This study focused on designing a large-scale producible vehicle for the pharmaceutically important compound berberine, to simultaneously improve its bioavailability against cancer cells and reduce cytotoxicity toward normal cells. This vehicle is composed of chitosan and tripolyphosphate, and was prepared with a simple ionic cross-linking method. The properties of the berberine-loaded chitosan-tripolyphosphate nanoparticles (BB-LCTNP) were dependent on berberine, chitosan, and tripolyphosphate concentrations. The bioavailability improvement and anticancer efficiency of the BB-LCTNPs were analyzed using MDA-MB-435 and Colo-205 cells. The results revealed that the particle size, loading efficiency, and IC50 of the BB-LCTNPs can be controlled easily. The pharmacodynamic availability of berberine increased up to 3 times when loaded into the nanoparticles because they directly targeted cancer cell nuclei. Moreover, the BB-LCTNPs were non-toxic toward normal cells. In vivo studies revealed that BB-LCTNPs can reduce drug dosages up to 3 times and suppress tumor growth. The surfaces of the prepared BB-LCTNPs were modified using mPEG acid, but the in vitro and in vivo studies of these particles are currently ongoing.
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