Incorporation With Dendrimer-Like Biopolymer Leads to Improved Soluble Amount and In Vitro Anticancer Efficacy of Paclitaxel

Abstract

The aim of this study was to explore the solubilization efficacy of octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer, in improving the soluble amount and efficacy of paclitaxel (PTX), a potent anticancer active pharmaceutical ingredient. PTX was incorporated with OHPP in the form of solid dispersion (PTX-OHPP SD), which was characterized for its PTX crystallinity, interactions between PTX and OHPP, PTX soluble amount and dissolution profile, and in vitro inhibitory efficacy against cancer cell lines. The incorporation with OHPP led to the amorphous state of PTX. FTIR spectra showed potential hydrogen bonding between PTX and OHPP, and hydrophobic interaction could play an important role in the association of PTX molecules with OHPP particulates. The soluble amount of PTX with PTX-OHPP SD was >14,000 times that of PTX alone. During dissolution, over 70% PTX dissolved in 5 min and this soluble amount was maintained for at least 180 min. With the 3 cancer cell lines tested, the PTX of PTX-OHPP SD showed a much lower IC50 than the dimethyl sulfoxide–assisted PTX solutions. Based on the result, the mechanism of using OHPP as a highly potent solubilizer for PTX was discussed.