Abstract
Objective: Ocular inserts offer many advantages over conventional dosage forms, like increased ocular residence, the possibility of releasing a drug at a slow and constant rate, accurate dosing, exclusion of preservatives, and increased shelf life. Besifloxacin is a very important drug for the treatment of infectious conjunctivitis. The present study was aimed to formulate and evaluate Besifloxacin Non-Erodible Ocular Insert using Pullulan and polyvinyl pyrrolidone as a drug reservoir, PEG 400 as a plasticizer, and Eudragit RS-100 as a rate-controlling membrane. Methods: Central composite design was employed to study the effect of independent variables, i.e., effects of Pullulan amount (X1) and PVP (X2) on the dependent variables, i.e., % moisture absorption and In vitro diffusion rate. After evaluation of all thirteen batches of ocular insert reservoir formulation, BSF2 and BSF4 were selected as a satisfactory formulation and was sandwiched between rate-controlling membrane, which was made up of Eudragit RS-100 (3 and 5%). Results: The drug content of all formulations was found to be in the range of 95.33 to 99.89 %. In vitro diffusion of Besifloxacin from reservoir formulations (BSF1 to BSF13) was found to be 62.44 to 70.62 %. In vitro diffusion rate of an ocular insert of Besifloxacin can offer benefits such as increasing residence time, prolonging drug release in the eye for 24 h. Eudragit RS-100, as a sustained drug release polymer, showed promising sustained released action. Conclusion: The study concluded that Besifloxacin non-erodible ocular inserts can be successfully developed using Pullulan and polyvinyl pyrrolidone, which will sustain the release of the drug also reduce the frequency of administration, and thereby may help to improve patient compliance.
Highlights
Infectious conjunctivitis has a high impact on public health, accounting for more than a third of eye conditions reported by health services worldwide
Bacterial conjunctivitis is an inflammation of the conjunctiva, characterized by persistent mucopurulent discharge and redness of the eye
Besifloxacin is a very important drug for the treatment of infectious conjunctivitis since it presents less occurrence of bacterial resistance than other drugs used for the same purpose and, at the same time, presents great efficacy and tolerability [3]
Summary
Infectious conjunctivitis has a high impact on public health, accounting for more than a third of eye conditions reported by health services worldwide. Bacterial conjunctivitis is an inflammation of the conjunctiva, characterized by persistent mucopurulent discharge and redness of the eye. It is generally a selflimiting disease and usually does not cause permanent loss of vision or structural damage to the eye [1]. Besifloxacin has an N-1 cyclo-propyl group, which provides broad-spectrum activity against aerobic bacteria. Besifloxacin inhibits both bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, in contrast to the older fluoroquinolones, which bind more strongly to one of the enzymes. Besifloxacin is a topical synthetic fluoroquinolone and represents the first chlorofluoroquinolone developed for the topical treatment of ophthalmic infections [4]
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