Development of Tapentadol Hydrochloride Loaded Proniosomal Gel using Main Effects Screening Design and in silico Verification using Parameter Sensitivity Analysis

Aim: Tapentadol Hydrochloride is a centrally acting opioid analgesic of biopharmaceutical classification system class I drug. Oral administration of tapentadol hydrochloride undergoes extensive first-pass metabolism leads to poor bioavailability. The present study was aimed to screen the critical material attributes to deliver the tapentadol hydrochloride through the transdermal route using a carrier proniosomal gel. Methodology: Main effect screening design has been constructed to screen the choice of surfactant used for the formulation of tapentadol hydrochloride proniosomal gel. The critical material attributes selected were surfactant, cholesterol, and soya lecithin, with responses entrapment efficiency (%), vesicle size (nm), and zeta potential (mV). All 24 runs of experiments were performed and evaluated to check the model fit. The in silico verification was analyzed using parameter sensitivity analysis. Results: The prediction profiler showed maximum desirability for Kolliphore RH 40 against the set goals. The design diagnostic efficiency was measured better for the constructed MESD. Also, parameter sensitivity analysis confirms that the vesicle size would play a principal role in the permeation of tapentadol hydrochloride proniosomal gel. Conclusion: Hence, Kolliphore RH 40 was considered for the further optimization process. The tapentadol hydrochloride proniosomal gel would be a better alternative to oral therapy.