Paclitaxel-Loaded β-Cyclodextrin-Modified Poly(Acrylic Acid) Nanoparticles through Multivalent Inclusion for Anticancer Therapy.

A nanoassembled drug delivery system for anticancer treatment, formed by the host-guest interactions between paclitaxel (PTX) and β-cyclodextrin (β-CD) modified poly(acrylic acid) (PCDAA), is successfully prepared. After such design, the aqueous solubility of PTX is greatly increased from 0.34 to 36.02 μg mL(-1), and the obtained PCDAA-PTX nanoparticles (PCDAA-PTX NPs) exhibit a sustained PTX release behavior in vitro. In vitro cytotoxicity finds that PCDAA-PTX NPs can accumulate significantly in tumor cells and remain the pharmacological activity of PTX. The in vivo real-time biodistribution of PCDAA-PTX NPs is investigated using near-infrared fluorescence imaging, indicating that the PCDAA-PTX NPs can effectively target to the tumor site by the enhanced permeability and retention effect in H22 tumor-bearing mice. Through in vivo antitumor examination, PCDAA-PTX NPs exhibit superior efficacy in impeding the tumor growth compared to the commercially available Taxol®.