Veenu P Mundada
India
Research Article
Enhanced Oral Bioavailability and Anticoagulant Activity of Dabigatran Etexilate by Self-Micro Emulsifying Drug Delivery System: Systematic Development, In vitro, Ex vivo and In vivo Evaluation
Author(s): Veenu P Mundada and Krutika K SawantVeenu P Mundada and Krutika K Sawant
Dabigatran etexilate (DE), a prodrug of Dabigatran, is a potent, oral, reversible and direct thrombin inhibitor with low oral bioavailability due to active efflux by intestinal P-glycoprotein receptors. No lipid based oral formulation is marketed for DE till date. Hence, we formulated and evaluated self-micro emulsifying drug delivery system (SMEDDS), by using P-gp modulator excipients to tackle this issue and elevate the systemic availability of DE. The SMEDDS were developed using Capmul MCM C8, Cremophor EL and Transcutol HP as oil, surfactant and co-surfactant respectively. The formulation was optimized using statistical D-optimal design. The globule size of 73.24 nm with 0.085 PDI was achieved upon spontaneous emulsification with >99% Transmittance at 250 times dilution and discrete globules were observed under TEM. The in vitro and ex vivo drug release from DE-SMEDDS was found.. View More»
DOI:
10.4172/2157-7439.1000480