Methodical design, development, and evaluation of transferosomal transdermal films for enhanced delivery of lornoxicam and thiocolchicoside.

AIM: The present work aimed to enhance systemic availability through optimized transferosomal transdermal films of lornoxicam (LXM) and thiocolchicoside (TCS). Transferosomes were prepared using the thin-film hydration method, in which LXM and TCS, which have low oral bioavailability and adverse effects, were loaded.

METHODS

A Box-Behnken design was used to develop 17 vesicles in which dipalmitoyl phosphatidylcholine (X1), Span-80 (X2), and sonication time (X3) were varied and assessed for size, polydispersity index , and entrapment efficiency. The best vesicles were made into films. Films were extensively tested for physical, in vivo, and in vitro permeation, and skin irritancy characteristics.

RESULTS

The findings revealed vesicle sizes of 124 ± 2.25 to 400 ± 1.55 nm and a zeta potential of -48 to -20 mV. The drug entrapment was more than 80% for both drugs. In vitro and ex vivo permeation showed that the deformable vesicle film permeated much better than plain LXM and TCS films, and the permeation was directly proportional to the Aloe vera leaf mucilage (AVLM) and lime oil (LO) concentration. Also, the deformable vesicle films were reported to be devoid of skin irritation.

CONCLUSION

The research finds that deformable vesicle films of LXM/ TCS are promising for effective transdermal delivery.