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Pharmaceutics
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Lipid-based Nanoparticle Systems for Drug Delivery
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Lipid-based Nanoparticle Systems for Drug Delivery

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

Deadline for manuscript submissions: closed (31 March 2021) | Viewed by 21213

Special Issue Editors

Prof. Dr. Aleksander F. Sikorski

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Guest Editor
Research and Development Centre, Regional Specialist Hospital in Wrocław, Kamieńskiego 73a, 51-124 Wrocław, Poland
Interests: biochemistry of biological membranes; membrane skeleton; membrane skeletal proteins; membrane raft organization and regulation; membrane raft proteins; targeted liposomal drug carriers
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Marek Langner

E-Mail Website
Guest Editor
Department of Biomedical Engineering, Faculty of Fundamental Problems of Technology, Wrocław University of Science and Technology, Pl. Grunwaldzki 13, 50-377 Wrocław, Poland
Interests: biophysics of biological membranes; mechanics and electrostatics of membranes; targeted liposomal drug carriers; calorimetric and fluorescence techniques

Special Issue Information

Dear Colleagues,

Nanocarrier technology in drug delivery research has achieved reasonable success in the development of modern therapies, permitting better bioavailability and pharmacodynamics, as well as reducing side effects and providing the possibility of specific targeting of the drug. In particular, due to their biocompatibility and flexibility, supramolecular lipid-aggregate-based nanocarriers, such as lipid nanoparticles, liposomes, nanoemulsions, and micelles, have been the subjects of extensive studies that resulted in several technologies and commercially available therapeutics, including Ambisome, Doxil or recently registered ONPATTRO (patisiran). These seem to be only a small fraction of the opportunities provided by the system built from naturally occurring lipids and similar non-toxic organic compounds. No commercial lipid-based preparation has explored the possibility of targeting the diseased site in the body with lipid aggregate-packed drugs. Hereby, we invite all researchers to contribute to this Special Issue, which will collect review articles devoted to various aspects of lipid aggregate-based drug nanocarrier studies.

Prof. Dr. Aleksander F. Sikorski
Prof. Dr. Marek Langner
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

  • lipid nanoparticles
  • liposomes
  • nanoemulsions
  • micelles
  • drug targeting
  • lipid nanoparticle technology

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Published Papers (5 papers)

