Synthesis and Chemical Characterization of a Polymeric Prodrug for Prolonged Release of Nitrofurazone

Abstract

Chitosan, a natural polysaccharide obtained from partial or total deacetylation of chitin, is a linear copolymer composed of β(1→4) linked N‐acetyl glucosamine and glucosamine monomer residues. Owing to its biological properties (such as biocompatibility, low toxicity, antimicrobial activity and haemostatic effect) chitosan has been widely exploited in the pharmaceutical industry to produce tablets, gels, nanoparticles and films. The aim of this study was to develop a polymeric prodrug for prolonged drug release of nitrofurazone (NF) on the skin, with chitosan as the carrier. The drug is conjugated to chitosan by means of ester bonds and the cleavage of these bonds by non‐specific cutaneous esterases provides the prolonged release of NF. This prodrug could be formulated in films or gels to accelerate wound healing, by acting as a physical barrier that prevents both loss of natural skin humidity and secondary microbial contamination, as well as to treat skin injuries caused by microorganisms susceptible to NF, whose antimicrobial spectrum is added to that of chitosan.

Abordagem da Latenciação de Fármacos como Ferramenta para Descoberta de novos Antichagásicos

“…O NFOH apresenta estabilidade in vitro, e é metabolizado em plasma (humano e de ratos) e também, provavelmente, pelo fígado. O NFOH, através dos estudos realizados, aliado à estabilidade química favorecida pela sua estrutura, é um potencial candidato a fármaco antichagásico para os estudos clínicos (SERAFIM, 2008;DAVIES et al, 2010;SANTOS;MATOS;FERREIRA, 2011).…”

Leishmanicidas potenciais: estudo da síntese de fármacos dirigidos dendriméricos de primeira geração com hidroximetilnitrofural

“…This compound also showed in vitro activity against Leishmania sp [10]. In murine model, this derivative was four times less toxic than its prototype.…”