Asialoglycoprotein receptor mediated hepatocyte targeting — Strategies and applications

D’Souza, Anisha A.; Devarajan, Padma V.

doi:10.1016/j.jconrel.2015.02.022

Cited by 393 publications

(273 citation statements)

References 227 publications

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“…36,37 The different cellular uptake of Lf-PLS in both HCC cell lines and NIH 3T3 cells might be mainly dependent on the different ASGPR expression on cell membranes. 13,36,37 Similar results were also obtained in the previous study of coumarin-6-loaded Lf-PLS binding to HepG2. 21 The cellular uptake results also suggested that more LfPLSs were endocytosed into HepG2 and BEL7402 cells than into SMMC7721 cells.…”

supporting

confidence: 83%

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Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma

Wei¹,

Guo

Tu³

et al. 2015

IJN

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Lactoferrin (Lf) is a potential-targeting ligand for hepatocellular carcinoma (HCC) cells because of its specific binding with asialoglycoprotein receptor (ASGPR). In this present work, a doxorubicin (DOX)-loaded, Lf-modified, polyethylene glycol (PEG)ylated liposome (Lf-PLS) system was developed, and its targeting effect and antitumor efficacy to HCC was also explored. The DOX-loaded Lf-PLS system had spherical or oval vesicles, with mean particle size approximately 100 nm, and had an encapsulation efficiency of 97%. The confocal microscopy and flow cytometry indicated that the cellular uptake of Lf-PLS was significantly higher than that of PEGylated liposome (PLS) in ASGPR-positive cells ( P <0.05) but not in ASGPR-negative cells ( P >0.05). Cytotoxicity assay by MTT demonstrated that DOX-loaded Lf-PLS showed significantly stronger antiproliferative effects on ASGPR-positive HCC cells than did PLS without the Lf modification ( P <0.05). The in vivo antitumor studies on male BALB/c nude mice bearing HepG2 xenografts demonstrated that DOX-loaded Lf-PLS had significantly stronger antitumor efficacy compared with PLS ( P <0.05) and free DOX ( P <0.05). All these results demonstrated that a DOX-loaded Lf-PLS might have great potential application for HCC-targeting therapy.

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supporting

confidence: 83%

“…11,13 Recently, lactoferrin (Lf), a mammalian cationic iron-binding glycoprotein belonging to the Tf family, has been demonstrated to bind ASGPR with high affinity in a galactoseindependent manner. [14][15][16][17] It might be suggested that Lf is a good ligand for ASGPR binding.…”

Section: Introductionmentioning

confidence: 99%

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma

Wei¹,

Guo

Tu³

et al. 2015

IJN

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“…Известно, что клетки печени содержат на своей поверхности асиалогликопротеиновые рецепторы и галектины, лигандами для которых служат галактозо-содержащие углеводы [10,13,14]. Поэтому для создания адресной композиции в данной работе липосомы модифицировали нейтральными углеводами, содержащими терминальный остаток лактозы.…”

Section: результаты и обсуждениеunclassified

“…Полученные соединения встраивали в липосомы в качестве лигандов направленной доставки в количестве 10% от липидного состава. Было установлено, что количество лигандов на поверхности липосомы имеет гораздо большее значение, чем их степень разветвлённости [10].…”

Section: результаты и обсуждениеunclassified

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Lactose-based glycoconjugates with variable spacers for design of liver-targeted liposomes

et al. 2017

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Asialoglycoprotein receptors are highly abundant on the hepatocyte surface and have specific binding sites for blood serum glycoproteins. Such discovery resulted in development of liver-targeted drug delivery systems because modification of the liposomal surface by carbohydrate derivatives results in an increase of endocytosis, which facilitates selective uptake of such systems by hepatocytes. In this study we have synthesized novel lactose derivatives containing a palmitic hydrophobic domain. They were used for modification of the liposome surface. Transfection activity of modified liposomes was analyzed on the HepG2 cell line (hepatocytes) and showed an increase in the transfection efficiency as compared to the non-modified liposomes. At the same time transfection activities of modified and non-modified liposomes were similar in the case of a non-hepatocyte cell line (293T). The novel lactose-based glycoconjugates may be a promising tool for developing efficient vectors for delivery of nucleic acids to hepatocytes.

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Multifunctional Glyco‐Nanofibers: siRNA Induced Supermolecular Assembly for Codelivery In Vivo

Chang

Peng

et al. 2017

Adv Funct Materials

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Targeted codelivery and controlled release of drug/siRNA (small interfering RNA) in a safe and effective vehicle hold great promises for overcoming drug resistance and optimal efficacy in cancer treatment; however, rational design and preparation of such vehicles remain a critical challenge. Thus, glyco‐nanofibers (GNFs) are fabricated via supermolecular assembly of polyanionic siRNA and cationic vesicles to simultaneously deliver siRNA and doxorubicin hydrochloride (DOX) in vitro and in vivo. The vesicles are created through self‐assembly of a positively charged amphiphilic lactose derivative featuring a lactose moiety and a ferrocenium unit on either end of the molecule. The GNFs display excellent biocompatibility, enhanced cell‐penetrating ability, and hepatoma targetability. The high transport efficiency of siRNA, effective gene silencing ability, and enhanced cytotoxicity to HepG2 cells of GNFs loaded with DOX are observed in vitro. Furthermore, in vivo experiments show reduced systemic toxicity and enhanced therapeutic efficacy of DOX to both HepG2 and HepG2/ADR subcutaneous tumor‐bearing nude mice. This work proves the electrostatic self‐assembly between cationic carbohydrates and polyanionic siRNA to be a convenient and effective strategy to fabricate a single vehicle for safe and effective codelivery of drug/siRNA, which can be used to combine chemo‐ and gene‐therapy against cancers and other diseases.

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Asialoglycoprotein receptor mediated hepatocyte targeting — Strategies and applications

Cited by 393 publications

References 227 publications

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma

Lactose-based glycoconjugates with variable spacers for design of liver-targeted liposomes

Multifunctional Glyco‐Nanofibers: siRNA Induced Supermolecular Assembly for Codelivery In Vivo

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Asialoglycoprotein receptor mediated hepatocyte targeting — Strategies and applications

Cited by 393 publications

References 227 publications

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to&nbsp;hepatocellular carcinoma

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to&nbsp;hepatocellular carcinoma

Lactose-based glycoconjugates with variable spacers for design of liver-targeted liposomes

Multifunctional Glyco‐Nanofibers: siRNA Induced Supermolecular Assembly for Codelivery In Vivo

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Product

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Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma

Lactoferrin-modified PEGylated liposomes loaded with doxorubicin for targeting delivery to hepatocellular carcinoma