Drug Delivery (Jan 2017)

Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats

  • Shaimaa S. Ibrahim,
  • Rihab Osman,
  • Nahed D. Mortada,
  • Ahmed-Shawky Geneidy,
  • Gehanne A. S. Awad

DOI
https://doi.org/10.1080/10717544.2016.1245368
Journal volume & issue
Vol. 24, no. 1
pp. 243 – 251

Abstract

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Pulmonary bed can retain microparticles (MP) larger than their capillaries’ diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity. The anticoagulant activity of the selected Alb MS was significantly sustained for up to 38 h compared to 5 h for the market product. Alb MS are promising delivery carriers for controlled and targeted delivery of Enox to the lungs for prophylaxis and treatment of pulmonary embolism.

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