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以甾体激素和非甾体抗炎药为模型药物的透皮载体的渗透效果

Permeation Efficacy of a Transdermal Vehicle with Steroidal Hormones and Nonsteroidal Anti-inflammatory Agents as Model Drugs.

作者信息

Junqueira Laura A, Polonini Hudson, Loures Sharlene, Raposo Nádia R B, Ferreira Anderson O, Brandão Marcos Antônio F

机构信息

NUPICS- Nucleo de Pesquisa e Inovacao em Ciencias da Saude, Universidade Federal de Juiz de Fora, Juiz de Fora, Brazil.

Ortofarma Laboratory, Matias Barbosa, Brazil.

出版信息

Curr Drug Deliv. 2019;16(2):136-141. doi: 10.2174/1567201815666181024141849.

Abstract

BACKGROUND

Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation.

OBJECTIVE

In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs.

METHODS

To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used.

RESULTS

After 24 h, the vehicle was able to deliver 18.32 µg/cm2 of progesterone and 92.07 µg/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied.

CONCLUSION

Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

摘要

背景

经皮给药是药物给药的一种替代途径。然而,这需要开发能够使药物穿过皮肤层并进入体循环的载体。

目的

在本研究中,使用黄体酮、雌二醇、雌二醇+雌三醇(倍美力)和酮洛芬作为模型药物评估一种新型经皮载体。

方法

为评估药物的离体渗透,使用了带有人类皮肤的Franz垂直扩散池。

结果

24小时后,该载体能够使18.32μg/cm²的黄体酮和92.07μg/cm²的酮洛芬透过皮肤进入受体介质。雌二醇、雌二醇(倍美力)、雌三醇(倍美力)、黄体酮和酮洛芬的渗透百分比分别为91%、78.8%、48.5%、73.2%和63.6%。对于所有药物,都输送了足够的量以产生全身效应,并且还可以减少乳液的涂抹量。

结论

因此,该载体表现出高性能,并且有可能用于经皮给药存在困难的药物。

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