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首页> 外文期刊>New Journal of Chemistry >Novel mono, di and tri-fatty acid esters bearing secondary amino acid ester head groups as transdermal permeation enhancers
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Novel mono, di and tri-fatty acid esters bearing secondary amino acid ester head groups as transdermal permeation enhancers

机译：载仲氨基酸酯头组作为透皮渗透增强剂的新型单声道，二和三脂肪酸酯

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摘要

The use of chemical permeation enhancers (CPEs) has widened the pool of drugs that can be delivered via the transdermal route. This study explored the synthesis and characterization of novel mono, di and tri-fatty acid (FA) esters bearing beta-alanine t-butyl ester head groups as transdermal permeation enhancers using tenofovir (TNF) as a model drug. The synthesized compounds were non-toxic to mammalian cells confirming their safety for pharmaceutical applications. All the synthesized derivatives displayed better transdermal permeation enhancement capabilities as compared to their respective individual FAs. The results showed that there was no correlation between the number of aliphatic carbon chains and the enhancement ratio (ER). The mono oleate derivative (MOAPE (4II)) displayed the greatest ER for TNF (5.87) at 1% w/w. Histological investigations of the rat skin treated with MOAPE (4II) revealed fluidization of the stratum corneum. Histological and transepithelial electrical resistance (TEER) studies corroborated with the findings of the in vitro permeation experiments and revealed that there was no significant change in the viable epidermis of the skin after 1% MOAPE (4II) exposure. The TEER findings also suggested that the permeation enhancement effects of MOAPE (4II) were not permanent and the results indicated a return towards original skin integrity after removal of the enhancer formulation.
机译：使用化学渗透增强剂（CPE）加宽了可通过透皮途径递送的药物池。该研究探讨了含β-丙氨酸叔丁酯头部基团的新型单氨基，二脂肪酸（Fa）酯的合成和表征，作为使用Tenofovir（TNF）作为模型药物的透皮渗透增强剂。合成的化合物对哺乳动物细胞无毒，证实了它们对药物应用的安全性。与各自的单个FA相比，所有合成的衍生物都显示出更好的透皮渗透增强能力。结果表明，脂族碳链的数量与增强比（ER）之间没有相关性。单糖果实衍生物（MOAPE（4II））以1％w / w为1％的TNF（5.87）显示最大的ER。用MOAPE（4II）处理的大鼠皮肤的组织学调查显示Stratum Corneum的流化。组织学和Transepealelial电阻（Teer）研究用体外渗透实验的结果证实，并显示出在1％Moae（4II）暴露后皮肤的活表皮没有显着变化。彼得发现还表明MOAPE（4II）的渗透增强效应不是永久性的，结果表明除了去除增强剂制剂后朝向原始皮肤完整性的恢复。

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  • 来源
    《New Journal of Chemistry》 |2018年第3期|共11页
  • 作者

    Rambharose S.; Kalhapure R. S.; Jadhav M.; Govender T.;

  • 作者单位

    Univ KwaZulu Natal Dept Pharmaceut Sci Private Bag X54001 ZA-4000 Durban South Africa;

    Univ KwaZulu Natal Dept Pharmaceut Sci Private Bag X54001 ZA-4000 Durban South Africa;

    Univ KwaZulu Natal Dept Pharmaceut Sci Private Bag X54001 ZA-4000 Durban South Africa;

    Univ KwaZulu Natal Dept Pharmaceut Sci Private Bag X54001 ZA-4000 Durban South Africa;

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  • 正文语种 eng
  • 中图分类 化学;
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