor treatment. However, its limited oral bioavailability and inadequate brain distribution hinder its efficacy. To address these challenges, this study developed nanostructured lipid carriers (NLCs) loaded with POH to improve its brain biodistribution. The NLCs prepared using hot homogenization exhibited an average diameter of 287 nm and a spherical morphology with a polydispersity index of 0.143. High encapsulation efficiency of 99.68% was achieved. X-ray diffraction analyses confirmed the semicrystalline state of POH-loaded NLCs. In vitro release studies demonstrated a biphasic release profile. Stability studies in simulated gastric and intestinal fluids confirmed their ability to withstand pH variations and digestive enzymes. In vivo pharmacokinetic studies in rats revealed significantly enhanced oral bioavailability of POH when encapsulated in the NLCs. Biodistribution studies showed increased POH concentration in brain tissue with NLCs compared with free POH, which was distributed more in non-target tissues such as the liver, lungs, kidneys, and spleen. These findings underscore the potential of NLCs as effective delivery systems for enhancing oral bioavailability and brain biodistribution of POH, providing a potential therapeutic strategy for brain tumor treatment. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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15 pages, 3503 KiB  
Article
Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma
by Sandeep Divate Satyanarayana, Amr Selim Abu Lila, Afrasim Moin, Ehssan H. Moglad, El-Sayed Khafagy, Hadil Faris Alotaibi, Ahmad J. Obaidullah and Rompicherla Narayana Charyulu
Pharmaceuticals 2023, 16(7), 1001; https://doi.org/10.3390/ph16071001 - 13 Jul 2023
Cited by 7 | Viewed by 1387
Abstract
Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer [...] Read more.
Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from relatively low ocular bioavailability. The objective of this study was to fabricate and optimize solid lipid nanoparticles (SLNs) containing Bimatoprost for ocular administration for the management of glaucoma. Bimatoprost-loaded SLNs were fabricated by solvent evaporation/ultrasonication technique. Glyceryl Monostearate (GMS) was adopted as solid lipid and poloxamer 407 as surfactant. Optimization of SLNs was conducted by central composite design. The optimized formulation was assessed for average particle size, entrapment efficiency (%), zeta potential, surface morphology, drug release study, sterility test, isotonicity test, Hen’s egg test-chorioallantoic membrane (HET-CAM) test and histopathology studies. The optimized Bimatoprost-loaded SLNs formulation had an average size of 183.3 ± 13.3 nm, zeta potential of −9.96 ± 1.2 mV, and encapsulation efficiency percentage of 71.8 ± 1.1%. Transmission electron microscopy (TEM) study revealed the nearly smooth surface of formulated particles with a nano-scale size range. In addition, SLNs significantly sustained Bimatoprost release for up to 12 h, compared to free drug (p < 005). Most importantly, HET-CAM test nullified the irritancy of the formulation was verified its tolerability upon ocular use, as manifested by a significant reduction in mean irritation score, compared to positive control (1% sodium dodecyl sulfate; p < 0.001). Histopathology study inferred the absence of any signs of cornea tissue damage upon treatment with Bimatoprost optimized formulation. Collectively, it was concluded that SLNs might represent a viable vehicle for enhancing the corneal permeation and ocular bioavailability of Bimatoprost for the management of glaucoma. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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17 pages, 3439 KiB  
Article
Baricitinib Lipid-Based Nanosystems as a Topical Alternative for Atopic Dermatitis Treatment
by Núria Garrós, Paola Bustos-Salgados, Òscar Domènech, María José Rodríguez-Lagunas, Negar Beirampour, Roya Mohammadi-Meyabadi, Mireia Mallandrich, Ana C. Calpena and Helena Colom
Pharmaceuticals 2023, 16(6), 894; https://doi.org/10.3390/ph16060894 - 18 Jun 2023
Cited by 1 | Viewed by 1870
Abstract
Atopic dermatitis (AD) is a chronic autoimmune inflammatory skin disorder which causes a significant clinical problem due to its prevalence. The ongoing treatment for AD is aimed at improving the patient’s quality of life. Additionally, glucocorticoids or immunosuppressants are being used in systemic [...] Read more.
