Formulation and Quality Control Tests for Nanoemulsion of Tofacitinib: A Novel Approach

Abstract

Background: Tofacitinib (TFB) is a pioneer JAK (Janus kinase) inhibitor mainly employed to treat rheumatoid arthritis. It has proven efficacy for the treatment of rheumatoid arthritis in the oral dosage form. Oral TFB exhibited several toxic effects. Current research aims to develop a topical formulation of TFB to achieve effective treatment without any adverse effects. Study Design: Ultrsonication Methods. Place and Duration of Study: Sample: Swami Dayanand Postgraduate Institute of Pharmaceuticals Sciences, University of Health Sciences, Rohtak; 2020-2021. Methods: Oleic acid, tween 80, and propylene glycol were selected as oil, surfactant, and co-surfactant, respectively. The ratio of oil:surfactant:co-surfactant was selected based on a ternary phase diagram using the aqueous titration method. The selected ratio was employed to develop eight formulations of TFB by ultra-sonication. The formulations (F1-F8) were characterized using several physicochemical methods like pH, viscosity, particle size distribution, zeta potential, drug content, and in vitro release. Results: The formulations (F1-F8) were formulated by using the ultrasonication (high energy) method. The optimized formulation selected on the basis of characterization methods for instance, F8 possessed particle size 127.4 nm, and -18.4 (mV) zeta potential. The in vitro release of F8 was found to be 88.1 ± 2.5% at 24 hours. It also passed the thermodynamic stability tests. Conclusion:  The current investigations conclude that tofacitinib-nanoemulsion (TFB-NE) can be used as an alternative to the oral route of TFB and is also useful in reducing the adverse effects associated with oral TFB.