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研究生物活性药物与 α-和 β-环糊精主体-客体包合物的生存能力,以进行安全监管释放。

Study to Probe Subsistence of Host-Guest Inclusion Complexes of α and β-Cyclodextrins with Biologically Potent Drugs for Safety Regulatory Dischargement.

机构信息

Department of Chemistry, University of North Bengal, Darjeeling, 734013, India.

Department of Microbiology, University of North Bengal, Darjeeling, 734013, India.

出版信息

Sci Rep. 2018 Aug 29;8(1):13031. doi: 10.1038/s41598-018-31373-x.

Abstract

Host-guest interaction of two significant drugs, phenylephrine hydrochloride and synephrine with α and β-cyclodextrins were studied systematically. Initially two simple but reliable physicochemical techniques namely conductance and surface tension were employed to find out saturation concentration for the inclusion and its stoichiometry. The obtained 1:1 stoichiometry was further confirmed by two spectrometric methods, UV-Vis study and spectrofluorimetry. Significant shifts in IR stretching frequency also support the inclusion process. Relative stabilities of the inclusion complexes were established by the association constants obtained from UV-Vis spectroscopic measurements, program based mathematical calculation of conductivity data. Calculations of the thermodynamic parameters dictates thermodynamic feasibility of the inclusion process. Spectrofluorometric measurement scaffolds the UV-Vis spectroscopic measurement validating stability of the ICs once again. Mass spectroscopic measurement gives the molecular ion peaks corresponding to the inclusion complex of 1:1 molar ratio of host and guest molecules. The mechanism of inclusion was drawn by H-NMR and 2D ROESY spectroscopic analysis. Surface texture of the inclusion complexes was studied by SEM. Finally, the cytotoxic activities of the inclusion complexes were analyzed and found, Cell viability also balances for non-toxic behavior of the ICs. Moreover, all the studies reveal the formation of inclusion complexes of two ephedra free, alternatively emerging drugs (after their banned product having ephedra) SNP, PEH with α and β-CD which enriches the drug delivery system with their regulatory release without any chemical modification.

摘要

系统研究了两种重要药物盐酸苯福林和辛弗林与α和β-环糊精的主体-客体相互作用。最初,使用了两种简单但可靠的物理化学技术,即电导率和表面张力,以确定包合的饱和浓度及其化学计量比。通过两种光谱方法,紫外可见光谱研究和荧光光谱法进一步证实了 1:1 的化学计量比。IR 伸缩频率的显著位移也支持包合过程。通过从紫外可见光谱测量获得的结合常数、基于程序的电导率数据的数学计算来确定配合物的相对稳定性。热力学参数的计算表明包合过程的热力学可行性。荧光光谱测量通过光谱荧光测量再次验证了 ICs 的稳定性,该测量验证了 UV-Vis 光谱测量的稳定性。质谱测量给出了与主体和客体分子摩尔比为 1:1 的包合配合物的分子离子峰。通过 H-NMR 和二维 ROESY 光谱分析得出包合的机制。通过 SEM 研究了包合物的表面纹理。最后,分析并发现了包合物的细胞毒性活性,细胞活力也平衡了 ICs 的非毒性行为。此外,所有研究都表明,在含有麻黄素的产品被禁用后,两种替代出现的药物(无麻黄素)SNP 和 PEH 与α和β-CD 形成包合物,通过其监管释放丰富了药物传递系统,而无需进行任何化学修饰。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/98d1/6115366/832fec39f91d/41598_2018_31373_Fig1_HTML.jpg

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