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Pharmaceutics
Special Issues
Advances in Formulation of Poorly Soluble Bioactive Compounds
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Advances in Formulation of Poorly Soluble Bioactive Compounds

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

Deadline for manuscript submissions: closed (31 January 2023) | Viewed by 3023

Special Issue Editor

Prof. Dr. Rosario Pignatello

E-Mail Website
Guest Editor
Department of Drug and Health Sciences, Università di Catania, 95125 Catania, Italy
Interests: drug delivery; nanomedicine; prodrugs; biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

A significant number of already existing or newly investigated drugs and bioactive molecules are severely hindered by their low solubility in water and biological fluids (e.g., BCS class II and IV compounds). This process affects the development of many formulations and the clinical success of theoretically promising compounds.
In recent decades, researchers have developed various ideas and strategies to improve the solubility of drugs, and to formulate and efficiently deliver poorly soluble compounds at a pharmacologically active concentration, for example, by their inclusion in polymers or cyclodextrins, through micro/nanotechnological approaches, or by chemical changes in the molecules.
This Special Issue invites submissions that discuss the advanced ideas and experiments in this specific area of pharmaceutical science, presenting a contemporary perspective supported by recent scientific evidence, of the potentiality of formulating “difficult” compounds. 

Prof. Dr. Rosario Pignatello
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

  • pharmaceutical technology
  • controlled releasae
  • drug delivery
  • drugs
  • BCS
  • solubility
  • bioavailability
  • pharmacokinetics

Published Papers (1 paper)

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Research

24 pages, 5531 KiB  
Article
Optimization of Lipid Nanoparticles by Response Surface Methodology to Improve the Ocular Delivery of Diosmin: Characterization and In-Vitro Anti-Inflammatory Assessment
by Elide Zingale, Salvatore Rizzo, Angela Bonaccorso, Valeria Consoli, Luca Vanella, Teresa Musumeci, Angelo Spadaro and Rosario Pignatello
Pharmaceutics 2022, 14(9), 1961; https://doi.org/10.3390/pharmaceutics14091961 - 16 Sep 2022
Cited by 10 | Viewed by 2633
Abstract
Diosmin is a flavonoid with a great variety of biological activities including antioxidant and anti-inflammatory ones. Its cytoprotective effect in retinal pigment epithelium cells under high glucose conditions makes it a potential support in the treatment of diabetic retinopathy. Despite its benefits, poor [...] Read more.
Diosmin is a flavonoid with a great variety of biological activities including antioxidant and anti-inflammatory ones. Its cytoprotective effect in retinal pigment epithelium cells under high glucose conditions makes it a potential support in the treatment of diabetic retinopathy. Despite its benefits, poor solubility in water reduces its potential for therapeutic use, making it the biggest biopharmaceutical challenge. The design of diosmin-loaded nanocarriers for topical ophthalmic application represents a novelty that has not been yet explored. For this purpose, the response surface methodology (RSM) was used to optimize nanostructured lipid carriers (NLCs), compatible for ocular administration, to encapsulate diosmin and improve its physicochemical issues. NLCs were prepared by a simple and scalable technique: a melt emulsification method followed by ultrasonication. The experimental design was composed of four independent variables (solid lipid concentration, liquid lipid concentration, surfactant concentration and type of solid lipid). The effect of the factors was assessed on NLC size and PDI (responses) by analysis of variance (ANOVA). The optimized formulation was selected according to the desirability function (0.993). Diosmin at two different concentrations (80 and 160 µM) was encapsulated into NLCs. Drug-loaded nanocarriers (D-NLCs) were subjected to a physicochemical and technological investigation revealing a mean particle size of 83.58 ± 0.77 nm and 82.21 ± 1.12 nm, respectively for the D-NLC formulation prepared with diosmin at the concentration of 80 µM or 160 µM, and a net negative surface charge (−18.5 ± 0.60 and −18.0 ± 1.18, respectively for the two batches). The formulations were analyzed in terms of pH (6.5), viscosity, and adjusted for osmolarity, making them more compatible with the ocular environment. Subsequently, stability studies were carried out to assess D-NLC behavior under different storage conditions up to 60 days, indicating a good stability of NLC samples at room temperature. In-vitro studies on ARPE-19 cells confirmed the cytocompatibility of NLCs with retinal epithelium. The effect of D-NLCs was also evaluated in-vitro on a model of retinal inflammation, demonstrating the cytoprotective effect of D-NLCs at various concentrations. RSM was found to be a reliable model to optimize NLCs for diosmin encapsulation. Full article
(This article belongs to the Special Issue Advances in Formulation of Poorly Soluble Bioactive Compounds)
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