Technology research and quality assessment on prescription of imperatorin lipid microspheres by central composite design-response surface method / 中草药

ABSTRACT

Objective To optimize prescription and evaluate the quality of imperatorin lipid microspheres (ILM) by central composite design-response surface methodology (CCD-RSM), therefore to use the mean particle size, particle size distribution (polydispersity index, PDI) and Zeta potential as the primary indicator. Methods Mean particle size, particle size distribution and Zeta potential of lipid microspheres were measured to investigate the effect of the concentration of egg yolk lecithin, poloxamer and percentage of soybean oil in oil phase on the properties of ILM preparation. Mathematic relation between indicator and factor was constructed by binominal fitting. Then the response surface method according to the best mathematical model of evaluation indicators was used to make predictive analysis of the best prescription. Optimized prescription was used to prepare ILM and evaluate its quality. Results Optimized prescription was egg yolk lecithin 1.50 g, F68 0.35 g, and MCT 10 g. All items of optimized prescription were similar to target values. According to the optimized prescription, mean particle size of ILM was (165.00 ± 0.22) nm, particle size distribution was 0.046 ± 0.070, Zeta potential was (−30.30 ± 0.13) mV, encapsulation efficiency was about 90.09%, drug-loading rate was 1.0 mg/mL. Conclusion Due to the better predictability of constructed mathematical model, CCD-RSM can be applied to optimize prescription of lipid microspheres and the optimized ILM meet pharmacy requirements.