Chitosan hydrogels containing nanoencapsulated phenytoin for cutaneous use: Skin permeation/penetration and efficacy in wound healing

Author(s):Show less -

Cardoso, Aline Marquez ^[1] ; de Oliveira, Edilene Gadelha ^[1] ; Coradini, Karine ^[1] ; Bruinsmann, Franciele Aline ^[1] ; Aguirre, Tanira ^[2] ; Lorenzoni, Ricardo ^[1] ; Silva Barcelos, Raquel Cristiane ^[3] ; Roversi, Karine ^[3] ; Rossato, Domenika Rubert ^[3] ; Pohlmann, Adriana Raffin ^{[4, 1]} ; Guterres, Silvia Staniscuaski ^[1] ; Burger, Marilise Escobar ^[3] ; Ruver Beck, Ruy Carlos ^[1]

Affiliation

^[1] Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS - Brazil

^[2] Univ Fed Ciencias Saude Porto Alegre, Programa Posgrad Biociencias, BR-90050017 Porto Alegre, RS - Brazil

^[3] Univ Fed Santa Maria, Dept Farmacol, Programa Posgrad Farmacol, BR-97105900 Santa Maria, RS - Brazil

^[4] Univ Fed Rio Grande do Sul, Inst Quim, Dept Quim Organ, BR-91501970 Porto Alegre, RS - Brazil

• Document type: Journal article
• Source: Materials Science & Engineering C-Materials for Biological Applications; v. 96, p. 205-217, MAR 2019.
• Web of Science Citations: 8

Abstract

Although phenytoin is an antiepileptic drug used in the oral treatment of epilepsy, its off-label use as a cutaneous healing agent has been studied in recent years due to the frequent reports of gingival hyperplasia after oral administration. However, the cutaneous topical application of phenytoin should prevent percutaneous skin permeation. Therefore, the aim of this study was to evaluate the in vitro skin permeation/retention and in vivo effects of nanocapsules and nanoemulsions loaded with phenytoin and formulated as chitosan hydrogels on the healing process of cutaneous wounds in rats. The hydrogels had adequate pH values (4.9-5.6) for skin application, drug content of 0.025% (w/w), and non-Newtonian pseudoplastic rheological behaviour. Hydrogels containing nanocapsules and nanoemulsions enabled improved controlled release of phenytoin and adhesion to skin, compared with hydrogels containing non-encapsulated phenytoin. In vitro skin permeation studies showed that phenytoin permeation to the receptor compartment, and consequently the risk of systemic absorption, may be reduced by nanoencapsulation without any change in the in vivo performance of phenytoin in the wound healing process in rats. (AU)

• FAPESP's process: 14/50928-2 - INCT 2014: Pharmaceutical Nanotechnology: a transdisciplinary approach
• Grantee: Maria Vitória Lopes Badra Bentley
• Support Opportunities: Research Projects - Thematic Grants