Heparin-based self-assembled nanoparticles for photodynamic therapy

• Published in: Macromolecular research Vol. 19; no. 5; pp. 487 - 494
• Main Authors: Li, Li, Moon, Hyun Tae, Park, Jin-Young, Heo, Yu Jung, Choi, Yongdoo, Tran, Thanh Huyen, Lee, Yong-kyu, Kim, So Yeon, Huh, Kang Moo
• Format: Journal Article
• Language: English
• Published: Heidelberg The Polymer Society of Korea 01.05.2011; 한국고분자학회
• Subjects: Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Complex Fluids and Microfluidics; Nanochemistry; Nanotechnology; Physical Chemistry; Polymer Sciences; Soft and Granular Matter; 고분자공학; heparin; drug delivery; self-assembled nanoparticles; photodynamic therapy
• ISSN: 1598-5032; 2092-7673
• DOI: 10.1007/s13233-011-0505-9

Novel heparin-based self-assembled nanoparticles were developed for photodynamic cancer therapy. A heparin-poly(β-benzyl- L -aspartate) (HP) amphiphilic copolymer was synthesized for effective delivery of a hydrophobic photosensitizer, pheophorbide a (Pheo). The anti-coagulant activity of the HP copolymer decreased significantly, as measured by an anti-FXa chromogenic assay. Pheo was effectively incorporated into the HP nanoparticles using a dialysis technique. A good drug-loading content was obtained by altering the composition of the HP copolymer and Pheo/HP feed ratio. The Pheo-loaded HP nanoparticles had an average diameter of 117–189 nm, a negatively charged surface, and a sustained drug release pattern. These properties may allow them to passively target the tumor site through an enhanced permeability and retention (EPR) effect. Furthermore, the Pheo-loaded HP nanoparticles demonstrated marked photocytotoxicity and minimal darktoxic without a light treatment. The 6HP-Pheo15 nanoparticles were internalized into SCC7 cancer cells and damaged the cells after a light treatment. This suggests that HP nanoparticles have potential as an effective delivery system for clinical PDT.