Thermosensitive hydrogels for vaginal delivery of secnidazole as an approach to overcome the systemic side-effects of oral preparations.

Autor: Argenta DF; Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Campus Reitor João David Ferreira Lima, s/n - Trindade, Florianópolis - SC, 88040-900, Brazil., Bernardo BDC; Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Campus Reitor João David Ferreira Lima, s/n - Trindade, Florianópolis - SC, 88040-900, Brazil., Chamorro AF; Department of Chemistry, Federal University of Santa Catarina, Campus Reitor João David Ferreira Lima, s/n - Trindade, Florianópolis - SC, 88040-900, Brazil., Matos PR; Department of Civil Engineering, Federal University of Santa Catarina, Campus Reitor João David Ferreira Lima, s/n - Trindade, Florianópolis - SC, 88040-900, Brazil., Caon T; Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Campus Reitor João David Ferreira Lima, s/n - Trindade, Florianópolis - SC, 88040-900, Brazil. Electronic address: thiagocaon@gmail.com.
Jazyk: angličtina
Zdroj: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2021 Apr 01; Vol. 159, pp. 105722. Date of Electronic Publication: 2021 Jan 19.
DOI: 10.1016/j.ejps.2021.105722
Abstrakt: Secnidazole (SEC) has been suggested as an alternative agent against Trichomonas vaginalis to overcome the adverse effects, antimicrobial resistance problems and poor adherence to the currently available therapy. Once no topical formulation may be found in the market until now, SEC was incorporated in thermosensitive bioadhesive systems to extend the contact time in the mucosa and to avoid a systemic drug disposition. Formulations containing 20% poloxamer 407, 1% poloxamer 188 and 1 or 2.5% chitosan showed suitable sol-gel transition temperature (> 30 °C), presenting a fast gelation time (100-115 s). Rheological, dynamic light scattering and infrared spectroscopy analysis suggested molecular interactions among polymers. Chitosan increased the mucoadhesion strength of the formulations. In addition, hydrogels showed a tendency to decrease the drug transport rate through mucosa when compared to the control. Mucin was also added onto mucosa for a more realistic simulation of permeability/retention. In the presence of this agent, hydrogels containing chitosan reduced the permeability/retention of the drug in approximately 2.0-fold when compared to the control. Therefore, the hydrogels presented suitable characteristics to remain in the vaginal environment, which would result in effective local treatment of trichomoniasis.
(Copyright © 2021. Published by Elsevier B.V.)
Databáze: MEDLINE
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