

Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies
Vaishali Yogesh Londhe (1,*)


(1) Department of Pharmaceutics, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’s NMIMS, Vile Parle West, Mumbai, Maharashtra 400056, India
(2) Department of Pharmaceutics, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM’s NMIMS, Vile Parle West, Mumbai, Maharashtra 400056, India
(*) Corresponding Author
Received: 22 Jul 2020 | Revised: 03 Sep 2020 | Accepted: 14 Sep 2020 | Published: 31 Dec 2020 | Issue Date: December 2020
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.
Announcements
One of our sponsors will cover the article processing fee for all submissions made between May 17, 2023 and June 16, 2023 (Voucher code: SPONSOR2023).
Editor-in-Chief
European Journal of Chemistry
Keywords
Full Text:
PDF

DOI: 10.5155/eurjchem.11.4.280-284.2010
Links for Article
| | | | | | |
| | | | | | |
| | | |
Related Articles
Article Metrics


References
[1]. Gribbon, P.; Andreas, S. Drug Discov. Today 2005, 1, 17-22.
https://doi.org/10.1016/S1359-6446(04)03275-1
[2]. Kim, C. K.; Park, J. S. Am. J. Drug Deliv. 2004, 2, 113-130.
https://doi.org/10.2165/00137696-200402020-00004
[3]. Leuner, C.; Dressman, J. Eur. J. Pharm. Biopharm. 2000, 50, 47-60.
https://doi.org/10.1016/S0939-6411(00)00076-X
[4]. Brewster, M. E.; Loftsson, T. Adva. Drug Deliv. Rev. 2007, 59, 645-666.
https://doi.org/10.1016/j.addr.2007.05.012
[5]. Loftsson, T.; Duchene, D. Inter. J. Pharm. 2007, 329, 1-11.
https://doi.org/10.1016/j.ijpharm.2006.10.044
[6]. Conceicao, J.; Adeoye, O.; Cabral-Marques, H. M.; Lobo, J. Curr. Pharm. Design 2018, 24, 1405-1433.
https://doi.org/10.2174/1381612824666171218125431
[7]. Sherje, A.; Londhe, V. Curr. Drug Discov. Tech. 2014, 11, 271-278.
https://doi.org/10.2174/1570163812666150109103618
[8]. Sigurdardottir, A. M.; Loftsson, T. Int. J. Pharm. 1995, 126, 73-78.
[9]. Danel, C.; Azaroual, N.; Chavaria, C.; Odou, V.; Martel, B.; Vaccher, C. Carbohydr. Polym. 2013, 92, 2282-2292.
https://doi.org/10.1016/j.carbpol.2012.11.095
[10]. Gaspar de Araujo, M. V. J. Mol. Struc. 2017, 1150, 146-154.
https://doi.org/10.17267/2317-3394rpds.v6i3.1596
[11]. Patel, P.; Agrawal, Y. K.; Sarvaiya, J. Int. J. Bio. Macromol. 2016, 84, 182-188.
https://doi.org/10.1016/j.ijbiomac.2015.11.075
[12]. Soliman, K. A.; Ibrahim, H. K.; Ghorab, M. M. Int. J. Pharm. 2016, 512, 168-177.
https://doi.org/10.1016/j.ijpharm.2016.08.044
[13]. Pokharkar, V.; Khanna, A.; Venkatpurwar, V.; Dhar, S.; Mandpe, L. Acta Pharm. 2009, 59, 121-132.
https://doi.org/10.2478/v10007-009-0001-3
[14]. Redenti, E.; Szente, L.; Szejtli, J. J. Pharm. Sci. 2000, 89, 1-8.
https://doi.org/10.1002/(SICI)1520-6017(200001)89:1<1::AID-JPS1>3.0.CO;2-W
[15]. Sherje, A. P.; Londhe, V. J. Pharm. Innov. 2015, 10, 324-334.
https://doi.org/10.1007/s12247-015-9229-2
[16]. Taupitz, T.; Dressman, J. B.; Buchanan, C. M.; Klein, S. Eur. J. Pharm. Biopharm. 2013, 83, 378-387.
https://doi.org/10.1016/j.ejpb.2012.11.003
[17]. Rakkaew, P.; Suksiriworapong, J.; Chantasart, D. Pharm. Dev. Technol. 2018, 23, 715-722.
https://doi.org/10.1080/10837450.2017.1344993
[18]. Germain, P.; Bilial, M.; De Brauner, C. Termochim. Acta 1995, 259, 187-198.
https://doi.org/10.1016/0040-6031(95)02260-9
[19]. Fenyvesi, E.; Vikmon, M.; Szema, J.; Redenti, E.; Del-canale, M.; Ventura, P.; Szejtli, J. J. Incl. Phenom. 1999, 33, 339-344.
https://doi.org/10.1023/A:1008094702632
[20]. Haque, N.; Prabhu, N. P. Biochem. Biophys. Res. Commun. 2018, 499, 907-912.
https://doi.org/10.1016/j.bbrc.2018.04.018
[21]. Li, X.; Yang, M.; Li, Y.; Gong, W.; Wang, Y.; Shan, L.; Shao, S.; Gao, C. Current Drug Deliv. 2017, 14, 1130-1143.
https://doi.org/10.2174/1567201813666161003151225
[22]. Daniel, D. G.; Zimbroff, D. L.; Potkin, S. G.; Reeves, K. R.; Harrigan, E. P.; Lakshmi Narayanan, M. Neuropsychopharmacology 1999, 20, 491-505.
https://doi.org/10.1016/S0893-133X(98)00090-6
[23]. Gauniya, A.; Mazumder, R.; Pathak, K. Int. J. Pharm. Pharm. Sci. 2015, 7, 146-150.
[24]. Thombre, A. G.; Shah, J. C.; Sagawa, K.; Caldwell, W. B. Int. J. Pharm. 2012, 428, 8-17.
https://doi.org/10.1016/j.ijpharm.2012.02.004
[25]. Mogal, P.; Derle, D. J. Drug Design Med. Chem. 2017, 3, 37-48.
https://doi.org/10.11648/j.jddmc.20170303.12
[26]. Kim, Y.; Oksanen, A. D.; Massefski, W.; Blake, F. J. Jr.; Duffy, M. E.; Chrunyk, B. J. Pharm. Sci. 1998, 87, 1560-1567.
https://doi.org/10.1021/js980109t
[27]. Thombre, A. G.; Herbig, S. M.; Alderman, J. A. Pharm. Res. 2011, 28, 3159-3170.
https://doi.org/10.1007/s11095-011-0505-7
[28]. Deshmukh, S. S.; Potnis, V. V.; Shelar, D. B.; Mahaparale, P. Indian Drugs 2007, 44, 677-682.
[29]. Miao, Y.; Chen, G.; Ren, L.; Pingkai, O. Drug Deliv. 2016, 23, 2163-2172.
https://doi.org/10.3109/10717544.2014.950768
[30]. Higuchi, T. K. A. C. Adv. Anal. Chem. Instrum. 1965, 4, 117-211.
[31]. Londhe, V. Y.; Deshmane, A. B.; Singh, S. R.; Kulkarni, Y. A. J. Mol. Struc. 2018, 1157, 395-400.
https://doi.org/10.1016/j.molstruc.2017.12.042
[32]. Dua, K.; Pubreja K.; Ramana, M. V.; Lather, V. J. Pharm. Bioallied Sci. 2011, 3(3), 417-425.
https://doi.org/10.4103/0975-7406.84457
[33]. National Library of Medicine, PubChem, Retrieved Mar 22, 2019, from https://pubchem. ncbi. nlm. nih. gov/compound/Ziprasidone
[34]. Londhe, V. Y.; Pawar A.; Kundaikar, H. J. Mol. Struc. 2020, 1220, 128615.
https://doi.org/10.1016/j.molstruc.2020.128615
How to cite
The other citation formats (EndNote | Reference Manager | ProCite | BibTeX | RefWorks) for this article can be found online at: How to cite item
DOI Link: https://doi.org/10.5155/eurjchem.11.4.280-284.2010

















