Construction of biotin-modified polymeric micelles for pancreatic cancer targeted photodynamic therapy / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1038-1044, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-257029
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pancreatic Neoplasms
/
Photochemotherapy
/
Biotin
/
Drug Carriers
/
Drug Screening Assays, Antitumor
/
Chemistry
/
Drug Therapy
/
Micelles
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2015
Type:
Article
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