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Enhancing Solubility and Bioavailability of Rosuvastatin into Self Nanoemulsifying Drug Delivery System

[ Vol. 15 , Issue. 7 ]

Author(s):

Hatice Yasim Karasulu*, Evren Gundogdu, Ugur Onsel Turk, Tugce Turgay, Sebnem Apaydin, Ilgin Yildirim Simsir, Condeger Yilmaz and Ercument Karasulu   Pages 1072 - 1082 ( 11 )

Abstract:


Objective: The aim of this study was to develop new Rosuvastatin calcium (RCa) self nanoemulsifying drug delivery system (SNEDDS) and to evaluate the bioavailability and pharmacodynamic effect of RCa-SNEDDS in Yorkshire pigs.

Methods: Firstly, SNEDDS was developed and prepared then RCa was incorporated into SNEDDS which was evaluated regarding their characterization, stability properties, drug release profiles, permeation and cytotoxicity studies. Finally, in vivo performance of RCa-SNEDDS (F1-RCa-SNEDDS) was examined by pharmacokinetic and pharmacodynamics studies. The average droplet size of RCa- SNEDDS ranged between 200 and 250 nm. RCa-SNEDDS that contained 12.8% Oleic acid, 11 % Labrafil M, 3.3 % Labrasol and 4.4 % Transcutol HP were found to be stable and exhibited approximately 4-fold higher permeation than commercial tablet (Crestor® 20 mg tablet).

Results: In pharmacokinetic studies, when F1-RCa-SNEDDS and commercial tablet were administered orally, F1-RCa-SNEDDS showed higher bioavailability of RCa than commercial tablet. Respectively, in pharmacodynamic studies, triglyceride and total cholesterol levels were significantly reduced with F1- RCa-SNEDDS formulation by 37% and 19% when compared to baseline values.

Conclusion: However, these decreases with commercial formulation were only 6% and 2% respectively. According to these findings, development formulation could be potentially used to enhance the oral absorption of RCa.

Keywords:

Rosuvastatin, bioavailability, SNEDDS, pharmacokinetic, oral absorption, baseline.

Affiliation:

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, Izmir, Department of Radiopharmacy, Faculty of Pharmacy, Ege University, Izmir, Ege University ARGEFAR Drug Development and Pharmacokinetic Research Center, Izmir, Ege University ARGEFAR Drug Development and Pharmacokinetic Research Center, Izmir, Ege University ARGEFAR Drug Development and Pharmacokinetic Research Center, Izmir, Ege University, Medicine Faculty, Department of Endocrinology, Izmir, Ege University, Medicine Faculty, Department of Endocrinology, Izmir, Ege University ARGEFAR Drug Development and Pharmacokinetic Research Center, Izmir

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