Self-assembled nanoparticles of hyaluronic acid/poly( dl-lactide-co-glycolide) block copolymer

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2012-02, Vol.90, p.28-35
• Main Authors: Jeong, Young-Il, Kim, Do Hyung, Chung, Chung-Wook, Yoo, Jin Ju, Choi, Kyung Ha, Kim, Cy Hyun, Ha, Seung Hee, Kang, Dae Hwan
• Format: Article
• Language: English
• Subjects: Antineoplastic Agents - chemistry; Antineoplastic Agents - metabolism; Antineoplastic Agents - pharmacology; Binding, Competitive; Block copolymer; Block copolymers; Blocking; Carcinoma - drug therapy; Carcinoma - immunology; Carcinoma - pathology; CD44; Cell Line, Tumor; colloids; Colonic Neoplasms - drug therapy; Colonic Neoplasms - immunology; Colonic Neoplasms - pathology; color; colorectal neoplasms; composite polymers; Delayed-Action Preparations - chemistry; Delayed-Action Preparations - metabolism; deuterium oxide; Deuterium Oxide - analysis; Deuterium Oxide - metabolism; doxorubicin; Doxorubicin - chemistry; Doxorubicin - metabolism; Doxorubicin - pharmacology; Drug Carriers - chemistry; Drug Carriers - metabolism; Endocytosis; Flow Cytometry; Fluorescence; Humans; Hyaluronan Receptors - immunology; Hyaluronan Receptors - metabolism; Hyaluronic acid; Hyaluronic Acid - chemistry; hydrophilicity; Hydrophobic and Hydrophilic Interactions; Hydroxyapatite; Lactic Acid - chemistry; Magnetic Resonance Spectroscopy; Molecular Targeted Therapy - methods; Nanoparticles; neoplasm cells; nuclear magnetic resonance spectroscopy; PLGA; Polyglycolic Acid - chemistry; Receptor-mediated endocytosis; Receptors; Tumors
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2011.09.043

We synthesized block copolymer composed of hyaluronic acid (HA) and poly( dl-lactide-co-glycolide) (PLGA) (HAbLG) for antitumor targeting. 1H NMR was employed to confirm synthesis of block copolymer. At 1H NMR study, HabLG nanoparticles showed HA intrinsic peaks only at D 2O, indicating that they contained HA as a hydrophilic outer-shell and PLGA as a inner-core. Anti-tumor activity was studied using CD44-overexpressing HCT-116 human colon carcinoma cells. Addition of doxorubicin (DOX)-incorporated nanoparticles to tumor cells resulted in the expression of a strong red fluorescence color while they expressed very weak fluorescence when CD44 receptor was blocked with free HA. Flow cytometry data also showed similar results, indicating that the fluorescence intensity of tumor cells treated with nanoparticles was significantly decreased when CD44 receptor was blocked. These results indicate that HAbLG nanoparticles were able to target CD44-overexpressing tumor cells via receptor-mediated endocytosis.