Special Issue "Formulation of Poorly Water-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 December 2023 | Viewed by 734

Special Issue Editors

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China
Interests: poorly water-soluble drugs; crystalline/amorphous drugs; amorphous solid dispersions; nanocrystals; novel drug-delivery systems
Center for Nanomedicine and Department of Anesthesiology, Brigham and Women’s Hospital, Harvard Medical School, Boston, MA 02115, USA
Interests: lipid nanoparticles; zwitterionic micelles; drug conjugates; nanosuspensions
Department of Pharmacy, The Second Affiliated Hospital and Yuying Children’s Hospital of Wenzhou Medical University, Wenzhou 325027, China
Interests: targeted drug delivery; metabolsim modulation; membrane transporters; novel drug-delivery systems

Special Issue Information

Dear Colleagues,

In recent years, the emergence of poorly water-soluble drug candidates in the drug development pipeline has been a challenging issue for the pharmaceutical industry. Increasing the bioavailability of these drugs via the improvement of solubility/dissolution has become a major concern in the efforts to develop a reasonable dosing regimen for patients. Many delivery systems, such as cocrystals, nanocrystals, nanoparticles, inclusion complex, amorphous solid dispersions, and lipid-based formulations have been developed to overcome these problems. The use of novel methods not only increases the solubility and permeability of the poorly bioavailable drugs but also improves their stability and targeting efficacy. Moreover, in order to select the best approach some critical considerations must be taken into account, for example the physicochemical properties of the drug, the possibility to scale-up the production process, the toxicological considerations of the use of adjuvant, and the development of a more patient-friendly dosage form.

This Special Issue aims to collect groundbreaking studies and valuable reviews on the formulation of poorly water-soluble drugs. 

Prof. Dr. Qiang Fu
Dr. Xiangfei Han
Dr. Longfa Kou
Guest Editors

Manuscript Submission Information

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Keywords

  • poorly water-soluble drugs
  • solubility
  • dissolution enhancement
  • oral bioavailability
  • physico-chemical properties
  • drug delivery
  • formulation design
  • cocrystals
  • nanocrystals
  • inclusion complex
  • amorphous solid dispersions
  • nanoparticles
  • liposome
  • lipid-based formulations.

Published Papers (1 paper)

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Research

Article
Cocrystals Enhance Biopharmaceutical and Antimicrobial Properties of Norfloxacin
Pharmaceutics 2023, 15(9), 2211; https://doi.org/10.3390/pharmaceutics15092211 - 26 Aug 2023
Viewed by 470
Abstract
A solvate cocrystal of the antimicrobial norfloxacin (NFX) was formed by using isonicotinamide (INA) as a coformer with the solvent evaporation technique. The cocrystal formation was confirmed by performing solid-state characterization techniques. We evaluated the dissolution under supersaturated conditions and also the solubility [...] Read more.
A solvate cocrystal of the antimicrobial norfloxacin (NFX) was formed by using isonicotinamide (INA) as a coformer with the solvent evaporation technique. The cocrystal formation was confirmed by performing solid-state characterization techniques. We evaluated the dissolution under supersaturated conditions and also the solubility at the vertex of triphasic domain of cocrystal and NFX in both water and Fasted-State Simulated Intestinal Fluid (FaSSIF). The antimicrobial activity was evaluated using the microdilution technique. The cocrystal showed 1.8 times higher dissolution than NFX in water at 60 min and 1.3 times higher in FaSSIF at 180 min in the kinetic study. The cocrystal also had an increase in solubility of 8.38 times in water and 6.41 times in FaSSIF. The biopharmaceutical properties of NFX with cocrystallization improved antimicrobial action, as shown in the results of minimum inhibitory concentration (MIC) and inhibitory concentrations of 50% (IC50%) and 90% (IC90%). This paper presents, for the first time, a more in-depth analysis of the cocrystal of NFX–INA concerning its dissolution, solubility, and antimicrobial activity. In all these criteria, the cocrystal obtained better results compared to the pure drug. Full article
(This article belongs to the Special Issue Formulation of Poorly Water-Soluble Drugs)
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