title: Self nanoemulsifying drug delivery system (SNEDDS) of rosuvastatin calcium: design, formulation, bioavailability and pharmacokinetic evaluation.
abstract: The aim of the present study is to improve solubility and bioavailability of Rosuvastatin calcium using self nanoemulsifying drug delivery system (SNEDDS). Self emulsifying property of various oils including essential oils was evaluated with suitable surfactants and co-surfactants. Ternary phase diagrams were constructed based on Rosuvastatin calcium solubility analysis for optimizing the system. The prepared formulations were evaluated for self emulsifying time, robustness to dilution, droplet size determination and zeta potential analysis. The system was found to be robust in different pH media and dilution volume. The globule size of the optimized system was less than 200nm which could be an acceptable nanoemulsion size range. The zeta potential of the selected CN 7 SNEDDS formulation (cinnamon oil 30%; labrasol 60%; Capmul MCM C8 10%) was -29.5±0.63 with an average particle size distribution of 122nm. In vitro drug release studies showed remarkable increase in dissolution of CN7 SNEDDS compared to marketed formulation. In house developed HPLC method for determination of Rosuvastatin calcium in rat plasma was used in the bioavailability and pharmacokinetic evaluation. The relative bioavailability of self nanoemulsified formulation showed an enhanced bioavailability of 2.45 times greater than that of drug in suspension. The obtained plasma drug concentration data was processed with PKSolver 2.0 and it was best fit into the one compartment model.
authors.affiliation: Department of Pharmaceutics, PSG College of Pharmacy, Coimbatore 641044, Tamil Nadu, India. Electronic address: balakumar_27@yahoo.co.uk.
authors.forename: Krishnamoorthy
authors.initials: K
authors.lastname: Balakumar
authors.forename: Chellan Vijaya
authors.initials: CV
authors.lastname: Raghavan
authors.forename: Natarajan Tamil
authors.initials: NT
authors.lastname: selvan
authors.forename: Ranganathan Hari
authors.initials: RH
authors.lastname: prasad
authors.forename: Siyad
authors.initials: S
authors.lastname: Abdu
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004655:Emulsions; D005464:Fluorobenzenes / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D008564:Membrane Potentials; D049329:Nanostructures / Q000737:chemistry*; D009821:Oils; D010316:Particle Size; D011743:Pyrimidines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D000068718:Rosuvastatin Calcium; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D013501:Surface-Active Agents
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D009821:Oils; D011743:Pyrimidines; D013449:Sulfonamides; D013501:Surface-Active Agents; D000068718:Rosuvastatin Calcium
keywords: Bioavailability; Pharmacokinetic study; Poorly water soluble drug; Rosuvastatin calcium; SNEDDS; Self nanoemulsifying drug delivery system