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利用胶体载体系统进行他克莫司的皮肤靶向给药。

Dermal targeting of tacrolimus using colloidal carrier systems.

机构信息

Faculty of Biosciences/Institute of Pharmacy, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Straße 4, 06120 Halle, Saale,

出版信息

Int J Pharm. 2011 Feb 14;404(1-2):159-68. doi: 10.1016/j.ijpharm.2010.11.029. Epub 2010 Nov 19.

DOI:10.1016/j.ijpharm.2010.11.029
PMID:21094231
Abstract

In the therapy of chronic inflammatory skin diseases, the epicutaneous application of anti-inflammatory drugs in combination with maintenance therapy leads to ideal therapeutic long term effects. In this work, the development of well-tolerated colloidal carrier systems (ME) containing tacrolimus is described. A comprehensive physico-chemical characterization of the novel systems was performed using different techniques. The potential of three ME compared to an ointment as suitable carrier for dermal delivery of tacrolimus was determined. The penetration studies demonstrated that in comparison to the standard vehicle ointment, all three ME resulted in higher concentrations of tacrolimus in the deeper skin layers independent of the time of incubation. Particularly, the percentage of the bioavailable amount of tacrolimus (sum of the amount found in the dermis and acceptor compartment) from the ME with concentrations up to 20.95 ± 12.03% after 1000 min incubation time differed significantly (p<0.01), when compared to the ointment which yielded a concentration of 6.41 ± 0.57%. As a result of these experiments, using colloidal carrier systems, the penetration profile of tacrolimus was enhanced significantly (p<0.01). High drug amounts penetrated the target site in a short period of time after applying the ME.

摘要

在慢性炎症性皮肤病的治疗中,将抗炎药物经皮应用于联合维持治疗可产生理想的长期治疗效果。在这项工作中,描述了含有他克莫司的良好耐受胶体载体系统(ME)的开发。使用不同的技术对新型系统进行了全面的物理化学特性描述。将三种 ME 与软膏相比,确定了它们作为他克莫司经皮递送合适载体的潜力。渗透研究表明,与标准载体软膏相比,所有三种 ME 都能使他克莫司在深层皮肤中的浓度更高,而与孵育时间无关。特别是,在 1000 分钟孵育时间后,浓度高达 20.95 ± 12.03%的 ME 中他克莫司的生物利用量(真皮和接受腔中发现的量之和)的百分比与软膏(6.41 ± 0.57%)相比差异显著(p<0.01)。由于这些实验,使用胶体载体系统,他克莫司的渗透特性得到了显著增强(p<0.01)。在施用 ME 后很短的时间内,大量药物渗透到靶位。

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