Submit to Pharmaceutics Review for Pharmaceutics Propose a Special Issue

Journal Browser

Engineering and Characterisation of Novel Nanomedicine Formulations

Print Special Issue Flyer
Special Issue Editors
Special Issue Information
Keywords
Related Special Issue
Published Papers

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (30 April 2023) | Viewed by 26683

Share This Special Issue

Special Issue Editors

Dr. Raquel Fernández García

E-Mail Website
Guest Editor

School of Pharmacy, University of Nottingham, University Park, Nottingham, NG7 2RD, UK
Interests: nanomedicine; antifungal therapy; liposomes; microfluidics
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Francisco Bolás-Fernández

E-Mail Website
Guest Editor

Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain
Interests: parasitology; leishmania; pharmacokinetics; immunology
Special Issues, Collections and Topics in MDPI journals

Dr. Ana Isabel Fraguas-Sánchez

E-Mail Website
Guest Editor

Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
Interests: antimicrobial agents; breast cancer; cannabinoids; drug delivery; drug targeting; in situ-forming implants; nanomedicine; ovarian cancer; polymers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to our Special Issue in engineering and characterisation of novel nanomedicines. Nanomedicine has been a hot topic in formulation science in the last few decades regarding selectively delivering drugs to target tissues. Nanomedicines can modify drug release and encapsulate poorly soluble drugs, allowing a selective targeting and minimising adverse effects. This is of key importance in antitumoral and anti-infectious therapies, in which an undesired drug release can lead to severe damage in healthy tissues. Moreover, they protect drugs from degradation, allowing the delivery of RNA. This Special Issue aims to highlight the most novel nano-approaches in the treatment of cancer and infectious diseases. In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following: nanoparticles, liposomes, nanocapsules and drug targeting, applied to anticancer and anti-infectious therapies.

We look forward to receiving your contributions.

Dr. Raquel Fernández García
Prof. Dr. Francisco Bolás-Fernández
Dr. Ana Isabel Fraguas-Sánchez
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. Pharmaceutics 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

nanoparticles
liposomes
solid lipid nanocapsules
drug targeting
cancer
infectious diseases
nanovaccines

Related Special Issue

Engineering and Characterisation of Novel Nanomedicine Formulations, 2nd Edition in Pharmaceutics (2 articles)

Published Papers (14 papers)

Download All Papers

Editorial

Jump to: Research, Review

4 pages, 194 KiB

Open AccessEditorial

Editorial for Special Issue ‘Engineering and Characterisation of Novel Nanomedicine Formulations’

by Raquel Fernández-García, Francisco Bolás-Fernández and Ana Isabel Fraguas-Sánchez

Pharmaceutics 2024, 16(5), 585; https://doi.org/10.3390/pharmaceutics16050585 - 26 Apr 2024

Viewed by 305

Abstract

Nanomedicine is the application of nanotechnology to achieve innovations in healthcare and involves the engineering of systems at the nanoscale (particle size < 1000 nm) with the aim of improving drug delivery [...] Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

Research

Jump to: Editorial, Review

15 pages, 4235 KiB

Open AccessArticle

Delicate Hybrid Laponite–Cyclic Poly(ethylene glycol) Nanoparticles as a Potential Drug Delivery System

by Shengzhuang Tang, Jesse Chen, Jayme Cannon, Mona Chekuri, Mohammad Farazuddin, James R. Baker, Jr. and Su He Wang

Pharmaceutics 2023, 15(7), 1998; https://doi.org/10.3390/pharmaceutics15071998 - 21 Jul 2023

