Effect of Penetration Enhancers on Transdermal Delivery of Oxcarbazepine, an Antiepileptic Drug Using Microemulsions

Oxcarbazepine (OXC) is an anticonvulsant drug, indicated for the treatment of the neurological disorder, epilepsy. The objective of the present study was to evaluate the transdermal delivery of OXC from microemulsions using different penetration enhancers. Transcutol^® P (TRC), oleic acid (OA), cineole (cin), Labrasol (LS), Tween 80 (T80) and N-Methyl-Pyrrolidone (NMP) were used as penetration enhancers as well as microemulsion components. Simple formulations of OXC in propylene glycol (PG) incorporating various penetration enhancers and combination of penetration enhancers were also evaluated for transdermal delivery.

Drug delivery and penetration enhancement were studied using human cadaver skin on Franz diffusion cells. The results showed that all penetration enhancers improved the rate of permeation of OXC compared to the control. The flux of drug delivery from the various formulations was found to be, in decreasing order, cin > OA + TRC > NMP > TRC > OA. Overall, microemulsions prepared using cineole, Tween 80 and Transcutol^® P (TRC) were shown to be provide the best penetration enhancement for OXC.

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Materials

OXC was purchased from Euticals Spa, Italy and used as the drug molecule. Cineole (cin), N-methyl-Pyrrolidone (NMP), oleic acid (OA) and Transcutol® P (TRC) were investigated as penetration enhancers. OA was a gift from Croda Inc., Edison, NJ, USA. TRC and Labrasol (LS) were gifts from Gattefosse Corporation, Paramus, NJ, USA. Cin, NMP, HPLC grade methanol and water, Propylene Glycol (PG), Polysorbate 80 (Tween 80), Isopropyl Myristate (IPM), Medium Chain Triglyceride (MCT), Polyethylene Glycol 400 (PEG-400), Sodium Lauryl Sulfate (SLS), Triethanolamine (TEA) and formic acid were obtained from Sigma-Aldrich, Saint Louis, MO, USA. Carbopol 980 was a gift from Lubrizol, Wickliffe, OH, USA. Ethanol was procured from Decon Labs, Inc., King of Prussia, PA, USA. Phosphate-Buffered Saline (PBS) was prepared by dissolving one PBS tablet in 100 mL of water. Add SLS to PBS at 5% and pH was adjusted to 5.8. PBS tablets were purchased from MP Biomedicals, Solon, OH, USA. Dermatomed human cadaver skin from the posterior torso region of 59-year-old male was used for the ex-vivo permeation study and was supplied by New York Firefighter Skin Bank, New York, NY, USA.

Virani, A.; Puri, V.; Mohd, H.; Michniak-Kohn, B. Effect of Penetration Enhancers on Transdermal Delivery of Oxcarbazepine, an Antiepileptic Drug Using Microemulsions. Pharmaceutics 2023, 15, 183. https://doi.org/10.3390/pharmaceutics15010183