European Journal of Chemistry

Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies

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Published: Dec 31, 2020
DOI: https://doi.org/10.5155/eurjchem.11.4.280-284.2010
Keywords:
Ziprasidone, β-Cyclodextrin, IR spectroscopy, X-ray diffraction, Ternary complexes, Solubility enhancement
Section
Research Article
Issue
Vol. 11 No. 4 (2020): December 2020
Dates
Received 2020-07-22
Accepted 2020-09-14
Published 2020-12-31
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Main Article Content

Vaishali Yogesh Londhe
Department of Pharmaceutics, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’s NMIMS, Vile Parle West, Mumbai, Maharashtra 400056, India
http://orcid.org/0000-0003-3718-9858
Sreevidya Ramesh Krishnan
Department of Pharmaceutics, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’s NMIMS, Vile Parle West, Mumbai, Maharashtra 400056, India
http://orcid.org/0000-0003-3523-6251

Abstract

Ziprasidone (ZPR) is an antipsychotic agent having less solubility. It is used for the treatment of schizophrenia. Complexation of hydrophobic drugs with cyclodextrins leads to enhanced solubility and dissolution. In this study, inclusion complexes were prepared by different methods, using ZPR, β-cyclodextrin (β-CD), and different auxiliary agents like hydrophilic polymer and hydroxy acid (1:1:0.5) to improve the aqueous solubility. The characterization of the ternary complexes was carried out using solubility study, Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier transformation infrared spectroscopy (FT-IR) and in vitro dissolution studies. DSC, XRD, and FT-IR studies showed interaction in drug, cyclodextrin, and auxiliary agents which are confirmed by enhancement of solubility and dissolution. Spray-dried dispersion showed less crystallinity and higher solubility as compared to the kneading method for both citric acid and Lutrol® F-68. Thus, the investigation concludes that the presence of the auxiliary agent has a synergistic action on complexation with cyclodextrin, which helps to modify the physicochemical properties of the drug.


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Londhe, V. Y.; Krishnan, S. R. Effect of Inclusion of Citric Acid and Lutrol® F-68 on Ziprasidone and β-Cyclodextrin Complexation: Characterization, Solubility and Dissolution Studies. Eur. J. Chem. 2020, 11, 280-284.

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