Abstract:

BACKGROUND: Polylactide-co-glycolide (PLGA) nanoparticles or nano-preparation of biodegradable microspheres for sustained release or targeted delivery system have been studied for almost 30 years, considered as a hot spot of research. The system can control the particle size, delay drug degradation, prolong drug release time, conduct targeted release, reduce drug toxicity and irritation.
OBJECTIVE: To explore the preparation method of the drug-loaded nanoparticles on particle size, encapsulation efficiency and other effects, and to determine the optimal preparation conditions using paclitaxel as a model drug and PLGA as the coating material.
METHODS: PLGA nanoparticles were prepared using emulsion-solvent evaporation technique. The particle size of nanoparticles was measured, and the encapsulation efficiency and drug loading of the nanoparticles were calculated. The preparation techniques of nanoparticles were optimized by orthogonal method.
RESULTS AND CONCLUSION: Through orthogonal test, the preparation techniques of nanoparticles were optimized. The optimization parameters are 15 minutes ultrasonic emulsification, 1% concentration of emulsifier, organic to water ratio of 1: 25, temperature 25 ℃. Under these conditions, the prepared nanoparticles size was 217.6 nm, drug loading was 1.79%, encapsulation efficiency was 85%. The preparation process is simple, stable and optimized. The paclitaxel-PLGA appropriate nanoparticles can be prepared at a high entrapment efficiency and suitable particle size.