A rapamycin-releasing perivascular polymeric sheath produces highly effective inhibition of intimal hyperplasia

J Control Release. 2014 Oct 10:191:47-53. doi: 10.1016/j.jconrel.2014.05.017. Epub 2014 May 20.

Abstract

Intimal hyperplasia produces restenosis (re-narrowing) of the vessel lumen following vascular intervention. Drugs that inhibit intimal hyperplasia have been developed, however there is currently no clinical method of perivascular drug-delivery to prevent restenosis following open surgical procedures. Here we report a poly(ε-caprolactone) (PCL) sheath that is highly effective in preventing intimal hyperplasia through perivascular delivery of rapamycin. We first screened a series of bioresorbable polymers, i.e., poly(lactide-co-glycolide) (PLGA), poly(lactic acid) (PLLA), PCL, and their blends, to identify desired release kinetics and sheath physical properties. Both PLGA and PLLA sheaths produced minimal (<30%) rapamycin release within 50days in PBS buffer. In contrast, PCL sheaths exhibited more rapid and near-linear release kinetics, as well as durable integrity (>90days) as evidenced in both scanning electron microscopy and subcutaneous embedding experiments. Moreover, a PCL sheath deployed around balloon-injured rat carotid arteries was associated with a minimum rate of thrombosis compared to PLGA and PLLA. Morphometric analysis and immunohistochemistry revealed that rapamycin-loaded perivascular PCL sheaths produced pronounced (85%) inhibition of intimal hyperplasia (0.15±0.05 vs 1.01±0.16), without impairment of the luminal endothelium, the vessel's anti-thrombotic layer. Our data collectively show that a rapamycin-loaded PCL delivery system produces substantial mitigation of neointima, likely due to its favorable physical properties leading to a stable yet flexible perivascular sheath and steady and prolonged release kinetics. Thus, a PCL sheath may provide useful scaffolding for devising effective perivascular drug delivery particularly suited for preventing restenosis following open vascular surgery.

Keywords: Intimal hyperplasia; Open vascular surgery; Perivascular drug delivery; Ploy(ε-caprolactone) (PCL) sheath; Rapamycin.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cardiovascular Agents / administration & dosage*
  • Cardiovascular Agents / chemistry
  • Carotid Artery Injuries / drug therapy*
  • Carotid Artery Injuries / pathology
  • Carotid Stenosis / pathology
  • Carotid Stenosis / prevention & control*
  • Cell Proliferation / drug effects
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Disease Models, Animal
  • Drug Carriers*
  • Hyperplasia
  • Kinetics
  • Linear Models
  • Male
  • Neointima*
  • Polyesters / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • Sirolimus / administration & dosage*
  • Sirolimus / chemistry
  • Solubility
  • Technology, Pharmaceutical / methods

Substances

  • Cardiovascular Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Polyesters
  • polycaprolactone
  • Sirolimus