Formula Optimization and Quality Evaluation of Testosterone Undecanoate Binary Ethosomes / 中国药师

ABSTRACT

To screen the optimal formula and evaluate the quality of testosterone undecanoate ( TU) binary ethosomes to lay the foundation for the transdermal delivery system of TU. Methods:The mixture of ethanol and propylene glycol was used as the softeners, and TU binary ethosomes were prepared by ethanol injection method. The ratio of TU to lipids ( A) , the quality percentage of the mixture of ethanol and propylene glycol ( B) and the ratio of ethanol to propylene glycol ( C) as the influencing factors, and the entrapment efficiency as the index, an orthogonal test was used to optimize the formula of TU binary ethosomes. The morphology, size, zeta potential, in vitro drug release and stability of TU binary ethosomes were studied. Results:The optimal formula of TU binary etho-somes were as followsthe ratio of TU to lipids was 1∶15, the quality percentage of the mixture of ethanol and propylene glycol was 10% and the ratio of propylene glycol to ethanol was 6∶4. The optimal TU binary ethosomes were concentric circles under an optical microscope with uniform size, and the average size was (185. 5 ± 52. 8)nm, zeta potential was ( -15. 87 ± 0. 26)mV, and the entrap-ment efficiency was (79. 14 ± 0. 66)%. TU release from the binary ethosomes in vitro was fitted the first-order equationQ=20. 79t-11. 01 (r2 =0. 998 4). Under the high temperature, the entrapment efficiency was decreased significantly, while under the other test conditions, all the indices of TU binary ethosomes showed no significant difference. Conclusion:The optimal TU binary ethosomes are easy to be prepared with promising quality and sustained release property in vitro, which are valuable to be studied further.