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A pre-formulation strategy for the liposome encapsulation of new thioctic acid conjugates for enhanced chemical stability and use as an efficient drug carrier for MPO-mediated atherosclerotic CVD treatment
New Journal of Chemistry ( IF 2.7 ) Pub Date : 2020/01/13 , DOI: 10.1039/c9nj05258e Premkumar Jayaraj 1, 2, 3, 4, 5 , Gopal Venkatesh Shavi 6, 7, 8 , Ananda Kumar Srinivasan 1, 5, 9, 10, 11 , Ramesh Raghavendra 6, 7, 8 , Akella Sivaramakrishna 1, 2, 3, 4, 5 , Rajagopal Desikan 1, 2, 3, 4, 5
New Journal of Chemistry ( IF 2.7 ) Pub Date : 2020/01/13 , DOI: 10.1039/c9nj05258e Premkumar Jayaraj 1, 2, 3, 4, 5 , Gopal Venkatesh Shavi 6, 7, 8 , Ananda Kumar Srinivasan 1, 5, 9, 10, 11 , Ramesh Raghavendra 6, 7, 8 , Akella Sivaramakrishna 1, 2, 3, 4, 5 , Rajagopal Desikan 1, 2, 3, 4, 5
Affiliation
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Lipoyl-apocynin and lipoyl-sesamol are bio-active conjugates of thioctic acid (also known as alpha-lipoic acid), synthesized using a benign chemical approach via the combination of thioctic acid and the powerful bio-phytonutrients, apocynin and sesamol, respectively. Encapsulation was performed for chemically modified thioctic acid conjugates within a liposome structure as a possible drug carrier for targeted site delivery without chemical degradation, which could be useful in myeloperoxidase (MPO) mediated atherosclerotic cardiovascular disease (CVD) treatment. A facile processing route for the thioctic acid conjugates with the complete chemical characterization and bio-encapsulation of these chemical entities in a liposome sphere was developed, and analysis to establish the encapsulation efficiency, zeta potential, vesicle size, surface morphology, and long-term sustained stability was performed. The liposome conjugates were also characterized via critical in vitro experiments. The encapsulation efficiency of the thioctic acid conjugates was found to be almost 70%. In addition, the vesicle size and zeta potential were also measured for the formulated thioctic acid conjugates. The chromatographic evaluation of the encapsulated conjugates revealed that the liposomes seem to protect the thioctic acid conjugates when incubated in simulated body fluid, preventing ester hydrolysis, thereby offering chemical stability to the thioctic acid conjugates. The liposome loaded conjugates were also determined to be potent agents for MPO mediated atherosclerotic CVD in relevant preclinical in vitro tests. This is the first report of a highly efficient and sustainable chemical method for the liposomal encapsulation of thioctic acid conjugates of apocynin and sesamol that has been substantiated using relevant in vitro assays, and it could be useful for MPO-mediated atherosclerotic CVD treatment.
中文翻译：
新型硫辛酸缀合物脂质体封装的预配制策略，可增强化学稳定性，并用作MPO介导的动脉粥样硬化CVD治疗的有效药物载体
脂酰芹菜素和硫辛酸是硫辛酸（也称为α-硫辛酸）的生物活性共轭物，使用良性化学方法通过硫辛酸和强大的生物植物营养素，阿朴西宁和芝麻酚的组合。脂质体结构内的化学修饰硫辛酸共轭物的包封是可能的药物载体，可在不发生化学降解的情况下进行靶向部位递送，这可用于髓过氧化物酶（MPO）介导的动脉粥样硬化性心血管疾病（CVD）治疗。建立了硫辛酸缀合物的简便加工路线，这些脂质在球形体中具有完整的化学特征和这些化学实体的生物封装，并进行了分析以建立封装效率，ζ电位，囊泡大小，表面形态和长期稳定性保持稳定。脂质体结合物也通过关键特征体外实验。发现硫辛酸缀合物的包封效率几乎为70％。另外，还测量了配制的硫辛酸缀合物的囊泡大小和ζ电位。包囊的缀合物的色谱评估表明，脂质体在模拟体液中孵育时似乎可以保护硫辛酸缀合物，防止酯水解，从而为硫辛酸缀合物提供化学稳定性。在相关的临床前体外，脂质体负载的偶联物也被确定为MPO介导的动脉粥样硬化CVD的有效药物测试。这是高效，可持续的化学方法，用于脂质体封装载脂蛋白A和西沙酚的硫辛酸共轭物的方法，该方法已通过相关的体外测定得到证实，它可用于MPO介导的动脉粥样硬化CVD治疗。
更新日期：2020-02-17
中文翻译：
新型硫辛酸缀合物脂质体封装的预配制策略，可增强化学稳定性，并用作MPO介导的动脉粥样硬化CVD治疗的有效药物载体
脂酰芹菜素和硫辛酸是硫辛酸（也称为α-硫辛酸）的生物活性共轭物，使用良性化学方法通过硫辛酸和强大的生物植物营养素，阿朴西宁和芝麻酚的组合。脂质体结构内的化学修饰硫辛酸共轭物的包封是可能的药物载体，可在不发生化学降解的情况下进行靶向部位递送，这可用于髓过氧化物酶（MPO）介导的动脉粥样硬化性心血管疾病（CVD）治疗。建立了硫辛酸缀合物的简便加工路线，这些脂质在球形体中具有完整的化学特征和这些化学实体的生物封装，并进行了分析以建立封装效率，ζ电位，囊泡大小，表面形态和长期稳定性保持稳定。脂质体结合物也通过关键特征体外实验。发现硫辛酸缀合物的包封效率几乎为70％。另外，还测量了配制的硫辛酸缀合物的囊泡大小和ζ电位。包囊的缀合物的色谱评估表明，脂质体在模拟体液中孵育时似乎可以保护硫辛酸缀合物，防止酯水解，从而为硫辛酸缀合物提供化学稳定性。在相关的临床前体外，脂质体负载的偶联物也被确定为MPO介导的动脉粥样硬化CVD的有效药物测试。这是高效，可持续的化学方法，用于脂质体封装载脂蛋白A和西沙酚的硫辛酸共轭物的方法，该方法已通过相关的体外测定得到证实，它可用于MPO介导的动脉粥样硬化CVD治疗。
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