Bodmeier R, Chen H, Tyle P, Jarosz P
College of Pharmacy, University of Texas, Austin 78712.
J Microencapsul. 1991 Apr-Jun;8(2):161-70. doi: 10.3109/02652049109071485.
Nanoparticles containing ibuprofen, indomethacin or propranolol were formed spontaneously after the addition of solutions of the drugs and acrylic polymers (Eudragit RS or RL 100) in the water-miscible solvents, acetone or ethanol, to water without sonication or microfluidization. The colloidal dispersions were stabilized by quaternary ammonium groups and did not require the addition of surfactants or polymeric stabilizers. The nanoparticles were compared to nanoparticles prepared either by a microfluidization-solvent evaporation method with a water-immiscible organic solvent, methylene chloride, or by a melt method with respect to particle size and redispersibility of freeze- or spray-dried samples. Nanoparticles prepared by microfluidization or the melt method were easily redispersed while Eudragit RS nanoparticles prepared by spontaneous emulsification were not redispersible. Flexible films were formed from the nanosuspensions after the addition of 15 per cent triethyl citrate, a water-soluble plasticizer. The release of propranolol from the films increased with increasing proportion of RL, but was independent of the order of mixing of the two polymers or nanosuspensions during film preparation. The drug release from indomethacin films was increased by adding water-soluble polymers to the nanosuspension.
在将含有布洛芬、吲哚美辛或普萘洛尔的药物溶液与丙烯酸聚合物（尤特奇RS或RL 100）在与水混溶的溶剂丙酮或乙醇中加入水中后，无需超声处理或微流化处理，即可自发形成纳米颗粒。胶体分散体通过季铵基团得以稳定，无需添加表面活性剂或聚合物稳定剂。将这些纳米颗粒与通过微流化 - 溶剂蒸发法（使用与水不混溶的有机溶剂二氯甲烷）或熔融法制备的纳米颗粒在粒径以及冷冻干燥或喷雾干燥样品的再分散性方面进行了比较。通过微流化法或熔融法制备的纳米颗粒易于再分散，而通过自发乳化制备的尤特奇RS纳米颗粒则不可再分散。在加入15%的水溶性增塑剂柠檬酸三乙酯后，纳米悬浮液形成了柔性薄膜。薄膜中普萘洛尔的释放量随RL比例的增加而增加，但与薄膜制备过程中两种聚合物或纳米悬浮液的混合顺序无关。通过向纳米悬浮液中添加水溶性聚合物，可增加吲哚美辛薄膜的药物释放量。
