In vitro skin permeation study of ethosome containing mycophenolic acid
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Abstract
Introduction: Ethosome are soft, malleable vesicles carrier which mainly composes of phospholipids, ethanol in relatively high concentration and water. This carrier presents interesting features correlated with its ability to permeate through the skin. in this study, the ethosome containing Mycophenolic acid (MPA) was prepared and characterized to obtain the optimized formulation. The in vitro skin permeation of the optimized formulation was tested for evaluation suit of applying as topical delivery system for MPA. Materials and method: The ethosome containing MPA were prepared according to the thin-film hydration method. The characterization of ethosome was evaluated in terms of physical appearances, particle size, size distribution, zeta potential, surface morphology and entrapment efficiency. in addition, in vitro skin permeation and skin retention studies of the appropriate ethosome were evaluated using modified Franz diffusion cell were carried out with the newborn pig skin. Results: The optimized ethosomal formulation (Etho-25) was composed of 4% w/v L-α-phosphatidylcholine from soybean (SPC): Cholesterol from lanolin (CHOL): Polyoxyethylene sorbitan monooleate (Tween 80): deoxycholic acid (DA) with a molar ratio was 6:2:1 1 as lipid component and 30% v/v ethanol in phosphate buffer pH 7.4 as dispersion medium. This formulation gave ethosome with 370.90±7.91 nm vesicular size (Polydispersity index Pl= 0.270±0.02 nm), the zeta potential of -45.58±4.50 mV and the entrapment efficiency of 56.01 ±1.10%. Further, the appropriate ethosome provided significantly higher skin permeation parameter such as the cumulative amount at 24 hours Q24 (307.29±24.93 µg/cm2), the steady state flux Jss (13.20±0.91 µg/cm2/h) and the skin permeation coefficient Kp (1.32+0.09 X10-3cm/h) compared to other formulations. The lag time T lag of ethosome was 1.16±4.67 hours. Furthermore, the ethosome system gave the MPA accumulated in the skin higher (45.46±6.80 µg/cm2) than aqueous suspension, liposome and liposome that was developed by Rattanat, 2008 (p<0.05). Conclusions: These results indicated that the ethosome could enhance the skin permeation and retention of MPA that leading to the efficiency in topical delivery system.
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