Construction of long circulating and deep tumor penetrating gambogic acid-hydroxyethyl starch nanoparticles

Gambogic acid (GA) has been approved to enter the phase III clinical trial. However, due to its short half-life, low water solubility, poor stability and inflammatory response, GA failed to pass the clinical superiority evaluation. Nano-preparations perform well in prolonging drug half-life, improving drug solubility, and enhancing drug stability etc. Therefore, a self-assembled nanoparticle (GA-HES/NPs) with long circulation and deep tumor penetration ability was designed, in which hydroxyethyl starch (HES) endowed GA-HES/NPs with longer circulation time as well as deep tumor penetration ability, and the simple synthesis method ensured the stability of GA structure. Experimental results showed that GA-HES/NPs owned a certain tumor targeting and deep tumor penetration ability, as well as longer circulation time, which could enhance the therapeutic effect of GA.