Design, optimization and characterization of novel topical formulations containing Triamcinolone Acetonide

Abstract

Triamcinolone Acetonide (TA), a lipid-soluble molecule, is a synthetic glucocorticosteroid with anti-scarring, immunosuppressive and anti-inflammatory activity. The penetration of TA through the hypertrophic scar is challenging due to the scar tissue is thicker than the normal skin tissue. To overcome this problem, it was planned to prepare liposomal systems which are using for their penetration enhancer effect in topical use. So, in the present study, TA loaded liposome and liposomal film formulations were prepared and optimized to increase release and also stability. For the optimization of liposome formulations, response surface methodology (RSM) was used and the selected independent variables were the amounts of phospholipon 90g (PH) and cholesterol (CH). Encapsulation efficiency, particle size and zeta potential which were selected as dependent variables for liposome were found as 85.18% +/- 2.01%, 185.2 +/- 2.15 nm and -7.48 +/- 0.42 mV, respectively. By using optimum liposome formulation, liposomal film formulations were prepared. The percentage of PVA ad PG were chosen as independent variables of liposomal film formulation. The dependent variables of the liposomal film formulations which were thickness, puncture strength and puncture deformation values were found to be 0.24 +/- 0.02 mm, 5.53 +/- 2.43 N/mm(2) and 8.65% +/- 1.45%, respectively. Spherical and uniform shapes of liposomes were confirmed by electron microscopy. The in-vitro bioadhesion work value of the optimum lipo-somal film formulation indicated that the films provide sufficient adhesion on the skin. In vitro release studies showed that the release behavior of TA from the optimized formulations fitted well with the Higuchi kinetic model. Physical stability tests demonstrated that optimized liposome and liposomal film were convenient for storage at 5 +/- 3 degrees C for at least 90 days. In conclusion, optimized liposome and liposomal film formulations of TA could be offered as a promising strategy regarding their release, particle size, high encapsulation efficiency and stability for the treatment of hypertrophic scars.