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首页> 外文期刊>American journal of applied sciences >Kinetic Optimization of Folic Acid Polymer Conjugates for Drug Targeting
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Kinetic Optimization of Folic Acid Polymer Conjugates for Drug Targeting

机译：叶酸聚合物结合物的动力学优化

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Problem statement: Folic Acid (FA) is an essential, bioavailable water soluble B-complex vitamin that helps in the replication of normal cells. It is obtained from natural sources and it deficiency can leads to oncogenic cells development. Within this frame work in mind, we designed and synthesized a new bioconjugate carrier that can enhance the effectiveness of FA. Approach: The polymeric carrier: Polysucscinimide (PSI) was synthesized via the polycondensation of aspartic acid by attaching 3-(N,N-Dimethylamino) Propylamine (DMP) and 1,3-P-propylenediamine (PDA) for solubility behavior and reactivity for FA site anchoring. Also the use of an ester 2-(lH-benzotrial-l-yl)-l,l,3,3-tetramethylurium Hexafluorophosphate (HBTU) as coupling agent to FA. The bioreversible binding of the water-soluble and biocompatible macromolecular were attested through kinetic studies. The kinetic reactions were investigated through the nuclear resonance (H'NMR) spectra analysis. Results and Conclusion: The H'NMR optimization reaction times were found within the range of 120-130 min (80-85%) as optimum coupling. The yield of the FA occurred within the same time range but with maximum incorporation between 90-100%. The growth of FA incorporation in terms of reaction time resulted to an increase inherent viscosity relative to the decrease of water solubility of the conjugate obtained.
机译：问题陈述：叶酸（FA）是必不可少的，可生物利用的水溶性B-复合维生素，有助于正常细胞的复制。它是从天然来源获得的，缺乏会导致致癌细胞发育。在此框架内，我们设计并合成了一种新型生物共轭载体，可以增强FA的有效性。方法：聚合载体：通过将3-（N，N-二甲基氨基）丙胺（DMP）和1,3-P-丙二胺（PDA）附着于天门冬氨酸的缩聚反应而合成聚蔗糖酰亚胺（PSI），以实现溶解性和FA站点锚定。还使用酯2-（1H-苯并三唑-1-基）-1,1,3,3-四甲基六氟磷酸铀（HBTU）作为FA的偶联剂。通过动力学研究证明了水溶性和生物相容性大分子的生物可逆结合。通过核共振（H'NMR）光谱分析研究了动力学反应。结果与结论：H'NMR优化反应时间为120-130分钟（80-85％），为最佳偶联。 FA的产率在相同的时间范围内发生，但最大掺入量在90-100％之间。相对于所获得的缀合物的水溶性降低，以反应时间计的FA掺入的增加导致固有粘度增加。

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