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Research

21 pages, 5151 KiB  
Article
Development of a Nanostructured Lipid Carrier (NLC) by a Low-Energy Method, Comparison of Release Kinetics and Molecular Dynamics Simulation
by Andrea C. Ortiz, Osvaldo Yañez, Edison Salas-Huenuleo and Javier O. Morales
Pharmaceutics 2021, 13(4), 531; https://doi.org/10.3390/pharmaceutics13040531 - 10 Apr 2021
Cited by 47 | Viewed by 6611
Abstract
Lipid nanocarriers have a great potential for improving the physicochemical characteristics and behavior of poorly water-soluble drugs, such as aqueous dispersibility and oral bioavailability. This investigation presents a novel nanostructured lipid carrier (NLC) based on a mixture of solid lipid glycerides, fatty acid [...] Read more.
Lipid nanocarriers have a great potential for improving the physicochemical characteristics and behavior of poorly water-soluble drugs, such as aqueous dispersibility and oral bioavailability. This investigation presents a novel nanostructured lipid carrier (NLC) based on a mixture of solid lipid glycerides, fatty acid esters of PEG 1500 (Gelucire® 44/14), and an oil mix composed of capric and caprylic triglycerides (Miglyol® 812). These NLCs were developed by a simple low-energy method based on melt emulsification to yield highly encapsulating and narrowly distributed nanoparticles (~100 nm, PdI = 0.1, and zeta potential = ~−10 mV). Rhodamine 123 was selected as a poorly water-soluble drug model and owing to its spectroscopic properties. The novel NLCs were characterized by dynamic light scattering (DLS), zeta potential, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and colloidal stability. The drug release was determined through a dialysis bag and vertical Franzs’ cells to provide insights about the methods’ suitability, revealing similar performance regardless of their different fluid dynamics. Rhodamine 123 followed a characteristic biphasic release profile owing to the swelling of the hydrophilic polymer coating and diffusion process from the lipid core as revealed by the Korsmeyers–Peppas kinetic modeling. Moreover, to elucidate the formation and incorporation of Rhodamine 123 into the NLC core, several molecular dynamics simulations were conducted. The temperature was shown to be an important condition to improve the formation of the nanoparticles. In addition, the liquid lipid incorporation to the formulation forms nanoparticles with imperfect centers, in contrast to nanoparticles without it. Moreover, Miglyol® 812 improves hydrophobic molecule solubility. These results suggest the potential of novel NLC as a drug delivery system for poorly water-soluble drugs. Full article
(This article belongs to the Special Issue Lipid-based Nanoparticle Systems for Drug Delivery)
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17 pages, 6058 KiB  
Article
Cyclosporine Lipid Nanocapsules as Thermoresponsive Gel for Dry Eye Management: Promising Corneal Mucoadhesion, Biodistribution and Preclinical Efficacy in Rabbits
by Lubna M. Eldesouky, Riham M. El-Moslemany, Alyaa A. Ramadan, Mahmoud H. Morsi and Nawal M. Khalafallah
Pharmaceutics 2021, 13(3), 360; https://doi.org/10.3390/pharmaceutics13030360 - 9 Mar 2021
Cited by 31 | Viewed by 4087
Abstract
An ophthalmic cyclosporine (CsA) formulation based on Lipid nanocapsules (LNC) was developed for dry eye management, aiming to provide targeting to ocular tissues with long-term drug levels and maximum tolerability. CsA-LNC were of small particle size (41.9 ± 4.0 nm), narrow size distribution [...] Read more.
An ophthalmic cyclosporine (CsA) formulation based on Lipid nanocapsules (LNC) was developed for dry eye management, aiming to provide targeting to ocular tissues with long-term drug levels and maximum tolerability. CsA-LNC were of small particle size (41.9 ± 4.0 nm), narrow size distribution (PdI ≤ 0.1), and high entrapment efficiency (above 98%). Chitosan (C) was added to impart positive charge. CsA-LNC were prepared as in-situ gels using poloxamer 407 (P). Ex vivo mucoadhesive strength was evaluated using bovine cornea, while in vivo corneal biodistribution (using fluorescent DiI), efficacy in dry eye using Schirmer tear test (STT), and ocular irritation using Draize test were studied in rabbits compared to marketed ophthalmic CsA nanoemulsion (CsA-NE) and CsA in castor oil. LNC incorporation in in-situ gels resulted in an increase in mucoadhesion, and stronger fluorescence in corneal layers seen by confocal microscopy, compared to the other tested formulations. Rate of recovery (days required to restore corneal baseline hydration level) assessed over 10 days, showed that CsA-LNC formulations produced complete recovery by day 7 comparable to CsA-NE. No Ocular irritation was observed by visual and histopathological examination. Based on data generated, CsA-LNC-CP in-situ gel proved to be a promising effective nonirritant CsA ophthalmic formulation for dry eye management. Full article
(This article belongs to the Special Issue Lipid-based Nanoparticle Systems for Drug Delivery)
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13 pages, 2404 KiB  
Article
A Proposed Methodology for a Risk Assessment-Based Liposome Development Process
by Zsófia Németh, Edina Pallagi, Dorina Gabriella Dobó and Ildikó Csóka
Pharmaceutics 2020, 12(12), 1164; https://doi.org/10.3390/pharmaceutics12121164 - 29 Nov 2020
Cited by 20 | Viewed by 3289
Abstract
The requirements of a liposomal formulation vary depending on the pharmaceutical indication, the target patient population, and the corresponding route of administration. Different preparation methods require various material attributes (MAs) (properties and characteristics of the components) and process parameters (PPs) (settings of the [...] Read more.
