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Solano, Ana Gabriela Reis; de Fátima Pereira, Adriana; Pinto, Flavia Carmo Horta; Ferreira, Letícia Gonçalves Resende; de Oliveira Barbosa, Leandro Augusto; Fialho, Silvia Ligório; de Oliveira Patricio, Patrícia Santiago; da Silva Cunha, Armando; da Silva, Gisele Rodrigues; Pianetti, Gérson Antônio
AAPS PharmSciTech, 06/2013, Volume: 14, Issue: 2Journal Article
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.
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