以聚氰基丙烯酸丁基酯製高水溶性藥品奈米載藥粒子方法與物化性質的研究探討

Study on nanoparticle containing high water soluble drug prepared by poly butyl caynoacrylate

田適豪(Shih-Hao Tien)

指導教授 ： 詹道明

高雄醫學大學/藥學院/藥學研究所/碩士(2010年)

摘要

以聚氰基丙烯酸丁基酯（poly (butyl cyanoacrylate)，PBCA）為材質之奈米顆粒。經由乳劑的界面聚合反應可以合成具間格架構的奈米粒子。以PBCA單體進行界面聚合反應，合成包覆水溶性藥物pyridostigmine bromide的PBCA奈米粒子。本研究希望藉由修改奈米粒子製備的方法，配合以混合分散溶劑、聚合物單體進行的混合試驗設計。希望藉此提高奈米粒子的包埋率與載藥率。同時檢視製劑上的變因及對模式藥在體外釋出的影響，藉此評估所製備之奈米粒子作為藥物載體的可行性。
PBCA粒子經由不同製備方法中，透過含有聚合單體奈米液滴系統的預先製備，可以發現粒徑大小與載藥率並沒有正相關關係。可能起因於聚合物單體在系統中呈現不同結構的液晶相（liquid crystal），而並非以單純球狀結構存在。經由W卅O卅W 乳化溶劑法製備的 PB PBCA 粒子有明顯控釋效果，由奈米粒子的體外釋離結果，可知改變預先配製奈米液滴系統的組成比例，除了對所形成奈米粒子之粒徑、包埋率、載藥率等有所影響外，對於藥物從粒子中釋離的速率也有會影響。最後透過Mixture Design試驗設計模型預測最佳化處方，可觀察到在粒徑、包埋率、載藥率等均有符合預測相對優秀的表現。

關鍵字

氰基丙烯酸烷基酯 ； 混合試驗

並列摘要

polymerization can be synthesized with the interface of templates droplet using poly butyl cyanoacrylate, PBCA, as the material. Water - soluble drugs pyridostigmine bromide is entrapped because of monomer working throughout the droplet. This study focuses on modification of the preparation of nanoparticle. Mixture experimental design gives an easy way to realize optimal formulation and increasing encapsulation efficiency of nanoparticle and drug loading. In order to assess the PBCA nanoparticle as a drug delivery, Study try to figure out variables of the preparation process how to affect drug release in vitro. There are different methods to prepare PBCA particles. In this study, droplet system containing monomer, pre-preparation, lead to all the result show non positive correlation between the particle size and drug loading. Polymer monomer present in the system with different structures of liquid crystal, rather than to simply spherical structure. PB PBCA particles show significant extended release in dissolution tests. Change to the system of pre-prepared droplet composition not only affecting particle size, EE%, DL% but release of drug. Optimal formulation prediction exported from model of Mixture Design, is observed a relatively good performance in line with expectations.

並列關鍵字

Alzheimer's disease ； caynoacrylate ； mixture desgn ； pyridostigmine bromide

參考文獻

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