Abstract
Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).
Highlights
Nanotechnology is the technology achieved on nanoscale having the application in the real world
The foremost criteria for selection of materials for formulation development are pharmaceutical acceptability, nonirritant and nonsensitizing nature, and their generally regarded as safe (GRAS) categorization
Further requirements for Solid lipid nanoparticles (SLNs) formulation are higher solubility of the drug in the nonaqueous phase to maintain the drug in solubilized form
Summary
Nanotechnology is the technology achieved on nanoscale having the application in the real world. It encompasses the production and application of physical, chemical, and biological systems at submicron dimensions as well as the integration of the resulting nanostructures into larger systems [1,2,3,4]. SLNs are at the forefront of the rapidly developing field of nanotechnology due to possibility for site specific drug delivery, controlled release, increased bioavailability, reduced side effects, smaller dosage form, dosage form stability, and reduction in fed/fasted variability [6, 7]. Enhancement of bioavailability of entrapped drugs via modification of dissolution rate and/or improvement of tissue distribution, and targeting of drugs by using SLNs have been reported in various application routes like parenteral (intravenously, intramuscularly, or subcutaneously), oral, rectal, ophthalmic, and topical (cosmetics and dermatological) preparations [8,9,10,11]
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