School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, Shanghai, People's Republic of China.
Int J Nanomedicine. 2013;8:3119-28. doi: 10.2147/IJN.S46207. Epub 2013 Aug 14.
Drug nanosuspensions are very promising for enhancing the dissolution and bioavailability of drugs that are poorly soluble in water. However, the poor stability of nanosuspensions, reflected in particle growth, aggregation/agglomeration, and change in crystallinity state greatly limits their applications. Solidification of nanosuspensions is an ideal strategy for addressing this problem. Hence, the present work aimed to convert drug nanosuspensions into pellets using fluid-bed coating technology.
Indomethacin nanosuspensions were prepared by the precipitation-ultrasonication method using food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) as stabilizers. Dried nanosuspensions were prepared by coating the nanosuspensions onto pellets. The redispersibility, drug dissolution, solid-state forms, and morphology of the dried nanosuspensions were evaluated.
The mean particle size for the nanosuspensions stabilized using soybean protein isolate, whey protein isolate, and β-lactoglobulin was 588 nm, 320 nm, and 243 nm, respectively. The nanosuspensions could be successfully layered onto pellets with high coating efficiency. Both the dried nanosuspensions and nanosuspensions in their original amorphous state and not influenced by the fluid-bed coating drying process could be redispersed in water, maintaining their original particle size and size distribution. Both the dried nanosuspensions and the original drug nanosuspensions showed similar dissolution profiles, which were both much faster than that of the raw crystals.
Fluid-bed coating technology has potential for use in the solidification of drug nanosuspensions.
药物纳米混悬剂在提高水中溶解度差的药物的溶解和生物利用度方面非常有前景。然而，纳米混悬剂的稳定性差，表现在颗粒生长、聚集/团聚以及结晶状态的变化，这极大地限制了它们的应用。纳米混悬剂的固化是解决这个问题的理想策略。因此，本工作旨在使用流化床包衣技术将药物纳米混悬剂转化为丸剂。
采用沉淀-超声法，以食用蛋白（大豆分离蛋白、乳清分离蛋白、β-乳球蛋白）为稳定剂制备吲哚美辛纳米混悬剂。通过将纳米混悬剂包衣到丸剂上来制备干燥的纳米混悬剂。评价了干燥纳米混悬剂的再分散性、药物溶出度、固体形态和形态。
用大豆分离蛋白、乳清分离蛋白和β-乳球蛋白稳定的纳米混悬剂的平均粒径分别为 588nm、320nm 和 243nm。纳米混悬剂可以成功地包衣到丸剂上，具有高包衣效率。干燥的纳米混悬剂和原始无定形状态的纳米混悬剂都可以在水中重新分散，保持其原始粒径和粒径分布。干燥的纳米混悬剂和原始药物纳米混悬剂都表现出相似的溶出曲线，都比原药晶体快得多。
流化床包衣技术在药物纳米混悬剂的固化中具有应用潜力。
