CCD based Development and Characterization of Tranexamic acid Loaded Transethosomes for Melasma

Abstract

This study was intended to develop and optimize Tranexamic acid (TXA) loaded transethosomal (TEL’s) patch for the treatment of melasma. Upon oral administration, TXA is reported to cause gastrointestinal (GI) sideeffects and showed 30-50% bioavailability. Hence an alternative transdermal drug delivery system has been designed in the form of transethosomes (TEL). TXA loaded TELwere prepared by the cold method using Phospholipon 90G as a lipoid, sodium cholate as an edge activator, ethanol, and water. Further size reduction was done using a probe sonicator. For optimization purposes central composite design (CCD) was used. Phospholipon 90G and sodium cholate were selected as independent variables. Particle size (PS) and entrapment efficiency (E.E) were selected as a response. Mathematical equations and 3-D response surface graphs were used to relate dependant and independent variables. The optimized model pre-predicted and experimentally gave the particle size of 72nm, zeta potential of -16mV, encapsulation efficiency of 94%, with an enhanced transdermal flux of 32.85μg/cm2 /h as compared to a conventional topical cream. In vitro and ex-vivo studies were done to check the efficacy of the formulation and the results showed improved release of drug in TEL formulation as compared to conventional marketed formulation.