| 引用本文: | 陈莉,吴浪琴,邹 欢.阿魏酸微乳-温敏凝胶经皮给药制剂的制备与评价[J].中国现代应用药学,2025,42(4):55-54. |
| chenli,Wu Langqin,Zou Huan.Preparation and Evaluation of Ferulic Acid Microemulsion-Thermosensitive gel for Transdermal Drug Delivery[J].Chin J Mod Appl Pharm(中国现代应用药学),2025,42(4):55-54. |
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| 摘要: |
| 目的 制备阿魏酸微乳-温敏凝胶并评价其体外理化性质、透皮吸收能力和皮肤滞留情况。方法 以泊洛沙姆188和泊洛沙姆407为凝胶基质，将阿魏酸微乳制备成温敏凝胶并评价其外观性状、微观形态、粒径、pH、黏度、胶凝温度、胶凝时间及稳定性；以雄性大鼠背部皮肤为渗透屏障，采用Franz扩散池法考察阿魏酸三种不同制剂和不同载药量的皮肤透过性和皮肤滞留量。结果 阿魏酸微乳-温敏凝胶的处方为泊洛沙姆188:泊洛沙姆407:水:阿魏酸预微乳=0.4:5.0:24.5:1.5（w/w/w/w)。室温下微乳-温敏凝胶为无色澄明可流动液体，达到皮肤温度时呈半固体状，其乳滴呈球形，平均粒径为（13.74±3.89）nm，PDI值为（0.263±0.071），pH值为（6.05±0.21），黏度为（179.76±15.34） mPa·s，胶凝温度为（31.91±0.14）℃，胶凝时间＜1 min，30 d内稳定性良好。阿魏酸混悬液、微乳和微乳-温敏凝胶的渗透速率常数分别为4.560 2、12.339、7.255 4 μg·cm-2·h-1，12 h累积透过量为（39.10±3.54）、（99.27±9.06）、（71.94±6.58） μg·cm-2，皮肤滞留量为（42.97±4.91）、（47.07±7.45）、（44.97±5.96） μg·cm-2。阿魏酸微乳-温敏凝胶低、中、高三种载药量的渗透速率常数分别为1.024 9、3.998 5、7.255 4 μg·cm-2·h-1，12 h累积透过量为（14.03±1.07）、（37.21±4.88）、（71.94±6.58） μg·cm-2，皮肤滞留量为（15.35±3.03）、（32.04±6.47）、（44.97±5.96） μg·cm-2。结论 阿魏酸微乳-温敏凝胶具有良好的温度敏感性、皮肤渗透性和滞留效果，可望开发成阿魏酸的新型局部给药制剂。 |
| 关键词: 阿魏酸 微乳 温敏凝胶 透皮吸收 皮肤滞留量 |
| DOI： |
| 分类号:R944 |
| 基金项目:基于中药芳香疗法治失眠理论构建载植物精油和阿魏酸的新型纳米乳喷鼻剂 |
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| Preparation and Evaluation of Ferulic Acid Microemulsion-Thermosensitive gel for Transdermal Drug Delivery |
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chenli, Wu Langqin, Zou Huan
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Zunyi Medical University
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| Abstract: |
| OBJECTIVE To prepare ferulic acid microemulsion-thermosensitive gel and evaluate its in vitro physicochemical properties, transdermal ability and skin retention. METHODS Ferulic acid microemulsion-thermosensitive gel was prepared by using poloxamer 188 and poloxamer 407 as gel matrix based on ferulic acid microemulsion, then its appearance, microscopic morphology, particle size, pH, viscosity, gel temperature, gelling time and stability were all evaluated. The transdermal permeability and skin retention of ferulic acid in three different preparations and drug loadings were studied by Franz diffusion cell method through the back skin of male rats. RESULTS The formulation composition of ferulic acid microemulsion-thermosensitive gel was poloxamer 188:poloxamer 407:water:ferulic acid pre-microemulsion=0.4:5.0:24.5:1.5(w/w/w/w). This gel would present a colorless, clear and flowable liquid at room temperature, then transform into semisolid at skin temperature. At the same time, the gel exhibited spherical microemulsion droplets, average particle size of (13.74±3.89) nm, the polydispersion coefficient of (0.263±0.071), pH value of (6.05±0.21), viscosity of (179.76±15.34) mPa·s, gelation temperature of (31.91±0.14) ℃, gelation time of less than 1 min, and good stability within 30 days. In suspension, microemulsion and microemulsion-thermosensitive gel, the penetration rate constant of ferulic acid was 4.560 2, 12.339, 7.255 4 μg·cm-2·h-1, the cumulative penetration rate within 12 h was (39.10±3.54), (99.27±9.06), (71.94±6.58) μg·cm-2, and the skin retention was (42.97±4.91), (47.07±7.45), (44.97±5.96) μg·cm-2, respectively. In microemulsion-thermosensitive gel with low, medium and high drug loading, The penetration rate constant of ferulic acid was 1.024 9, 3.998 5, 7.255 4 μg·cm-2·h-1, the cumulative penetration rate within 12 h was (14.03±1.07), (37.21±4.88), (71.94±6.58) μg·cm-2, and the skin retention was (15.35±3.03), (32.04±6.47), (44.97±5.96) μg·cm-2, separately. CONCLUSION Ferulic acid microemulsion-thermosensitive gel has favorable temperature sensitivity, transdermal permeability and skin retention effect, which is expected to be a novel vehicle for the topical use of ferulic acid. |
| Key words: ferulic acid microemulsion thermosensitive gel transdermal absorption skin retention |