Cited by 2 | Viewed by 1019

Abstract

The objective of the study was to explore the feasibility of a new drug delivery system using laponite (LAP) and cyclic poly(ethylene glycol) (cPEG). Variously shaped and flexible hybrid nanocrystals were made by both the covalent and physical attachment of chemically homogeneous cyclized PEG to laponite nanodisc plates. The size of the resulting, nearly spherical particles ranged from 1 to 1.5 µm, while PEGylation with linear methoxy poly (ethylene glycol) (mPEG) resulted in fragile sheets of different shapes and sizes. When infused with 10% doxorubicin (DOX), a drug commonly used in the treatment of various cancers, the LAP-cPEG/DOX formulation was transparent and maintained liquid-like homogeneity without delamination, and the drug loading efficiency of the LAP-cPEG nano system was found to be higher than that of the laponite-poly(ethylene glycol) LAP-mPEG system. Furthermore, the LAP-cPEG/DOX formulation showed relative stability in phosphate-buffered saline (PBS) with only 15% of the drug released. However, in the presence of human plasma, about 90% of the drug was released continuously over a period of 24 h for the LAP-cPEG/DOX, while the LAP-mPEG/DOX formulation released 90% of DOX in a 6 h burst. The results of the cell viability assay indicated that the LAP-cPEG/DOX formulation could effectively inhibit the proliferation of A549 lung carcinoma epithelial cells. With the DOX concentration in the range of 1–2 µM in the LAP-cPEG/DOX formulation, enhanced drug effects in both A549 lung carcinoma epithelial cells and primary lung epithelial cells were observed compared to LAP-mPEG/DOX. The unique properties and effects of cPEG nanoparticles provide a potentially better drug delivery system and generate interest for further targeting studies and applications. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

16 pages, 2845 KiB

Open AccessArticle

Increased Bone Marrow Uptake and Accumulation of Very-Late Antigen-4 Targeted Lipid Nanoparticles

by Laura E. Swart, Marcel H. A. M. Fens, Anita van Oort, Piotr Waranecki, L. Daniel Mata Casimiro, David Tuk, Martijn Hendriksen, Luca van den Brink, Elizabeth Schweighart, Cor Seinen, Ryan Nelson, Anja Krippner-Heidenreich, Tom O’Toole, Raymond M. Schiffelers, Sander Kooijmans and Olaf Heidenreich

Pharmaceutics 2023, 15(6), 1603; https://doi.org/10.3390/pharmaceutics15061603 - 27 May 2023

Cited by 1 | Viewed by 2920

Abstract

Lipid nanoparticles (LNPs) have evolved rapidly as promising delivery systems for oligonucleotides, including siRNAs. However, current clinical LNP formulations show high liver accumulation after systemic administration, which is unfavorable for the treatment of extrahepatic diseases, such as hematological disorders. Here we describe the specific targeting of LNPs to hematopoietic progenitor cells in the bone marrow. Functionalization of the LNPs with a modified Leu-Asp-Val tripeptide, a specific ligand for the very-late antigen 4 resulted in an improved uptake and functional siRNA delivery in patient-derived leukemia cells when compared to their non-targeted counterparts. Moreover, surface-modified LNPs displayed significantly improved bone-marrow accumulation and retention. These were associated with increased LNP uptake by immature hematopoietic progenitor cells, also suggesting similarly improved uptake by leukemic stem cells. In summary, we describe an LNP formulation that successfully targets the bone marrow including leukemic stem cells. Our results thereby support the further development of LNPs for targeted therapeutic interventions for leukemia and other hematological disorders. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

18 pages, 2204 KiB

Open AccessArticle

Co-Encapsulation of Simvastatin and Doxorubicin into pH-Sensitive Liposomes Enhances Antitumoral Activity in Breast Cancer Cell Lines

by Jaqueline Aparecida Duarte, Eliza Rocha Gomes, André Luis Branco De Barros and Elaine Amaral Leite

Pharmaceutics 2023, 15(2), 369; https://doi.org/10.3390/pharmaceutics15020369 - 21 Jan 2023

