European Journal of Biomedical and Pharmaceutical Sciences

PREPARATION AND CHARACTERIZATION OF GLYCEROSOMES FORMULATION CONTAINING TOFACITINIB FOR ENHANCED TRANSDERMAL DELIVERY

Arslaan Khan*, Dr. Sandesh Asati, Dr. Vishnu Raj

ABSTRACT

The present study was aimed at the preparation and characterization of Tofacitinib-loaded glycerosomes for enhanced transdermal drug delivery. Tofacitinib, a poorly water-soluble drug, exhibits limited bioavailability, thereby necessitating the development of a suitable vesicular carrier system to improve its solubility, stability, and controlled release profile. Pre-formulation studies confirmed that Tofacitinib is a white to off-white crystalline solid with a melting point of 199°C, λ max at 286 nm, and pH of 5.3, indicating good purity and physicochemical suitability for formulation development. The drug showed poor aqueous solubility but was freely soluble in methanol and DMSO, supporting the need for a lipid-based delivery system. Glycerosomes were prepared using appropriate lipid and glycerol concentrations and evaluated for physicochemical properties, including particle size, zeta potential, entrapment efficiency, morphology, in vitro drug release, and stability. Among the formulated batches (GSF1–GSF5), GSF3 was identified as the optimized formulation, showing a particle size of 141.8 nm, zeta potential of −43.5 mV, and highest entrapment efficiency of 93.65%, indicating superior vesicular stability and drug loading capacity. Scanning electron microscopy revealed submicron-sized, porous vesicles with irregular morphology, favorable for enhanced drug permeation. The in vitro release study demonstrated a sustained release of 95.97% over 14 hours, following zero-order kinetics (R² = 0.9826), suggesting controlled and predictable drug release behavior. Stability studies performed as per ICH guidelines confirmed that the optimized formulation remained stable over 90 days under both normal and accelerated conditions, with negligible changes in particle size (approximately 166–168 nm) and entrapment efficiency (> 92%). Overall, the study concludes that glycerosomes are an effective vesicular delivery system for Tofacitinib, significantly enhancing its stability, controlled release, and transdermal delivery potential. The optimized formulation (GSF3) demonstrated promising characteristics for improving therapeutic efficacy and may serve as a potential carrier system for transdermal drug delivery applications.

Keywords: Tofacitinib; Glycerosomes; Vesicular drug delivery system; Transdermal delivery; Entrapment efficiency; Controlled drug release; Zeta potential; Stability studies.