Preparation and properties of docetaxel-loaded nanobubbles / 国际药学研究杂志

ABSTRACT

Objective To optimize the formulation and preparation technology of docetaxel (DTX)-loaded nanobubbles, and evaluate their properties. Methods The best ratio of methoxypoly(ethylene glycol)-poly(.DL-lactide-co-glycolide) (mPEG-PLGA) and different membrane stabilizers were optimized with Langmuir membrane balance. DTX-Loaded nano-micelles were encapsulated by mPEG-PLGA with an injection method. Nanoemulsions was formed after being added with perfluoropentane (PFP, the boiling point of 29.5 °C) as the organic phase. The formulations and preparation techniques of nanoemulsions were optimized and the conditions of nanobubbles formulaion was also evaluated. Cytotoxicity of DTX-loaded nanobubbles on MCF-7 cells was evaluated with the MTT method. Results The best ratio of mPEG-PLGA and Span 20 was 10: 1 (mol/mol). The membrane elasticity of the prepared nanobubbles with optimized formulations and the preparation techniques was good. In addition, they were obviously temperature-sensitive and ultrasonic-sensitive. The particle size of nanobubbles increased with higher temperature and decreased with lower temperature. The size of nanobubbles increased upon ultrasound application and then decreased a little. The cytotoxicity of DTX-loaded nanobubbles on MCF-7 cells was obvious and dose-dependent. Conclusion DTX-Loaded nanobubbles are a novel formulation with tumor-targeted and ultrasound-sensitive drug release.