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

Centro de Investigacion en Alimentacion y Desarrollo, A.C. Carretera Gustavo E. Aztiazaran 46, Hermosillo 83304, Sonora, Mexico
Departamento de Investigacion en Fisica. Universidad de Sonora, P.O. Box 5-088, Hermosillo, C.P. 83190, Mexico
Author to whom correspondence should be addressed.
Molecules 2019, 24(7), 1382;
Received: 25 January 2019 / Revised: 27 March 2019 / Accepted: 4 April 2019 / Published: 9 April 2019
(This article belongs to the Special Issue Glycotherapeutics: Emerging Roles of Glycans in Medicine)
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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. View Full-Text
Keywords: nanoparticles; BSA-lactosylate; HepG2 cell line; asialoglycoprotein receptor nanoparticles; BSA-lactosylate; HepG2 cell line; asialoglycoprotein receptor

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Teran-Saavedra, N.G.; Sarabia-Sainz, J. .-I.; Silva-Campa, E.; Burgara-Estrella, A.J.; Guzmán-Partida, A.M.; Ramos-Clamont Montfort, G.; Pedroza-Montero, M.; Vazquez-Moreno, L. Lactosylated Albumin Nanoparticles: Potential Drug Nanovehicles with Selective Targeting Toward an In Vitro Model of Hepatocellular Carcinoma. Molecules 2019, 24, 1382.

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