The preparation of dextran microspheres in an all-aqueous system: Effect of the formulation parameters on particle characteristics

被引:96
作者
Stenekes, RJH
Franssen, O
van Bommel, EMG
Crommelin, DJA
Hennink, WE
机构
[1] Univ Utrecht, Groningen Utrecht Inst Drug Explorat, Untrecht Inst Pharmaceut Sci, Dept Pharmaceut, NL-3508 TB Utrecht, Netherlands
[2] OctoPlus BV, NL-2333 CA Leiden, Netherlands
关键词
aqueous two phase system; phase diagram; microsphere preparation; dextran; hydrogel; poly(ethylene glycol);
D O I
10.1023/A:1011925709873
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Purpose. 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. Methods. 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. Results. 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 mu m. 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. Conclusions. 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.
引用
收藏
页码:557 / 561
页数:5
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