Microfluidic fabricated bisdemethoxycurcumin thermosensitive liposome with enhanced antitumor effect.

[Display omitted] • The microfluidic chip is simply prepared by the laser cutting machine and assembled in low-cost. • The fabricated bisdemethoxycurcumin thermal liposome based on microfluidic platform, are decomposed under mild local hyperthermia and could be beneficial to enhance the antitumor effect of raw insoluble materials, which could promote the translation of liposome. • Glycyrrhizin was slected as the surfactant to improve the solubility of bisdemethoxycurcumin and effectively increased the drug loading of liposome to 5.46 ± 0.001%. Bisdemethoxycurcumin (BDMC) is the main active ingredient that is isolated from Zingiberaceae plants, wherein it has excellent anti-tumor effects. However, insolubility in water limits its clinical application. Herein, we reported a microfluidic chip device that can load BDMC into the lipid bilayer to form BDMC thermosensitive liposome (BDMC TSL). The natural active ingredient glycyrrhizin was selected as the surfactant to improve solubility of BDMC. Particles of BDMC TSL had small size, homogenous size distribution, and enhanced cultimulative release in vitro. The anti-tumor effect of BDMC TSL on human hepatocellular carcinomas was investigated via 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method, live/dead staining, and flowcytometry. These results showed that the formulated liposome had a strong cancer cell inhibitory, and presented a dose-dependent inhibitory effect on migration. Further mechanistic studies showed that BDMC TSL combined with mild local hyperthermia could significantly upregulate B cell lymphoma 2 associated X protein levels and decrease B cell lymphoma 2 protein levels, thereby inducing cell apoptosis. The BDMC TSL that was fabricated via microfluidic device were decomposed under mild local hyperthermia, which could beneficially enhance the anti-tumor effect of raw insoluble materials and promote translation of liposome. [ABSTRACT FROM AUTHOR]