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采用体内微透析法评价补骨脂素醇质体经皮给药。

Evaluation of psoralen ethosomes for topical delivery in rats by using in vivo microdialysis.

机构信息

Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.

出版信息

Int J Nanomedicine. 2014 Jan 23;9:669-78. doi: 10.2147/IJN.S57314. eCollection 2014.

Abstract

This study aimed to improve skin permeation and deposition of psoralen by using ethosomes and to investigate real-time drug release in the deep skin in rats. We used a uniform design method to evaluate the effects of different ethosome formulations on entrapment efficiency and drug skin deposition. Using in vitro and in vivo methods, we investigated skin penetration and release from psoralen-loaded ethosomes in comparison with an ethanol tincture. In in vitro studies, the use of ethosomes was associated with a 6.56-fold greater skin deposition of psoralen than that achieved with the use of the tincture. In vivo skin microdialysis showed that the peak concentration and area under the curve of psoralen from ethosomes were approximately 3.37 and 2.34 times higher, respectively, than those of psoralen from the tincture. Moreover, it revealed that the percutaneous permeability of ethosomes was greater when applied to the abdomen than when applied to the chest or scapulas. Enhanced permeation and skin deposition of psoralen delivered by ethosomes may help reduce toxicity and improve the efficacy of long-term psoralen treatment.

摘要

本研究旨在通过使用醇质体提高补骨脂素的皮肤渗透和沉积,并研究其在大鼠深层皮肤中的实时药物释放。我们采用均匀设计方法来评估不同醇质体配方对包封效率和药物皮肤沉积的影响。通过体外和体内方法,我们研究了与乙醇酊剂相比,负载补骨脂素的醇质体的皮肤渗透和释放。在体外研究中,与使用酊剂相比,醇质体的使用使补骨脂素的皮肤沉积增加了 6.56 倍。体内皮肤微透析显示,醇质体中补骨脂素的峰浓度和曲线下面积分别约为酊剂中补骨脂素的 3.37 倍和 2.34 倍。此外,研究还表明,将醇质体应用于腹部时,其经皮渗透能力大于应用于胸部或肩胛部时。醇质体递送的补骨脂素的渗透和皮肤沉积增强可能有助于降低毒性并提高长期补骨脂素治疗的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e93/3904810/68576f9c64a8/ijn-9-669Fig1.jpg

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