Mucoadhesive paclitaxel-loaded chitosan-poly (isobutyl cyanoacrylate) core-shell nanocapsules containing copaiba oil designed for oral drug delivery

Abstract

The development of drug delivery systems for potent anticancer drugs like paclitaxel remains a challenger. The aim of this work was to study the mucoadhesive properties of paclitaxel-loaded chitosan-poly (isobutyl cyanoacrylate) core-shell nanocapsules designed for oral drug delivery. Using an experimental design approach, the nanocapsules were produced and, then, physicochemically characterized. Mucoadhesion assays were performed in-vitro by the aggregation test with mucin and ex-vivo, in Ussing Chamber, using freshly excised rat intestinal mucosa. [3H]-paclitaxel dosages were carried out by liquid scintillation. Paclitaxel-loaded nanocapsules showed a mean hydrodynamic diameter of 470 nm with low polydispersity index and spherical form. Encapsulation efficiency and drug loading of paclitaxel were 74 ± 1% and 1.70 ± 0.02%, respectively. After drying, nanocapsules could be redispersed with no changes on their nanostructure. Dispersions of nanocapsules were stable in simulated gastric medium for 120 min, and after six months of storage at 4 °C. They showed interesting mucoadhesive properties with mucins and good association (9%) with the intestinal mucosa of the rat. Taking together, results from the present work are encouraging to pursue the development of chitosan-coated nanocapsules for oral delivery of paclitaxel as a new treatment for cancer with possible synergetic anticancer effect with the therapeutically active components found in copaiba oil.