| 摘要: |
| 目的 考察改装滚轮微针在人增生性瘢痕皮肤中对醋酸曲安奈德的促透作用.方法 采用亚甲蓝和H-E染色法观察不同针长的微针刺入人增生性瘢痕皮肤的形态;建立高效液相色谱法测定醋酸曲安奈德含量;采用洗脱法、匀浆法分别考察给药1、12 h时增生性瘢痕皮肤醋酸曲安奈德在体吸收特性;采用经皮水分流失(TEWL)测量法、激光多普勒血流量法考察其皮肤刺激性.结果 所优选的针长500 μm滚轮微针能有效穿透角质层,形成的微孔分布相对均匀;微针处理1、12 h后,分别有27.42%、60.64%药物吸收进入皮肤.给药12 h,皮内注射醋酸曲安奈德皮肤中滞留药量较给药1 h下降至45.98%,而微针、直接涂布醋酸曲安奈德乳膏分别增加到2.73、4.18倍,微针组皮肤中滞留药量是直接涂布乳膏组的3.56倍(P<0.05).皮内注射12 h皮肤药量分布并不均匀,均值为(4.83±5.51) μg,微针组均值为(0.93±0.14) μg,分布相对均匀.TEWL法显示微针处理与皮内注射的皮肤刺激性差异无统计学意义,但激光多普勒血流量法显示皮内注射的皮肤刺激性是微针处理的8.40倍.结论 改装滚轮微针处理后涂布醋酸曲安奈德乳膏较皮内注射醋酸曲安奈德在人增生性瘢痕中吸收均匀、皮肤刺激性较小,但其瘢痕治疗效果尚有待进一步验证. |
| 关键词: 滚轮微针 改装 曲安奈德 瘢痕 皮肤吸收 |
| DOI：10.3724/SP.J.1008.2015.00058 |
| 投稿时间：2014-06-25修订日期：2014-12-28 |
| 基金项目:浦东新区卫生系统重点学科建设项目(PWZXK 2010-11) |
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| Modified microneedle roller enhancing percutaneous absorption of triamcinolone acetonide by human hyperplastic scar skin |
| LI Ya1,ZHANG Juan-juan2,ZHANG Li-chao1*,ZHU Quan-gang3,YU Hai2,WU Zhi-hong2 |
(1. Graduate School of Ningxia Medical University, Yinchuan 750004, Ningxia, China;
2. Department of Pharmacy, Shanghai Traditional Chinese Medicine Hospital, Shanghai 200071, China;
3. Department of Pharmacy, Yueyang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200437, China
*Corresponding author) |
| Abstract: |
| Objective To evaluate the role of modified microneedle roller in promoting permeation of triamcinolone acetonide across human hyperplastic scar skin. Methods The morphology of human hyperplastic scar skin was visualized by methylene blue staining and H-E staining after the insertion by microneedles of different lengths.The content of triamcinolone acetonide was determined by high performance liquid chromatography (HPLC). The in vivo absorption characteristics across human hyperplastic scar skin were investigated by elution method and the homogenization method at 1 h and 12 h after drug application.Skin irritation was assessed by transepidermal water-loss (TEWL) measurement and laser Doppler flowmetry. Results The preferred microneedle length of 500 μm effectively penetrated through the stratum corneum,and the distribution of the microchannels was homogeneous.It was found that 27.42% and 60.64% of the drug administered entered the skin at 1 h and 12 h,respectively.The drug accumulation in the skin at 12 h decreased to 45.98% of that at 1 h after intracutaneous injection,while the accumulation increased to 2.73-fold and 4.18-fold in the microneedle group and direct application of triamcinolone acetonide cream group,respectively,with the content of microneedle group being 3.56-fold that of the direct cream application group (P<0.05).Triamcinolone acetonide distribution was not homogeneous at 12 h after intracutaneous injection,with the level being (4.83±5.51) μg,while the distribution in the microneedle group was homogenous,with the level being (0.93±0.14) μg.TEWL results showed no significant difference in skin irritation between microneedle and intracutaneous injection group; however, laser Doppler flowmetry showed that the skin irritation of intracutaneous injection group was 8.40-fold that of microneedle treatment group. Conclusion Modified microneedle roller treatment followed by cream application, compared with intracutaneous injection, can yield more homogeneous distribution and less skin irritation in human hyperplastic scar skin, but its efficacy for scar treatment remains to be further verified. |
| Key words: microneedle roller modification triamcinolone acetonide cicatrix skin absorption |
