Preparation and characterization of mucoadhesive microcapsules of paclitaxel

Abstract

The objective of the present work is to develop paclitaxel encapsulated muco-adhesive microcapsules. The improvement aims to enhance its usefulness and control the drug release in cancer patients. Paclitaxel microcapsules with a coat consisting of sodium alginate and a muco-adhesive polymer such as acacia, Carbomer 941, Povidone K-30, Macrogol (PEG 6000) were prepared by ionotropic gelation technique. These microcapsules were evaluated for morphological characters, drug content, loading efficiency, drug-polymer interactions, swelling ratio, muco-adhesive properties and in vitro drug release. The resulting microcapsules were discrete, spherical, and free-flowing with a particle size range of 534 to 822 µm. The microencapsulation efficiency was 45.09–99.83%. The microcapsules prepared with alginate along with macrogol (F4M) have exhibited excellent muco-adhesive property in the in vitro wash-off test. The swelling ratio of microcapsules was enhanced with an increased alginate concentration, and the formulation (F4) showed the highest index of swelling, that is 2666. Paclitaxel release from these muco-adhesive microcapsules was slow and extended throughout six h and further depends upon the concentration of the alginate. The per cent drug release of alginate-acacia microcapsules (F4Ac) was higher than other formulations in the present study. In conclusion, alginate-acacia muco-adhesive microcapsules could be a promising vehicle for oral controlled release of paclitaxel.