Atopic dermatitis (AD) is a chronic autoimmune inflammatory skin disorder which causes a significant clinical problem due to its prevalence. The ongoing treatment for AD is aimed at improving the patient’s quality of life. Additionally, glucocorticoids or immunosuppressants are being used in systemic therapy. Baricitinib (BNB) is a reversible Janus-associated kinase (JAK)-inhibitor; JAK is an important kinase involved in different immune responses. We aimed at developing and evaluating new topical liposomal formulations loaded with BNB for the treatment of flare ups. Three liposomal formulations were elaborated using POPC (1-palmitoyl-2-oleoyl-glycero-3-phosphocholine), CHOL (Cholesterol) and CER (Ceramide) in different proportions: (i) POPC, (ii) POPC:CHOL (8:2, mol/mol) and (iii) POPC:CHOL:CER (3.6:2.4:4.0 mol/mol/mol). They were physiochemically characterized over time. In addition, an in vitro release study, ex vivo permeation and retention studies in altered human skin (AHS) were also performed. Histological analysis was used to study the tolerance of the formulations on the skin. Lastly, the HET-CAM test was also performed to evaluate the irritancy capacity of the formulations, and the modified Draize test was performed to evaluate the erythema and edema capacity of the formulations on the altered skin. All liposomes showed good physicochemical properties and were stable for at least one month. POPC:CHOL:CER had the highest flux and permeation, and the retention in the skin was equal to that of POPC:CHOL. The formulations exhibited no harmful or irritating effects, and the histological examination revealed no changes in structure. The three liposomes have shown promising results for the aim of the study. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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19 pages, 3867 KiB  
Article
Preparation, Characterization, and In Vivo Evaluation of Gentiopicroside-Phospholipid Complex (GTP-PC) and Its Self-Nanoemulsion Drug Delivery System (GTP-PC-SNEDDS)
by Yingpeng Tong, Wen Shi, Qin Zhang and Jianxin Wang
Pharmaceuticals 2023, 16(1), 99; https://doi.org/10.3390/ph16010099 - 09 Jan 2023
Cited by 1 | Viewed by 1806
Abstract
The objective of the present study was to develop a gentiopicroside-phospholipid complex (GTP-PC) and its self-nanoemulsion drug delivery system (GTP-PC-SNEDDS) to increase the oral bioavailability of gentiopicroside (GTP). The factors affecting the formation of GTP-PC were studied with the complexation efficiency and dissociation [...] Read more.
The objective of the present study was to develop a gentiopicroside-phospholipid complex (GTP-PC) and its self-nanoemulsion drug delivery system (GTP-PC-SNEDDS) to increase the oral bioavailability of gentiopicroside (GTP). The factors affecting the formation of GTP-PC were studied with the complexation efficiency and dissociation rate. The properties of the complex were investigated by means of differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectra (FT-IR), dissolution, etc. Then, GTP-PC was loaded into SNEDDS by investigating the effects of weight ratios of GTP-PC to blank SNEDDS, preparation technology, dilution media, and dilution multi, based on the screening results of oils, surfactants, and cosurfactants. In rats, GTP, GTP-PC, and GTP-PC-SNEDDS were orally administered at different times, and GTP concentrations were determined using RP-HPLC. The optimal GTP-PC was prepared with tetrahydrofuran as the reaction solvent, GTP:phospholipid = 1:2, and stirring for 4 h. The optimal prescription for GTP-PC-SNEDDS was as follows: Maisin 35-1:Miglycol = 30%, Labrasol:Cremophor EL = 1:4 = 40%, Transcutol P = 30%; Maisin 35-1:Miglycol = 12, and the ratio of GTP-PC to blank was 1:10—then the mixture was stirred at 37 °C for 1 d and then placed for 2 d to form stable GTP-PC-SNEDDS. After oral administration of GTP, GTP-PC and GTP-PC-SNEDDS, and mean plasma GTP concentration–time curves were all in accordance with the single-compartment model. The Cmax, AUC0–∞, and Fr of the three formulations were significantly higher than that of GTP, demonstrating that GTP was metabolized rapidly, and its higher bioavailability could be achieved by the formation of GTP-PC and GTP-PC-SNEDDS. Among the three formations, the bioavailability of GTP-PC-SNEDDS was highest, with approximately 2.6-fold and 1.3-fold of Fr value, compared with GTP-PC (suspension) and GTP-PC (oil solution), respectively. Compared with GTP, GTP-PC and GTP-PC-SNEDDS enhanced the bioavailability of GTP significantly. In the future, this study could serve as a reference for clinical trials using GTP-PC and GTP-PC-SNEDDS. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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23 pages, 3613 KiB  
Article
Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues
by María Rincón, Lupe Carolina Espinoza, Marcelle Silva-Abreu, Lilian Sosa, Jessica Pesantez-Narvaez, Guadalupe Abrego, Ana Cristina Calpena and Mireia Mallandrich
Pharmaceuticals 2022, 15(10), 1185; https://doi.org/10.3390/ph15101185 - 24 Sep 2022
Cited by 6 | Viewed by 2055
Abstract
Transmucosal delivery is commonly used to prevent or treat local diseases. Pranoprofen is an anti-inflammatory drug prescribed in postoperative cataract surgery, intraocular lens implantation, chorioretinopathy, uveitis, age-related macular degeneration or cystoid macular edema. Pranoprofen can also be used for acute and chronic management [...] Read more.