Cited by 7 | Viewed by 1610

Abstract

Doxorubicin (DOX) is a potent chemotherapeutic drug used as the first line in breast cancer treatment; however, cardiotoxicity is the main drawback of the therapy. Preclinical studies evidenced that the association of simvastatin (SIM) with DOX leads to a better prognosis with reduced side effects and deaths. In this work, a novel pH-sensitive liposomal formulation capable of co-encapsulating DOX and SIM at different molar ratios was investigated for its potential in breast tumor treatment. Studies on physicochemical characterization of the liposomal formulations were carried out. The cytotoxic effects of DOX, SIM, and their combinations at different molar ratios (1:1; 1:2 and 2:1), free or co-encapsulated into pH-sensitive liposomes, were evaluated against three human breast cancer cell lines (MDA-MB-231, MCF-7, and SK-BR-3). Experimental protocols included cell viability, combination index, nuclear morphological changes, and migration capacity. The formulations showed a mean diameter of less than 200 nm, with a polydispersity index lower than 0.3. The encapsulation content was ~100% and ~70% for DOX and SIM, respectively. A more pronounced inhibitory effect on breast cancer cell lines was observed at a DOX:SIM molar ratio of 2:1 in both free and encapsulated drugs. Furthermore, the 2:1 ratio showed synergistic combination rates for all concentrations of cell inhibition analyzed (50, 75, and 90%). The results demonstrated the promising potential of the co-encapsulated liposome for breast tumor treatment. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

17 pages, 5291 KiB

Open AccessArticle

Native Study of the Behaviour of Magnetite Nanoparticles for Hyperthermia Treatment during the Initial Moments of Intravenous Administration

by Valentina Marassi, Ilaria Zanoni, Simona Ortelli, Stefano Giordani, Pierluigi Reschiglian, Barbara Roda, Andrea Zattoni, Costanza Ravagli, Laura Cappiello, Giovanni Baldi, Anna L. Costa and Magda Blosi

Pharmaceutics 2022, 14(12), 2810; https://doi.org/10.3390/pharmaceutics14122810 - 15 Dec 2022

Cited by 6 | Viewed by 1370

Abstract

Magnetic nanoparticles (MNPs) present outstanding properties making them suitable as therapeutic agents for hyperthermia treatments. Since the main safety concerns of MNPs are represented by their inherent instability in a biological medium, strategies to both achieve long-term stability and monitor hazardous MNP degradation are needed. We combined a dynamic approach relying on flow field flow fractionation (FFF)-multidetection with conventional techniques to explore frame-by-frame changes of MNPs injected in simulated biological medium, hypothesize the interaction mechanism they are subject to when surrounded by a saline, protein-rich environment, and understand their behaviour at the most critical point of intravenous administration. In the first moments of MNPs administration in the patient, MNPs change their surrounding from a favorable to an unfavorable medium, i.e., a complex biological fluid such as blood; the particles evolve from a synthetic identity to a biological identity, a transition that needs to be carefully monitored. The dynamic approach presented herein represents an optimal alternative to conventional batch techniques that can monitor only size, shape, surface charge, and aggregation phenomena as an averaged information, given that they cannot resolve different populations present in the sample and cannot give accurate information about the evolution or temporary instability of MNPs. The designed FFF method equipped with a multidetection system enabled the separation of the particle populations providing selective information on their morphological evolution and on nanoparticle–proteins interaction in the very first steps of infusion. Results showed that in a dynamic biological setting and following interaction with serum albumin, PP-MNPs retain their colloidal properties, supporting their safety profile for intravenous administration. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

12 pages, 4707 KiB

Open AccessArticle

Development and Evaluation of Ethosomes Loaded with Zingiber zerumbet Linn Rhizome Extract for Antifungal Skin Infection in Deep Layer Skin

by Kampanart Huanbutta, Napapat Rattanachitthawat, Kunlathida Luangpraditkun, Pornsak Sriamornsak, Vivek Puri, Inderbir Singh and Tanikan Sangnim

Pharmaceutics 2022, 14(12), 2765; https://doi.org/10.3390/pharmaceutics14122765 - 09 Dec 2022

