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Preparation, Characterization, and Effect of Lipid Nanoparticles Used in Different Application Fields IV

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Nanochemistry".

Deadline for manuscript submissions: closed (31 December 2024) | Viewed by 7376

Special Issue Editor

Special Issue Information

Dear Colleagues,

Nanotechnology profoundly impacts our lives in many ways, both positively and negatively. The recent interest in nanoscale products emerged from modern nanotechnology as a multidisciplinary area. Many studies have demonstrated that lipid-based nanoparticles (e.g., nanostructured lipid carriers, solid lipid nanoparticles, nanoemulsions, liposomes, and cubosomes) are largely used to ameliorate the solubility of active principles or to obtain a controlled or target release, creating a modifiable system able to be adapted according to the product requirements. Lipid-based nanoparticles demonstrated their ability to solubilize a number of molecules with different physicochemical properties in well-established, safe, biocompatible and biodegradable matrixes, contributing, as a natural resource, to green nanosystems. When these properties are taken together, lipid-based nanosystems are versatile systems with applications in many fields, including the environmental, veterinary, nutraceutical, cosmetic, biotechnological, biomedical, and pharmaceutical industries. The great level of interest in the various applications of lipid nanoparticles presented in the first three editions of this Special Issue motivated us to propose a fourth installment in this series in order to provide an open forum with the aim of encouraging elaboration upon the research and findings in the field of nanotechnology. Submissions may be in the form of original research or review articles and may focus on a range of issues, such as the production, characterization, structure, and innovative aspects of lipid nanoparticles, possibly presenting new preparation methods, advantages, disadvantages, lipid nanoparticle functionalization, and new applications. Studies with multidisciplinary inputs offering innovative methodologies or insights are also welcome.

Prof. Dr. Rita Cortesi
Guest Editor

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Keywords

  • nanocarriers
  • nanotechnology
  • SLN
  • NLC
  • liposomes
  • drug delivery
  • nanomedicine
  • green agriculture

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Related Special Issue

Published Papers (4 papers)

