BACKGROUND: Poly(lactide) (PLA) and its copolymer are a class of biodegradable polymer materials with good biocompatibility, which have been widely used for biodegradable sustained release drugs or targeted drug delivery systems.
OBJECTIVE: To explore the preparation method of the drug-loaded nanoparticles on entrapment rates (ER) and drug loading (DL) efficiency, and to determine the optimal preparation conditions using tocopheryl polyethylene glycol succinate (TPGS) as emulsifier, curcumin as a model drug and PLA as carriers.
METHODS: Curcumin loaded PLA nanoparticles (NPs) were prepared by an O/W emulsion-solvent evaporation method. The ER and DL were used as the main guiders. Singe factor test was used in order to find the effect of all kinds of parameters on the NP’s preparation, and then NP’s formulations were optimized by orthogonal design test.
RESULTS AND CONCLUSION: The optimal preparation conditions of NPs were determined through orthogonal experiment. The optimal technique parameters were followed: water to organic ratio of 10:1, polymer concentration of 15 g/L, drug concentration of 3 g/L, emulsifier TPGS concentration of 0.03%. NPs prepared under the optimum condition were spherical and smooth with narrow particle size distribution and sustained drug release. The mean diameter was 167.5 nm, the ER was 89.52%, and the DL was 13.72%. This preparation process is stable, simple and feasible, and the NPs with a highly ER, DL, and uniform size distribution can be prepared under optimal preparation conditions.