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通过带电荷的超可变形脂质体提高欧前胡素经皮给药的皮肤渗透效率。

Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery.

作者信息

Lin Hongwei, Xie Qingchun, Huang Xin, Ban Junfeng, Wang Bo, Wei Xing, Chen Yanzhong, Lu Zhufen

机构信息

Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.

Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.

出版信息

Int J Nanomedicine. 2018 Feb 8;13:831-842. doi: 10.2147/IJN.S150086. eCollection 2018.

Abstract

AIM

The aim of this work was to develop a novel vesicular carrier, ultradeformable liposomes (UDLs), to expand the applications of the Chinese herbal medicine, imperatorin (IMP), and increase its transdermal delivery.

METHODS

In this study, we prepared IMP-loaded UDLs using the thin-film hydration method and evaluated their encapsulation efficiency, vesicle deformability, skin permeation, and the amounts accumulated in different depths of the skin in vitro. The influence of different charged surfactants on the properties of the UDLs was also investigated.

RESULTS

The results showed that the UDLs containing cationic surfactants had high entrapment efficiency (60.32%±2.82%), an acceptable particle size (82.4±0.65 nm), high elasticity, and prolonged drug release. The penetration rate of IMP in cationic-UDLs was 3.45-fold greater than that of IMP suspension, which was the highest value among the vesicular carriers. UDLs modified with cationic surfactant also showed higher fluorescence intensity in deeper regions of the epidermis.

CONCLUSION

The results of our study suggest that cationic surfactant-modified UDLs could increase the transdermal flux, prolong the release of the drug, and serve as an effective dermal delivery system for IMP.

摘要

目的

本研究旨在开发一种新型囊泡载体——超柔性脂质体(UDLs),以拓展中药欧前胡素(IMP)的应用,并提高其经皮递送能力。

方法

在本研究中,我们采用薄膜水化法制备了负载IMP的UDLs,并在体外评估了它们的包封率、囊泡变形性、皮肤渗透性以及在皮肤不同深度的蓄积量。还研究了不同带电表面活性剂对UDLs性质的影响。

结果

结果表明,含有阳离子表面活性剂的UDLs具有较高的包封率(60.32%±2.82%)、可接受的粒径(82.4±0.65 nm)、高弹性和延长的药物释放。IMP在阳离子UDLs中的渗透速率比IMP混悬液高3.45倍,这是囊泡载体中的最高值。用阳离子表面活性剂修饰的UDLs在表皮较深区域也显示出较高的荧光强度。

结论

我们的研究结果表明,阳离子表面活性剂修饰的UDLs可以增加经皮通量,延长药物释放,并作为IMP的有效皮肤递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e7b5/5811179/fb316c0578a6/ijn-13-831Fig1.jpg

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