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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Interaction between nitroheterocyclic compounds with beta-cyclodextrins: phase solubility and HPLC studies.
Nathalie F S de Melo1, Renato Grillo, André Henrique Rosa
1Departamento de Engenharia Ambiental, Universidade Estadual Paulista Júlio de Mesquita Filho, Campus Sorocaba, Av. Três de Março 511, CEP 18087-180, Sorocaba, São Paulo, Brazil.
This study investigated cyclodextrin complexation of nitrofurazone (NF) and NFOH to improve Chagas disease treatments. Complexation enhances drug characterization, aiding the development of effective therapeutic options against Trypanosoma cruzi.
Area of Science:
- Pharmaceutical Sciences
- Medicinal Chemistry
- Analytical Chemistry
Background:
- Chagas disease, caused by Trypanosoma cruzi, poses a significant health burden in Latin America.
- Nitrofurazone (NF) and its analog NFOH show activity against T. cruzi, but formulation challenges may limit therapeutic efficacy.
Purpose of the Study:
- To investigate the complexation of NF and NFOH with beta-cyclodextrin (beta-CD) and dimethyl-beta-cyclodextrin (DM-beta-CD).
- To characterize the impact of complexation on the UV absorption and chromatographic behavior of NF and NFOH.
- To determine the stability constants of the formed complexes for potential pharmaceutical applications.
Main Methods:
- High-Performance Liquid Chromatography (HPLC) with a reversed-phase C18 column.
- Mobile phase consisting of acetonitrile-water with beta-CD or DM-beta-CD additives.
- Phase-solubility studies using the Higuchi and Connors method.
Main Results:
- Complexation with beta-CD and DM-beta-CD altered the UV absorption and significantly decreased the retention times of NF and NFOH.
- HPLC analysis allowed for the determination of complex stability constants.
- Phase-solubility studies indicated a 1:1 stoichiometry for NF/NFOH-cyclodextrin complexes.
Conclusions:
- Cyclodextrin complexation offers a viable strategy for characterizing and potentially formulating NF and NFOH.
- Understanding these complexation dynamics is crucial for developing improved therapeutic agents for Chagas disease.
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