Abstract
This study was based on the preparation, characterization, and animal in vivo experiments performed to evaluate nanoparticles of poly(ɛ-caprolactone) (PCL) and chitosan as carriers of enoxaparin. The nanoparticles were characterized and presented satisfactory results in terms of size, polydispersity, and encapsulation efficiency. Anticoagulant activity of the nanoparticles was maintained for 14 hours when the administration was subcutaneous; however no activity was observed after oral administration. There was a significant reduction in thrombus size, in vivo, for both free and encapsulated enoxaparin in comparison with the control group after subcutaneous administration. Oral administration results however were indifferent. In conclusion, the double emulsion method w/o/w was efficient for enoxaparin encapsulation, producing spherical nanoparticles with high encapsulation efficiency. For in vivo studies, the encapsulated enoxaparin showed a sustained anticoagulant activity for a higher period of time compared to free enoxaparin, with an antithrombotic effect when administered subcutaneously.
Highlights
Deep vein thrombosis (DVT) is one of the most important public health problems, with an annual incidence estimated as 67 per 100.000 individuals in the population [1, 2]
There were no significant changes in the size and zeta potential of PCL-chitosan nanoparticles with and without enoxaparin, evidencing the stability of these particles for a period of 50 days at 4∘C, as shown in Figures 1(a) and 1(b)
The PCL-chitosan nanoparticles produced by w/o/w double emulsion showed an entrapment efficiency of 99.04 ± 0.001%, demonstrating being a good method for hydrophilic drug encapsulation
Summary
Deep vein thrombosis (DVT) is one of the most important public health problems, with an annual incidence estimated as 67 per 100.000 individuals in the population [1, 2]. Heparin is a drug with antithrombotic action, widely used since 1930 [3]. Low molecular weight heparin (LMWH) exhibits superior pharmacodynamic and pharmacokinetic properties compared to heparin and shows low affinity for plasma and cellular proteins. LMWH exhibited a more predictable and reproducible anticoagulant response than heparin and did not require monitoring in most clinical situations [4]. The new direct oral anticoagulants available present limitations of antidotes for anti-Xa drugs and lack laboratory tests which would be used in special situations such as bleeding or emergency procedures [5]. Adherence to treatment is a challenge in clinical practice for medications with continuous daily use. The possibility of drugs with a prolonged half-life which do not increase bleeding represent a good opportunity for a better management of those patients
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