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Molecules. 2019 Apr 9;24(7). pii: E1382. doi: 10.3390/molecules24071382.

Lactosylated Albumin Nanoparticles: Potential Drug Nanovehicles with Selective Targeting Toward an In Vitro Model of Hepatocellular Carcinoma.

Author information

1
Centro de Investigacion en Alimentacion y Desarrollo, A.C. Carretera Gustavo E. Aztiazaran 46, Hermosillo 83304, Sonora, Mexico. naye_krebs@hotmail.com.
2
Departamento de Investigacion en Fisica. Universidad de Sonora, P.O. Box 5-088, Hermosillo, C.P. 83190, Mexico. andreisarabia@gmail.com.
3
Departamento de Investigacion en Fisica. Universidad de Sonora, P.O. Box 5-088, Hermosillo, C.P. 83190, Mexico. erika.silva@difus.uson.mx.
4
Departamento de Investigacion en Fisica. Universidad de Sonora, P.O. Box 5-088, Hermosillo, C.P. 83190, Mexico. alexel.burgara@gmail.com.
5
Centro de Investigacion en Alimentacion y Desarrollo, A.C. Carretera Gustavo E. Aztiazaran 46, Hermosillo 83304, Sonora, Mexico. gupa@ciad.mx.
6
Centro de Investigacion en Alimentacion y Desarrollo, A.C. Carretera Gustavo E. Aztiazaran 46, Hermosillo 83304, Sonora, Mexico. gramos@ciad.mx.
7
Departamento de Investigacion en Fisica. Universidad de Sonora, P.O. Box 5-088, Hermosillo, C.P. 83190, Mexico. mpedroza@cifus.uson.mx.
8
Centro de Investigacion en Alimentacion y Desarrollo, A.C. Carretera Gustavo E. Aztiazaran 46, Hermosillo 83304, Sonora, Mexico. lvazquez@ciad.mx.

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.

KEYWORDS:

BSA-lactosylate; HepG2 cell line; asialoglycoprotein receptor; nanoparticles

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