Cited by 2 | Viewed by 1506

Abstract

Skin fungal infection is still a serious public health problem due to the high number of cases. Even though medicines are available for this disease, drug resistance among patients has increased. Moreover, access to medicine is restricted in some areas. One of the therapeutic options is herbal medicine. This study aims to develop an ethosome formulation loaded with Zingiber zerumbet (L.) Smith. rhizome extract for enhanced antifungal activity in deep layer skin, which is difficult to cure. Ethosomes were successfully prepared by the cold method, and the optimized formulation was composed of 1% (w/v) phosphatidylcholine and 40% (v/v) ethanol. Transmission electron microscope (TEM) images revealed that the ethosomes had a vesicle shape with a diameter of 205.6–368.5 nm. The entrapment of ethosomes was 31.58% and could inhibit the growth of Candida albicans at a concentration of 312.5 μg/mL. Finally, the ethosome system significantly enhanced the skin penetration and retention of the active compound (zerumbone) compared with the liquid extract. This study showed that Z. zerumbet (L.) rhizome extract could be loaded into ethosomes. The findings could be carried over to the next step for clinical application by conducting further in vivo penetration and permeation tests. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

17 pages, 1687 KiB

Open AccessArticle

Mitigating Cardiotoxicity of Dendrimers: Angiotensin-(1-7) via Its Mas Receptor Ameliorates PAMAM-Induced Cardiac Dysfunction in the Isolated Mammalian Heart

by Saghir Akhtar, Fawzi Babiker, Usman A. Akhtar and Ibrahim F. Benter

Pharmaceutics 2022, 14(12), 2673; https://doi.org/10.3390/pharmaceutics14122673 - 01 Dec 2022

Cited by 5 | Viewed by 1296

Abstract

Aim: The influence of the physiochemical properties of dendrimer nanoparticles on cardiac contractility and hemodynamics are not known. Herein, we investigated (a) the effect of polyamidoamine (PAMAM) dendrimer generation (G7, G6, G5, G4 and G3) and surface chemistry (-NH₂, -COOH and -OH) on cardiac function in mammalian hearts following ischemia-reperfusion (I/R) injury, and (b) determined if any PAMAM-induced cardiotoxicity could be mitigated by Angiotensin-(1-7) (Ang-(1-7), a cardioprotective agent. Methods: Hearts isolated from male Wistar rats underwent regional I/R and/or treatment with different PAMAM dendrimers, Ang-(1-7) or its MAS receptors antagonists. Thirty minutes of regional ischemia through ligation of the left anterior descending coronary artery was followed by 30 min of reperfusion. All treatments were initiated 5 min prior to reperfusion and maintained during the first 10 min of reperfusion. Cardiac function parameters for left ventricular contractility, hemodynamics and vascular dynamics data were acquired digitally, whereas cardiac enzymes and infarct size were used as measures of cardiac injury. Results: Treatment of isolated hearts with increasing doses of G7 PAMAM dendrimer progressively exacerbated recovery of cardiac contractility and hemodynamic parameters post-I/R injury. Impairment of cardiac function was progressively less on decreasing dendrimer generation with G3 exhibiting little or no cardiotoxicity. Cationic PAMAMs (-NH₂) were more toxic than anionic (-COOH), with neutral PAMAMs (-OH) exhibiting the least cardiotoxicity. Cationic G7 PAMAM-induced cardiac dysfunction was significantly reversed by Ang-(1-7) administration. These cardioprotective effects of Ang-(1-7) were significantly revoked by administration of the MAS receptor antagonists, A779 and D-Pro⁷-Ang-(1-7). Conclusions: PAMAM dendrimers can impair the recovery of hearts from I/R injury in a dose-, dendrimer-generation-(size) and surface-charge dependent manner. Importantly, PAMAM-induced cardiotoxicity could be mitigated by Ang-(1-7) acting through its MAS receptor. Thus, this study highlights the activation of Ang-(1-7)/Mas receptor axis as a novel strategy to overcome dendrimer-induced cardiotoxicity. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

15 pages, 3459 KiB

Open AccessArticle

Synthesis of Dipyridylaminoperylenediimide–Metal Complexes and Their Cytotoxicity Studies

by José Garcés-Garcés, Marta Redrado, Ángela Sastre-Santos, María Concepción Gimeno and Fernando Fernández-Lázaro

Pharmaceutics 2022, 14(12), 2616; https://doi.org/10.3390/pharmaceutics14122616 - 27 Nov 2022

