Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G
Sparfloxacin loaded PLGA nanoparticles for sustained ocular drug delivery. [JOURNAL ARTICLE]
Nanomedicine 2009 Oct 23.
Poor ocular bioavailability of drugs (<1%) from conventional eye drops (i.e. solution, suspension and ointments) is mainly due to the eye physiological barriers. In general, ocular efficacy is closely related to ocular drug bioavailability, which may be enhanced by increasing corneal drug penetration and prolonging precorneal drug residence time. In our present work we develop and evaluate new colloidal system i.e. PLGA nanoparticle for sparfloxacin ophthalmic delivery to improve precorneal residence time and ocular penetration. Nanoparticles were prepared by nanoprecipitation technique and characterized for various properties like particle size, zeta potential, in vitro drug release, statistical model fitting, stability etc. Microbiological assay was carried out against Pseudomonas aeruginosa using cup-plate method. Precorneal residence time was studied on albino rabbits by gamma scintigraphy after radiolabelling of sparfloxacin by Tc-99m. Ocular tolerance of developed nanosuspension was also studied by HET-CAM method. The developed nanosuspension showed a mean particle size in the range of 180-190 nm, suitable for ophthalmic application with zeta potential of-22mV. In vitro release from developed nanosuspension showed an extended release profile of sparfloxacin according to peppas model. The observation of acquired gamma camera images showed good retention over the entire precorneal area for developed nanosuspension as compared to marketed formulation. Marketed drug formulation cleared very rapidly from the corneal region and reached to systemic circulation through nasolachrymal drainage system, as significant radioactivity was recorded in kidney and bladder after 6 h of ocular administration, whereas developed nanosuspension cleared at a very slow rate (p<0.05) and remained at corneal surface for longer duration as no radioactivity was observed in systemic circulation. HET-CAM assay with 0 score in 8 h, indicates the non irritant property of developed nanosuspension. The developed lyophilized nanosuspension was found to be stable for longer duration of time than the conventional marketed formulation with a good shelf life.
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