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摘要
Objective: To study the preparation, quality evaluation, and therapeutic effect of pseudolaric acid B liposome gel in mice with atopic dermatitis thus to overcome the disadvantages of high irritation, unstable quality, and poor patient adherence of tincture of Cortex Pseudolaricis. Methods: The liposome preparation conditions were screened by using encapsulation rate as the evaluation index, and the best preparation conditions were optimized by using univariate analysis and Box-Behnken response surface method. Then the quality of the further produced liposome gels was evaluated. The transdermal permeation and skin retention of pseudolaric acid B liposome gel and normal gel were compared using Franz diffusion cell. The anti-inflammatory efficacy of pseudolaric acid B liposome gel was evaluated using a mouse model of atopic dermatitis. Results: The optimal prescription composition for the preparation of pseudolaric acid B liposomes by the thin film dispersion method was as follows: the phospholipid type was 1, 2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC); the mass ratio of phospholipid:cholesterol:pseudolaric acid B was 18:3:1; the amount of phosphate used for hydration had little effect on the encapsulation rate; the maximum encapsulation rate was 63.9%. The average particle size of the best prescribed liposomes was 173.6 nm with a normal particle size distribution, the polydispersity index (PDI) was 0.259, and the average potential was -46.2 mV. The quality evaluation results of the liposomal gel showed that its appearance, properties, and stability were in accordance with the quality requirements. In vitro transdermal experiments showed that the 24 h cumulative penetration quantity of pseudolaric acid B liposome gel was less than that of the normal gel, but the skin retention quantity was greater than that of the normal gel. The efficacy experiments in mice with atopic dermatitis showed that the medium-dose liposomal gel of pseudolaric acid B (5 mg?g-1) and the high-dose group (10 mg?g-1) were not significantly different from the positive control drug (1 mg?g-1) in terms of skin lesion score, ear thickness, scratching times, serum IgE and IL-13 indexes, but the low-dose group (1 mg?g-1) was significantly different from the positive control drug (1 mg?g-1) in the above indexes. Conclusion: The optimized liposome gel of pseudolaric acid B has simple preparation process, stable quality, confirmed efficacy in treating mice with atopic dermatitis and is comfortable to use, which laid the foundation for the development and clinical application of pseudolaric acid B transdermal preparation.
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