Mevacor/Poly(vinyl acetate/2-hydroxyethyl methacrylate) as Solid Solution: Preparation, Solubility Enhancement and Drug Delivery

Abstract

Mevacor/Poly(vinyl acetate-co-2-hydroxyethyl methacrylate) drug carrier systems (MVR/VAC-HEMA) containing different Mevacor (MVR) contents were prepared in one pot by free radical copolymerization of vinyl acetate with 2-hydroxyethyl methacrylate using an LED lamp light in the presence of camphorquinone as a photoinitiator and Mevacor as a drug filler. The prepared material was characterized by FTIR, 1H NMR, DSC, SEM and XRD methods. Different parameters influencing the efficiency in the Mecvacor-water solubility and the drug delivery of this system, such as the swelling capacity of the carrier, the amount of Mevacor loaded and the pH medium have been widely investigated. The results obtained revealed that the Mevacor particles were uniformly dispersed in their molecular state in the copolymer matrix forming a solid solution; the cell toxicity of the virgin poly(vinyl acetate-co-2-hydroxy ethyl methacrylate) (VAC-HEMA) and MVR/VAC-HEMA drug carrier system exhibited no significant effect on their viability when between 0.25 and 2.00 wt% was loaded in these materials; the average swelling capacity of VAC-HEMA material in water was found to be 45.16 wt%, which was practically unaffected by the pH medium and the solubility of MVR deduced from the release process reached more than 22 and 37 times that of the powder dissolved directly in pH 1 and 7 media, respectively. The in vitro MVR release kinetic study revealed that the MVR/VAC-HEMA system containing 0.5 wt% MVR exhibited the best performance in the short gastrointestinal transit (GITT), while that containing 2.0 wt% is for the long transit as they were able to considerably reduce the minimum release of this drug in the stomach (pH1).