目的 以金银花Lonicerae Japonicae Flos-蒲公英Taraxaci Herba提取液纳米相态为对象进行凝胶剂制备处方研究并对其进行药效评价。方法 通过适量卡波姆940、甘油、透明质酸钠、1,3-丁二醇、丙二醇及蒸馏水合成金银花-蒲公英提取液纳米相态凝胶剂并构建评价方法，采用单因素考察及Box-Behnken设计-响应面法（Box-Behnken design-response surface method，BBD-RSM）考察卡波姆940、甘油、pH值、载药量对凝胶剂综合评分的影响并对凝胶剂外观性状、涂展性、离心稳定性、低温稳定性、高温稳定性进行评价以确定最优工艺；建立大鼠痤疮模型，通过耳廓肿胀率、炎症因子含量等对比考察金银花-蒲公英提取液纳米相态凝胶剂内服、外用、内外合用的抗炎药效。结果 金银花-蒲公英提取液纳米相态凝胶剂最优制备处方为金银花-蒲公英提取物纳米相冻干粉6.89%、卡波姆940 1.31%、甘油4.82%、透明质酸钠0.05%、1,3-丁二醇2.5%、丙二醇2.5%，pH 5.09；金银花-蒲公英提取液纳米相态凝胶剂内服、外用、内外合用均可显著降低痤疮模型大鼠耳廓肿胀率（P＜0.01、0.001）及大鼠血清炎症因子肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）、白细胞介素-6（interleukin-6，IL-6）、胰岛素样生长因子-1（insulin-like growth factor-1，IGF-1）含量（P＜0.001），有效改善痤疮大鼠耳部的病理损害。结论 金银花-蒲公英提取液纳米相态凝胶剂对痤疮丙酸杆菌诱导的痤疮炎症反应具有显著的抑制作用，为中药药对提取液纳米相态治疗痤疮的制剂开发提供参考。

Objective The preparation process of the gel was studied and its pharmacodynamic evaluation was carried out with the nano phase state of the extract of Jinyinhua (Lonicerae Japonicae Flos, LJF)-Pugongying (Taraxaci Herba, TH). Methods The LJF-TH extract nanophase was subjected to gel preparation by using appropriate amount of carbomer 940, glycerol, sodium hyaluronate, 1,3-butanediol, propylene glycol, and distilled water, and the gel evaluation method was established. The effects of carbomer 940, glycerol, pH value and drug load on the comprehensive score of gels were investigated by single factor investigation and Box-Behnken design-response surface method, and the appearance properties, spreadability, centrifugal stability, low temperature stability and high temperature stability of gels were evaluated to determine the optimal process. The experimental model of acne was established in rats, and the anti-inflammatory effects of taking the nano phase gel orally, applying it and internal-external combination’s methods of administration were investigated by comparing the swelling rate of auricle and the content of inflammatory factors. Results The optimal preparation process of LJF-TH extract nanophase gel was as follows: LJF-TH extract nanophase lyophilized powder 6.89%, carbomer 940 1.31%, glycerol 4.82%, sodium hyaluronate 0.05%, 1,3-butanediol 2.5%, propylene glycol 2.5%, pH 5.09. All of taking the nano phase gel orally, applying it and internal-external combination’s method of administration can significantly reduce the swelling rate of the auricle (P < 0.01, 0.001) and the content of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) and insulin-like growth factor-1 (IGF-1) in the serum of rats, and effectively improve the pathological damage of the ears of acne rats (P < 0.001). Conclusion The nano phase gel of LJF-TH extract has a significant inhibitory effect on acne inflammation induced by Propionibacterium acnes, which provides a reference for the development of Chinese medicine pair extract nano phase preparation for acne treatment.

R283.6

江西省重点研发计划项目（20224BBG71023）;江西省高层次高技能领军人才培养工程（12623001）;江西省教育厅科学技术研究项目（GJJ2400801）;中药学重点学科项目（2023jzzdxk016）;博士科研启动基金项目（2023WBZR007）