Abstract
An inclusion complex formation with cyclodextrin (CD) is a promising method for enhancing solubility and bioavailability of medicines. Ataluren (ALN) is a reading-through drug for overriding premature stop codons that is practically insoluble in water. By incresing the solubility of this molecule in aqueous media, its bioavailability in its oral dosage form may be improved. Inclusion complexes of ALN with alpha (αCD), beta (βCD), gamma (γCD), hydroxypropyl beta (HPβCD), randomly methylated beta (RMβCD) and sulfobutyl ether beta (SBECD) cyclodextrins were prepared. Phase solubility studies, Job's plot, Proton nuclear magnetic resonance (1HNMR), Differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and Fourier transform Infrared (FTIR) analysis were used for the characterization of the inclusion complexes. The phase solubility profiles are AL type but each cyclodextrin behaves differently in interaction with ALN. The Job's plot revealed 1:1 stoichiometry in ALNCD complexes. The stability constants of ALN with αCD, βCD, γCD, HPβCD, RMβCD, and SBECD were 35 M − 1, 674 M − 1, 163 M − 1, 132 M − 1, 324 M − 1, and 232 M − 1 respectively. All CDs increased ALN solubility in aqueous media and RMβCD showed the maximun value of 121.0 times increment of ALN solubility in aqueous media.
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