Descriptive Study: In silico and Physicochemical Assessment of the Effectiveness of Hydroxy / Amino Acids as Auxiliary Substances to Improve the Complexation Efficiency of β-cyclodextrin towards Bosentan

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Descriptive Study: In silico and Physicochemical Assessment of the Effectiveness of Hydroxy / Amino Acids as Auxiliary Substances to Improve the Complexation Efficiency of β-cyclodextrin towards Bosentan

December 30, 2020 Chemical Science 0

To improve its physicochemical performance, the effectiveness of certain hydroxy and amino acids as an auxiliary substance in improving the complexation efficiency (CE) of β -cyclodextrin ( β CD) against Bosentan (BOS), a poorly soluble endothelin receptor antagonist, has been evaluated. A better choice of L-Arginine (ARG) as an auxiliary substance to enhance CE and interaction constant (Ks) of β CD was demonstrated by phase solubility studies conducted in distilled water. As additional proof, the stability, potential interactions and geometry of BOS inside the CD cavity were predicted in silico calculations, optimising ARG as an auxiliary substance again. The solution state thermodynamic investigations subsequently revealed an entropy-driven mechanism of complexation. FTIR, DSC, XRPD and SEM were used to classify the lyophilized complexes. Thermodynamic research has shown that the process of inclusion is entropy-driven and random. Prepared lyophilized complexes provided a smooth, transparent water solution suggesting the complexes achieved by the inclusion phenomenon with lower sized particles of the drug. The inclusion phenomenon arising from the protein binding analysis was responsible for keeping the unbound drug in plasma, resulting in dose and dose frequency minimization. In the overall evaluation, the efficiency of the ternary complex was found to be appreciated, suggesting better efficacy of ARG as an auxiliary substance in improving the CE of CD towards BOS.

Author(s) Details

Yogesh V. Pore
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, 415 124, India.

Priyanka H. Jadhav
Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, 415 124, India.

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