Glyceryl mono oleate cubosome / ca-alginate microparticulate system: a new matrix to improve the release properties of a water-soluble model drug

Citation:
Kassem, M. A., S. U. Z. A. N. AMIN, A. M. I. R. I. B. R. A. H. I. M. MOHAMED, and O. A. A. Ahmed, "Glyceryl mono oleate cubosome / ca-alginate microparticulate system: a new matrix to improve the release properties of a water-soluble model drug", International journal of pharmaceutical research and bio-science, vol. 3 (5), issue 2277-8713, pp. 177-193, 2014.

Abstract:

Objective: Alginate polymers suffer from rapid release of water soluble drugs in physiologic salt concentration. In this study, a new microsphere delivery system composed of GMO-cubosome embedded in Ca-alginate was designed to improve the release properties of a water-soluble model drug (Clindamycin). Methods: GMO-alginate based microspheres were prepared by w/o emulsion method, and formulation variables such as alginate molecular weight, concentration, surfactant ratio, and homogenization speed were fixed, while alginate:GMO ratio and drug concentration were investigated. Results: Alginate:GMO ratio significantly affected the particle size and morphology. Microparticles with low GMO contents (1:0.25) were spherical in shape with average diameter of 35.2 μm, with increasing GMO contents (1:0.5 to 1:1), microparticles become more flattened, collapsed and larger in size. Degradation study revealed that the erosion of microspheres decreased significantly by GMO-cubosomes addition as compared to blank Ca-alginate microspheres. 50% weight loss was reached at approximately 8hrs for 1:0.25 GMO containing microspheres as compared to 5.5hrs for blank microspheres without cubosomes, indicating that the presence of cubosomes increased the stability of Ca-alginate microspheres. Additionally, the extent of Clindamycin release from the Alginate:GMO(1:0.25) microspheres was 47% lower than the release from the conventional microspheres. Conclusions: These novel microparticles have a uniform structure, confined size distribution, satisfactory entrapment efficiency, and acceptable sustained release properties.

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