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Design of cholesterol arabinogalactan anchored liposomes for asialoglycoprotein receptor mediated targeting to hepatocellular carcinoma: In silico modeling, in vitro and in vivo evaluation

P. Pathak, V. Dhawan, A. Magarkar, R. Danne, S. Govindarajan, S. Ghosh, F. Steiniger, P. Chaudhari, V. Gopal, A. Bunker, T. Róg, A. Fahr, M. Nagarsenker,

. 2016 ; 509 (1-2) : 149-58. [pub] 20160523

Language English Country Netherlands

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc17023952

We have developed active targeting liposomes to deliver anticancer agents to ASGPR which will contribute to effective treatment of hepatocellular carcinoma. Active targeting is achieved through polymeric ligands on the liposome surface. The liposomes were prepared using reverse phase evaporation method and doxorubicin hydrocholoride, a model drug, was loaded using the ammonium sulphate gradient method. Liposomes loaded with DOX were found to have a particle size of 200nm with more than 90% entrapment efficiency. Systems were observed to release the drug in a sustained manner in acidic pH in vitro. Liposomes containing targeting ligands possessed greater and selective toxicity to ASGPR positive HepG2 cell lines due to specific ligand receptor interaction. Bio-distribution studies revealed that liposomes were concentrated in the liver even after 3h of administration, thus providing conclusive evidence of targeting potential for formulated nanosystems. Tumor regression studies indicated greater tumor suppression with targeted liposomes thereby establishing superiority of the liposomal system. In this work, we used a novel methodology to guide the determination of the optimal composition of the targeting liposomes: molecular dynamics (MD) simulation that aided our understanding of the behaviour of the ligand within the bilayer. This can be seen as a demonstration of the utility of this methodology as a rational design tool for active targeting liposome formulation.

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$a We have developed active targeting liposomes to deliver anticancer agents to ASGPR which will contribute to effective treatment of hepatocellular carcinoma. Active targeting is achieved through polymeric ligands on the liposome surface. The liposomes were prepared using reverse phase evaporation method and doxorubicin hydrocholoride, a model drug, was loaded using the ammonium sulphate gradient method. Liposomes loaded with DOX were found to have a particle size of 200nm with more than 90% entrapment efficiency. Systems were observed to release the drug in a sustained manner in acidic pH in vitro. Liposomes containing targeting ligands possessed greater and selective toxicity to ASGPR positive HepG2 cell lines due to specific ligand receptor interaction. Bio-distribution studies revealed that liposomes were concentrated in the liver even after 3h of administration, thus providing conclusive evidence of targeting potential for formulated nanosystems. Tumor regression studies indicated greater tumor suppression with targeted liposomes thereby establishing superiority of the liposomal system. In this work, we used a novel methodology to guide the determination of the optimal composition of the targeting liposomes: molecular dynamics (MD) simulation that aided our understanding of the behaviour of the ligand within the bilayer. This can be seen as a demonstration of the utility of this methodology as a rational design tool for active targeting liposome formulation.
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$a Dhawan, Vivek $u Bombay College of Pharmacy, University of Mumbai, Mumbai 400098, India.
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$a Magarkar, Aniket $u Academy of the Sciences of the Czech Republic, Prague, Czech Republic; Centre for Drug Research, Division of Pharmaceutical Bioscience, Faculty of Pharmacy, University of Helsinki, FI-00014 Helsinki, Finland.
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$a Danne, Reinis $u Department of Physics, Tampere University of Technology, PO Box 692, FI-33101 Tampere, Finland.
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$a Govindarajan, Srinath $u Council of Scientific and Industrial Research-Centre for Cellular and Molecular Biology (CSIR-CCMB), Hyderabad 500007, India.
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$a Ghosh, Sandipto $u Small Animal Imaging Facility (SAIF), Advanced Centre for Treatment Research and Education in Cancer (ACTREC), Kharghar, Mumbai 410210, India.
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$a Steiniger, Frank $u Center for Electron Microscopy of the Medical Faculty, Friedrich-Schiller-University Jena, Ziegelmühlenweg 1, D-07740 Jena, Germany.
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$a Bunker, Alex $u Centre for Drug Research, Division of Pharmaceutical Bioscience, Faculty of Pharmacy, University of Helsinki, FI-00014 Helsinki, Finland.
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$a Róg, Tomasz $u Department of Physics, Tampere University of Technology, PO Box 692, FI-33101 Tampere, Finland.
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$a Fahr, Alfred $u Department of Pharmaceutical Technology, Friedrich-Schiller-University Jena, Lessing-str. 8, D-07743 Jena, Germany.
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$a Nagarsenker, Mangal $u Bombay College of Pharmacy, University of Mumbai, Mumbai 400098, India. Electronic address: mangal.nagarsenker@gmail.com.
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