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Pharmaceutics
Special Issues
Innovative Formulations of Poorly Soluble Drugs
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Innovative Formulations of Poorly Soluble Drugs

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 31 October 2024 | Viewed by 5283

Special Issue Editor

Dr. Wenbing Dai

E-Mail Website
Guest Editor
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Interests: macromolecular drug delivery; hydrogels; nanosuspensions; peptide amphiphiles; self-assembled prodrug; peptide-drug conjugate; long-acting injectables
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Since poorly soluble drugs make up more than 70% of new molecular entities currently in development and about 40% of marketed products, it is a constant challenge for scientists to effectively increase their druggability and develop innovative formulations through pharmaceutical technologies. Various physical and chemical approaches, such as size reduction, solid dispersion, co-crystal or co-amorphous formation, inclusion complexation, lipid/polymer-based delivery systems, and prodrug design, have been employed to enhance solubility, dissolution, and ultimately increase the oral bioavailability of poorly soluble drugs. While new application scenarios of poorly water-soluble therapeutics are emerging, novel or more sophisticated techniques are urgently needed for development and investigation.

This Special Issue aims to highlight the latest progress and research of pharmaceutical technologies to solve delivery problems in the context of new application scenarios of poorly soluble drugs. We invite articles on aspects of establishment of novel delivery technologies of poorly water-soluble drugs, studies of mode of function and new application of technologies, development, and evaluation of relevant innovative formulations.

Dr. Wenbing Dai
Guest Editor

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

  • poorly soluble drugs
  • innovative formulations
  • bioavailability
  • drug delivery systems
  • routes of administration
  • pharmaceutical technology
  • new application scenarios
  • 505(b)(2)

Published Papers (3 papers)

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Research

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22 pages, 32030 KiB  
Article
Design of Etched- and Functionalized-Halloysite/Meloxicam Hybrids: A Tool for Enhancing Drug Solubility and Dissolution Rate
by Valeria Friuli, Claudia Urru, Chiara Ferrara, Debora Maria Conti, Giovanna Bruni, Lauretta Maggi and Doretta Capsoni
Pharmaceutics 2024, 16(3), 338; https://doi.org/10.3390/pharmaceutics16030338 - 28 Feb 2024
Viewed by 601
Abstract
The study focuses on the synthesis and characterization of Meloxicam–halloysite nanotube (HNT) composites as a viable approach to enhance the solubility and dissolution rate of meloxicam, a poorly water-soluble drug (BCS class II). Meloxicam is loaded on commercial and modified halloysite (acidic and [...] Read more.
The study focuses on the synthesis and characterization of Meloxicam–halloysite nanotube (HNT) composites as a viable approach to enhance the solubility and dissolution rate of meloxicam, a poorly water-soluble drug (BCS class II). Meloxicam is loaded on commercial and modified halloysite (acidic and alkaline etching, or APTES and chitosan functionalization) via a solution method. Several techniques (XRPD, FT-IR, 13C solid-state NMR, SEM, EDS, TEM, DSC, TGA) are applied to characterize both HNTs and meloxicam–HNT systems. In all the investigated drug–clay hybrids, a high meloxicam loading of about 40 wt% is detected. The halloysite modification processes and the drug loading do not alter the structure and morphology of both meloxicam and halloysite nanotubes, which are in intimate contact in the composites. Weak drug–clay and drug-functionalizing agent interactions occur, involving the meloxicam amidic functional group. All the meloxicam–halloysite composites exhibit enhanced dissolution rates, as compared to meloxicam. The meloxicam–halloysite composite, functionalized with chitosan, showed the best performance both in water and in buffer at pH 7.5. The drug is completely released in 4–5 h in water and in less than 1 h in phosphate buffer. Notably, an equilibrium solubility of 13.7 ± 4.2 mg/L in distilled water at 21 °C is detected, and wettability dramatically increases, compared to the raw meloxicam. These promising results can be explained by the chitosan grafting on the outer surface of halloysite nanotubes, which provides increased specific surface area (100 m2/g) disposable for drug adsorption/desorption. Full article
(This article belongs to the Special Issue Innovative Formulations of Poorly Soluble Drugs)
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21 pages, 28882 KiB  
Article
Development of a Luliconazole Nanoemulsion as a Prospective Ophthalmic Delivery System for the Treatment of Fungal Keratitis: In Vitro and In Vivo Evaluation
by Jingjing Yang, Zhen Liang, Ping Lu, Fei Song, Zhen Zhang, Tianyang Zhou, Jingguo Li and Junjie Zhang
Pharmaceutics 2022, 14(10), 2052; https://doi.org/10.3390/pharmaceutics14102052 - 26 Sep 2022
Cited by 8 | Viewed by 1732
Abstract
Luliconazole (LCZ), a novel imidazole drug, has broad-spectrum and potential antifungal effects, which makes it a possible cure for fungal keratitis; nevertheless, its medical use in ocular infections is hindered by its poor solubility. The purpose of this study was to design and [...] Read more.
Luliconazole (LCZ), a novel imidazole drug, has broad-spectrum and potential antifungal effects, which makes it a possible cure for fungal keratitis; nevertheless, its medical use in ocular infections is hindered by its poor solubility. The purpose of this study was to design and optimize LCZ nanoemulsion (LCZ-NE) formulations using the central composite design-response surface methodology, and to investigate its potential in improving bioavailability following ocular topical administration. The LCZ-NE formulation was composed of Capryol 90, ethoxylated hydrogenated castor oil, Transcutol® P and water. The shape of LCZ-NE was spherical and uniform, with a droplet size of 18.43 ± 0.05 nm and a low polydispersity index (0.070 ± 0.008). The results of an in vitro release of LCZ study demonstrated that the LCZ-NE released more drug than an LCZ suspension (LCZ-Susp). Increases in the inhibition zone indicated that the in vitro antifungal activity of the LCZ-NE was significantly improved. An ocular irritation evaluation in rabbits showed that the LCZ-NE had a good tolerance in rabbit eyes. Ocular pharmacokinetics analysis revealed improved bioavailability in whole eye tissues that were treated with LCZ-NE, compared with those treated with LCZ-Susp. In conclusion, the optimized LCZ-NE formulation exhibited excellent physicochemical properties, good tolerance, enhanced antifungal activity and bioavailability in eyes. This formulation would be safe, and shows promise in effectively treating ocular fungal infections. Full article
(This article belongs to the Special Issue Innovative Formulations of Poorly Soluble Drugs)
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Review

