Stenekes R J, Franssen O, van Bommel E M, Crommelin D J, Hennink W E
Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), The Netherlands.
Pharm Res. 1998 Apr;15(4):557-61. doi: 10.1023/a:1011925709873.
The purpose of this study was to investigate the effect of the formulation parameters on the characteristics of dextran-based microspheres, prepared in an all-aqueous system.
Dextran microspheres were formed by polymerization of methacryloyl groups attached to dextran (dexMA), emulsified in an aqueous poly(ethylene glycol) (PEG) solution. DexMA/PEG/water phase diagrams were established.
The binodals in the phase diagrams shifted to higher concentrations of dextran and PEG with decreasing molecular weight of both polymers, and with increasing degree of MA substitution. The volume-number mean diameter of the microspheres, varied between 2.5 and 20 microns. For a given formulation, the particle size was independent of the PEG/dexMA volume ratio > 40 and increased for volume ratios < 40. Furthermore, larger particles were obtained with decreasing viscosity of the continuous phase and increasing viscosity of the discontinuous phase.
Particle characteristics of dextran microspheres prepared in an all-aqueous system, among which the size and initial water content, can be tailored by adjusting the formulation parameters.
本研究旨在探究配方参数对在全水体系中制备的基于葡聚糖的微球特性的影响。
通过连接在葡聚糖(dexMA)上的甲基丙烯酰基的聚合反应形成葡聚糖微球,将其乳化于聚乙二醇(PEG)水溶液中。建立了dexMA/PEG/水相图。
随着两种聚合物分子量的降低以及MA取代度的增加,相图中的双节线向葡聚糖和PEG浓度更高的方向移动。微球的体积-数量平均直径在2.5至20微米之间变化。对于给定配方,当PEG/dexMA体积比>40时,粒径与该比例无关,而当体积比<40时粒径增大。此外,连续相粘度降低和分散相粘度增加时可获得更大的颗粒。
在全水体系中制备的葡聚糖微球的颗粒特性,包括尺寸和初始含水量,可通过调整配方参数来定制。