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聚羟基丁酸酯-羟基戊酸酯微胶囊在汉克斯缓冲液、新生小牛血清、胰蛋白酶和合成胃液中的体外生物降解。

In vitro biodegradation of polyhydroxybutyrate-hydroxyvalerate microcapsules exposed to Hank's buffer, newborn calf serum, pancreatin and synthetic gastric juice.

作者信息

Atkins T W, Peacock S J

机构信息

Department of Pharmaceutical and Biological Sciences, Aston University, Birmingham, UK.

出版信息

J Microencapsul. 1997 Jan-Feb;14(1):35-49. doi: 10.3109/02652049709056466.

DOI:10.3109/02652049709056466
PMID:8994074
Abstract

Spherical microporous reservoir-type microcapsules, fabricated using a W/O/W double emulsion technique with solvent evaporation and composed of 330 kD poly(beta-hydroxybutyrate-hydroxyvalerate (P(HB-HV)) (10.8% HV)/20% PCL II containing a range of bovine serum albumin (BSA) loadings, were incubated in Hank's buffer, pH 7.4, newborn calf serum (NCS), 1.5% pancreatin and synthetic gastric juice containing 10% pepsin over 30 days, and their percentage weight loss (PWL) and change in ultrastructural morphology monitored by gravimetry and stereoscan electron microscopy (SEM), respectively. The greatest percentage weight loss from microcapsules was observed after incubation in NCS and decreased in the other NCS > pancreatin > synthetic gastric juice > Hank's buffer. Only 5, 10 and 15% bovine serum albumin (BSA) loaded microcapsules incubated in Hank's buffer and synthetic gastric juice showed a significant increase in PWL with increasing percentage BSA loading. The overall sequence of changes in structural morphology due to biodegradation occurred at different rates in the different 'physiological' media. An initial increase in micropore diameter was followed by the coalescence of microspores to form macroporous pits (Hank's buffer). Further biodegradation in NCS, pancreatin and synthetic juice was characterized by significant surface and bulk erosion. Only in pancreatin and NCS did biodegradation proceed to a loss of spherical shape and partial (pancreatin) and almost total (NCS) disruption of microcapsule structure after 30 days.

摘要

采用W/O/W双乳液技术结合溶剂蒸发法制备的球形微孔储库型微胶囊,由330 kD的聚(β-羟基丁酸-羟基戊酸)(P(HB-HV))(10.8% HV)/20%聚己内酯II组成,含有一系列不同牛血清白蛋白(BSA)负载量,将其在pH 7.4的汉克斯缓冲液、新生小牛血清(NCS)、1.5%胰蛋白酶和含10%胃蛋白酶的合成胃液中孵育30天,分别通过重量法和立体扫描电子显微镜(SEM)监测其失重百分比(PWL)和超微结构形态的变化。微胶囊在NCS中孵育后失重百分比最大,在其他介质中的失重情况为NCS>胰蛋白酶>合成胃液>汉克斯缓冲液。仅在汉克斯缓冲液和合成胃液中孵育的负载5%、10%和15%牛血清白蛋白(BSA)的微胶囊,其PWL随BSA负载百分比的增加而显著增加。在不同的“生理”介质中,由于生物降解导致的结构形态变化的总体顺序以不同速率发生。最初微孔直径增加,随后微球合并形成大孔坑(汉克斯缓冲液)。在NCS、胰蛋白酶和合成胃液中的进一步生物降解的特征是显著的表面和整体侵蚀。仅在胰蛋白酶和NCS中,30天后生物降解导致微胶囊失去球形形状,并部分(胰蛋白酶)和几乎完全(NCS)破坏微胶囊结构。

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