Preparation and evaluation of targeted albumin lipid nanoparticles with lactobionic acid for targeted drug delivery of sorafenib in hepatocellular carcinoma

Sorafenib (SF) is an anticancer drug used to treat hepatocellular carcinoma (HCC), but it is associated with a wide range of side effects. The objective of this research was to prepare SF-loaded albumin lipid nanoparticles (ALNs) consisting of medium-chain triglycerides and lactobionic acid-human serum albumin conjugate (LA-HSA conjugate) as a targeted drug delivery system of SF for the treatment of HCC. HSA was modified with ethylenediamine and conjugated to LA as a targeting agent. ALNs were characterized concerning particle size, zeta potential, drug encapsulation efficiency, and in vitro drug release. The cytotoxicity and cellular uptake of the targeted and untargeted ALNs were also evaluated in HepG2 cells. The results showed that the optimized targeted ALNs, which consisted of 10% (w/v) of HSA-LA, 5% (w/v) of poloxamer, and 5% of organic phase ratio with 0.1% (w/v) of lecithin, showed the particle size of 280.1 & nbsp; +/-& nbsp; 4.4 nm, the zeta potential of & nbsp; -12.3 & nbsp; +/- & nbsp;0.9 mV, and the entrapment efficiency of 97.6 & nbsp; +/-& nbsp; 2.2%. MTT assay and cellular uptake studies showed that the targeted ALNs had more cytotoxicity and cellular uptake than the untargeted ones in HepG2 cells (P < 0.05). Overall, the targeted delivery system reported here can enhance the therapeutic efficacy of SF in HCC.

Automated summary

This study developed sorafenib-loaded albumin lipid nanoparticles (ALNs) for targeted drug delivery in hepatocellular carcinoma (HCC). The ALNs, consisting of medium-chain triglycerides and lactobionic acid-human serum albumin conjugate (LA-HSA conjugate), showed enhanced cytotoxicity and cellular uptake in HepG2 cells compared to untargeted ALNs. Overall, the targeted ALNs can improve the therapeutic efficacy of sorafenib in HCC.