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Research

20 pages, 6144 KiB  
Article
Remote Co-Loading of Doxorubicin and Hydralazine into PEGylated Liposomes: In Vitro Anti-Proliferative Effect Against Breast Cancer
by Walhan Alshaer, Zainab Lafi, Hamdi Nsairat, Baidaa AlQuaissi, Dana A. Alqudah, Hadil Zureigat and Islam Hamad
Molecules 2025, 30(7), 1549; https://doi.org/10.3390/molecules30071549 - 31 Mar 2025
Viewed by 1045
Abstract
Doxorubicin (DOX), an anthracycline chemotherapeutic agent, demonstrates efficacy against various types of cancer. Combining DOX with the antihypertensive drug hydralazine (HDZ) has been proposed as cardioprotective combination therapy, allowing for the use of a reduced DOX dose. The current study describes the remote [...] Read more.
Doxorubicin (DOX), an anthracycline chemotherapeutic agent, demonstrates efficacy against various types of cancer. Combining DOX with the antihypertensive drug hydralazine (HDZ) has been proposed as cardioprotective combination therapy, allowing for the use of a reduced DOX dose. The current study describes the remote co-loading of DOX and HDZ into PEGylated liposomes using, for the first time, a simultaneous pH gradient technique. First, PEGylated liposomes were prepared using an ethanol injection method and remotely loaded with DOX and HDZ. Then, DOX- and HDZ-loaded liposomes (Lip-DOX-HDZ) were characterized using DLS, TEM, FTIR, thermal analysis, drug leakage, and stability. Furthermore, the cellular uptake and cytotoxicity were evaluated in two human breast cancer cell lines (MCF7 and MDA-MB-231) and two normal cell lines (human dermal fibroblasts (HDFs) and rat cardiac cells (H9C2)). The results revealed that Lip-DOX-HDZ had a particle size of 158 ± 18 nm, PDI of 0.22 ± 0.08, and zeta potential of −22 ± 5 mV. The encapsulation efficiency of DOX and HDZ was 90% and 30%, respectively. Moreover, the IC50 values of Lip-DOX-HDZ showed higher cytotoxicity against the MDA-MB-231 (5.5 ± 0.4 µM) and MCF7 (6.25 ± 0.9 µM) breast cancer cell lines compared to normal cells: HDF cells (20 ± 3.0 µM) and H9C2 cardiac cells (19.37 ± 2.0 µM). Our study found that remotely loaded Lip-DOX-HDZ showed a ~4-fold lower toxicity and selectivity for normal cells (HDFs and H9C2), compared to breast cancer cells. This suggests that Lip-DOX-HDZ is a promising nanocarrier for both DOX and HDZ, clinically potent molecules. Full article
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17 pages, 2926 KiB  
Article
Optimization of Glibenclamide Loaded Thermoresponsive SNEDDS Using Design of Experiment Approach: Paving the Way to Enhance Pharmaceutical Applicability
by Abdelrahman Y. Sherif, Ehab M. Elzayat and Mohammad A. Altamimi
Molecules 2024, 29(21), 5163; https://doi.org/10.3390/molecules29215163 - 31 Oct 2024
Viewed by 1203
Abstract
Thermoresponsive self-nanoemulsifying drug delivery systems (T-SNEDDS) offer a promising solution to the limitations of conventional SNEDDS formulations. Liquid SNEDDS are expected to enhance drug solubility; however, they are susceptible to leakage during storage. Even though solid SNEDDS offers a solution to this storage [...] Read more.
Thermoresponsive self-nanoemulsifying drug delivery systems (T-SNEDDS) offer a promising solution to the limitations of conventional SNEDDS formulations. Liquid SNEDDS are expected to enhance drug solubility; however, they are susceptible to leakage during storage. Even though solid SNEDDS offers a solution to this storage instability, they introduce new challenges, namely increased total dosage and potential for drug trapping within the formulation. The invented T-SNEDDS was used to overcome these limitations and improve the dissolution of glibenclamide (GBC). Solubility and transmittance studies were performed to select a suitable oil and surfactant. Design of Experiments (DoE) software was used to study the impact of propylene glycol and Poloxamer 188 concentrations on measured responses (liquefying temperature, liquefying time, and GBC solubility). The optimized formulation was subjected to an in vitro dissolution study. The optimized T-SNEDDS consisted of Kolliphor EL and Imwitor 308 as surfactants and oil. The optimized propylene glycol and Poloxamer 188 concentrations were 13.7 and 7.9% w/w, respectively. It exhibited a liquefying temperature of 35.0 °C, a liquefying time of 119 s, and a GBC solubility of 5.51 mg/g. In vitro dissolution study showed that optimized T-SNEDDS exhibited 98.8% dissolution efficiency compared with 2.5% for raw drugs. This study presents a promising approach to enhance pharmaceutical applicability by resolving the limitations of traditional SNEDDS. Full article
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19 pages, 5096 KiB  
Article
Solid Lipid Nanoparticles Encapsulating a Benzoxanthene Derivative in a Model of the Human Blood–Brain Barrier: Modulation of Angiogenic Parameters and Inflammation in Vascular Endothelial Growth Factor-Stimulated Angiogenesis
by Giuliana Greco, Aleksandra Agafonova, Alessia Cosentino, Nunzio Cardullo, Vera Muccilli, Carmelo Puglia, Carmelina Daniela Anfuso, Maria Grazia Sarpietro and Gabriella Lupo
Molecules 2024, 29(13), 3103; https://doi.org/10.3390/molecules29133103 - 28 Jun 2024
Viewed by 1893
Abstract
Lignans, a class of secondary metabolites found in plants, along with their derivatives, exhibit diverse pharmacological activities, including antioxidant, antimicrobial, anti-inflammatory, and antiangiogenic ones. Angiogenesis, the formation of new blood vessels from pre-existing ones, is a crucial process for cancer growth and development. [...] Read more.
Lignans, a class of secondary metabolites found in plants, along with their derivatives, exhibit diverse pharmacological activities, including antioxidant, antimicrobial, anti-inflammatory, and antiangiogenic ones. Angiogenesis, the formation of new blood vessels from pre-existing ones, is a crucial process for cancer growth and development. Several studies have elucidated the synergistic relationship between angiogenesis and inflammation in various inflammatory diseases, highlighting a correlation between inflammation and vascular endothelial growth factor (VEGF)-induced angiogenesis. Thus, the identification of novel molecules capable of modulating VEGF effects presents promising prospects for developing therapies aimed at stabilizing, reversing, or even arresting disease progression. Lignans often suffer from low aqueous solubility and, for their use, encapsulation in a delivery system is needed. In this research, a bioinspired benzoxantene has been encapsulated in solid lipid nanoparticles that have been characterized for their pharmacotechnical properties and their thermotropic behavior. The effects of these encapsulated nanoparticles on angiogenic parameters and inflammation in VEGF-induced angiogenesis were evaluated using human brain microvascular endothelial cells (HBMECs) as a human blood–brain barrier model. Full article
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20 pages, 20959 KiB  
Article
Development of A Nanostructured Lipid Carrier-Based Drug Delivery Strategy for Apigenin: Experimental Design Based on CCD-RSM and Evaluation against NSCLC In Vitro
by Xiaoxue Wang, Jinli Liu, Yufei Ma, Xinyu Cui, Cong Chen, Guowei Zhu, Yue Sun and Lei Tong
Molecules 2023, 28(18), 6668; https://doi.org/10.3390/molecules28186668 - 17 Sep 2023
Cited by 8 | Viewed by 2366
Abstract
Non-small-cell lung cancer (NSCLC) is the main cause of cancer-related deaths worldwide, with a low five-year survival rate, posing a serious threat to human health. In recent years, the delivery of antitumor drugs using a nanostructured lipid carrier (NLC) has become a subject [...] Read more.
Non-small-cell lung cancer (NSCLC) is the main cause of cancer-related deaths worldwide, with a low five-year survival rate, posing a serious threat to human health. In recent years, the delivery of antitumor drugs using a nanostructured lipid carrier (NLC) has become a subject of research. This study aimed to develop an apigenin (AP)-loaded nanostructured lipid carrier (AP-NLC) by melt sonication using glyceryl monostearate (GMS), glyceryl triacetate, and poloxamer 188. The optimal prescription of AP-NLC was screened by central composite design response surface methodology (CCD-RSM) based on a single-factor experiment using encapsulation efficiency (EE%) and drug loading (DL%) as response values and then evaluated for its antitumor effects on NCI-H1299 cells. A series of characterization analyses of AP-NLC prepared according to the optimal prescription were carried out using transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). Subsequent screening of the lyophilization protectants revealed that mannitol could better maintain the lyophilization effect. The in vitro hemolysis assay of this formulation indicated that it may be safe for intravenous injection. Moreover, AP-NLC presented a greater ability to inhibit the proliferation, migration, and invasion of NCI-H1299 cells compared to AP. Our results suggest that AP-NLC is a safe and effective nano-delivery vehicle that may have beneficial potential in the treatment of NSCLC. Full article
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