Galactosylated alginate-curcumin micelles for enhanced delivery of curcumin to hepatocytes

• Galactosylated and nongalactosylated alginate-curcumin conjugates were prepared.
• The conjugates could self assemble to micelle with size in nano meter range.
• LANH2-Alg Ald-Cur demonstrated enhanced toxicity over Alg-Cur toward HepG2 cells.
• Cellular uptake of LANH2-Alg Ald-Cur materialized via ASGPR mediated endocytosis.

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.

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