Preparation and in Vitro Evaluation of Indomethacin Binary Ethosomes Gel
Objective:To optimize the formulation process of indomethacin (IND) binary ethosomes gel,and research its pharmacodynamics and stability. Methods:With the mean particle size Y1 and encapsulation rate Y2 as dependent vari-ables,the amount of phospholipid X1,the amount of mixed alcohol X2,and the amount of propylene glycol X3 as indepen-dent variables,the preparation process of IND diethosome was optimized by central point design and response surface method. IND binary ethosomes gel was prepared in 1∶1 ratio with Carbomer gel matrix. The in vitro transdermal properties of IND gel,nano emulsion and binary ethosomes gel were investigated by modified Franz diffusion cell method,and the pre-liminary stability of IND binary ethosomes gel was investigated,and in vivo analgesic effects of IND were investigated by hot plate method and acetic acid writhing method. Results:The optimal formulation process was IND 0.50 g,phospholipid 0.46 g,mixed alcohol 8.45 mL,propylene glycol 2.15 mL,the average particle size of IND binary ethosomes gel was (81.80±1.04) nm,encapsulation rate was (72.61±1.01)％. The relative errors were 2.36％ and 2.29％,respectively. The steady permeation rate constant of IND binary ethosomes gel is (0.6467±0.0073) μg·cm-2·h-1,which is 2.16 times of that of ordinary gel and 1.43 times of that of nano emulsion,IND binary ethosomes gel could significantly inhibit hot plate load-ing and acetic acid writhing in mice. Conclusion:The prepared IND binary ethosomes gel has small particle size,relatively uniform distribution,good transdermal absorption performance,in vivo analgesia and good stability,which provides a ba-sis for the study of a new dosage form of IND for the treatment of local inflammation.
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