Characterization of Best Optimized Levobunolol Hydrochloride Occusert Formulations with Special Reference to Glaucoma Treatment

摘要

The aim of present study was to characterize best optimized Levobunolol HCI occusert formulations with special reference to glaucoma treatment, biologically. Levobunolol HCI occuserts were prepared using hydroxypropyl methylcellulose (HPMC, 3% & 4%), poly vinyl pyrrolidone (PVP, 1%), methyl cellulose (MC, 1% & 2%) as polymers by solvent casting technique with objectives of increasing contact time, achieving controlled release, reduction in frequency of administration and greater therapeutic efficacy. Based on their physiochemical and in-vitro drug release characterization, formulations (F_2& F_1)containing 4 % and 3 % HPMC were selected as best optimized formulations. Further, these formulations were subjected to biological characterization such as microbial sterility testing, Modified Draize eye irritation and in-vivo drug release studies for their efficacy, reliability and clinical safety. Finally, accelerated stability testing (aging study) was also carried out. Results of these studies revealed that, occusert formulations (F_2& F_1) passed the test for sterility, there was no irritation to the sensitive ocular tissues and in-vivo study had released drug contents, 77.14 % and 69.83 % (F_2& F_1) respectively over an extended period of 12 hr. Finally, the ocular inserts were found stable and there was no effect on the drug content for a period of 2 months. It was found that, best optimized polymeric occuserts have appreciable strength biologically. ^g>Characterization, Glaucoma, Levobunolol HCI, Occusert.