Formulation Optimization For High Drug Loading Colonic Drug Delivery Carrier

文献类型： 外文期刊

第一作者： Wang, Yichao

作者： Wang, Yichao;Li, Puwang;Kong, Lingxue;Peng, Zheng;Luo, Yongyue

作者机构：

关键词： 5-Fluorouracil (5-FU);PLGA;optimization;nanoparticles

期刊名称：2010 3RD INTERNATIONAL CONFERENCE ON BIOMEDICAL ENGINEERING AND INFORMATICS (BMEI 2010), VOLS 1-7

ISSN： 1948-2914

年卷期： 2010 年

页码：

收录情况： SCI

摘要： High drug loading (DL) carrier is an effective way to cure the cancerous cells. High drug loading is also one of the key issues in the drug delivery research, especially the colonic drug delivery system by oral administration. The times of drug intake could be remarkably reduced if high drug loading carriers are administered. At the same time, the related formulation materials could be effectively utilized. One major obstacle with the preparation of this system is the difficulty to encapsulate the hydrophilic drug into hydrophobic encapsulation polymer. A design of high drug loading delivery system with biodegradable, biocompatible materials and optimization of the fabrication process is a potential solution to solve the problem. So in this research, 5-Fluorouracil (5-FU) loaded Poly (lactide-co-glycolide) (PLGA) nanoparticles were prepared by double emulsion and solvent evaporation method. Several fabrication parameters including theoretical drug loading, volume ratio of outer water phase to the first emulsion, pH value of outer aqueous phase and emulsifier PVA concentration were optimized to get a high drug loading nanoparticles. The result shows that with the increase of theoretical drug loading, the actual drug loading increased gradually. When adjusted the pH value of outer aqueous phase to the isoelectric point (8.02) of 5-Fluorouracil, the drug loading exhibited a higher one compared to other pH value solution. Relative higher volume ratio of outer water phase to the first emulsion was also beneficial for the enhancement of drug loading. But the nanoparticles size increased simultaneously due to the lower shearing force. When increased the PVA concentration, the drug loading showed an increase first and following a drop.

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