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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
摘要

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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Sigma-Aldrich
硫代乙醇酸钠, ≥96.5% (iodometric)
Sigma-Aldrich
N-碘代琥珀酰亚胺, 95%
Sigma-Aldrich
乙胺丁醇 二盐酸盐, antimycobacterial
Sigma-Aldrich
山梨醇酐硬脂酸酯, meets FCC analytical specifications
Sigma-Aldrich
双十六烷基磷酸酯
乙胺丁醇 盐酸盐, European Pharmacopoeia (EP) Reference Standard
乙胺丁醇, European Pharmacopoeia (EP) Reference Standard