title: Galactosylated alginate-curcumin micelles for enhanced delivery of curcumin to hepatocytes.
abstract: Galactosylated alginate-curcumin conjugate (LANH2-Alg Ald-Cur) is synthesized for targeted delivery of curcumin to hepatocytes exploiting asialoglycoprotein receptor (ASGPR) on hepatocytes. The synthetic procedure includes oxidation of alginate (Alg), modification of lactobionic acid (LA), grafting of targeting group (modified lactobinic acid, LANH2) and conjugation of curcumin to alginate. Alginate-curcumin conjugate (Alg-Cur) without targeting group is also prepared for the comparison of properties. LANH2-Alg Ald-Cur self assembles to micelle with diameter of 235 ± 5 nm and zeta potential of -29 mV in water. Cytotoxicity analysis demonstrates enhanced toxicity of LANH2-Alg Ald-Cur over Alg-Cur on HepG2 cells. Cellular uptake studies confirm that LANH2-Alg Ald-Cur can selectively recognize HepG2 cells and shows higher internalization than Alg-Cur conjugate. Results indicate that LANH2-Alg Ald-Cur conjugate micelles are suitable candidates for targeted delivery of curcumin to HepG2 cells.
authors.affiliation: Department of Chemistry, Indian Institute of Space Science and Technology (IIST), Valiamala, Thiruvananthapuram, Kerala 695 547, India. Electronic address: sarikapaithal@gmail.com.
authors.forename: P R
authors.initials: PR
authors.lastname: Sarika
authors.affiliation: Department of Chemistry, Indian Institute of Space Science and Technology (IIST), Valiamala, Thiruvananthapuram, Kerala 695 547, India. Electronic address: nirmala@iist.ac.in.
authors.forename: Nirmala Rachel
authors.initials: NR
authors.lastname: James
authors.affiliation: Tissue Culture Laboratory, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Poojappura, Thiruvananthapuram, Kerala 695 012, India. Electronic address: anilkumarpr@sctimst.ac.in.
authors.forename: P R Anil
authors.initials: PR
authors.lastname: Kumar
authors.affiliation: Tissue Culture Laboratory, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences and Technology, Poojappura, Thiruvananthapuram, Kerala 695 012, India. Electronic address: kdeeps3@gmail.com.
authors.forename: Deepa K
authors.initials: DK
authors.lastname: Raj
mesh_terms: D000464:Alginates / Q000737:chemistry*; D001692:Biological Transport; D016923:Cell Death / Q000187:drug effects; D003474:Curcumin / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005690:Galactose / Q000737:chemistry*; D020723:Glucuronic Acid / Q000737:chemistry; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000378:metabolism*; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D008823:Micelles; D013499:Surface Properties
chemical_list: D000464:Alginates; D004337:Drug Carriers; D006603:Hexuronic Acids; D008823:Micelles; D020723:Glucuronic Acid; D003474:Curcumin; D005690:Galactose
keywords: Alginate; Curcumin; Micelle; Polymer drug conjugate; Self assembly