title: [Construction of biotin-modified polymeric micelles for pancreatic cancer targeted photodynamic therapy].
abstract: In this study, we explored the feasibility of biotin-mediated modified polymeric micelles for pancreatic cancer targeted photodynamic therapy. Poly (ethylene glycol)-distearoyl phosphatidyl ethanolamine (mPEG2000-DSPE) served as the drug-loaded material, biotin-poly(ethylene glycol)-distearoyl phosphatidyl ethanolamine (Biotin-PEG3400-DSPE) as the functional material and the polymeric micelles were prepared by a thin-film hydration method. The targeting capability of micelles was investigated by cell uptake assay in vitro and fluorescence imaging in vivo and the amounts of Biotin-PEG-DSPE were optimized accordingly. Hypocrellin B (HB), a novel photosensitizer was then encapsulated in biotinylated polymeric micelles and the anti-tumor efficacy was evaluated systemically in vitro and in vivo. The results showed that micelles with 5 mol % Biotin-PEG-DSPE demonstrated the best targeting capability than those with 20 mol % or 0.5 mol % of corresponding materials. This formulation has a small particle size [mean diameter of (36.74 ± 2.16) nm] with a homogeneous distribution and high encapsulation efficiency (80.06 ± 0.19) %. The following pharmacodynamics assays showed that the biotinylated micelles significantly enhanced the cytotoxicity of HB against tumor cells in vitro and inhibited tumor growth in vivo, suggesting a promising potential of this formulation for treatment of pancreatic cancer, especially those poorly permeable, or insensitive to radiotherapy and chemotherapy.
authors.forename: Chun-yue
authors.initials: CY
authors.lastname: Deng
authors.forename: Ying-ying
authors.initials: YY
authors.lastname: Long
authors.forename: Sha
authors.initials: S
authors.lastname: Liu
authors.forename: Zhang-bao
authors.initials: ZB
authors.lastname: Chen
authors.forename: Chong
authors.initials: C
authors.lastname: Li
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry*; D001710:Biotin; D004337:Drug Carriers / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008823:Micelles; D010190:Pancreatic Neoplasms / Q000188:drug therapy*; D010778:Photochemotherapy
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D001710:Biotin