Preparation and in vitro release of tripterygium glycosides-loaded nanoparticles modified by chitosan / 中草药

ABSTRACT

Objective: To prepare tripterygium glycosides-loaded nanoparticles modified by 50% N-acetylated low molecular weight chitosan (LMWC-TG-NPs) and to investigate their in vitro release behavior. Methods: The LMWC-TG-NPs were prepared by modified self-emulsifying solvent diffusion method; The formulation of TG-NPs was optimized by orthogonal design and the modified condition of LMWC was determined based on the single factor analysis. The in vitro drug release of LMWC-TG-NPs was characterized with PBS (pH 7.4) containing 20% ethanol. Results: The optimized formulation of TG-NPs was as follows: Poloxamer 188 (1.0%), PLA (80 mg), organic phase (12 mL), and acetone-ethanol (2:3) were used to prepare TG-NPs suspension. The LMWC-TG-NPs were prepared by incubating TG-NPs suspension with 10% LMWC solution at the ratio of 1:1. The shape of the prepared LMWC-TG-NPs was spherical. The mean particle size, polydispersity index, entrapment efficiency, and drug loading were (207.6 ± 3.4) nm, 0.078 ± 0.009, (61.83 ± 2.43)%, and (10.70 ± 0.37)% (n=3), respectively. The in vitro release characteristics of LMWC-TG-NPs conform to Higuchi equation in PBS buffer composed of 20% ethanol at pH 7.4. Conclusion: The prepared LMWC-TG-NPs show a sustained-release characteristics with well-distributed particle size as well as high entrapment efficiency and drug loading, which could lay the foundation for the research on kidney targeting and toxicity.