Transmucosal delivery is commonly used to prevent or treat local diseases. Pranoprofen is an anti-inflammatory drug prescribed in postoperative cataract surgery, intraocular lens implantation, chorioretinopathy, uveitis, age-related macular degeneration or cystoid macular edema. Pranoprofen can also be used for acute and chronic management of osteoarthritis and rheumatoid arthritis. Quality by Design (QbD) provides a systematic approach to drug development and maps the influence of the formulation components. The aim of this work was to develop and optimize a nanostructured lipid carrier by means of the QbD and factorial design suitable for the topical management of inflammatory processes on mucosal tissues. To this end, the nanoparticles loading pranoprofen were prepared by a high-pressure homogenization technique with Tween 80 as stabilizer and Lanette® 18 as the solid lipid. From, the factorial design results, the PF-NLCs-N6 formulation showed the most suitable characteristics, which was selected for further studies. The permeability capacity of pranoprofen loaded in the lipid-based nanoparticles was evaluated by ex vivo transmucosal permeation tests, including buccal, sublingual, nasal, vaginal, corneal and scleral mucosae. The results revealed high permeation and retention of pranoprofen in all the tissues tested. According to the predicted plasma concentration at the steady-state, no systemic effects would be expected, any neither were any signs of ocular irritancy observed from the optimized formulation when tested by the HET-CAM technique. Hence, the optimized formulation (PF-NLCs-N6) may offer a safe and attractive nanotechnological tool in topical treatment of local inflammation on mucosal diseases. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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Review

Jump to: Editorial, Research

39 pages, 2276 KiB  
Review
Use of Nanocarriers Containing Antitrypanosomal Drugs for the Treatment of Chagas Disease
by Diogo de Freitas Paiva, Ana Paula dos Santos Matos, Denise de Abreu Garófalo, Tatielle do Nascimento, Mariana Sato de Souza de Bustamante Monteiro, Ralph Santos-Oliveira and Eduardo Ricci-Junior
Pharmaceuticals 2023, 16(8), 1163; https://doi.org/10.3390/ph16081163 - 15 Aug 2023
Cited by 1 | Viewed by 1199
Abstract
Chagas disease, caused by the Trypanosoma cruzi parasitic protozoan, is a neglected tropical disease (NTD) of significant incidence in Latin America. Transmission to humans and other mammals is mainly via the vector insect from the Reduviidae family, popularly known as the kissing bug. [...] Read more.
Chagas disease, caused by the Trypanosoma cruzi parasitic protozoan, is a neglected tropical disease (NTD) of significant incidence in Latin America. Transmission to humans and other mammals is mainly via the vector insect from the Reduviidae family, popularly known as the kissing bug. There are other transmission means, such as through congenital transmission, blood transfusions, organ transplantations, and the consumption of contaminated food. For more than 50 years, the disease has been treated with benznidazole and nifurtimox, which are only effective during the acute phase of the disease. In addition to their low efficacy in the chronic phase, they cause many adverse effects and are somewhat selective. The use of nanocarriers has received significant attention due to their ability to encapsulate and release therapeutic agents in a controlled manner. Generally, their diameter ranges from 100 to 300 nanometers. The objective of this scoping review was to perform a search of the literature for the use of nanocarriers as an alternative for improving the treatment of Chagas disease and to suggest future research. Bibliographic searches were carried out in the Web of Science and PubMed scientific databases from January 2012 to May 2023, using the “Chagas disease and Trypanosoma cruzi and nanoparticles” keywords, seeking to gather the largest number of articles, which were evaluated using the inclusion and exclusion criteria. After analyzing the papers, the results showed that nanocarriers offer physiological stability and safety for the transport and controlled release of drugs. They can increase solubility and selectivity against the parasite. The in vitro assays showed that the trypanocidal activity of the drug was not impaired after encapsulation. In the in vivo assays, parasitemia reduction and high survival and cure rates in animals were obtained during both phases of the disease using lower doses when compared to the standard treatment. The scoping review showed that nanocarriers are a promising alternative for the treatment of Chagas disease. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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27 pages, 4417 KiB  
Review
From Bench to Bedside: Implications of Lipid Nanoparticle Carrier Reactogenicity for Advancing Nucleic Acid Therapeutics
by Tetiana Korzun, Abraham S. Moses, Parham Diba, Ariana L. Sattler, Olena R. Taratula, Gaurav Sahay, Oleh Taratula and Daniel L. Marks
Pharmaceuticals 2023, 16(8), 1088; https://doi.org/10.3390/ph16081088 - 31 Jul 2023
Cited by 4 | Viewed by 3116
Abstract
In biomedical applications, nanomaterial-based delivery vehicles, such as lipid nanoparticles, have emerged as promising instruments for improving the solubility, stability, and encapsulation of various payloads. This article provides a formal review focusing on the reactogenicity of empty lipid nanoparticles used as delivery vehicles, [...] Read more.
