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一种用于生物粘附性微球分析的微张力计。

A microtensiometer for the analysis of bioadhesive microspheres.

作者信息

Chickering D E, Harris W P, Mathiowitz E

机构信息

Department of Molecular Pharmacology and Biotechnology, Brown University, Providence, Rhode Island 02912, USA.

出版信息

Biomed Instrum Technol. 1995 Nov-Dec;29(6):501-12.

PMID:8574265
Abstract

Bioadhesive polymer microspheres are potential vehicles for the delivery of bioactive agents to mucosal tissues. Bioadhesive delivery devices could improve drug absorption, enhance bioavailability, and increase patient compliance by minimizing dosing regimens. Identification of bioadhesive materials is the first phase in developing bioadhesive drug delivery systems. Additionally, quantification and analysis of the bioadhesive event are essential to successful development of a new generation of adhesive delivery systems. A unique, microbalance-based instrument was developed to analyze bioadhesive forces between polymer microspheres and mucosal tissue segments. A contact angle analyzer, with a custom-made physiologic tissue chamber, was linked to a computer via the serial port. Software was used to modify the microbalance operation to behave as a microtensiometer with a sensitivity of 0.1 microN. After mounting a microsphere and tissue segment in the balance and adjusting the experimental settings, the instrument performs a tensile experiment and automatically determines the following parameters: compressive deformation, peak compressive load, compressive work, yield point, deformation to yield, returned work, peak tensile load, deformation to peak tensile load, fracture strength, deformation to failure, and tensile work. Using this device the authors identified several bioadhesive materials ideally suited for orally-delivered, controlled-release systems. GI-transit studies in rats showed strong correlation between increased GI-residence time and strong bioadhesive interactions.

摘要

生物黏附性聚合物微球是将生物活性剂递送至黏膜组织的潜在载体。生物黏附性给药装置可通过减少给药方案来改善药物吸收、提高生物利用度并增加患者顺应性。生物黏附材料的鉴定是开发生物黏附性药物递送系统的第一阶段。此外,生物黏附事件的定量和分析对于新一代黏附性递送系统的成功开发至关重要。开发了一种独特的、基于微量天平的仪器来分析聚合物微球与黏膜组织片段之间的生物黏附力。一台配备定制生理组织腔室的接触角分析仪通过串口与计算机相连。使用软件对微量天平的操作进行修改,使其作为一台灵敏度为0.1微牛顿的微张力计。在将一个微球和组织片段安装到天平上并调整实验设置后,该仪器进行拉伸实验并自动确定以下参数:压缩变形、峰值压缩载荷、压缩功、屈服点、屈服变形、回弹力、峰值拉伸载荷、峰值拉伸载荷变形、断裂强度、破坏变形和拉伸功。使用该装置,作者鉴定出了几种非常适合口服控释系统的生物黏附材料。在大鼠中进行的胃肠道转运研究表明,胃肠道停留时间增加与强烈的生物黏附相互作用之间存在很强的相关性。

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