Preparation and Bioavailability Assessment of SMEDDS Containing Valsartan

Abstract

A self-microemulsifying drug delivery system (SMEDDS) has been developed to enhance diffusion rate and oral bioavailability of valsartan. The solubility of valsartan was checked in different oils, surfactants, and cosurfactants and ternary phase diagrams were constructed to evaluate the microemulsion domain. The valsartan SMEDDS was prepared using Capmul MCM (oil), Tween 80 (surfactant), and polyethylene glycol 400 (cosurfactant). The particle size distribution, zeta potential, and polydispersity index were determined and were found to be 12.3 nm, -0.746, and 0.138, respectively. Diffusion rate of valsartan was measured by in vitro dialysis bag method using phosphate buffer pH 6.8 as diffusion media. Developed high-performance liquid chromatography method was used to determine drug content in diffusion media. Oral bioavailability of valsartan SMEDDS was checked by using rabbit model. Results of diffusion rate and oral bioavailability of valsartan SMEDDS were compared with those of pure drug solution and of marketed formulation. Diffusion of valsartan SMEDDS showed maximum drug release when compared to pure drug solution and marketed formulation. The area under curve and time showed significant improvement as the values obtained were 607 ng h/mL and 1 h for SMEDDS in comparison to 445.36 and 1.36 h for market formulation suggesting significant increase (p < 0.01) in oral bioavailability of valsartan SMEDDS.

Formulation design and evaluation of a self-microemulsifying drug delivery system of lovastatin

“…The purpose was to arrive at a composition that contained minimum amount of surfactant and co-surfactant without compromising its globule size and stability (9). From Fig.…”

“…To determine the concentration of SMEDDS components that resulted in maximum microemulsion existence area, pseudoternary phase diagrams were constructed employing the water titration method at ambient temperature (25°C) (9). Mixtures of surfactant and co--surfactant (S mix ) in different ratios by mass (1:1, 1:2, 2:1) were prepared.…”

Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system

“…1 After oral administration of a capsule (VST 80 mg), absolute bioavailability (BA) of VST was relatively low at ~23%, which might be due to the limited solubility in water and acidic pH of the stomach. 2 In order to enhance the solubility and oral absorption of VST, various formulation approaches, such as solid dispersion, spray-dried emulsion, spray-dried nanosuspension, and supercritical antisolvent process, have been studied. [3][4][5][6] Self-microemulsifying drug delivery systems (SMEDDS) are widely known to overcome low solubility and poor oral absorption of water-insoluble drugs.…”

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“…[22] Several studies have been published reporting MC glycerides for developing SEDDS of a wide variety of drugs. [23][24][25][26] According to these studies, being small molecular volume oil phase, medium chain glycerides showed the high solvent capacity and excellent miscibility with other surfactants and co-surfactants and enhanced the permeability and bioavailability of candidate drugs. While SCT, such as Triacetin, has not been widely explored for preparing SMEDDS.…”