title: Galactosylated pullulan-curcumin conjugate micelles for site specific anticancer activity to hepatocarcinoma cells.
abstract: Galactosylated pullulan-curcumin conjugate (LANH2-Pu Ald-Cur SA) is developed for target specific delivery of curcumin to hepatocarcinoma cells by five step synthetic strategy, which includes oxidation of pullulan (Pu Ald), introduction of amino group to the targeting ligand (LANH2), grafting of the LANH2 to Pu Ald, modification of curcumin (Cur SA) and conjugation of Cur SA to pullulan. Nongalactosylated pullulan-curcumin conjugate (Pu-Cur SA) is also prepared to compare the enhancement in cytotoxicity offered by the targeting group. Both LANH2-Pu Ald-Cur SA and Pu-Cur SA conjugates could self assemble to micelle in water with hydrodynamic diameters of 355±9nm and 363±10nm, respectively. Both conjugates show spherical morphology and enhance stability of curcumin in physiological pH. Compared to Pu-Cur SA, LANH2-Pu Ald-Cur SA exhibits higher toxicity and internalization towards HepG2 cells. This indicates the enhanced uptake of LANH2-Pu Ald-Cur SA conjugate via ASGPR (asialoglycoprotein receptor) mediated endocytosis into 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: Indian Institute of Science Education and Research Bhopal, Bhauri, Madhya Pradesh 462 066, India. Electronic address: nishna@iiserb.ac.in.
authors.forename: N
authors.initials: N
authors.lastname: Nishna
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
authors.initials: PR
authors.lastname: Anil 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: D000970:Antineoplastic Agents / Q000494:pharmacology*; D003474:Curcumin / Q000737:chemistry* / Q000494:pharmacology; D004355:Drug Stability; D005690:Galactose / Q000737:chemistry*; D005936:Glucans / Q000737:chemistry* / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000473:pathology*; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D008855:Microscopy, Electron, Scanning
chemical_list: D000970:Antineoplastic Agents; D005936:Glucans; D008823:Micelles; C009109:pullulan; D003474:Curcumin; D005690:Galactose
keywords: Curcumin; Micelle; Polymer drug conjugate; Pullulan; Self assembly