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Angiopep-2 modified PE-PEG based polymeric micelles for amphotericin B delivery targeted to the brain

Kun Shao1, Rongqin Huang, Jianfeng Li

  • 1Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, PR China.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|July 9, 2010
PubMed

Insights

Angiopep-2 modified nanoparticles effectively deliver the antifungal Amphotericin B across the blood-brain barrier (BBB), enhancing treatment for fungal infections of the central nervous system (CNS). This novel drug delivery system improves brain penetration and reduces toxicity.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Biotechnology

Background:

  • Amphotericin B (AmB) is a crucial antifungal agent for central nervous system (CNS) infections but exhibits poor blood-brain barrier (BBB) penetration.
  • Targeting the low-density lipoprotein receptor-related protein (LRP) on the BBB with ligands like Angiopep-2 offers a strategy for enhanced brain drug delivery.

Purpose of the Study:

  • To develop and evaluate an Angiopep-2 modified PE-PEG micellar drug delivery system for improved brain targeting of Amphotericin B.
  • To assess the efficiency of this system in enhancing AmB accumulation within the brain and its ability to cross the BBB.

Main Methods:

  • Preparation of PE-PEG based micelles encapsulating Amphotericin B.
  • Modification of micelles with Angiopep-2 ligand to target LRP on the BBB.
  • In vitro and in vivo evaluation of micelle-mediated drug transport across the BBB.
  • Assessment of Angiopep-2 micelles' ability to overcome efflux proteins like P-glycoprotein.

Main Results:

  • Angiopep-2 modified micelles demonstrated superior in vitro and in vivo efficiency in penetrating the BBB compared to unmodified micelles and Fungizone.
  • The drug delivery system showed high drug entrapment efficiency, improved AmB solubilization, and reduced mammalian cell toxicity.
  • Angiopep-2 modified micelles enhanced the transport of encapsulated substances (e.g., Rho 123) across the BBB, potentially overcoming efflux pump activity.

Conclusions:

  • Angiopep-2 modified polymeric micelles represent a promising novel drug delivery system for targeting the brain.
  • This approach can significantly improve the delivery of antifungal drugs like Amphotericin B to the CNS for treating infections.
  • The strategy holds potential for overcoming biological barriers like the BBB and efflux proteins for effective brain drug delivery.

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