Inclusion Complexes of New Ibuprofen Thiazolidin-4-Ones with β-Cyclodextrin †
by
,
Ioana Vasincu
1,*, 
Anca Roxana Petrovici
2
,
Maria Apotrosoaei
1,
Florentina Lupașcu
1,
Narcisa Marangoci
2,
Mariana Pinteală
2 and
Lenuța Profire
1 1
Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy of Iasi, 16 Universitatii Street, 700,115 Iasi, Romania
2
“Petru Poni” Institute of Macromolecular Chemistry, 41A Grigore Ghica Voda Alley, 700,487 Iasi, Romania
*
Author to whom correspondence should be addressed.
†
Presented at the 1st International Electronic Conference on Pharmaceutics , 1–15 December 2020;
Available online: https://iecp2020.sciforum.net/.
Proceedings 2021, 78(1), 2; https://doi.org/10.3390/IECP2020-08785
Published: 1 December 2020
(This article belongs to the Proceedings of The 1st International Electronic Conference on Pharmaceutics)
Abstract
:(1) Background: Cyclodextrins are used in various areas due to their ability to form inclusion complexes and to modify some properties of the guest molecule. The characteristics that can be improved are related to the solubility of poorly water-soluble drugs, the stabilization of labile guests against the degradative effects of the environment (oxidation, light and heat), bioavailability, decreasing side effects, taste modification or odour elimination and controlling of drug release. Additionally, ibuprofen is a widely used nonsteroidal anti-inflammatory drug in treating pain and inflammation, but the long-term use of this drug has been associated with gastrointestinal side effects and nephrotoxicity. This led to the introduction of new compounds of ibuprofen with an improved profile. Aim. The research project combines two actual topics in the pharmaceutical area: developing new safer drugs and improving the pharmacokinetic and pharmacotoxicological profile through complexation with cyclodextrins. The main objective was to develop drug delivery systems based on cyclodextrins and new ibuprofen thiazolidin-4-ones as potential analgesic and anti-inflammatory drugs. (2) Methods: Thiazolidin-4-one derivatives of ibuprofen were included in β-cyclodextrin complexes by co-precipitation (1:1M) and lyophilization methods. The inclusion complexes were characterized using spectral methods such as infrared analysis (FTIR), NMR spectroscopy and phase solubility studies. The surface morphology was studied using scanning electron microscopy (SEM). (3) Results and Conclusions: Four inclusion complexes with β-cyclodextrin and new ibuprofen derivatives with a thiazolidin-4-one structure were obtained and characterized. These can confirm the theoretical premises for an improved pharmacological and safety toxicological profile and can continue with future studies (in vivo biological evaluation of pharmacokinetic, analgesic and anti-inflammatory profile).
Author Contributions
Conceptualization, I.V. and N.M.; methodology, I.V., A.R.P. and F.L.; validation, L.P. and M.P.; investigation, I.V., M.A. and F.L.; resources, L.P., M.P., N.M.; data curation, I.V. and A.R.P.; writing—original draft preparation, I.V. and A.R.P.; writing—review and editing, I.V. and A.R.P.; visualization, I.V.; supervision, L.P. and M.P.; funding acquisition, L.P., I.V., N.M. and M.P. All authors have read and agreed to the published version of the manuscript.
Funding
This research was funded by University of Medicine and Pharmacy “Grigore T. Popa” Iasi, based on contracts no. 30341/28.12.2017, by AUF-IFA 2019–2020, contract no. 28/2019, and by a grant of the Romanian Ministry of Research and Innovation, CCCDI–UEFISCDI, project number PN-III-P1-1.2-PCCDI-2017-0697/13PCCDI/2018, within PNCDI III.
Institutional Review Board Statement
Not applicable.
Informed Consent Statement
Not applicable.
Conflicts of Interest
The authors declare no conflict of interest. The founding sponsors had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. |
© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
Share and Cite
MDPI and ACS Style
Vasincu, I.; Petrovici, A.R.; Apotrosoaei, M.; Lupașcu, F.; Marangoci, N.; Pinteală, M.; Profire, L. Inclusion Complexes of New Ibuprofen Thiazolidin-4-Ones with β-Cyclodextrin. Proceedings 2021, 78, 2. https://doi.org/10.3390/IECP2020-08785
AMA Style
Vasincu I, Petrovici AR, Apotrosoaei M, Lupașcu F, Marangoci N, Pinteală M, Profire L. Inclusion Complexes of New Ibuprofen Thiazolidin-4-Ones with β-Cyclodextrin. Proceedings. 2021; 78(1):2. https://doi.org/10.3390/IECP2020-08785
Chicago/Turabian StyleVasincu, Ioana, Anca Roxana Petrovici, Maria Apotrosoaei, Florentina Lupașcu, Narcisa Marangoci, Mariana Pinteală, and Lenuța Profire. 2021. "Inclusion Complexes of New Ibuprofen Thiazolidin-4-Ones with β-Cyclodextrin" Proceedings 78, no. 1: 2. https://doi.org/10.3390/IECP2020-08785
