Preparation of tranexamic acid transfersomes and investigation on their characteristics / 中草药

ABSTRACT

Objective: To optimize the formulation and prepration of tranexamic acid (TA) transfersomes by central composite design-response surface method. Methods: The transfersomes were prepared using the reverse rotary evaporation method. The effects of phosphatidylcholine (SPC)-cholesterol (CH) ratio, SPC-drug ratio, and the concentration of sodium deoxycholic acid on the entrapment efficiency (EE) were investigated, the results were fitted with binomial equation, and the optimal formulation was predicted by response surface method. Results: The preparation conditions were optimized as SPC-CH (2:1), SPC-drug (6:1), and the concentration of sodium deoxycholic acid 20 mg. Under these conditions, the evaluated EE, drug-loading, average partical size, and Zeta potential of TA transfersomes were (81.28 ± 1.06)%, (4.67 ± 0.28)%, (105.3 ± 7.2) nm, and (-38.5 ± 2.3) mV. The deviation of measured and predicated values was smaller. Conclusion: The central composite design-response surface method is applicable for the optimization of TA transfersomes and the resulting optimal preparation technique is stable and feasible.