Chung T W, Huang Y Y, Liu Y Z
Department of Biomedical Engineering, Chung-Yuan Christian University, 32023, Chung-Li, Taiwan, ROC.
Int J Pharm. 2001 Jan 16;212(2):161-9. doi: 10.1016/s0378-5173(00)00574-3.
We investigated the effects of the rate of solvent removal by varying ambient pressure at a fixed temperature on the morphology, particle sizes, drug encapsulation efficiency and releases pattern of lidocaine loaded poly-L-lactatide (PLLA) and poly-D,L-lactatide (PDLLA) microspheres, prepared with O/W emulsion-solvent evaporation process. Prepared in the fast rate of solvent evaporation (FRSE) process by reducing ambient pressure, smoothly morphological surface of drug loaded PLLA and PDLLA microspheres was observed. While in the normal rate of solvent evaporation (NRSE) process, roughness or pinhole surface was only found at drug loaded PLLA microspheres. Fabricated in the FRSE process, both PLLA and PDLLA microspheres showed smaller particle sizes and lower drug encapsulation efficiencies than those prepared in NRSE process. In regard to two materials, PLLA microspheres had higher drug encapsulation efficiencies than PDLLA ones for both processes. Although initial burst releases of drug were observed for both PLLA and PDLLA microspheres prepared in whatever solvent removal process, drug release for PLLA microspheres was slightly less than that for PDLLA ones in the earlier stage of drug release. However, in the subsequent stage of drug release, there was no difference between two materials. In corporation with different crystalline characteristics of PLA polymer and its derivatives, FRSE process by reducing ambient pressure could be further applied to produce different characteristics of microspheres for drug delivery.
我们通过在固定温度下改变环境压力来研究溶剂去除速率对利多卡因负载的聚-L-丙交酯(PLLA)和聚-D,L-丙交酯(PDLLA)微球的形态、粒径、药物包封效率和释放模式的影响,这些微球采用水包油乳液-溶剂蒸发法制备。通过降低环境压力以快速溶剂蒸发(FRSE)过程制备时,观察到载药PLLA和PDLLA微球具有光滑的形态表面。而在正常溶剂蒸发(NRSE)过程中,仅在载药PLLA微球上发现粗糙度或针孔表面。在FRSE过程中制备的PLLA和PDLLA微球均显示出比在NRSE过程中制备的微球更小的粒径和更低的药物包封效率。对于这两种材料,在两种过程中PLLA微球的药物包封效率均高于PDLLA微球。尽管无论采用何种溶剂去除过程制备的PLLA和PDLLA微球均观察到药物的初始突释,但在药物释放的早期阶段,PLLA微球的药物释放略低于PDLLA微球。然而,在药物释放的后续阶段,两种材料之间没有差异。结合聚乳酸聚合物及其衍生物的不同结晶特性,通过降低环境压力的FRSE过程可进一步应用于制备具有不同特性的药物递送微球。