Nanoformulations of the vascular inhibitors: Combretastatin A4 and combretastatin A4 phosphate / 国际药学研究杂志

ABSTRACT

Combretastatin A4 (CA4), a vascular inhibitor, can target tubulin and inhibit tubulin polymerization, thus it can inhibit the tumor blood vessels and has antitumor effect. But it is insoluble in water and has low bioavailability. CA4 phosphate (CA4P), the derivative of CA4, can improve the solubility of CA4 and convert into CA4. CA4P is undergoing phase II/III clinical trials abroad. However, CA4P has several undesirable side effects and relative short half-life in vivo. Nanoformulations can increase the dissolution and absorption of the drug and obtain controlled release and targeting, prolong the efficacy and reduce side effects. Working on the physical and chemical characteristics and biological pharmacy defects of CA4 and CA4P nanoformulations may change the dissolution, absorption and distribution of the drug. This paper reviews the current nanoformulations of CA4 and CA4P, including den-drimer, polymeric micelle (PM), nanoparticles (NP), long-circulating liposome (LCL), and discusses the prospects of their nanoformulations.