Abstract
Nanoparticular combination chemotherapy with polymer-drug graft has been designed to overcome the limitations of traditional chemotherapy. In this purpose, all-trans retinoic acid (ATRA) grafted poly β-amino ester (ATRA-g-PBAE copolymer) was applied to encapsulate docetaxel (DTX) by the solvent displacement method and to make DTX loaded ATRA-g-PBAE nanoparticles (NPs). The size of NPs was optimized using response surface methodology (RSM). The size and zeta potential of NPs were measured by Zetasizer, and the morphology was evaluated by transmission electron microscopy (TEM). In vitro release was performed at pH 7.4 and 5.8. The anti-angiogenic effect, cytotoxicity, and blood compatibility of DTX loaded ATRA-g-PBAE NPs were investigated. The optimum size of the NPs was 137.9 ± 2.09 nm. The in vitro release of ATRA and DTX from NPs was pH-dependent, and it accelerated as pH decreased from 7.4–5.8. Results demonstrated that NPs had higher cytotoxicity and anti-angiogenic activity than that of free ATRA and DTX. In conclusion, biocompatible ATRA-g-PBAE NPs are a promising controlled released system for co-delivery of ATRA and DTX in chemotherapy.
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