A facile carrier-free co-assembly nanoplatform for effective enhanced oral chemotherapy

Oral absorption of carrier-free self-assembly nanoplatform was limited by mucus barrier, p-gp efflux and liver metabolism. In this study, Pip-Cur-TA nanoparticle were constructed by co-assembly of tannic acid, curcumin and piperine via inter-molecular hydrogen-bonded and π-π interaction to improve the oral chemotherapy. The optimized Pip-Cur-TA nanoparticle showed an average diameter of 60 nm with a drug encapsulation efficiency of 67.02% and loading capacity of 61.37%. Pip-Cur-TA nanoparticles showed pH-dependent drug release, mucosal adhesion, inhibition of p-gp and liver metabolism and improved membrane permeability. Oral Pip-Cur-TA nanoparticle produced high oral delivery efficiency and relative oral bioavailability of 12.84% in rats, and further showed significant tumor inhibition on PC-3 tumor cells. These findings confirmed that Pip-Cur-TA nanoparticle might be a promising oral drug formulation for chemotherapy.