Inclusion Properties Of Cyclodextrin And Calixarene And Their Pharmaceutical Application

Chapter 1: The recent development of cyclodextrins and calixarenes has been reviewed, especially its development in drug delivery system. At the same time, the application of the cyclodextrins and calixarenes on carotenoids was expatiated.Chapter 2: The interaction of Piroxicam with sulfobutylether-β-cyclodextrin (SBE-β-CD) was compared with that of hydroxypropyl-β-cyclodextrin (HP-β-CD). The stability constants of the inclusion complexes were obtained by steady-state fluorescence technique. Experimental conditions including concentrations of the two cyclodextrins and media acidity were investigated for the inclusion formation in detail. The results suggested that the interaction of Piroxicam with charged CD (SBE-β-CD) is much stronger than that with neutral CD (HP-β-CD) at any pH studied, in terms of a synergetic effect of hydrophobic and electrostatic interactions.Chapter 3: Water-soluble inclusion compounds of β-cyclodextrin with β-carotene were prepared by two methods: (1) complexation in solution and (2) complexation by kneading. It was found that UV-Vis absorption spectra of the inclusion compounds in water were different from those of β-carotene in water-miscible organic solvents (DMF) and β-cyclodextrin in water, which confirmed the formation of the inclusion compounds. Specific interaction of β-carotene and β-cyclodextrin caused great changes in absorbance maximum of β-carotene. It is considered that in water the hydrophobic moiety (β-carotene) of such inclusion complexes should tend to self-associate forming large supramolecular aggregates.Chapter 4: Inclusion compounds of β-carotene with CDs including β-CD, HP-β-CD and SBE-β-CD had been prepared by using improved method andcharacterized via UV-Vis absorption spectroscopy, IR spectra and 'H NMR technique. The solubilization and stabilization of inclusion compounds were investigated in detail. Experimental results on the stability cyclodextrins complexed P-carotene against light, heat and oxygen proved the benefits. The water solubility of the inclusion compounds was improved. SBE-P-CD was found to be the most potent solubilizing agent for P-carotene.Chapter 5: The formation of the inclusion complex of p-carotene with the calix[4]arene was studied by fluorescence spectroscopy. The related mechanism was discussed by means of "H NMR method. The fluorescence intensities of the calix[4]arene was gradually decreased with increasing of the concentration of P-carotene. The formation constant of complex was obtained by using Stern-Volmer equation. A new selective and sensitive method for the spectrofluorimetric determination of P-carotene was developed. This method is based on the quenching of fluorescence of calix[4]arene due to the formation of calix[4]arene-P-carotene complex.