Formulation Optimization of Hydrophobically-Pullulan Nanoparticles by Box-Behnken Response Surface Methodology / 中国药学杂志

ABSTRACT

OBJECTIVE: To optimize the preparation of self-assembled doxorubicin-loaded cholesterol-modified pullulan nanoparticles(DOX-CHSP-SAN) by response surface methodology. METHODS: DOX-CHSP-SAN was prepared by dialysis method with the amphiphilic carrier of cholesterol-modified pullulan (CHSP) and the model drug of doxorubicin(DOX). Box-Behnken Design (BBD) response surface method was used to optimize the preparation process of DOX-CHSP-SAN. The morphology, average particle size, Zeta potentia, the encapsulation efficiency, drug loading of doxorubicin and the drug release characteristics in vitro were determined. RESULTS: The optimized DOX-CHSP-SAN has a round spherical shape with an average particle size of (117.1±3.4) nm, PDI of (0.205±0.023), Zeta potential of (-26.1±0.135) mV, the encapsulation efficiency was (68.17±0.93)%, and the drug loading was (6.84±0.47)%. The in vitro release behavior in PBS of pH 7.4 was consistent with the Weibull equation. CONCLUSION The DOX-CHSP-SAN prepared by the dialysis method and optimized by the response surface method is round and smooth, the particle size is small and uniform, the encapsulation efficiency and the drug loading amount are high, and the in vitro release has the sustained release characteristics.