Encapsulation of orlistat in biodegradable polymeric nanocapsules improves its antiproliferative effect against cervical cancer cells

• Autor(a) principal: Olegário, Isadora do Canto
• Data de Publicação: 2018
• Tipo de documento: Trabalho de conclusão de curso
• Idioma: eng
• Título da fonte: Repositório Institucional da UFRGS
• Texto Completo: http://hdl.handle.net/10183/264962
• topic: Farmácia; Fatty acid synthase; Nanocapsules; Orlistat; Cervical cancer

Orlistat is a drug that has been studied for having promising antitumor properties, since it has been discovered as an irreversible inhibitor of fatty acid synthase (FASN), the main enzyme responsible for de novo synthesis of fatty acids, which is overexpressed in different types of cancer. In this study, it was evaluated the antiproliferative effect of orlistat in its nanoencapsulated form (NC-ORL), using a biodegradable polymer, compared to the non-encapsulated drug solution (ORL) against the cervical cancer cell line HeLa. NC-ORL and unloaded nanocapsules (NC-U) were prepared by interfacial deposition of preformed polymer method, and showed mean diameters of about 211 nm and 217 nm, respectively, with an encapsulation efficiency of almost 100%. Cell counting by flow cytometry was used to evaluate cell number after 48 h of treatment. Initially, it was demonstrated that NC-U was not toxic to HeLa cells in the experimental conditions. Then, it was observed that NC-ORL had a more pronounced effect on cell number compared to ORL, especially at the higher concentrations tested, in which there was a significant decrease in the number of cells. In conclusion, this novel nanoformulation of orlistat showed greater antiproliferative effect against HeLa cells over the non-encapsulated drug solution, overcoming disadvantageous physicochemical proprieties like poor water solubility and low oral bioavailability related to ORL, and seems to be a promising alternative for the treatment of cervical cancer in the future.