Xie Yunchang, Yi Yueneng, Hu Xiongwei, Shangguan Mingzhu, Wang Lijuan, Lu Yi, Qi Jianping, Wu Wei
a Key Laboratory of Smart Drug Delivery of PLA and Ministry of Education , School of Pharmacy, Fudan University , Shanghai , China.
Pharm Dev Technol. 2016 Sep;21(6):672-9. doi: 10.3109/10837450.2015.1045616. Epub 2015 May 13.
The development of polymeric carriers loaded with extracts suffers from the drawback not to be able to incorporate simultaneously various pharmacological compounds into the formulation. The aim of this study was therefore to achieve synchronous microencapsulation of multiple components of silymarin into poly (lactic-co-glycolic acid) nanoparticle, the most commonly used polymeric carrier with biodegradability and safety. The main strategy taken was to improve the overall entrapment efficiency and to reduce the escaping ratio of the components of different physicochemical properties. The optimized nanoparticles were spherical in morphology with a mean particle size of 150 ± 5 nm. Under common preparative conditions, silybin and isosilybin were entrapped in high efficiency, whereas taxifolin, silychristin and silydianin, especially taxifolin, showed less entrapment because they were more hydrophilic. By changing the pH of the outer aqueous phase and saturating it with silymarin, the entrapment efficiency of taxifolin, silychristin and silydianin could be significantly improved to over 90%, the level similar to silybin and isosilybin, thereby achieving synchronous encapsulation. It could be concluded that synchronous encapsulation of multiple components of silymarin was achieved by optimizing the preparative variables.
负载提取物的聚合物载体的发展存在一个缺点，即无法将多种药理化合物同时纳入制剂中。因此，本研究的目的是将水飞蓟素的多种成分同步微囊化到聚（乳酸 - 乙醇酸）纳米颗粒中，这是最常用的具有生物可降解性和安全性的聚合物载体。所采用的主要策略是提高整体包封效率，并降低不同理化性质成分的逃逸率。优化后的纳米颗粒呈球形，平均粒径为150±5nm。在常规制备条件下，水飞蓟宾和异水飞蓟宾的包封效率较高，而紫杉叶素、水飞蓟亭和水飞蓟宁，尤其是紫杉叶素，由于它们更具亲水性，包封率较低。通过改变外部水相的pH值并用西利马林使其饱和，紫杉叶素、水飞蓟亭和水飞蓟宁的包封效率可显著提高到90%以上，达到与水飞蓟宾和异水飞蓟宾相似的水平，从而实现同步包封。可以得出结论，通过优化制备变量实现了水飞蓟素多种成分的同步包封。