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22 pages, 4413 KiB  
Review
Nano and Microemulsions for the Treatment of Depressive and Anxiety Disorders: An Efficient Approach to Improve Solubility, Brain Bioavailability and Therapeutic Efficacy
by Patrícia C. Pires, Ana Cláudia Paiva-Santos and Francisco Veiga
Pharmaceutics 2022, 14(12), 2825; https://doi.org/10.3390/pharmaceutics14122825 - 16 Dec 2022
Cited by 12 | Viewed by 2299
Abstract
Most drugs used for the treatment of depression, anxiety and related disorders have low absorption, high metabolism, low brain targeting and/or low water solubility, which can make it hard to formulate them at high strength and can also lead to decreased bioavailability. Incorporating [...] Read more.
Most drugs used for the treatment of depression, anxiety and related disorders have low absorption, high metabolism, low brain targeting and/or low water solubility, which can make it hard to formulate them at high strength and can also lead to decreased bioavailability. Incorporating these drugs into nanometric emulsions can solve these issues. Hence, the aim of the present review was to assess the potential of nano and micro emulsions for the delivery of antidepressant and anxiolytic drugs. The results from several studies showed that nanometric emulsions were able to increase drug strength up to 20,270-fold (compared to aqueous solubility). Moreover, in general, the formulations showed droplet size, polydispersity index, zeta potential, viscosity, osmolality, pH, in vitro drug release and ex vivo drug permeation as adequate for the intended effect and administration route. In vivo animal pharmacokinetic experiments showed that nanometric emulsions improved systemic drug bioavailability and/or brain targeting, and in vivo pharmacodynamic studies showed that they had antidepressant and/or anxiolytic effects, also being apparently safe. Hence, the current review provides proof of the potential of nano and microemulsions for improving solubilization and increasing the overall bioavailability of antidepressant and/or anxiolytic drugs, providing evidence of a possible useful strategy for future therapies. Full article
(This article belongs to the Special Issue Innovative Formulations of Poorly Soluble Drugs)
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