Pharmaceutical Technology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, Penang, Malaysia.
AAPS PharmSciTech. 2012 Mar;13(1):35-45. doi: 10.1208/s12249-011-9707-x. Epub 2011 Nov 19.
Microencapsulation of water-soluble drugs using coacervation-phase separation method is very challenging, as these drugs partitioned into the aqueous polymeric solution, resulting in poor drug entrapment. For evaluating the effect of ovalbumin on the microencapsulation of drugs with different solubility, pseudoephedrine HCl, verapamil HCl, propranolol HCl, paracetamol, and curcuminoid were used. In addition, drug mixtures comprising of paracetamol and pseudoephedrine HCl were also studied. The morphology, encapsulation efficiency, particle size, and in vitro release profile were investigated. The results showed that the solubility of the drug determined the ratio of ovalbumin to be used for successful microencapsulation. The optimum ratios of drug, ovalbumin, and gelatin for water-soluble (pseudoephedrine HCl, verapamil HCl, and propranolol HCl), sparingly water-soluble (paracetamol), and water-insoluble (curcuminoid) drugs were found to be 1:1:2, 2:3:5, and 1:3:4. As for the drug mixture, the optimum ratio of drug, ovalbumin, and gelatin was 2:3:5. Encapsulated particles prepared at the optimum ratios showed high yield, drug loading, entrapment efficiency, and sustained release profiles. The solubility of drug affected the particle size of the encapsulated particle. Highly soluble drugs resulted in smaller particle size. In conclusion, addition of ovalbumin circumvented the partitioning effect, leading to the successful microencapsulation of water-soluble drugs.
使用凝聚相分离法对水溶性药物进行微囊化非常具有挑战性,因为这些药物会分配到水性聚合物溶液中,导致药物包封率差。为了评估卵清蛋白对不同溶解性药物微囊化的影响,使用了盐酸伪麻黄碱、盐酸维拉帕米、盐酸普萘洛尔、对乙酰氨基酚和姜黄素类化合物。此外,还研究了包含对乙酰氨基酚和盐酸伪麻黄碱的药物混合物。考察了形态、包封效率、粒径和体外释放曲线。结果表明,药物的溶解度决定了用于成功微囊化所需的卵清蛋白的比例。水溶性(盐酸伪麻黄碱、盐酸维拉帕米和盐酸普萘洛尔)、低水溶性(对乙酰氨基酚)和水不溶性(姜黄素类化合物)药物的最佳药物、卵清蛋白和明胶比例分别为 1:1:2、2:3:5 和 1:3:4。对于药物混合物,药物、卵清蛋白和明胶的最佳比例为 2:3:5。在最佳比例下制备的包封颗粒具有较高的产率、载药量、包封效率和持续释放曲线。药物的溶解度影响包封颗粒的粒径。高溶解性药物导致粒径较小。总之,添加卵清蛋白可避免分配效应,从而成功地对水溶性药物进行微囊化。