Abstract
Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.
Highlights
Ampelopsin, isolated from the tender stem and leaves of the plant species Ampelopsis grossedentata (Hand-Mazz) W
Capmul MCM showed higher solubilising capacity compared to other vehicles
Capmul MCM was selected as the oil phase
Summary
Ampelopsin, isolated from the tender stem and leaves of the plant species Ampelopsis grossedentata (Hand-Mazz) W. The ampelopsin has very less solubility in water (0.2 mg/mL at 25◦C), it has very low permeability through intestinal mucosa [5]. As a modern drug carrier system, microemulsions are defined as single optically isotropic and thermodynamically stable solution with droplet sizes in the submicron range. They consist of an oil phase, a surfactant, a cosurfactant, and an aqueous phase. Use of ampelopsin in most pharmaceutical preparations and some research experiments was thereby limited due to its low water solubility, low intestine permeability and degradation in solution. The main aim of this study was to improve the bioavailability of Ampelopsin by preparing its ME.
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