Impregnated with hydroxypropyl methylcellulose films

Background and Objective: Continuous delivery of drugs to the eye offers major advantages over conventional therapies that involve administration of drug solutions or suspensions as eye drops. Eye drop administration often results in poor bioavailability and therapeutic response due to rapid precorneal elimination of the drug and is also associated with patient compliance problems. Ophthalmic inserts offer many advantages over conventional dosage forms, like increased ocular residence, possibility of releasing drugs at a slow and constant rate, accurate dosing, exclusion of preservatives and increased shelf life. The aim of this study was to prepare and incorporate of Eudragit ®L100 nanoparticles in hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol base as film insert for ophthalmic drug delivery system.Material and Methods: The nanoparticles were prepared adapting the spontaneous emulsification technique. Specified amounts of Eudragit ®L100 polymers and drugs were dissolved in methanol. This organic phase was slowly poured with constant speed into aqueous phase containing polyvinyl alcohol, where the nanoparticles were formed spontaneously. The ocular films with nanoparticles were obtained by addition of HPMC in 14 ml of nanoparticle solution. The solutions were then poured in a Mold covered for film casting preparation and were placed on a leveled surface at 60ºC temperature. Size, zeta potential, SEM and loading analyses of the nanoparticles, mechanical properties of the films were analyzed. In vivo drug release tests in eyes rabbits were carried out.Findings: In vivo release studies in eye rabbits revealed a release during the 96 h followed. The overall results of the sterility test showed that ocular formulation prepared passes the sterility test as there was no evidence of the growth found in the negative control test tubes. SEM characterization confirmed that nanoparticles were in nanosize range. The physicochemical properties showed that the Eudragit nanoparticles loaded PVA-HPMC films could be an effective carrier for drug.Conclusion: Azithromycin loaded Eudragit were successfully prepared by spontaneous emulsification technique. The obtained results showed that Eudragit could be a useful nanocarrier for antibiotical drugs. The use of a water-soluble polymer enhanced the contact time and possibly also the penetration of the drug in nanoparticles.

کلیدواژه ها:

Nanoparticles ، Ophthalmic drug delivery ، ocular insert ، Azithromycin