| 吴婷,钟家浩,姚文栋.载神经毒素的透明质酸可溶性微针评价及镇痛作用研究[J].浙江中西医结合杂志,2024,34(3): |
| 载神经毒素的透明质酸可溶性微针评价及镇痛作用研究 |
|
| 投稿时间：2023-09-06 修订日期：2023-12-04 |
| DOI： |
| 中文关键词: 神经毒素 可溶性微针 透明质酸 镇痛 透皮递送 |
| 英文关键词:neurotoxin dissolving microneedles hyaluronic acid analgesic effect transdermal drug delivery |
| 基金项目:浙江省药学会医院药学专项科研资助项目(“石药集团”专项)(2019ZYY23) |
|
| 摘要点击次数: 455 |
| 全文下载次数: 0 |
| 中文摘要: |
| 摘要：目的 将中华眼镜蛇的神经毒素（NT）制备成透皮给药的可溶性微针（DMN-NT），并考察其理化性质及透皮镇痛效果。 方法 以透明质酸（HA）作为针体材料，羧甲基纤维素为背衬层材料，采用两步离心法制备DMN-NT。显微镜表征其形态，HPLC法测定其载药量，并考察稳定性；采用Franz扩散池考察其体外透皮性能；热板法、醋酸扭体法及鼠尾测痛法考察其镇痛效果。结果 通过单因素考察确定30 mg/mL的HA为制备DMN-NT的最佳浓度。DMN-NT针体呈四棱锥形，表面平整，长度约为500 μm，底部宽度为350 μm；每片载药量为 (2.2 ± 0.2) μg，且3个月内稳定性良好。离体皮肤渗透结果显示，2 h后DMN-NT中NT的累积渗透量达90 %，而NT溶液几乎没有透过皮肤，证明可溶性微针对NT透皮递送具有良好的促进作用，能有效穿透大鼠离体皮肤。NT与DMN-NT均具有中枢镇痛和外周镇痛作用，DMN-NT的作用时间明显长于NT。 结论 本研究制备的 DMN-NT 实现了大分子多肽NT的无痛透皮递送，可以延长NT镇痛作用时间。 |
| 英文摘要: |
| Abstract: Objective To evaluate Naja naja atra’s neurotoxin (NT) loaded dissolving microneedle (DMN-NT) in vitro and its analgesic effect. Methods Hyaluronic acid (HA) as the needle material and carboxymethyl cellulose (CMC) as the backing layer material, DMN-NT was prepared by a two-step centrifugation method. And the morphological characteristics were observed under an optical microscope; the drug loading content and the stability was determined by HPLC. Franz diffusion cell was used to investigate its in vitro skin permeation characteristics. Analgesic effect was studied by the acetic acid-writhing test, the hot-plate test and the tail pain test. Results Through the single-factor exploration, we confirmed that 30 mg/mL of HA was the best concentration for DMN-NT preparation. The DMN-NT had a pyramidal shape with a smooth surface and a length of approximately 500 μm. The drug loading content of per patch was (2.2 ± 0.2) μg. DMN-NT had good stability within 3 months at -20 ℃. The results of in vitro skin permeation assay showed that the cumulative penetration of NT in DMN-NT could reach 90 % in 2 h, while NT solution barely penetrated the skin. The results of analgesic effect experiment displayed that the characteristics of NT’s analgesic effect remained unchanged and the analgesic effect time was significantly prolonged via DMN-NT. Conclusion In this study, DMN-NT realized the transdermal painless drug delivery of macromolecular drugs, prolonging the analgesic effect of NT. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
