Low molecular weight heparin-loaded polymeric nanoparticles: formulation, characterization, and release...

Area of Science:

• Drug Delivery
• Nanotechnology
• Biomaterials Science

Background:

• Oral administration of heparin is limited due to poor bioavailability.
• Development of effective oral heparin carriers is crucial for anticoagulant therapy.
• Nanoparticle-based drug delivery offers potential for enhanced oral absorption.

Purpose of the Study:

• To prepare and characterize low molecular weight heparin (LMWH) nanoparticles (NP) for oral administration.
• To evaluate the encapsulation efficiency, release profile, and biological activity of LMWH-loaded NP.
• To investigate the role of different polymers in NP formulation and LMWH delivery.

Main Methods:

• Water-in-oil-in-water (w/o/w) emulsification and solvent evaporation techniques were employed.
• Biodegradable (PCL, PLGA) and non-biodegradable (Eudragit RS/RL) polymers were used for NP formulation.
• Nanoparticle size, surface potential, encapsulation efficiency, in vitro release, and anti-factor Xa activity were assessed.

Main Results:

• LMWH-loaded NP size ranged from 240 to 490 nm, influenced by polymer solution viscosity.
• Eudragit polymers significantly improved LMWH encapsulation efficiency compared to PCL and PLGA.
• In vitro LMWH release was sustained, with increased release in the presence of esterase.
• Released LMWH retained its anti-factor Xa activity, confirming preserved biological function.

Conclusions:

• Formulation of LMWH nanoparticles using Eudragit polymers demonstrated high encapsulation efficiency.
• These LMWH nanoparticles show potential as viable oral heparin carriers.
• The preserved biological activity of released LMWH supports its suitability for oral administration.