In biomedical applications, nanomaterial-based delivery vehicles, such as lipid nanoparticles, have emerged as promising instruments for improving the solubility, stability, and encapsulation of various payloads. This article provides a formal review focusing on the reactogenicity of empty lipid nanoparticles used as delivery vehicles, specifically emphasizing their application in mRNA-based therapies. Reactogenicity refers to the adverse immune responses triggered by xenobiotics, including administered lipid nanoparticles, which can lead to undesirable therapeutic outcomes. The key components of lipid nanoparticles, which include ionizable lipids and PEG-lipids, have been identified as significant contributors to their reactogenicity. Therefore, understanding the relationship between lipid nanoparticles, their structural constituents, cytokine production, and resultant reactogenic outcomes is essential to ensure the safe and effective application of lipid nanoparticles in mRNA-based therapies. Although efforts have been made to minimize these adverse reactions, further research and standardization are imperative. By closely monitoring cytokine profiles and assessing reactogenic manifestations through preclinical and clinical studies, researchers can gain valuable insights into the reactogenic effects of lipid nanoparticles and develop strategies to mitigate undesirable reactions. This comprehensive review underscores the importance of investigating lipid nanoparticle reactogenicity and its implications for the development of mRNA–lipid nanoparticle therapeutics in various applications beyond vaccine development. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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22 pages, 1135 KiB  
Review
Advances with Lipid-Based Nanosystems for siRNA Delivery to Breast Cancers
by Md Abdus Subhan, Nina Filipczak and Vladimir P. Torchilin
Pharmaceuticals 2023, 16(7), 970; https://doi.org/10.3390/ph16070970 - 06 Jul 2023
Cited by 6 | Viewed by 2705
Abstract
Breast cancer is the most frequently diagnosed cancer among women. Breast cancer is also the key reason for worldwide cancer-related deaths among women. The application of small interfering RNA (siRNA)-based drugs to combat breast cancer requires effective gene silencing in tumor cells. To [...] Read more.
Breast cancer is the most frequently diagnosed cancer among women. Breast cancer is also the key reason for worldwide cancer-related deaths among women. The application of small interfering RNA (siRNA)-based drugs to combat breast cancer requires effective gene silencing in tumor cells. To overcome the challenges of drug delivery to tumors, various nanosystems for siRNA delivery, including lipid-based nanoparticles that protect siRNA from degradation for delivery to cancer cells have been developed. These nanosystems have shown great potential for efficient and targeted siRNA delivery to breast cancer cells. Lipid-based nanosystems remain promising as siRNA drug delivery carriers for effective and safe cancer therapy including breast cancer. Lipid nanoparticles (LNPs) encapsulating siRNA enable efficient and specific silencing of oncogenes in breast tumors. This review discusses a variety of lipid-based nanosystems including cationic lipids, sterols, phospholipids, PEG-lipid conjugates, ionizable liposomes, exosomes for effective siRNA drug delivery to breast tumors, and the clinical translation of lipid-based siRNA nanosystems for solid tumors. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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27 pages, 1267 KiB  
Review
Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms
by Viliana Gugleva and Velichka Andonova
Pharmaceuticals 2023, 16(3), 474; https://doi.org/10.3390/ph16030474 - 22 Mar 2023
Cited by 12 | Viewed by 3103
Abstract
Sufficient ocular bioavailability is often considered a challenge by the researchers, due to the complex structure of the eye and its protective physiological mechanisms. In addition, the low viscosity of the eye drops and the resulting short ocular residence time further contribute to [...] Read more.