Viewed by 1386

Abstract

A new family of perylenediimide (PDI) silver and copper complexes has been successfully synthesized by reacting ortho- and bay-substituted (dipyrid-2′,2″-ylamino)perylenediimide ligands with metal phosphine fragments. The coordination of the metal center did not reveal a significant effect on the photophysical properties, which are mainly due to the PDI ligands, and in some cases quenching of the luminescence was observed. The antiproliferative effect of the free perylenediimide ligands and the metalloPDI complexes against the cervix cancer cell line HeLa was determined by MTT assay. The free perylenediimide ligands exhibited a moderate cytotoxic activity, but the coordination of silver or copper to the dypyridylamino fragment greatly enhanced the activity, suggesting a synergistic effect between the two fragments. In attempts to elucidate the cellular biodistribution of the PDIs and the complexes, a colocalization experiment using specific dyes for the lysosomes or mitochondria as internal standards revealed a major internalization inside the cell for the metal complexes, as well as a partial mitochondrial localization. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

25 pages, 7084 KiB

Open AccessArticle

Investigation of the Antitumor Activity and Toxicity of Tumor-Derived Exosomes Fused with Long-Circulating and pH-Sensitive Liposomes Containing Doxorubicin

by Eliza Rocha Gomes, Fernanda Rezende Souza, Geovanni Dantas Cassali, Adriano de Paula Sabino, André Luis Branco de Barros and Mônica Cristina Oliveira

Pharmaceutics 2022, 14(11), 2256; https://doi.org/10.3390/pharmaceutics14112256 - 22 Oct 2022

Cited by 7 | Viewed by 1618

Abstract

Exosome–liposome hybrid nanocarriers containing chemotherapeutic agents have been developed to enhance drug delivery, improve the efficacy of the treatment of metastatic cancer, and overcome chemoresistance in cancer therapy. Thus, the objectives of this study were to investigate the toxicological profiles of exosomes fused with long-circulating and pH-sensitive liposomes containing doxorubicin (ExoSpHL-DOX) in healthy mice and the antitumor activity of ExoSpHL-DOX in Balb/c female mice bearing 4T1 breast tumors. The acute toxicity was determined by evaluating the mortality and morbidity of the animals and conducting hematological, biochemical, and histopathological analyses after a single intravenous administration of ExoSpHL-DOX. The results of the study indicated that the ExoSpHL-DOX treatment is less toxic than the free doxorubicin (DOX) treatment. ExoSpHL-DOX showed no signs of nephrotoxicity, even at the highest dose of DOX, indicating that the hybrid nanosystem may alter the distribution of DOX and reduce the kidney damage. Regarding the antitumor activity, ExoSpHL-DOX showed an antitumor effect compared to the control group. Furthermore, the hybrid nanocarrier of tumor-derived exosomes fused with long-circulating and pH-sensitive liposomes reduced the number of metastatic foci in the lungs. These results indicate that ExoSpHL-DOX may be a promising nanocarrier for the treatment of breast cancer, reducing toxicity and inhibiting metastasis, mainly in the lungs. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Graphical abstract

19 pages, 3329 KiB

Open AccessArticle

The Rate of Cisplatin Dosing Affects the Resistance and Metastatic Potential of Triple Negative Breast Cancer Cells, Independent of Hypoxia

by Omkar Bhatavdekar, Inês Godet, Daniele Gilkes and Stavroula Sofou

Pharmaceutics 2022, 14(10), 2184; https://doi.org/10.3390/pharmaceutics14102184 - 13 Oct 2022