The requirements of a liposomal formulation vary depending on the pharmaceutical indication, the target patient population, and the corresponding route of administration. Different preparation methods require various material attributes (MAs) (properties and characteristics of the components) and process parameters (PPs) (settings of the preparation method). The identification of the quality target product profile for a liposome-based formulation, the critical quality attributes of the liposomes, and the possible MAs and PPs that may influence the key characteristics of the vesicles facilitates pharmaceutical research. Researchers can systematise their knowledge by using the quality by design (QbD) approach. The potential factors that influence the quality of the product can be collected and studied through a risk assessment process. In this paper, the requirements of a liposome formulation prepared via the thin-film hydration preparation technique are presented; furthermore, the possible factors that have an impact on the quality of the final product and have to be considered and specified during the development of a liposomal formulation are herein identified and collected. The understanding and the application of these elements of QbD in the pharmaceutical developments help to influence the quality, the achievements, and the success of the formulated product. Full article
(This article belongs to the Special Issue Lipid-based Nanoparticle Systems for Drug Delivery)
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20 pages, 3000 KiB  
Article
Celecoxib Loaded In-Situ Provesicular Powder and Its In-Vitro Cytotoxic Effect for Cancer Therapy: Fabrication, Characterization, Optimization and Pharmacokinetic Evaluation
by Ali M. Nasr, Sameh S. Elhady, Shady A. Swidan and Noha M. Badawi
Pharmaceutics 2020, 12(12), 1157; https://doi.org/10.3390/pharmaceutics12121157 - 28 Nov 2020
Cited by 7 | Viewed by 2450
Abstract
Introduction: Several recent studies have shown that the role of cyclooxygenase 2 (COX-2) in carcinogenesis has become more evident. It affects angiogenesis, apoptosis, and invasion, and plays a key role in the production of carcinogens. It has also been reported that COX-2 inhibitors [...] Read more.
Introduction: Several recent studies have shown that the role of cyclooxygenase 2 (COX-2) in carcinogenesis has become more evident. It affects angiogenesis, apoptosis, and invasion, and plays a key role in the production of carcinogens. It has also been reported that COX-2 inhibitors such as celecoxib (CLX) might play an effective role in preventing cancer formation and progression. Formulation of CLX into nanovesicles is a promising technique to improve its bioavailability and anticancer efficacy. Aim: The aim of this study is to optimize and evaluate the anticancer efficacy of CLX-loaded in-situ provesicular powder composed of surfactants and fatty alcohol-based novel nanovesicles in-vitro and determine its pharmacokinetic parameters in-vivo. Methods: The novel provesicular powders were prepared by the slurry method and optimized by 32 full factorial design using the desirability function. Results: Small mean particle size was achieved by the formed vesicles with value of 351.7 ± 1.76 nm and high entrapment efficacy of CLX in the formed vesicles of 97.53 ± 0.84%. Solid state characterization of the optimized formulation showed that the powder was free flowing, showed no incompatibilities between drug and excipients and showed smooth texture. The cytotoxic study of the optimized formula on HCT-116, HepG-2, A-549, PC-3 and MCF-7 cell lines showed significant increase in activity of CLX compared to its free form. The pharmacokinetic study on albino rabbits after oral administration showed significant increase in the area under the curve (AUC)0–24 h and significantly higher oral relative bioavailability of the optimized formulation compared to Celebrex® 100 mg market product (p < 0.05). Conclusion: All findings of this study suggest the potential improvement of efficacy and bioavailability of CLX when formulated in the form of in-situ provesicular powder composed of surfactants and fatty alcohol-based novel nanovesicles for its repositioned use as an anticancer agent. Full article
(This article belongs to the Special Issue Lipid-based Nanoparticle Systems for Drug Delivery)
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19 pages, 2418 KiB  
Article
Enhancing the Oral Bioavailability of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers: In Vitro Characterization and Absorption in Rats after Oral Administration
by Walid Anwar, Hamdy M. Dawaba, Mohsen I. Afouna, Ahmed M. Samy, Mohammed H. Rashed and Abdelaziz E. Abdelaziz
Pharmaceutics 2020, 12(11), 1047; https://doi.org/10.3390/pharmaceutics12111047 - 31 Oct 2020
Cited by 29 | Viewed by 3917
Abstract
Candesartan Cilexetil (CC) is a prodrug widely used in the treatment of hypertension and heart failure, but it has some limitations, such as very poor aqueous solubility, high affinity to P-glycoprotein efflux mechanism, and hepatic first-pass metabolism. Therefore, it has very low oral [...] Read more.
Candesartan Cilexetil (CC) is a prodrug widely used in the treatment of hypertension and heart failure, but it has some limitations, such as very poor aqueous solubility, high affinity to P-glycoprotein efflux mechanism, and hepatic first-pass metabolism. Therefore, it has very low oral bioavailability. In this study, glyceryl monostearate (GMS) and Capryol™ 90 were selected as solid and liquid lipids, respectively, to develop CC-NLC (nanostructured lipid carrier). CC was successfully encapsulated into NLP (CC-NLC) to enhance its oral bioavailability. CC-NLC was formulated using a hot homogenization-ultrasonication technique, and the physicochemical properties were characterized. The developed CC-NLC formulation was showed in nanometric size (121.6 ± 6.2 nm) with high encapsulation efficiency (96.23 ± 3.14%). Furthermore, it appeared almost spherical in morphology under a transmission electron microscope. The surgical experiment of the designed CC-NLC for absorption from the gastrointestinal tract revealed that CC-NLC absorption in the stomach was only 15.26% of that in the intestine. Otherwise, cellular uptake study exhibit that CC-NLCs should be internalized through the enterocytes after that transported through the systemic circulation. The pharmacokinetic results indicated that the oral bioavailability of CC was remarkably improved above 2-fold after encapsulation into nanostructured lipid carriers. These results ensured that nanostructured lipid carriers have a highly beneficial effect on improving the oral bioavailability of poorly water-soluble drugs, such as CC. Full article
(This article belongs to the Special Issue Lipid-based Nanoparticle Systems for Drug Delivery)
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