Preparation and release studies of alkannin-containing microcapsules.

Microcapsules containing the pharmaceutical substance alkannin were prepared by the solvent evaporation method to enhance alkannin stability (reduce photo-oxidation, polymerization), to decrease its hydrophobicity and to control its release rate. The effect of various parameters, such as the type of polymeric matrix, the type of surfactant used for microcapsules preparation and the addition of Pistacia lentiscus resin in the core, on the characteristics of the produced microcapsules and the release rate of alkannin were investigated experimentally. Among the polymers tested for matrix, ethylcellulose of viscosity 46cp was the most successful, while ethylcellulose 10cp gave microcapsules with good morphological characteristics but high release rate. Beeswax resulted in flocculation and P. lentiscus resin with or without colophony as the matrix resulted in compact particles with no pores and much slower release, but did not allow alkannin to release easily from the matrix. Sodium dodecyl sulfate resulted in microcapsules with desirable morphological and physicochemical characteristics, while acacia and tragacanth gums were not indicated as surfactants in alkannin microencapsulation since they gave a high release rate and a great extent of particle size, respectively. The incorporation of Pistacia lentiscus resin in the capsule core increased loading and microencapsulation efficiency. Ethylcellulose of 46cp viscosity with sodium dodecyl sulfate as surfactant had the best characteristics studied for alkannin microencapsulation. Finally, the dissolution rate of alkannin from microcapsules was studied in a simulated intestinal and gastric environment and an external environment. Alkannin-containing microcapsules with improved properties can be used internally and externally as a new drug-delivery system.