Kinetic Optimization of Folic Acid Polymer Conjugates for Drug Targeting

Abstract

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-Ppropylenediamine (PDA) for solubility behavior and reactivity for FA site anchoring. Also the use of an ester 2-(1H-benzotrial-1-yl)-1,1,3,3-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 (H¹NMR) spectra analysis. Results and Conclusion: The H¹NMR 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.