Abstract
Hepatocellular carcinoma (HCC) ranks fifth in occurrence and second in mortality of all cancers. The development of effective therapies for HCC is urgently needed. Anticancer drugs targeted to the liver-specific asialoglycoprotein receptors (ASGPRs) are viewed as a promising potential treatment for HCC. ASGPRs facilitate the recognition and endocytosis of molecules, and possibly vehicles with galactose end groups, by the liver. In this study, bovine serum albumin (BSA) was conjugated with lactose using a thermal treatment. The formation of lactosylated BSA (BSA-Lac) was confirmed by a change of the chemical structure, increased molecular mass, and Ricinus communis lectin recognition. Subsequently, the low-crosslinking BSA-Lac nanoparticles (LC BSA-Lac NPs) and high-crosslinking BSA-Lac nanoparticles (HC BSA-Lac NPs) were synthesized. These nanoparticles presented spherical shapes with a size distribution of 560 ± 18.0 nm and 539 ± 9.0 nm, as well as an estimated surface charge of −26 ± 0.15 mV and −24 ± 0.45 mV, respectively. Both BSA-Lac NPs were selectively recognized by ASGPRs as shown by biorecognition, competition, and inhibition assays using an in vitro model of HCC. This justifies pursuing the strategy of using BSA-Lac NPs as potential drug nanovehicles with selective direction toward hepatocellular carcinoma.
Highlights
Hepatocellular carcinoma (HCC) is a public health concern because HCC is fifth in the occurrence rate for all cancers, and second only to lung cancers in mortality rate [1,2]
The aim of the present work was to synthesize bovine serum albumin (BSA)-lactose monohydrate (Lac) NPs and test their specific biorecognition by asialoglycoprotein receptors (ASGPRs) present on HepG2 cells, which is a line derived from an HCC
Albumin glycated with lactose (BSA-glucose-β (4-1) galactose) provides galactose residues that are available for biological recognition by specific receptors such as those involved in bacterial adhesins or plant lectins [15,18]
Summary
Hepatocellular carcinoma (HCC) is a public health concern because HCC is fifth in the occurrence rate for all cancers, and second only to lung cancers in mortality rate [1,2]. HCC is usually diagnosed in the advanced stages when prognosis for the disease recovery is meager, and survival is one to two months [5,6]. Recent reports suggest that targeting drugs to a specific tissue allows high concentrations of the drug within a tumor; this results in high efficacy and low toxicity in the organism [2,7]. In this sense, nanovehicles targeted to tumor sites could potentially be used as anticancer therapies with greater safety and efficacy [1,2]
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