Viewed by 1908

Abstract

To best control tumor growth and/or metastasis in triple negative breast cancer (TNBC), it may be useful to understand the effect(s) of chemotherapy delivery (i.e., the rate and pattern of exposure to the drug) on cell sub-populations that have experienced different levels of hypoxia (and/or acidosis). In this spirit, MDA-MB-231 TNBC cells, and their hypoxia-reporter counterparts, were characterized for their sensitivity to cisplatin. When in the form of multicellular spheroids, that capture the diffusion-limited transport that generates hypoxic and acidic subregions within the avascular areas of solid tumors, the effects of the rate and pattern of exposure to cisplatin on cell viability and motility/migration potential were evaluated for each cell sub-population. We demonstrated that cell sensitivity to cisplatin was not dependent on acidosis, but cell resistance increased with exposure to hypoxia. In spheroids, the increase of the rates of cell exposure to cisplatin, at a constant cumulative dose, increased sensitivity to chemotherapy and lowered the cells’ metastatic potential, even for cells that had experienced hypoxia. This effect was also shown to be caused by nanocarriers engineered to quickly release cisplatin which deeply penetrated the spheroid interstitium, resulting in the fast and uniform exposure of the TNBC tumors to the agent. This rate and dosing-controlled model may effectively limit growth and/or metastasis, independent of hypoxia. This mode of chemotherapy delivery can be enabled by engineered nanocarriers. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

18 pages, 2446 KiB

Open AccessArticle

A Pseudovirus Nanoparticle-Based Trivalent Rotavirus Vaccine Candidate Elicits High and Cross P Type Immune Response

by Ming Xia, Pengwei Huang and Ming Tan

Pharmaceutics 2022, 14(8), 1597; https://doi.org/10.3390/pharmaceutics14081597 - 30 Jul 2022

Cited by 9 | Viewed by 1823

Abstract

Rotavirus infection continues to cause significant morbidity and mortality globally. In this study, we further developed the S₆₀-VP8* pseudovirus nanoparticles (PVNPs) displaying the glycan receptor binding VP8* domains of rotavirus spike proteins as a parenteral vaccine candidate. First, we established a scalable method for the large production of tag-free S₆₀-VP8* PVNPs representing four rotavirus P types, P[8], P[4], P[6], and P[11]. The approach consists of two major steps: selective precipitation of the S-VP8* proteins from bacterial lysates using ammonium sulfate, followed by anion exchange chromatography to further purify the target proteins to a high purity. The purified soluble proteins self-assembled into S₆₀-VP8* PVNPs. Importantly, after intramuscular injections, the trivalent vaccine consisting of three PVNPs covering VP8* antigens of P[8], P[4], and P[6] rotaviruses elicited high and broad immunogenicity in mice toward the three predominant P-type rotaviruses. Specifically, the trivalent vaccine-immunized mouse sera showed (1) high and balanced IgG and IgA antibody titers toward all three VP8* types, (2) high blocking titer against the VP8*-glycan receptor interaction, and (3) high and broad neutralizing titers against replications of all P[8], P[4], and P[6] rotaviruses. Therefore, trivalent S₆₀-VP8* PVNPs are a promising non-replicating, parenteral vaccine candidate against the most prevalent rotaviruses worldwide. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

19 pages, 1611 KiB

Open AccessArticle

Critical Analysis and Quality Assessment of Nanomedicines and Nanocarriers in Clinical Trials: Three Years of Activity at the Clinical Trials Office

by Diego Alejandro Dri, Elisa Gaucci, Ilaria Torrieri, Maria Carafa, Carlotta Marianecci and Donatella Gramaglia

Pharmaceutics 2022, 14(7), 1438; https://doi.org/10.3390/pharmaceutics14071438 - 09 Jul 2022

Viewed by 1251

Abstract

Investigational medicinal products submitted over the course of 3 years and authorized at the Clinical Trials Office of the Italian Medicines Agency as part of a request for authorization of clinical trials were scrutinized to identify those encompassing nanomedicines. The quality assessment reports performed on the documentation submitted were analyzed, classifying and discussing the most frequently detected issues. The identification of nanomedicines retrieved and the information on their quality profiles are shared to increase the transparency and availability of information, providing feedback that can support sponsors in optimizing the quality part of the documentation and of the information submitted. Results confirm that nanomedicines tested as investigational medicinal products in clinical trials are developed and authorized in agreement with the highest standards of quality, meeting safety profiles according to the strong regulatory requirements in the European Union. Some key points are highlighted and indicate that the regulatory approach to innovation in a clinical trial setting could potentially be renewed to ride the wave of innovation, particularly in the nanotechnology field, capitalizing on lessons learned and still ensuring a strong and effective framework. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Graphical abstract

