| 石德顺 李富利 吴东泽 曾抗 朱晓亮.利多卡因醇质体的理化性质及其皮肤刺激性研究[J].,2015,15(9):1654-1658 |
| 利多卡因醇质体的理化性质及其皮肤刺激性研究 |
| The Study of Physicochemical Properties and Skin Irritation ofLidocaine Ethosomes |
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| DOI： |
| 中文关键词: 利多卡因 醇质体 皮肤刺激性 |
| 英文关键词: Lidocaine Ethosomes Skin irritancy |
| 基金项目:国家自然科学基金项目（30902019） |
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| 中文摘要: |
| 目的：制备利多卡因醇质体，并对其理化性质及皮肤刺激性进行研究。方法：采用超声注入法制备利多卡因醇质体，使用透
射电镜观察和激光粒度仪分析其形态、粒径大小及分布，采用透析法和HPLC法测定利多卡因醇质体的包封率，对不同温度下保
存60 天后的利多卡因醇质体的包封率进行测定以评估其稳定性，通过豚鼠皮肤刺激试验对利多卡因醇质体的皮肤刺激性进行
分析。结果：利多卡因醇质体为圆形囊泡结构，粒径为31.33± 2.63 nm，多分散指数为0.42± 0.21，显示粒径分布较为均匀，其包封
率为(52.85± 0.36) %，保存在25± 1 ℃时泄露最少，豚鼠完整及破损皮肤经利多卡因醇质体处理后均未见红斑和水肿反应，行组
织学检查也未见明显炎症改变。结论：利多卡因醇质体具备理想的理化性质且对皮肤无刺激性，有望成为一种新型经皮局麻制
剂。 |
| 英文摘要: |
| Objective:To prepare the lidocaine ethosomes and investigate its physicochemical properties and skin irritancy.Methods:The lidocaine ethosomes was prepared by ultrasonic injection method. The morphology was examined by transmission electron
microscope. The particle size and distribution were detected by Zetasizer instrument. The free drug was separated by dialysis method and
the encapsulation efficiency of lidocaine ethosomes was determined by HPLC. The encapsulation efficiency at different temperatures was
determined at sixtieth days to evaluate the stability. The guinea pigs were utilized to investigate the skin irritations of lidocaine
ethosomes.Results:The lidocaine ethosomes was spherical vesicles, its size distribution was narrow with polydispersity index of 0.42±
0.21, and its particle diameter and encapsulation efficiency were 31.33± 2.63nm and (52.85 ± 0.36)%, respectively, the leakage of
lidocaine ethosomes was lowest in storing at 25± 1℃. There had no edema and erythema could be observed on the guinea pigs skin, and
had no inflammation changes in the histopathological observation.Conclusion:The lidocaine ethosomes with ideal physicochemical
properties has no skin irritation and is expected to be a new topical anaesthetic preparation. |
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