title: Development and evaluation of sustained-release etoposide-loaded poly(ε-caprolactone) implants.
abstract: Poly(ε-caprolactone) implants containing etoposide, an important chemotherapeutic agent and topoisomerase II inhibitor, were fabricated by a melt method and characterized in terms of content uniformity, morphology, drug physical state, and sterility. In vitro and in vivo drug release from the implants was also evaluated. The cytotoxic activity of implants against HeLa cells was studied. The short-term tolerance of the implants was investigated after subcutaneous implantation in mice. The original chemical structure of etoposide was preserved after incorporation into the polymeric matrix, in which the drug was dispersed uniformly. Etoposide was present in crystalline form in the polymeric implant. In vitro release study showed prolonged and controlled release of etoposide, which showed cytotoxicity activity against HeLa cells. After implantation, good correlation between in vitro and in vivo drug release was found. The implants demonstrated good short-term tolerance in mice. These results tend to show that etoposide-loaded implants could be potentially applied as a local etoposide delivery system.
authors.affiliation: Department of Pharmaceuticals Products, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil. anagabriela@ufsj.edu.br
authors.forename: Ana Gabriela Reis
authors.initials: AG
authors.lastname: Solano
authors.forename: Adriana
authors.initials: A
authors.lastname: de Fátima Pereira
authors.forename: Flavia Carmo Horta
authors.initials: FC
authors.lastname: Pinto
authors.forename: Letícia Gonçalves Resende
authors.initials: LG
authors.lastname: Ferreira
authors.forename: Leandro Augusto
authors.initials: LA
authors.lastname: de Oliveira Barbosa
authors.forename: Silvia Ligório
authors.initials: SL
authors.lastname: Fialho
authors.forename: Patrícia Santiago
authors.initials: PS
authors.lastname: de Oliveira Patricio
authors.forename: Armando da Silva
authors.initials: Ada S
authors.lastname: Cunha
authors.forename: Gisele Rodrigues
authors.initials: GR
authors.lastname: da Silva
authors.forename: Gérson Antônio
authors.initials: GA
authors.lastname: Pianetti
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004343:Drug Implants; D005047:Etoposide / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D011091:Polyesters / Q000737:chemistry* / Q000633:toxicity; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004343:Drug Implants; D011091:Polyesters; C016240:polycaprolactone; D005047:Etoposide