Design and evaluation of aceclofenac ocular inserts with special reference to cataracts and conjunctivitis  

作　　者：Vivek Dave Sachdev Yadav Sarvesh Paliwal Swapnil Sharma Dhirendra Kumar 

机构地区：[1]Department of Pharmacy, Banasthali University [2]Manipal College of Pharmaceutical Sciences

出　　处：《Journal of Chinese Pharmaceutical Sciences》2013年第5期449-455,共7页中国药学（英文版）

摘　　要：The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals.While absorption by this route is bungling,there are a few side effects with conventional dosage forms.Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac.The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose(HPMC,3% to 5%),chitosan(3% to 5%),poly vinyle alcohol(PVA,3% to 5%),methyl cellulose(MC,3% to 5%) as drug reservoir and ethyl cellulose(EC) polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time,achieving controlled release and greater therapeutic efficiency.The prepared ocular insert were then evaluated for physical appearances tensile strength,elongation at break(%),weight variation,uniformity of thickness,moisture absorption(%),pH,folding endurance,Fourier Transform Infrared spectroscopy,differential scanning calorimetry.Physicochemical characterization and in vitro transcorneal permeation studies reveals that,the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content,98.54% and 96.24%,respectively,over an extended period of 24 h.Hence these formulations were selected as best optimized formulations.It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system.Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release,proving a promising controlled release delivery system.The eyes present unique opportunities and challenges when it comes to the delivery of pharmaceuticals. While absorption by this route is bungling, there are a few side effects with conventional dosage forms. Ocular inserts were prepared with prolonged release of drug and minimum swelling within cul-de-sac using aceclofenac. The work focused on treatment of conjunctivitis and cataracts by formulating ocular inserts of different polymeric combination of aceclofenac using hydroxypropyl methyl cellulose （HPMC, 3% to 5%）, chitosan （3% to 5%）, poly vinyle alcohol （PVA, 3% to 5%）, methyl cellulose （MC, 3% to 5%） as drug reservoir and ethyl cellulose （EC） polymer as rate controlling membrane by solvent casting technique with the objective of increasing contact time, achieving controlled release and greater therapeutic efficiency. The prepared ocular insert were then evaluated for physical appearances tensile strength, elongation at break （%）, weight variation, uniformity of thickness, moisture absorption （%）, pH, folding endurance, Fourier Transform Infrared spectroscopy, differential scanning calorimetry. Physicochemical characterization and in vitro transcorneal permeation studies reveals that, the prepared ocular insert formulations F2 and F8 containing HPMC and PVA had released their drug content, 98.54% and 96.24%, respectively, over an extended period of 24 h. Hence these formulations were selected as best optimized formulations. It can be concluded that hydroxy propyl methyl cellulose is a good film forming hydrophilic polymer which shows potential agent for ocular drug delivery system. Incorporation of polyethylene glycol enhances the permeability of aceclofenac ocular insert and has perfect zero order release, proving a promising controlled release delivery system.

关 键 词：Transcomeal Nasolacrimal Rate controlling membrane Drug reservoir 

分 类 号：R776.1[医药卫生—眼科]