Comparative pharmacokinetic studies of transferosomes loaded gel and pressure sensitive adhesive based patch formulation for transdermal delivery of benztropine mesylate

• Published in: Journal of drug delivery science and technology 2024-02, Vol.92, p.105287, Article 105287
• Main Authors: Chabru, Afridi S., Salve, Pramod S., Ghumare, Gaurav D., Dhamak, Rushikesh S., Tiwari, Deepak R., Waghmare, Darshan S.
• Format: Article
• Language: English
• Subjects: Benztropine mesylate; In vivo pharmacokinetic study; Parkinson's disease; Pressure sensitive adhesive; Transdermal drug delivery; Transferosomes
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2023.105287

Oral bioavailability of benztropine mesylate (BZM) is low due to its limited gastric absorption, low biological half-life, and susceptibility to extensive hepatic first pass metabolism. It is an anti-muscarinic drug used for the management of Parkinson's disease. The goal of the present research work was to compare a BZM transferosome-loaded Carbopol 940 gel formulation and an acrylate pressure sensitive adhesive based transdermal patch for their efficacy in transdermal penetration and pharmacokinetic profiles. BZM transferosomes were formulated using the thin-film hydration method. The developed formulation showed a (-) 12.0 mV zeta potential and a mean vesicle size of 138.5 nm. When compared to aqueous BZM solution, transferosomes exhibited a considerable increase in transdermal penetration in an ex vivo study across isolated rat skin. When compared to oral, intravenous, and drug-in-adhesive transdermal patch, in vivo pharmacokinetic investigations in Wistar rats revealed an increase in AUC, Tmax, and MRT and a higher and prolonged drug release from transferosome-loaded gel formulations. The findings suggest that the BZM transferosome-loaded gel might be a better and more patient-friendly alternative to oral administration of BZM for the management of Parkinson's disease. [Display omitted]