响应面法优化松多酚微粒制备工艺

Optimization of Preparation Process for Pinecone Polyphenol Microparticles by Response Surface Methodology

依据聚电解质自组装原理,利用黑木耳多糖酸性片段(acidic polysaccharide fragments from Auricularia auricula,AAP)和多聚赖氨酸(polylysine,PLL)将松多酚(pine polyphenols from Pinuskoraiensis,PPH)包裹为微粒以防止胃环境对多酚类化合物结构的破坏,并且采用响应面试验设计优化制备工艺。通过分析AAP、PLL和PPH的质量浓度3个因素及其交互作用对PPH微粒包埋率的影响,建立该工艺的二次多项数学模型;利用扫描电镜观察优化后PPH微粒的形貌,并在模拟胃肠道环境中检测多酚释放率。结果显示响应面回归方程拟合性良好,AAP、PLL和PPH的质量浓度对响应值均有显著影响。在AAP质量浓度为900μg/mL、PPH质量浓度为110μg/mL以及PLL质量浓度为30μg/mL的条件下,PPH微粒的包埋率为(86.57±1.07)%,载药量为(24.03±0.81)%。扫描电镜观察表明PPH微粒的直径为200～500 nm,其在模拟胃环境中释放缓慢而在模拟肠道环境中释放迅速。本研究中PPH微粒包埋率的实测值与预测值相比,相对误差较低,说明本研究方法是一种适合PPH微粒制备的方法,并且优化后的PPH微粒可以降低胃环境对PPH的降解。

In order to minimize the degradation of pinecone polyphenols in the stomach, pinecone polyphenols from Pinus koraiensis(PPH) were encapsulated by acidic polysaccharide fragments from Auricularia auricula(AAP) and polylysine(PLL) according to the principle of polyelectrolyte self-assembly, and response surface methodology was used to optimize the preparation process. The effect of AAP, PLL and PPH concentration as well as interaction between them on the encapsulation ef?ciency was evaluated. As a result, a quadratic polynomial model was established describing the process. Scanning electron microscopy(SEM) was used to investigate the morphology of the microparticles prepared under optimized conditions, and the release rate was studied in simulated gastrointestinal environment. The results showed that the?tness of the model was good. All of the three variables had signi?cant effects on the response. The encapsulation ef?ciency of polyphenol microparticles were(86.57 ± 1.07)% and the drug loading was(24.03 ± 0.81)% at 900 μg/mL AAP, 30 μg/mL PLL and 110 μg/mL PPH concentration. The diameter of the microparticles was 200–500 nm. They were released slowly in simulated gastric environment but rapidly in simulated intestinal environment. The measured encapsulation ef?ciency matched with the predicted value, indicating that response surface methodology was a suitable method for optimizing the preparation of pinecone polyphenol microparticles. The degradation of pinecone polyphenol microparticles in the stomach environment was decreased relative to free pine polyphenols.