Abstract
Abstract
Background: Transferosomes are suitable possibilities for the delivery of active compounds because of their structural resemblance to cell vesicles or exocytotic vesicles and are appropriate for controlled medication release and targeted drug delivery. Rivaroxaban was the first orally dosed, direct Factor Xa inhibitor, a small-molecule oxazolidinone derivative. It binds directly and reversibly to Factor Xa via the S1 and S4 pockets.
Objective: Formulation of rivaroxaban nanotransferosome gel and in vivo comparison with oral rivaroxaban suspension.
Methods: Rivaroxaban-loaded nanotransferosome dispersion was used as the base system and combined with Carbopol 934 gels (1 w/v, 1.5 w/v, and 2% w/v) to prepare rivaroxaban nanotransferosome gels (TDG1, TDG2, and TDG3). The designed formulations were screened for pH, spreadability, viscosity, in vitro release was assessed over 24 h, and ex vivo permeation across rat skin using Franz diffusion cells. TDG2 formulation was nominated for in vivo pharmacokinetic studies in adult male Wistar rats for comparison the transdermal TDG2 with an oral rivaroxaban suspension. Plasma rivaroxaban concentrations were counted using a validated HPLC-UV method.
Results: TDG2 released 85 ± 2.5% of rivaroxaban over 24 h. Ex vivo, TDG2 exhibited a seven fold higher flux (94.68 µg cm⁻² h⁻¹) than rivaroxaban suspension (11.93 µg cm⁻² h⁻¹). In vivo, the transdermal formulation (TDG2) attained significantly greater systemic exposure with AUC₀–₂₄ = 138.63 ± 0.37 µg. h/ml versus 117.69 ± 0.31 µg. h/ml for oral dosing (P < 0.05), indicating enhanced bioavailability.
Conclusion: The TDG2 represents a stable transdermal platform that distinctly improves skin permeation and systemic exposure related to oral administration, backup its therapeutic potential.
| Has the manuscript been published | not published |
|---|---|
| Intend to be published in the IJPS ? | Yes |
