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Biosynthesis of a Flavonol from a Flavanone by Establishing a One-pot Bienzymatic Cascade
Published on: August 14, 2019
Complexation with beta-cyclodextrin confers oral activity on the flavonoid dioclein
Bruno A Rezende1, Steyner F Cortes, Frederico B De Sousa
1Departamento de Fisiologia e Biofísica, ICB, Universidade Federal de Minas Gerais, Av Antônio Carlos 6627, 31270-901 Belo Horizonte, MG, Brazil.
International Journal of Pharmaceutics
|October 29, 2008
Summary
This study created a new complex of dioclein and beta-cyclodextrin (beta-CD) to improve its cardiovascular benefits. The complex enhanced dioclein's oral activity and bioavailability, enabling effective hypotensive effects after oral administration.
Area of Science:
- Cardiovascular Pharmacology
- Drug Delivery Systems
- Natural Product Chemistry
Background:
- Dioclein, a flavonoid, exhibits cardiovascular benefits like vasorelaxant and hypotensive activities.
- Pharmaceutical application of dioclein is hindered by poor oral bioavailability and low water solubility.
Purpose of the Study:
- To enhance the oral activity and bioavailability of dioclein.
- To develop a 1:1 inclusion complex (IC) of dioclein with beta-cyclodextrin (beta-CD).
Main Methods:
- Formation and characterization of the dioclein-beta-CD inclusion complex using spectroscopy (NMR, IR).
- Evaluation of the complex's hypotensive and vasodilator effects in mice.
- Comparison of oral and intraperitoneal administration of free dioclein versus the inclusion complex.
Main Results:
- The inclusion complex significantly increased dioclein's water solubility by 44%.
- Oral administration of the inclusion complex induced a pronounced hypotensive effect, unlike free dioclein.
- The inclusion complex demonstrated a higher and more sustained hypotensive effect compared to free dioclein after intraperitoneal administration.
Conclusions:
- The novel dioclein-beta-CD inclusion complex effectively improves dioclein's oral bioavailability and hypotensive efficacy.
- Beta-cyclodextrin likely protects dioclein from in vivo degradation, enhancing its therapeutic potential.
- This formulation strategy enables dioclein to be orally administered for cardiovascular applications.
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