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聚(β-羟基丁酸酯-羟基戊酸酯)微球在汉克斯缓冲液、新生牛血清、胰酶和合成胃液中的体外生物降解。

In vitro biodegradation of poly(beta-hydroxybutyrate-hydroxyvalerate) microspheres exposed to Hanks' 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 Biomater Sci Polym Ed. 1996;7(12):1075-84. doi: 10.1163/156856296x00561.

Abstract

Spherical BSA loaded microporous matrix type microspheres composed of P(HB-HV) blended with 20% PCL II and fabricated using 0/W emulsification with solvent evaporation have been incubated in Hanks' buffer, pH 7.4; newborn calf serum; 1.5% pancreatin and synthetic gastric juice over 30 days and their percentage weight loss (PWL) and changes in ultrastructural morphology monitored by gravimetry and SEM respectively. The greatest percentage weight loss was observed after incubation in newborn calf serum and decreased in the order newborn calf serum > pancreatin > synthetic gastric juice > Hanks' buffer. Only incubation in synthetic gastric juice and Hanks' buffer produced a significant increase in PWL with increasing theoretical percentage loading. Incubation in Hanks' buffer produced limited surface erosion leading to an increase in micropore diameter and the coalescence of micropores to from surface pits. With pancreatin, surface erosion led to the disappearance of surface micropores and a reduction in microsphere diameter. Subsequent fracturing of the microsphere surface facilitated the breakup of the matrix. In synthetic gastric juice there was little surface erosion and surface flaking and bulk erosion were responsible for the breakup of the matrix. In newborn calf serum, spherical shape was maintained despite a reduction in microsphere diameter. Bulk erosion in the form of large macroporous pits extending deep into the matrix gave the microspheres a hollow appearance. The enhanced biodegradation in NCS and significant surface erosion in pancreatin was assumed to be due to the effects of exogenous enzyme activity in addition to simple ester hydrolysis.

摘要

由20%聚己内酯II(PCL II)与聚(3-羟基丁酸酯-3-羟基戊酸酯)(P(HB-HV))共混制成的球形载牛血清白蛋白(BSA)微孔基质型微球,采用水包油(0/W)乳化溶剂蒸发法制备。将其在pH 7.4的汉克斯缓冲液、新生牛血清、1.5%胰蛋白酶和合成胃液中孵育30天,分别通过重量法和扫描电子显微镜(SEM)监测其失重百分比(PWL)和超微结构形态变化。在新生牛血清中孵育后观察到的失重百分比最大,失重顺序为新生牛血清>胰蛋白酶>合成胃液>汉克斯缓冲液。只有在合成胃液和汉克斯缓冲液中孵育时,随着理论负载百分比的增加,PWL显著增加。在汉克斯缓冲液中孵育导致有限的表面侵蚀,从而使微孔直径增加且微孔合并形成表面凹坑。用胰蛋白酶处理时,表面侵蚀导致表面微孔消失且微球直径减小。随后微球表面的破裂促进了基质的分解。在合成胃液中几乎没有表面侵蚀,表面剥落和整体侵蚀导致基质分解。在新生牛血清中,尽管微球直径减小,但仍保持球形。深入基质的大孔坑形式的整体侵蚀使微球呈现中空外观。推测在新生牛血清中增强的生物降解和在胰蛋白酶中的显著表面侵蚀是由于除了简单的酯水解外,外源性酶活性的作用。

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