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多层乳液对低效局部类固醇诱导的局部不良反应的预防作用。

Preventive effects of multi-lamellar emulsion on low potency topical steroid induced local adverse effect.

作者信息

Sul Geun Dong, Park Hyun Jung, Bae Jong Hwan, Hong Keum Duck, Park Byeong Deog, Chun Jaesun, Jeong Se Kyoo, Lee Seung Hun, Ahn Sung Ku, Kim Hyun Jung

机构信息

Department of Biology Education, Korea National University of Education, Cheongwon, Korea.

出版信息

Ann Dermatol. 2013 Feb;25(1):5-11. doi: 10.5021/ad.2013.25.1.5. Epub 2013 Feb 14.

Abstract

BACKGROUND

Topical steroid treatment induces diverse local Wand systemic adverse effects. Several approaches have been tried to reduce the steroid-induced adverse effects. Simultaneous application of physiological lipid mixture is also suggested.

OBJECTIVE

Novel vehicles for topical glucocorticoids formulation were evaluated for the efficacy of reducing side-effects and the drug delivery properties of desonide, a low potency topical steroid.

METHODS

Transcutaneous permeation and skin residual amount of desonide were measured using Franz diffusion cells. The in vivo anti-inflammatory activity was evaluated using murine model.

RESULTS

Topical steroids formulation containing desonide, in either cream or lotion form, were prepared using multi-lamellar emulsion (MLE), and conventional desonide formulations were employed for comparison. MLE formulations did not affect the anti-inflammatory activity of the desonide in phobol ester-induced skin inflammation model, compared with conventional formulations. While the penetrated amounts of desonide were similar for all the tested formulations at 24 hours after application, the increased lag time was observed for the MLE formulations. Interestingly, residual amount of desonide in epidermis was significantly higher in lotion type MLE formulation. Steroid-induced adverse effects, including permeability barrier function impairment, were partially prevented by MLE formulation.

CONCLUSION

Topical desonide formulation using MLE as a vehicle showed a better drug delivery with increased epidermal retention. MLE also partially prevented the steroid-induced side effects, such as skin barrier impairment.

摘要

背景

局部用类固醇治疗会引发多种局部和全身不良反应。人们尝试了多种方法来减少类固醇诱导的不良反应。同时也建议应用生理脂质混合物。

目的

评估新型局部用糖皮质激素制剂载体在降低副作用方面的效果以及低效能局部用类固醇地奈德的药物递送特性。

方法

使用Franz扩散池测量地奈德的经皮渗透和皮肤残留量。使用小鼠模型评估体内抗炎活性。

结果

使用多层乳液(MLE)制备了乳膏或洗剂形式的含地奈德的局部用类固醇制剂,并采用传统的地奈德制剂进行比较。与传统制剂相比,在佛波酯诱导的皮肤炎症模型中,MLE制剂对地奈德的抗炎活性没有影响。虽然在应用后24小时所有测试制剂的地奈德渗透量相似,但MLE制剂的滞后时间延长。有趣的是,洗剂型MLE制剂中地奈德在表皮中的残留量显著更高。MLE制剂部分预防了包括通透性屏障功能受损在内的类固醇诱导的不良反应。

结论

以MLE为载体的局部用地奈德制剂表现出更好的药物递送,表皮滞留增加。MLE还部分预防了类固醇诱导的副作用,如皮肤屏障受损。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/735c/3582928/f8a6e155ddc9/ad-25-5-g001.jpg

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