The efficacy of bergenin prepared with osmotic-pump-controlled release is much lower than expected. In this study, biodegradable polylactic acid is used to modify bergenin and immobilize it with chemical methods. Bergenin-PLA obtained by this method has low molecular weight and good thermal stability, as well as prolonged in vitro release time along with increased molecular weight. Biocompatibility tests and in vitro antitumor tests showed that bergenin-PLA at a ratio of 1:30 has good biological properties and low cytotoxicity at t three concentrations, and its antitumor activity was significantly increased compared to bergenin. The chemical immobilization of bergenin not only provides a good mode of administration for patients but also provides a good foundation for the sustained release of drugs over time.
Keywords: Antineoplastic activity; Bergenin; Bergenin-polylactic acid; Blood compatibility; Controlled-release; l-Lactic acid O-carboxyanhydrides.
Copyright © 2018 Elsevier B.V. All rights reserved.