Formulation Development of Tranexamic Acid loaded Transethosomal Patch for Melasma

Abstract

Nanotechnology based drug delivery systems are employed to overcome the hitches associated with conventional therapies. Melasma is a chronic, acquired, therapeutically challenging, universally relapsing hyperpigmentation disorder that causes greyish-brown spots on the skin, mainly on the face. Tranexamic acid (TXA) is a newer medication used to treat melasma that can be administered topically as well as orally. TXA has an oral bioavailability of 30-50%. The current study aimed to create a transethosomal (TEL) patch, for transdermal delivery of TXA for the treatment of melasma as an alternative to the oral route's hindrance. The cold technique was used to prepare TEL. They are composed of phospholipid (Phospholipon 90G), ethanol, water, and an edge activator (sodium cholate). Drug excipient compatibility study was done using Differential scanning colorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy techniques. TEL batches were further characterized based on particle size (PS) and entrapment efficiency (EE). The optimized batch's PS and EE were found to be 72 nm and 94%, respectively. The average zeta potential was -16 mV, indicating a stable formulation. Vesicular morphology was monitored by Scanning electron microscopy (SEM) analysis. The in vitro and ex vivo release of TXA was evaluated by Franz diffusion study and showed the release of about 93.97% over the period of 24 hrs, which was better than that of a conventional topical cream. All of the above findings showed that TEL may be a good carrier alternative for delivery of TXA into deeper layers, and hence good for treating melasma.