The current study aimed to develop and optimize a transferosomal gel and transdermal patch formulation of repaglinide to enhance its transdermal delivery and antidiabetic efficacy. Transferosomes were formulated using the reverse phase evaporation method and optimized through a full factorial design considering particle size and entrapment efficiency as critical parameters. The optimized formulation (NTF7) displayed a particle size of 266.9 nm, a zeta potential of 33.2 mV, and high entrapment efficiency of 97.8%, indicating excellent stability and effective drug encapsulation. In vitro drug release from the transferosomes and the Carbopol 934-based transferosomal gel (NTFG7) showed sustained release of 97.95% and 96.54%, respectively, over 12 hours, following Korsmeyer-Peppas kinetics indicative of a non-Fickian, anomalous release mechanism. Transdermal patches (NTFG7 P) prepared from the optimized gel also exhibited controlled release (94.78% over 12 hours) and favorable physicochemical properties. In vivo studies on STZ and HFD-induced diabetic rats demonstrated significant glucose-lowering effects with both gel and patch formulations, with NTFG7 P achieving greater glycemic control and negligible skin irritation (PDII = 0.33). Histopathological analysis revealed protective effects on pancreatic tissues. The developed transferosomal gel and patch systems represent promising, patient-friendly alternatives to oral repaglinide, offering improved bioavailability, sustained release, and enhanced therapeutic outcomes in diabetes management.
Mishra et al. (Mon,) studied this question.