纳米蛹虫草活性肽靶向型微囊制备工艺和性能研究

Preparation technology and properties of active peptide targeting microcapsules from nano-cordyceps militaris

为研究纳米蛹虫草活性肽靶向型微囊的制备工艺及性能情况,分别以明胶、乙基纤维素、聚乳酸(PLA)为囊材制备蛹虫草肽微囊。以包封率、载药量及48 h的释药量为主要指标做评价,在单因素试验的基础上采用响应面法对微囊制备工艺进行优化,对微囊进行了包封率、成球率、载药量、平均粒径测定,电镜形态观察,红外光谱分析,稳定性分析及毒性分析,利用3T3-L1脂肪细胞胰岛素抵抗模型进行了降血糖活性检测试验。结果表明:以聚乳酸为囊材制备蛹虫草肽微囊性能最优,在PVA质量分数为3.56%,温度为40.8℃,PLA质量分数为8.11%,油水比为1∶8时蛹虫草肽聚乳酸微囊包封率可达到87.2%±0.02%,成球率为86.90%,载药量为58%。聚乳酸微囊圆而规整,平均粒径为50.4μm,电镜下观察聚乳酸微囊外形椭圆,表面光滑,包封率良好,符合微囊要求。降血糖活性检测试验证实纳米蛹虫草活性肽靶向型微囊具有一定的降血糖作用,且稳定无毒。

In order to study the preparation process and performance of active peptide-targeted microcapsules from nanometer Cordyceps militaris, in this experiment, Cordyceps militaris peptide microcapsules were prepared with gelatin, ethyl cellulose and polylactic acid(PLA) as capsule materials respectively. Taking the encapsulation efficiency, drug loading and drug release in 48 hours as the main indicators for evaluation, on the basis of single factor test, the preparation process of microcapsules was optimized by response surface methodology. The encapsulation efficiency, spheroidization rate, drug loading, average particle size, morphology observation by electron microscope, infrared spectrum analysis, stability analysis and toxicity analysis were carried out on the microcapsules. 3 T3-L1 adipocyte insulin resistance model was used to detect hypoglycemic activity. The results showed that the preparation of Cordyceps militaris peptide microcapsules with polylactic acid as the capsule material has the best performance, when the PVA concentration is 3.56%, the temperature is 40.8 ℃, the PLA concentration is 8.11%, and the oil-water ratio is 1:8. The encapsulation rate can reach 87.2%±0.02%, the spheroidization rate is 86.90%, and the drug loading is 58%. The polylactic acid microcapsules are round and regular, with an average particle size of 50.4 μm. The polylactic acid microcapsules are oval in shape, smooth in surface, and good in encapsulation efficiency, meeting the requirements of microcapsules. The hypoglycemic activity detection test confirmed that the active peptide-targeted microcapsules from nano-Cordyceps militaris have a certain hypoglycemic effect, and are stable and non-toxic.