title: Improved pharmacokinetics and antihyperlipidemic efficacy of rosuvastatin-loaded nanostructured lipid carriers.
abstract: In the present study, rosuvastatin calcium-loaded nanostructured lipid carriers were developed and optimized for improved efficacy. The ROS-Ca-loaded NLC was prepared using melt emulsification ultrasonication technique and optimized by Box-Behnken statistical design. The optimized NLC composed of glyceryl monostearate (solid lipid) and capmul MCM EP (liquid lipid) as lipid phase (3% w/v), poloxamer 188 (1%) and tween 80 (1%) as surfactant. The mean particle size, polydispersity index (PDI), zeta potential (ζ) and entrapment efficiency (%) of optimized NLC formulation was observed to be 150.3 ± 4.67 nm, 0.175 ± 0.022, -32.9 ± 1.36 mV and 84.95 ± 5.63%, respectively. NLC formulation showed better in vitro release in simulated intestinal fluid (pH 6.8) than API suspension. Confocal laser scanning showed deeper permeation of formulation across rat intestine compared to rhodamine B dye solution. Pharmacokinetic study on female albino Wistar rats showed 5.4-fold increase in relative bioavailability with NLC compared to API suspension. Optimized NLC formulation also showed significant (p < 0.01) lipid lowering effect in hyperlipidemic rats. Therefore, NLC represents a great potential for improved efficacy of ROS-Ca after oral administration.
authors.affiliation: a Formulation Research Lab, Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , New Delhi , India.
authors.forename: Md
authors.initials: M
authors.lastname: Rizwanullah
authors.affiliation: a Formulation Research Lab, Department of Pharmaceutics, Faculty of Pharmacy , Jamia Hamdard , New Delhi , India.
authors.forename: Saima
authors.initials: S
authors.lastname: Amin
authors.affiliation: b Department of Pharmaceutics , National Institute of Pharmaceutical Education and Research (NIPER) , Raebareli , India.
authors.forename: Javed
authors.initials: J
authors.lastname: Ahmad
mesh_terms: D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D065546:Drug Liberation; D005260:Female; D006949:Hyperlipidemias / Q000097:blood / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D007082:Ileum / Q000378:metabolism; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability; D017208:Rats, Wistar; D000068718:Rosuvastatin Calcium / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013499:Surface Properties
chemical_list: D004337:Drug Carriers; D000960:Hypolipidemic Agents; D008055:Lipids; D000068718:Rosuvastatin Calcium
keywords: Box–Behnken design; hyperlipidemia; in vitro release; nanostructured lipid carriers; oral bioavailability; rosuvastatin calcium