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 1H-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.
Highlights
In supramolecular chemistry of cyclodextrins various guest molecules having hydrophobic part, influenced by non-covalent interaction, can be inserted into the hydrophobic cavity of cyclodextrin molecules
It is imperative to find out the suitability of Phenylephrine hydrochloride (PEH) as the same done by the Phenylpropanolamine, pseudoephedrine and ephedrine for the treatment of nasal or sinus congestion and to find out the way of delivery with biocompatibility
The suggestion obtained from surface tension and conductometric study for the formation of 1:1 host-guest inclusion complexes of SNP and PEH with α and β-cyclodextrins are established by UV-Vis spectroscopy, spectrofluorimetry, 2D rotating-frame NOE spectroscopy (ROESY) NMR spectrometry and Scanning Electron Microscope (SEM) technique by analyzing surface texture of the solid inclusion complexes
Summary
In supramolecular chemistry of cyclodextrins various guest molecules having hydrophobic part, influenced by non-covalent interaction, can be inserted into the hydrophobic cavity of cyclodextrin molecules. Structural characterization of Host-Guest inclusion complexes of α-CD and β-CD with two bio-active molecules, PEH and SNP were done over here in terms of geometry and structural preferences by means of a variety of physical and spectroscopic methods in solid state and solution phase. Phenylpropanolamine, pseudoephedrine and ephedrine are used as nasal decongestant as the substitute of PEH8,9. Cyclodextrins, mostly α-cyclodextrin, are found to form complexes with the dietary fat which are stable enough to undergo enzymatic hydrolysis by lipase. This restrains accumulation of fat in human body[21,22]. Inclusion complex of SNP and cyclodextrins can be of a great deal for the weight loss/weight management dietary food supplement for sportsman or obese person[23]
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