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Merck
  • Niosomal encapsulation of ethambutol hydrochloride for increasing its efficacy and safety.

Niosomal encapsulation of ethambutol hydrochloride for increasing its efficacy and safety.

Drug delivery (2013-12-24)
Mohammed Shafik El-Ridy, Soad Aly Yehia, Mahfouz Abd-El-Megeid Kassem, Dina Mahmoud Mostafa, Essam Amin Nasr, Marwa Hasanin Asfour
要旨

Tuberculosis (TB) is a worldwide health concern. In 2011, about 8.7 million new cases developed TB and 1.4 million people died from it. Enhancement of ethambutol hydrochloride activity and safety in treatment of TB through niosomal encapsulation. Niosomes were prepared by the thin-film hydration method. They were characterized, investigated for in vitro release, lung disposition and in vivo biological evaluation. Entrapment efficiency of ethambutol hydrochloride ranged from 12.20% to 25.81%. Zeta potential values inferred stability of neutral and negatively charged formulations. In vitro release was biphasic. Lung targeting was increased by niosomal encapsulation. Biological evaluation revealed superiority of niosomal ethambutol hydrochloride over the free drug. Neutral and negatively charged niosomal vesicles are dispersed homogenously unlike positively charged vesicles. Niosomal encapsulation results in controlled drug release. Niosomal formulations targeted more drugs to mice lungs for a prolonged period of time resulting in: decreased root-specific lung weight, bacterial counts in lung homogenates and optimizing pathological effect on guinea pigs lungs, livers and spleens. Encapsulation of ethambutol hydrochloride in niosomal formulations for the treatment of TB provides higher efficacy and safety compared with the free drug.

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製品番号
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製品内容

Sigma-Aldrich
チオグリコール酸ナトリウム, ≥96.5% (iodometric)
Sigma-Aldrich
N-ヨードスクシンイミド, 95%
Sigma-Aldrich
エタンブトール 二塩酸塩, antimycobacterial
Sigma-Aldrich
ソルビタンモノステアラート, meets FCC analytical specifications
Sigma-Aldrich
ジヘキサデシルリン酸
エタンブトール 二塩酸塩, European Pharmacopoeia (EP) Reference Standard
システム適合性用エタンブトール, European Pharmacopoeia (EP) Reference Standard