T. M. Taha, S. H. Allehyani
Abstract: Objective: Repurposing of rosuvastatin calcium as antiangiogenic molecule for the better management of diabetic retinopathy and to formulate surface modified rosuvastatin calcium loaded nlc to improve the permeability. To study the toxicity and antiangiogenic activity of the formulation. Methods: Rosuvastatin calcium was formulated my micro emulsion technique. Permeability of drug solution and formulation was studied using goat cornea and antiangiogenic property of drug and formulation was studied by Ex vivo HET CAM ASSAY. Results: Rosuvastatin calcium was more soluble in Tripalmitin, oleic acid and tween 80 (2 %), Eutragit RS PO was used as surface modifier. particle size of without surface modified and with surface modified formulation was found to be 140.5nm and 151.8nm. Zeta potential was changed from -24 to +22.8 after surface modification. Entrapment efficiency of optimized F3 was found to be 88 %. SEM analysis showed particle size of without surface modified and with surface modified formulation was found to be 133nm and 168nm. Formulation showed sustained release and followed peppas model in release kinetics. Permeability study was done with drug solution (8.28), uncoated formulation (25.88 %) and coated formulation (34.7 %). Formulation was found to be sterile FTM (fluid thioglycolate medium), NB (nutrient broth) and SCDM (soya bean casein digests medium). IC 50 value of drug and formulation was found to be 100g/ml and 4000g/ml. Formulation does not show toxicity at 15g/ml. From antiangiogenic study Rosuvastatin Calcium loaded NLC showed a reduction in blood vessel growth. Conclusions: Rosuvastatin calcium showed antiangiogenic activity and % permeability is increased by surface modification of the formulation. So Rosuvastatin Calcium can be used for the better management of DR.
Keywords: Diabetic retinopathy, antiangiogenic activity, Repurposing of drug, Ocular drug delivery