Carmen Anatolia Gafitanu1, Daniela Filip2, Corina Cernatescu3, Daniela Rusu4, Cristina Gabriela Tuchilus5, Doina Macocinschi2, Mirela-Fernanda Zaltariov6. 1. Department of Pharmaceutical Technology, Faculty of Pharmacy, "Gr. T. Popa" University of Medicine and Pharmacy, 16 Universităţii Street, 700115, Iaşi, Romania. 2. Laboratory of Polyaddition and Photochemistry, "Petru Poni" Institute of Macromolecular Chemistry, Aleea Gr. Ghica Vodă 41 A, 700487, Iaşi, Romania. 3. Department of Organic, Biochemical and Food Engineering, Faculty of Chemical Engineering and Environmental Protection, "Gheorghe Asachi" Technical University of Iaşi, Mangeron Avenue 73, 700050, Iaşi, Romania. 4. Polymer Materials Physics, "Petru Poni" Institute of Macromolecular Chemistry, Aleea Gr. Ghica Vodă 41 A, 700487, Iaşi, Romania. 5. Microbiology Department, Faculty of Medicine, "Gr. T. Popa" University of Medicine and Pharmacy, 16 Universităţii Street, 700115, Iaşi, Romania. 6. Department of Inorganic Polymers, "Petru Poni" Institute of Macromolecular Chemistry, Aleea Gr. Ghica Vodă 41 A, 700487, Iaşi, Romania. zaltariov.mirela@icmpp.ro.
Abstract
PURPOSE: Aim of this work was preparation of bioadhesive gel formulations based on Hydroxypropyl methylcellulose (HPMC), Poly(acrylic acid) (PAA) or Sodium alginate (SA) loaded with anise/fluconazole β-cyclodextrin inclusion complexes in 1:2 and 1:3 ratios intended for vaginal applications. METHODS: Freeze-drying method was effectively utilized and superporous morphology was obtained. The superporous morphology of the lyophilized gels, dynamic water vapor sorption measurements, drug release kinetics studies and their antimicrobial activities are presented. RESULTS: HPMC content influences especially the sorption/desorption behaviour of HPMC-based PAA gels and the morphology of the gel formulations with fluconazole/β-cyclodextrin inclusion complexes, due to the interactions among the gel networks absorbing water molecules. It was found that fluconazole release kinetics correspond to quasi-Fickian, Fickian diffusion and non-Fickian mechanisms for the studied hydrogels. The tested vaginal formulations with β-cyclodextrin inclusion complexes exhibited selectivity toward S. aureus ATCC 25923 and all tested Candida strains in comparison with the gel formulation without β-cyclodextrin. CONCLUSIONS: The fluconazole/β cyclodextrin inclusion complexes ensure a controlled release of fluconazole over a few days, the highest amount of drug release (92%) being observed after 43 h. These bioadhesive gel formulations could be very promising topical alternative for treatment of vaginal fungal infections.
PURPOSE: Aim of this work was preparation of bioadhesive gel formulations based on Hydroxypropyl methylcellulose (HPMC), Poly(acrylic acid) (PAA) or Sodium alginate (SA) loaded with anise/fluconazole β-cyclodextrin inclusion complexes in 1:2 and 1:3 ratios intended for vaginal applications. METHODS: Freeze-drying method was effectively utilized and superporous morphology was obtained. The superporous morphology of the lyophilized gels, dynamic water vapor sorption measurements, drug release kinetics studies and their antimicrobial activities are presented. RESULTS:HPMC content influences especially the sorption/desorption behaviour of HPMC-based PAA gels and the morphology of the gel formulations with fluconazole/β-cyclodextrin inclusion complexes, due to the interactions among the gel networks absorbing water molecules. It was found that fluconazole release kinetics correspond to quasi-Fickian, Fickian diffusion and non-Fickian mechanisms for the studied hydrogels. The tested vaginal formulations with β-cyclodextrin inclusion complexes exhibited selectivity toward S. aureus ATCC 25923 and all tested Candida strains in comparison with the gel formulation without β-cyclodextrin. CONCLUSIONS: The fluconazole/β cyclodextrin inclusion complexes ensure a controlled release of fluconazole over a few days, the highest amount of drug release (92%) being observed after 43 h. These bioadhesive gel formulations could be very promising topical alternative for treatment of vaginal fungal infections.
Entities:
Keywords:
antimicrobial activity; bioadhesive formulations; fluconazole release; vaginal gel
Authors: Mohammad A S Abourehab; Rahul R Rajendran; Anshul Singh; Sheersha Pramanik; Prachi Shrivastav; Mohammad Javed Ansari; Ravi Manne; Larissa Souza Amaral; A Deepak Journal: Int J Mol Sci Date: 2022-08-12 Impact factor: 6.208