Ghaderi R, Artursson P, Carlfors J
Uppsala University, BMC, Department of Pharmaceutics, Sweden.
Pharm Res. 1999 May;16(5):676-81. doi: 10.1023/a:1018868423309.
We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles.
The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) and Polycaprolactone (PCL), were used for preparation of microparticles using SEDS. Solutions of the polymers in organic solvents were dispersed and sprayed with supercritical CO2. Extraction of the organic solvents resulted in the formation of solid microparticles. The amounts of highly toxic solvents such as dichloromethane (MC) were reduced in the process.
Microparticles were obtained from all polymers. The mean particle size and shape varied with the polymer used. The morphology of the particles was strongly affected by the choice of polymer solvent. Discrete spherical microparticles of DL-PLG were produced with a mean volumetric diameter of 130 microm. The microparticles of the L-PLA were almost spherical, and their size increased from 0.5 to 5 microm as the density of supercritical CO2 decreased. PCL formed microparticles with diameters of 30-210 microm and showed a strong tendency to form films at high pressure.
The SEDS process appears a promising method for production of microparticles from biodegradable polymers without the use of toxic solvents.
我们评估了一种新的工艺，即超临界流体增强溶液分散法（SEDS）用于制备聚合物微粒。
使用可生物降解的聚合物聚（DL-丙交酯-共-乙交酯）：共聚物组成50:50（DL-PLG）、聚（L-丙交酯）（L-PLA）、聚（DL-丙交酯）（DL-PLA）和聚己内酯（PCL），通过SEDS制备微粒。将聚合物在有机溶剂中的溶液分散并用超临界二氧化碳喷雾。有机溶剂的萃取导致形成固体微粒。该过程减少了二氯甲烷（MC）等高毒性溶剂的用量。
从所有聚合物中均获得了微粒。平均粒径和形状随所用聚合物而变化。颗粒的形态受聚合物溶剂选择的强烈影响。制备出了平均体积直径为130微米的离散球形DL-PLG微粒。L-PLA微粒几乎呈球形，随着超临界二氧化碳密度的降低，其尺寸从0.5微米增加到5微米。PCL形成了直径为30 - 210微米的微粒，并且在高压下显示出强烈的成膜倾向。
SEDS工艺似乎是一种无需使用有毒溶剂即可从可生物降解聚合物制备微粒的有前景的方法。