Sufficient ocular bioavailability is often considered a challenge by the researchers, due to the complex structure of the eye and its protective physiological mechanisms. In addition, the low viscosity of the eye drops and the resulting short ocular residence time further contribute to the observed low drug concentration at the target site. Therefore, various drug delivery platforms are being developed to enhance ocular bioavailability, provide controlled and sustained drug release, reduce the number of applications, and maximize therapy outcomes. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) exhibit all these benefits, in addition to being biocompatible, biodegradable, and susceptible to sterilization and scale-up. Furthermore, their successive surface modification contributes to prolonged ocular residence time (by adding cationic compounds), enhanced penetration, and improved performance. The review highlights the salient characteristics of SLNs and NLCs concerning ocular drug delivery, and updates the research progress in this area. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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19 pages, 5171 KiB  
Review
Endogenous Lipid Carriers—Bench-to-Bedside Roadblocks in Production and Drug Loading of Exosomes
by Terjahna Richards, Himaxi Patel, Ketan Patel and Frank Schanne
Pharmaceuticals 2023, 16(3), 421; https://doi.org/10.3390/ph16030421 - 10 Mar 2023
Cited by 4 | Viewed by 2027
Abstract
Exosomes are cell-derived, nano-sized extracellular vesicles comprising a lipid bilayer membrane that encapsulates several biological components, such as nucleic acids, lipids, and proteins. The role of exosomes in cell–cell communication and cargo transport has made them promising candidates in drug delivery for an [...] Read more.
Exosomes are cell-derived, nano-sized extracellular vesicles comprising a lipid bilayer membrane that encapsulates several biological components, such as nucleic acids, lipids, and proteins. The role of exosomes in cell–cell communication and cargo transport has made them promising candidates in drug delivery for an array of diseases. Despite several research and review papers describing the salient features of exosomes as nanocarriers for drug delivery, there are no FDA-approved commercial therapeutics based on exosomes. Several fundamental challenges, such as the large-scale production and reproducibility of batches, have hindered the bench-to-bedside translation of exosomes. In fact, compatibility and poor drug loading sabotage the possibility of delivering several drug molecules. This review provides an overview of the challenges and summarizes the potential solutions/approaches to facilitate the clinical development of exosomal nanocarriers. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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26 pages, 2297 KiB  
Review
Intranasal Lipid Nanoparticles Containing Bioactive Compounds Obtained from Marine Sources to Manage Neurodegenerative Diseases
by Joana Torres, Inês Costa, Andreia F. Peixoto, Renata Silva, José Manuel Sousa Lobo and Ana Catarina Silva
Pharmaceuticals 2023, 16(2), 311; https://doi.org/10.3390/ph16020311 - 16 Feb 2023
Cited by 2 | Viewed by 2222
Abstract
Marine sources contain several bioactive compounds with high therapeutic potential, such as remarkable antioxidant activity that can reduce oxidative stress related to the pathogenesis of neurodegenerative diseases. Indeed, there has been a growing interest in these natural sources, especially those resulting from the [...] Read more.
Marine sources contain several bioactive compounds with high therapeutic potential, such as remarkable antioxidant activity that can reduce oxidative stress related to the pathogenesis of neurodegenerative diseases. Indeed, there has been a growing interest in these natural sources, especially those resulting from the processing of marine organisms (i.e., marine bio-waste), to obtain natural antioxidants as an alternative to synthetic antioxidants in a sustainable approach to promote circularity by recovering and creating value from these bio-wastes. However, despite their expected potential to prevent, delay, or treat neurodegenerative diseases, antioxidant compounds may have difficulty reaching the brain due to the need to cross the blood–brain barrier (BBB). In this regard, alternative delivery systems administered by different routes have been proposed, including intranasal administration of lipid nanoparticles, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), which have shown promising results. Intranasal administration shows several advantages, including the fact that molecules do not need to cross the BBB to reach the central nervous system (CNS), as they can be transported directly from the nasal cavity to the brain (i.e., nose-to-brain transport). The benefits of using SLN and NLC for intranasal delivery of natural bioactive compounds for the treatment of neurodegenerative diseases have shown relevant outcomes through in vitro and in vivo studies. Noteworthy, for bioactive compounds obtained from marine bio-waste, few studies have been reported, showing the open potential of this research area. This review updates the state of the art of using SLN and NLC to transport bioactive compounds from different sources, in particular, those obtained from marine bio-waste, and their potential application in the treatment of neurodegenerative diseases. Full article
(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems 2023)
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