Transfersomes Mediated Transdermal Delivery of Curcumin: In Vitro and In Vivo Evaluation

Abstract

Background: Curcumin is an herbal anti-inflammatory drug that, when administered orally, shows low bioavailability owing to its poor water solubility, instability in acidic and neutral pH, and rapid intestinal metabolism. In this study, we aimed to improve curcumin delivery through the skin and systemically deliver the drug using transferosomes as carriers. Methods: The formulations were prepared via thin-film hydration using soya lecithin, cholesterol, and surfactants (plurol oleique/Tween 80). After optimization trials using a central composite design, particle size analysis, zeta potential, TEM, DSC, FTIR, entrapment efficiency, drug release profiles, and ex vivo drug permeation were studied. In vivo investigations were performed using a rat model. Results: Drug entrapment was observed in 12 formulations (74–91%). Drug release from the formulations over a 24 h study period varied from 63% to 77%. FTIR and DSC studies confirmed the absence of appreciable interactions between curcumin and the excipients. The mean particle size of the optimized formula was 164 nm and the zeta potential was -41 mV. The TEM results revealed evenly distributed spherical vesicles. The transdermal flux exhibited by the transfersome-loaded gel was ~2.5 fold higher than that of the drug-loaded gel. When subjected to a pharmacokinetic study, a stable, non-irritant optimized curcumin transfersome gel formulation showed enhanced bioavailability (AUC) compared to oral curcumin suspension. Conclusion: The developed transfersomes have the potential to improve skin permeation, ensure an enhanced systemic effect, and improve the therapeutic efficacy of curcumin.