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Nanoencapsulation of Antitubercular Drug Isoniazid and Its Lipopeptide Conjugate

机译:抗结核药异烟肼及其脂肽结合物的纳米囊封

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Isoniazid (INH) is a first line drug for treatment of the widespread deadly disease caused by Mycobacterium tuberculosis. Peptide conjugate of INH was designed and synthesised for targeted and receptor mediated cellular uptake of INH. Chemical composition, hydrophobicity (n-octanol/water partition coefficient), and membrane affinity (using a Langmuir lipid monolayer as a model system) of the conjugate were characterised. Hydrophilicity of the drug was remarkably decreased by the conjugation which resulted in improved interaction with lipid layer and allowed its efficient encapsulation into polylactic/glycolic acid nanoparticles enhancing the bioavailability of the drug.View full textDownload full textKeywordsAntituberculotic drug conjugate, drug encapsulation, membrane affinity, nanoprecipitation, PLGA nanoparticlesRelated var addthis_config = { ui_cobrand: "Taylor & Francis Online", services_compact: "citeulike,netvibes,twitter,technorati,delicious,linkedin,facebook,stumbleupon,digg,google,more", pubid: "ra-4dff56cd6bb1830b" }; Add to shortlist Link Permalink http://dx.doi.org/10.1080/01932691.2011.616128
机译:异烟肼(INH)是一线药物,用于治疗由结核分枝杆菌引起的广泛的致命疾病。设计并合成了INH的肽缀合物,用于靶向和受体介导的INH细胞摄取。表征了缀合物的化学组成,疏水性(正辛醇/水分配系数)和膜亲和力(使用Langmuir脂质单层作为模型系统)。药物的结合显着降低了其亲水性,从而改善了与脂质层的相互作用并使其有效地包封在聚乳酸/乙醇酸纳米颗粒中,从而增强了药物的生物利用度。查看全文下载全文关键词抗结核药物偶联物,药物包封,膜亲和力,纳米沉淀法,PLGA纳米粒子相关变量,add var addthis_config = {ui_cobrand:“泰勒和弗朗西斯在线”,servicescompact:“ citeulike,netvibes,twitter,technorati,delicious,linkedin,facebook,stumbleupon,digg,google,更多”,发布:“ ra-4dff56cd6bb1830b” };添加到候选列表链接永久链接http://dx.doi.org/10.1080/01932691.2011.616128

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