المؤلفون: Datta Maroti Pawde, Tamilvanan Shunmugaperumal, Syed Nazrin Ruhina Rahman, Victor Hmingthansanga, Oly Katari

المصدر: AAPS PharmSciTech. 21

مصطلحات موضوعية: Materials science, Central composite design, Calcineurin Inhibitors, Pharmacology toxicology, Pharmaceutical Science, Administration, Ophthalmic, 02 engineering and technology, In Vitro Techniques, Aquatic Science, 030226 pharmacology & pharmacy, Taguchi design, 03 medical and health sciences, 0302 clinical medicine, Cyclosporin a, Drug Discovery, Humans, Particle Size, Ecology, Evolution, Behavior and Systematics, Chromatography, Model equation, Ecology, General Medicine, 021001 nanoscience & nanotechnology, Drug Liberation, Toxicity, Emulsion, Cyclosporine, Drug release, Dry Eye Syndromes, Emulsions, 0210 nano-technology, Agronomy and Crop Science

الوصف: The objectives of the present investigations are (1) to envisage a risk assessment plan for nonphospholipid-based topical ophthalmic emulsions with the help of failure mode and effect analysis (FMEA), (2) to screen the risky formulation and process variables by the Taguchi design, (3) to optimize systematically an emulsion formula by face-centered central composite design (CCD), (4) to incorporate cyclosporin A (0.05 or 0.1% w/w) into the optimized emulsions and predict the in vitro drug release kinetic via a particle diffusion-controlled mathematical model equation, and (5) to assess the emulsion's toxicity using in vitro hemolysis study. Through the risk priority number (RPN) scores of FMEA, half-normal and Pareto charts of the Taguchi design, 3D-response surface graphs, and overlay plots of CCD, the emulsion formula was systematically optimized. Irrespective of the two different drug loadings into optimized emulsions, the drug entrapment efficiency values ranged from 73.20 ± 0.13 to 74.42 ± 0.15%. The film diffusion or ion-exchange process fails to interpret the in vitro drug release kinetic profile. A permissible percentage hemolysis value of above 10% but below 25% guidance was observed for emulsions with or without cyclosporin A. The systematically optimized phospholipidless ophthalmic emulsions could further be exploited commercially for managing dry-eye syndrome.

URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4dc24d99b1c130032cabef483ad4a5ea
https://doi.org/10.1208/s12249-019-1587-5