title: Development and Optimization of Self-emulsifying Drug Delivery Systems (SEDDS) for Enhanced Dissolution and Permeability of Rosuvastatin.
abstract: Rosuvastatin calcium is commonly used statin for treatment of dyslipidemia. It has low bioavailability. The aim of this study was to develop new rosuvastatin calcium self-emulsifying drug delivery systems (SEDDS) as an alternative formulation and to evaluate the permeability of rosuvastatin calcium SEDDS by using Caco-2 cells. Rosuvastatin calcium SEDDSs were developed by using pseudo ternary phase diagram and characterized by using heating cooling cycle, robustness to dilution, stability and in vitro drug release and permeability. The permeability studies of rosuvastatin calcium SEDDS (Papp (A→B) for F1-RS=1.492×10-5±0.413×10-5 and Papp (A→B) for F2-RS=1.254×10-5±0.19×10-5) across Caco-2 cells showed that permeability value from apical to basolateral was higher than permeability value of commercial formulation (Papp (A→B) =7.13×10-5±0.668×10-5). In conclusion, SEDDS as a drug carrier may be used as an effective and alternative hyperlipidemia therapy for oral delivery of rosuvastatin calcium.
authors.affiliation: Ege University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Izmir, Turkey. karasuluy@gmail.com.
authors.forename: H Y
authors.initials: HY
authors.lastname: Karasulu
authors.forename: E
authors.initials: E
authors.lastname: Gündoğdu
authors.forename: T
authors.initials: T
authors.lastname: Turgay
authors.forename: U Ö
authors.initials: UÖ
authors.lastname: Türk
authors.forename: S
authors.initials: S
authors.lastname: Apaydın
authors.forename: I Yildırım
authors.initials: IY
authors.lastname: Şimşir
authors.forename: C
authors.initials: C
authors.lastname: Yilmaz
authors.forename: E
authors.initials: E
authors.lastname: Karasulu
mesh_terms: D001682:Biological Availability; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D005026:Ethylene Glycols / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D019301:Oleic Acid / Q000737:chemistry; D010539:Permeability; D011092:Polyethylene Glycols / Q000737:chemistry; D000068718:Rosuvastatin Calcium / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D013607:Tablets
chemical_list: D004655:Emulsions; D005026:Ethylene Glycols; D005989:Glycerides; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; C514708:Labrafil M 1944 CS; D013607:Tablets; D019301:Oleic Acid; D011092:Polyethylene Glycols; D000068718:Rosuvastatin Calcium; C010111:carbitol