| چکیده | Design and evaluation of polymeric controlled release Azithromycin ocular insert Shahla Mirzaeei, Amin Hosseini Inroduction: Many ocular surface disorders involving the tear film, eyelids, and adnexal structures are associated with chronic, low-grade bacterial infection and may potentially lead to decreased vision secondary to corneal scarring. Various topical antibiotic and steroid combinations are commonly used with variable clinical response and known potential side effects. However, the long-lasting antibacterial and additional anti-inflammatory properties of topical azithromycin(AZ) might offer an effective treatment. Transport of drugs applied by traditional dosage forms is restricted to the eye, and therapeutic drug concentrations are not maintained for a long duration since the eyes are protected by a unique anatomy and physiology so repeated instillations of antibiotics are required to reach therapeutic level, above the minimal inhibitory concentration (MIC). Direct intravitreal implants, Using biodegradable or non biodegradable polymer technology, have been widely investigated for treatment of chronic vitreoretinal diseases. We have incorporated AZ in insert polymeric drug delivery system, with a mucoadhesive and hydrophilic properties in order to extent release. Method: Solvent casting technique was followed to prepare ocular films using different polymers such as, eudragit RL-100, hydroxy propyl methyl cellulose and hydroxyl ethyl cellulose at various proportion and combinations using glyserol as plasticizer. The prepared insert were evaluated for their physicochemical parameters; drug content, weight uniformity, folding endurance, thickness, % moisture absorption and water vapour transmission rate. The in vitro drug release from the formulations was studied and the in vitro release kinetic datas were treated according to the diffusion models proposed by Higuchi and Peppas in order to access the mechanism of drug release. Results: All the formulations showed no change in the physical appearance and the FTIR studies indicated no possibility of interaction between drug and polymer. In vitro release studies revealed that the best ocular inserts formulation followed near to zero-order release kinetics. The controlled release ocular insert was more suitable as compared to conventional dosage form. Shelf-life of the product was found to be more than one year. Conclusion: The insert ophthalmic formulations of azithromycin, have been shown to have long half-lives in the conjunctiva while providing very low systemic exposure. It can potentially be administered at a much lower dosing frequency than the marketed anitbiotics for the treatment of bacterial conjunctivitis. Keywords: Ocular Insert; Azithromycin; controlled release |