Poly(ε-caprolactone)-block-poly(ethyl Ethylene Phosphate) Micelles for Brain-targeting Drug Delivery: in Vitro and in Vivo Valuation

Overview

Journal Pharm Res

Specialties Pharmacology
Pharmacy

Date 2010 Sep 18

PMID 20848303

Citations 10

Authors

Pengcheng Zhang

Luojuan Hu

Yucai Wang

Jun Wang

Linyin Feng

Yaping Li

Affiliations

Soon will be listed here.

Abstract

Purpose: The purpose of this work was to investigate the potential of poly(ε-caprolactone)-block-poly(ethyl ethylene phosphate) (PCL-PEEP) micelles for brain-targeting drug delivery.

Method: The coumarin-6-loaded PCL-PEEP micelles (CMs) were prepared and characterized. The cellular uptake of CMs was evaluated on in vitro model of brain-blood barrier (BBB), and the brain biodistribution of CMs in ICR mice was investigated.

Results: PCL-PEEP could self-assemble into 20 nm micelles in water with the critical micelle concentration (CMC) 0.51 μg/ml and high coumarin-6 encapsulation efficiency (92.5 ± 0.7%), and the micelles were stable in 10% FBS with less than 25% leakage of incorporated coumarin-6 during 24 h incubation at 37°C. The cellular uptake of CMs by BBB model was significantly higher and more efficient than coumarin-6 solution (CS) at 50 ng/ml. Compared with CS, 2.6-fold of coumarin-6 was found in the brains of CM-treated mice, and C(max) of CMs was 4.74% of injected dose/g brain. The qualitative investigation on the brain distribution of CMs indicated that CMs were prone to accumulate in hippocampus and striatum.

Conclusion: These results suggest that PCL-PEEP micelles could be a promising brain-targeting drug delivery system with low toxicity.

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