Micromeritics and In-Vivo Bioavailability study for PEG400 and labrasol Based Liquisolid Compacts of Tacrolimus
Author(s): M. Somesu, Chinam Niranjan Patra*, Goutam Kumar Jena, Saroj Kumar Raul, Anjan Kumar and P. Bharghava Bhusan Rao
Abstract
The objective of this study is to enhance flowability, compressibility and oral bioavailability of tacrolimus using the liquisolid technique. Tacrolimus primarily functions as an immunosuppressant. The primary obstacles for developing effective formulations for this compound are its limited aqueous solubility and low bioavailability, reported to be 25%. To address this, we formulated cinacalcet HCl liquisolid compacts with PEG 400 and labrasol as the non-volatile solvents, sylysia 350 as the carrier material, and aerosil as the coating material. Our comprehensive analysis included Differential Scanning Calorimetry (DSC), Powder
X-ray Diffraction (P-XRD), kawakita analysis, quality control tests and pharmacokinetic study. The results indicated improved flowability, compressibity, no drug-excipient interaction and tacrolimus presence in the porous carrier in a dissolved state. Notably, selected formulation (L6) exhibited enhanced dissolution rate, disintegrating in less than 3 min with significant improvement in oral bioavailability. Overall, the liquisolid approach holds promise for developing a stable and scalable solid dosage form with improved flowability, compressibility and oral bioavailability.
