A novel impinging aerosols method for production of propranolol hydrochloride-loaded alginate gel microspheres for oral delivery

摘要

Propranolol hydrochloride was directly encapsulated in alginate gel microspheres (40-50 p,m in diameter) using a novel method involving impinging aerosols of CaCI2 cross-linking solution and sodium alginate solution containing the drug. Microspheres formulated using 0.1 M CaCI2 exhibited the highest drug loading (14%, w/w of dry microspheres) with 66.5% encapsulation efficiency. Less than 4% and 35% propranolol release occurred from hydrated and dried microspheres, respectively, in 2 h in simulated gastric fluid (SGF). The majority of the drug load (90%) was released in 5 and 7 h from hydrated and dried microspheres, respectively, in simulated intestinal fluid (SIF). Prior incubation of hydrated microspheres (cross-linked using 0.5 M CaCI2) in SGF prolonged the time of release in SIF to 10 h, which has implications for the design of protocols and correlation with in vivo release behaviour. Restricted propranolol release in SGF and complete extraction in SIF demonstrate the potential of alginate gel microspheres for oral delivery of pharmaceuticals.