In-vitro and in-vivo evaluation of austocystin D liposomes

Abstract

Objectives: The purpose this study is to enhance the anti-tumour activity of austocystin D (AD) by AD-loaded liposomes (AD-Ls).

Methods: AD-Ls were prepared by the film dispersion-ultrasonication method and characterized in terms of particle size and zeta potential, encapsulation efficiency and in-vitro drug release. In vivo, the pharmacokinetics, biodistribution and anti-tumour effect were also compared with those of the solution.

Key findings: The obtained liposomes were a mildly translucent suspension, with a particle size of 71.26 ± 6.43 nm, a polydispersity index of 0.259 ± 0.017 and a zeta potential of -9.9 ± 1.8 mV. Transmission electron microscope examination showed that the liposomes had a spherical shape and a multilayer structure. The encapsulation efficiency ofAD-Ls was 83.74 ± 1.26%. AD was continuously released from liposomes up to 72 h in in-vitro experiments. The growth of HT-29 tumours in animal models was controlled more effectively by AD-LS than by AD solution. Pharmacokinetic study showed that AD-Ls had higher t½β and mean retention time. Biodistribution results in tumour-bearing mice showed that the AD-LS could target to liver and tumour.

Conclusions: This study indicates that AD-Ls are a potential carrier of AD for the treatment of tumours in the liver, increasing the cure efficiency and decreasing the side effects on other tissues.