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用于控释药物的双壁聚合物微球。

Double-walled polymer microspheres for controlled drug release.

作者信息

Pekarek K J, Jacob J S, Mathiowitz E

机构信息

Division of Biology and Medicine, Brown University, Providence, Rhode Island 02912.

出版信息

Nature. 1994 Jan 20;367(6460):258-60. doi: 10.1038/367258a0.

Abstract

One approach to the controlled release of drugs involves incorporation of the drug molecules into the matrix of microscopic polymer spheres or capsules. Existing methods for preparing such microparticles do not, however, always guarantee a constant release rate, for example because drug molecules may be trapped preferentially at the surface, because they have to diffuse through an increasing thickness of polymer when the particles are non-eroding or because the surface area changes for eroding particles. In other situations pulsed release may be required--an application to which simple polymer microspheres do not readily lend themselves. Multi-walled microspheres might solve some of these problems. Here we describe a one-step process for preparing double-walled polymer microspheres with diameters ranging from about 20 to 1,000 micrometers. Our technique involves the phase separation of a polymer mixture owing to solvent evaporation: with an appropriate choice of interfacial tensions and evaporation rate, a spherical droplet of one polymer becomes coated with a highly uniform layer of the other. This process, which might be adapted to yield multi-walled microspheres, should make possible the engineering of highly specific drug-release properties.

摘要

药物控释的一种方法是将药物分子掺入微观聚合物球体或胶囊的基质中。然而,现有的制备此类微粒的方法并不总能保证恒定的释放速率,例如,药物分子可能优先被困在表面,因为当颗粒不发生侵蚀时它们必须扩散通过越来越厚的聚合物层,或者因为侵蚀颗粒的表面积会发生变化。在其他情况下,可能需要脉冲释放——简单的聚合物微球并不容易适用于这种应用。多层微球可能会解决其中一些问题。在此,我们描述了一种制备直径约为20至1000微米的双壁聚合物微球的一步法。我们的技术涉及由于溶剂蒸发导致聚合物混合物的相分离:通过适当选择界面张力和蒸发速率,一种聚合物的球形液滴会被另一种聚合物的高度均匀层包覆。这个过程可能适用于生产多层微球,应该能够实现高度特异性药物释放特性的工程设计。

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