Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats.
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.
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Shaimaa S
SS
Ibrahim
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Rihab
R
Osman
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Nahed D
ND
Mortada
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Ahmed-Shawky
AS
Geneidy
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt.
Gehanne A S
GA
Awad
D061605:Administration, Intravenous / Q000379:methods; D000418:Albumins / Q000737:chemistry; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage*; D003692:Delayed-Action Preparations / Q000008:administration & dosage*; D016503:Drug Delivery Systems / Q000379:methods; D017984:Enoxaparin / Q000008:administration & dosage*; D008168:Lung / Q000187:drug effects*; D008297:Male; D008863:Microspheres; D051381:Rats
D000418:Albumins; D000925:Anticoagulants; D003692:Delayed-Action Preparations; D017984:Enoxaparin
Albumin; anticoagulant; controlled delivery; enoxaparin; microspheres; passive lung targeting