19 pages, 4919 KiB

Open AccessArticle

Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol^® Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study

by Nilesh R. Rarokar, Sunil S. Menghani, Deweshri R. Kerzare, Pramod B. Khedekar, Ashish P. Bharne, Abdulhakeem S. Alamri, Walaa F. Alsanie, Majid Alhomrani, Nagaraja Sreeharsha and Syed Mohammed Basheeruddin Asdaq

Pharmaceutics 2022, 14(7), 1393; https://doi.org/10.3390/pharmaceutics14071393 - 30 Jun 2022

Cited by 14 | Viewed by 2497

Abstract

The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic^® F68 (surfactant) employing high-pressure homogenization. The ratio of drug with respect to lipid was optimized, considering factors such as desired particle size and highest percent encapsulation efficiency. Lyophilized SLNs were then incorporated in the hydrogel prepared from 0.2–1.0% w/v carbopol 934P and further evaluated for rheological parameters. The z-average, zeta potential and polydispersity index were found to be 241.3 nm, −15.2 mV and 0.415, respectively. The SLNs show a higher entrapment efficiency of about 98.36%, with 2.12 to 6.3602% drug loading. SEM images, XRD and the results of the DSC, FTIR show successful preparation of SLNs after freeze drying. The TH-loaded SLNs hydrogel showed sustained drug release (95.47 ± 1.45%) over a period of 24 h. The results reported in this study show a significant effect on the zone of inhibition than the marketed formulation and pure drug in Candida albicans cultures, with better physical stability at cooler temperatures. It helped to enhance skin deposition inthe ex vivostudy and improved, in vitro and in vivo, the antifungal activity. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Figure 1

Review

Jump to: Editorial, Research

45 pages, 3469 KiB

Open AccessEditor’s ChoiceReview

Microfluidic Manufacture of Lipid-Based Nanomedicines

by Karim Osouli-Bostanabad, Sara Puliga, Dolores R. Serrano, Andrea Bucchi, Gavin Halbert and Aikaterini Lalatsa

Pharmaceutics 2022, 14(9), 1940; https://doi.org/10.3390/pharmaceutics14091940 - 14 Sep 2022

Cited by 16 | Viewed by 4832

Abstract

Nanoparticulate technologies have revolutionized drug delivery allowing for passive and active targeting, altered biodistribution, controlled drug release (temporospatial or triggered), enhanced stability, improved solubilization capacity, and a reduction in dose and adverse effects. However, their manufacture remains immature, and challenges exist on an industrial scale due to high batch-to-batch variability hindering their clinical translation. Lipid-based nanomedicines remain the most widely approved nanomedicines, and their current manufacturing methods remain discontinuous and face several problems such as high batch-to-batch variability affecting the critical quality attributes (CQAs) of the product, laborious multistep processes, need for an expert workforce, and not being easily amenable to industrial scale-up involving typically a complex process control. Several techniques have emerged in recent years for nanomedicine manufacture, but a paradigm shift occurred when microfluidic strategies able to mix fluids in channels with dimensions of tens of micrometers and small volumes of liquid reagents in a highly controlled manner to form nanoparticles with tunable and reproducible structure were employed. In this review, we summarize the recent advancements in the manufacturing of lipid-based nanomedicines using microfluidics with particular emphasis on the parameters that govern the control of CQAs of final nanomedicines. The impact of microfluidic environments on formation dynamics of nanomaterials, and the application of microdevices as platforms for nanomaterial screening are also discussed. Full article

(This article belongs to the Special Issue Engineering and Characterisation of Novel Nanomedicine Formulations)

► Show Figures

Graphical abstract

Journal Menu

Journal Browser

Engineering and Characterisation of Novel Nanomedicine Formulations

Share This Special Issue

Special Issue Editors

Special Issue Information

Keywords

Related Special Issue

Published Papers (14 papers)

Editorial

Research

Review

Further Information

Guidelines

MDPI Initiatives

Follow MDPI