European Journal of Chemistry 2020, 11(4), 280-284 | doi: https://doi.org/10.5155/eurjchem.11.4.280-284.2010 | Get rights and content
Refbacks
- There are currently no refbacks.
Copyright (c) 2020 Authors

This work is published and licensed by Atlanta Publishing House LLC, Atlanta, GA, USA. The full terms of this license are available at http://www.eurjchem.com/index.php/eurjchem/pages/view/terms and incorporate the Creative Commons Attribution-Non Commercial (CC BY NC) (International, v4.0) License (http://creativecommons.org/licenses/by-nc/4.0). By accessing the work, you hereby accept the Terms. This is an open access article distributed under the terms and conditions of the CC BY NC License, which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited without any further permission from Atlanta Publishing House LLC (European Journal of Chemistry). No use, distribution or reproduction is permitted which does not comply with these terms. Permissions for commercial use of this work beyond the scope of the License (http://www.eurjchem.com/index.php/eurjchem/pages/view/terms) are administered by Atlanta Publishing House LLC (European Journal of Chemistry).
© Copyright 2010 - 2023 • Atlanta Publishing House LLC • All Right Reserved.
The opinions expressed in all articles published in European Journal of Chemistry are those of the specific author(s), and do not necessarily reflect the views of Atlanta Publishing House LLC, or European Journal of Chemistry, or any of its employees.
Copyright 2010-2023 Atlanta Publishing House LLC. All rights reserved. This site is owned and operated by Atlanta Publishing House LLC whose registered office is 2850 Smith Ridge Trce Peachtree Cor GA 30071-2636, USA. Registered in USA.