Cell permeable peptide conjugated nanoerythrosomes of fasudil prolong pulmonary arterial vasodilation in PAH rats

Eur J Pharm Biopharm. 2014 Nov;88(3):1046-55. doi: 10.1016/j.ejpb.2014.10.012.

Abstract

In this study, we tested the hypothesis that a cell permeable peptide, CARSKNKDC (CAR), conjugated nanoerythrosomes (NERs) containing fasudil, a rho-kinase (ROCK) inhibitor, produces prolonged pulmonary preferential vasodilation. CAR conjugated NERs containing fasudil were prepared by hypotonic lysis and extrusion method, and optimized for various physicochemical properties in-vitro. The formulations were then used to study the hemodynamic efficacy in a monocrotaline-induced rodent model of pulmonary arterial hypertension (PAH). CAR-NERs-Fasudil was spherical in shape with an average vesicle size and entrapment efficiency of 161.3 ± 1.37 nm and 48.81 ± 1.96%, respectively. Formulations were stable for ~3 weeks when stored at 4 °C and the drug was released in a controlled fashion for >48 h. The uptake of CAR-NERs-Fasudil by TGF-b activated pulmonary arterial smooth muscle cell was ~1.5-fold greater than the uptake of NERs-Fasudil. CAR-NERs-Fasudil inhibited ROCK activity and 5-hydroxytryptamine induced cell proliferation. In terms of reduction of pulmonary arterial pressure, intratracheal administration of CAR-NERs-Fasudil was ~2-fold more specific to the lungs compared with plain fasudil. Overall,CAR peptide grafted nanoerythrosomes offers a new platform for improving the therapeutic efficacy ofa rho-kinase inhibitor, fasudil, without affecting peripheral vasodilation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / administration & dosage
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / metabolism
  • Animals
  • Cell Membrane Permeability / drug effects
  • Cell Membrane Permeability / physiology*
  • Drug Carriers / administration & dosage
  • Drug Carriers / metabolism
  • Hypertension, Pulmonary / drug therapy
  • Hypertension, Pulmonary / metabolism*
  • Male
  • Nanoparticles / administration & dosage
  • Nanoparticles / metabolism*
  • Peptides / administration & dosage
  • Peptides / metabolism
  • Proteolipids / administration & dosage
  • Proteolipids / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Vasodilation / drug effects
  • Vasodilation / physiology*

Substances

  • Drug Carriers
  • Peptides
  • Proteolipids
  • proteoliposomes
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • fasudil