Abstract
Purpose: To develop suitable solid lipid nanoparticles (SLN) containing carvedilol (CL) for controlled delivery to site of action.Methods: Solid lipid nanoparticles (SLNs) containing carvedilol (CL) were prepared by hot homogenization and ultrasonication methods. The SLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, polydispersity index, cytotoxicity, solid state characterization and drug release. The stability of the formulations was investigated by monitoring their properties for a period of 3 months.Results: The mean size of the nanoparticles was in the range of 130.70 ± 1.80 to 154.40 ± 2.40 nm. Solid state analysis showed that carvedilol was uniformly dispersed in the lipid nanoparticles. Drug entrapment efficiency ranged from 96.03 ± 0.13 to 93.46 ± 0.21 % while in vitro cumulative drug release from the nanoparticles in simulated intestinal fluid (SIF) and phosphate buffer containing 30% PEG (pH 6.8) was 96.57 ± 0.40 and 75.13 ± 0.15 %, respectively, at the end of 24 h. In vitro release of carvedilol from SLNs followed fist order kinetics and Higuchi diffusion model.Conclusion: The SLNs developed in this study represent a promising safe system for the sustained and controlled delivery of carvedilol.Keywords: Carvedilol, Solid lipid nanoparticles, Antihypertensive, Sustained release
Highlights
Cardiovascular diseases cause a significant number of deaths around the world
In vitro drug release of CL from optimized solid lipid nanoparticles (SLN) formulations were studied through dialysis bag which was sealed with clamps and stirred at 50 rpm using magnetic stirrer
In order to study the mechanism of drug release from the SLNs, the release data were fitted to different equations with DDSolver programme [16]
Summary
Cardiovascular diseases cause a significant number of deaths around the world. Considering the number of patients worldwide who experience cardiovascular problems, concerted efforts have been made to develop drugs to prevent and/ or treat cardiovascular diseases. Constant volume (20 μL) of formulations were dispersed in 1 mL of distilled water and particle size (PI) and zeta potential were recorded (n=3). Characteristics of the solid lipid structures of SLNs as well as stability changes in CL after the preparation of the formulation was analysed using powdered X-ray diffractometry (PXRD), product of Rigaku, Tokyo, Japan. In vitro drug release of CL from optimized SLN formulations were studied through dialysis bag (cellulose membrane) which was sealed with clamps and stirred at 50 rpm using magnetic stirrer. At pre-determined time intervals, 1-mL samples were withdrawn from the dissolution media respectively and analyzed for the drug content using HPLC (Shimadzu Corporation, Kyoto, Japan) at 242 nm and fresh 1 mL, of each medium was added to the appropriate system. In order to study the mechanism of drug release from the SLNs, the release data were fitted to different equations with DDSolver programme [16]
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