3-羥基丁酸酯與3-羥基戊酸酯共聚物微粒製備與藥物制放

Preparation and Drug Delivery of Microspheres from 3-Hydroxybutyrate and 3-Hydroxyvalerate Copolymers

盧正慧(Jen-Hui Lu) ； 王賢達(Hsin-Ta Wang)

《臺北科技大學學報》 40卷1期 (2007/03) Pp. 123-135

https://doi.org/10.29768/JNTUT.200703.0011

摘要

本研究是以雙乳化(W1/O/W2)溶劑揮發法製備含小牛血清蛋白(BSA；bovin serum albumin)之3-羥基丁酸酯與3-羥基戊酸酯共聚物(PHBV；poly (3-hydroxybutric acid-co-3-hydroxyvaleric acid)微粒。製備參數包括乳化溫度、攪拌速度、BSA濃度、PHBV濃度、界面活性劑種類和界面活性劑濃度，以了解會對微粒產率、BSA含量、粒徑、表面形態和藥物制放的影響。
乳化溫度和攪拌速度的改變並未造成微粒產率、BSA含量和粒徑較大的變動。BSA濃度的降低和PHBV濃度的增加，造成BSA 含量和微粒產率的提升。PHBV的濃度增加也增大了粒徑。聚乙烯醇(PVA；polyvinyl alcohol)界面活性劑濃度的增加降低了粒徑和BSA含量，但增加了粒子表面孔洞性。山梨醇單油酸酯(Span 80；sorbitan monooleate)界面活性劑濃度的增加，降低了粒徑和BSA 含量，但增加了粒子表面平滑性。使用Pluronic F-68 界面活性劑降低了BSA含量。
含BSA微粒的制放曲線大致開始以較大的制放，隨後就是微緩的制放或是趨近於零的制放。微粒製備使用低濃度的PHBV、相對較高濃度的PVA或Pluronic F-68會有較高的BSA起始制放；使用Span 80界面活性劑製備的微粒，其BSA起始制放較小。使用低濃度PHBV製備微粒具有較多的孔洞，因而造成隨後BSA微緩制放。

關鍵字

3-羥基丁酸酯與3-羥基戊酸酯共聚物 ； 微粒 ； 雙乳化溶劑揮發法 ； 藥物制放

並列摘要

Microspheres of 3-hydroxybutyrate and 3-hydroxyvalerate copolymers (PHBV) containing bovine serum albumin (BSA) were prepared using double emulsion (W1/O/W2) solvent evaporation method. Temperature of emulsification, stirring velocity, concentrations of BSA and PHBV, and species of surfactants were varied for microsphere preparation. Yields of different preparation methods, BSA incorporation efficiency, average microsphere diameter, surface morphology of microspheres and BSA delivery were investigated.
BSA incorporation efficiency and average diameter of microspheres were not influenced by emulsification temperatures and stirring velocities in preparation. Higher BSA concentration used in microsphere preparation would not cause higher BSA incorporation. Higher PHBV concentration, polyvinyl alcohol(PVA) and sorbitan monooleate(Span 80) used as surfactants, applied in preparation gave higher yield and larger average diameter of microspheres. Higher concentrations of PVA and Span 80 used in formulation produced microspheres with lower BSA incorporation and average diameter. Both PVA and Span 80 used in preparation would give microspheres with much smooth surface. The use of Pluronic F-68 (PF-68) surfactant lowered BSA incorporation efficiency of microspheres.
The cumulative BSA release curves for microspheres showed two stages, a burst release and a slow release. Microspheres with different formulations would cause different level of burst release in two days. Microspheres prepared with both PVA and Span 80 surfactants displayed extensive release character in 10 days, and surface porosity of microspheres was believed to be the major reason of BSA release.

並列關鍵字

Poly 3-hydroxybutyrate-co-3-hydroxyvalerate ； Microsphere ； Double Emulsion Solvent Evaporation Method ； Drug Delivery