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Improved Biological Activity and Stability of enzyme L-Asparaginase in Solid Lipid Nanoparticles Formulation

机译:固体脂质纳米颗粒制剂中L-天冬酰胺酶的生物活性和稳定性的改善

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To protect the biological activity of an enzyme during the development of formulations is one of the biggest challenges. The tetrameric form of L-Asparaginase is used to treat Acute Lymphocytic Leukaemia. It possesses shorter in vivo half–life. Using a modified (water/oil)/water-emulsion method followed by solvent evaporation L-Asn was successfully encapsulated at the core of Solid Lipid Nanoparticles made of lipid glyceryl monostearate. This study elucidated that the preparation of L-Asn loaded SLN develop a colloidal formulation with enhanced activity. The in-vitro release pro?le of the enzyme revealed ?rst bursts has been increased. The study of the lyophilised formulation also shows that the enzyme holds its biological activity and retains its particle size distribution. Consequently, by using an apt combination of homogenisation speed, temperature and additives the storage and biological activity of L-Asn in SLN formulation can be improved.
机译:在制剂开发过程中保护酶的生物活性是最大的挑战之一。 L-天冬酰胺酶的四聚体形式用于治疗急性淋巴细胞白血病。它具有较短的体内半衰期。使用改进的(水/油)/水乳化方法,然后进行溶剂蒸发,L-Asn成功地封装在由单硬脂酸甘油酯制成的固体脂质纳米颗粒的核心。该研究阐明了负载L-Asn的SLN的制备开发了具有增强活性的胶体制剂。该酶的体外释放特性表明,首次爆发增加了。冻干制剂的研究还表明该酶保持其生物学活性并保留其粒度分布。因此,通过使用均质化速度,温度和添加剂的适当组合,可以改善SLN配方中L-Asn的储存和生物活性。

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