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Complexation of the interferon inducer, bropirimine, with hydroxypropyl-beta-cyclodextrin.
M Echezarreta-López1, J J Torres-Labandeira, L Castiñeiras-Seijo
1Departamento de Farmacia e Tecnoloxía Farmacéutica, Universidade de Santiago de Compostela, Facultade de Farmacia, Campus Universitario Sur, E-15706, Santiago de Compostela, Spain.
Summary
Hydroxypropyl-beta-cyclodextrin (HPbetaCD) enhances the water solubility and dissolution rate of bropirimine (ABPP), an immunomodulator drug. This complexation improves ABPP
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Medicinal Chemistry
Background:
- Bropirimine (ABPP) is an orally active immunomodulator used for bladder carcinoma.
- Poor oral absorption of ABPP is due to its low water solubility.
Purpose of the Study:
- To develop a method to increase the water solubility of bropirimine (ABPP).
- To evaluate the complexation of ABPP with cyclodextrin derivatives.
Main Methods:
- Studied interaction of ABPP with alpha-, beta-, gamma-, and hydroxypropyl-beta-cyclodextrin (HPbetaCD).
- Characterized the ABPP-HPbetaCD inclusion complex using 1H-NMR, DSC, X-ray diffractometry, and mass spectrometry.
- Evaluated the effect of complexation on ABPP water solubility and dissolution rate.
Main Results:
- Hydroxypropyl-beta-cyclodextrin (HPbetaCD) showed the best results, forming a 1:1 molar ratio complex with ABPP.
- The dissolution rate of ABPP from the HPbetaCD solid inclusion complex increased compared to the powdered drug.
- No significant difference in dissolution rate was observed between the complex and a physical mixture.
Conclusions:
- Complexation with HPbetaCD effectively increases the dissolution rate of bropirimine (ABPP).
- The enhanced dissolution is attributed to the breakdown of drug dimers and complex formation in solution.
- HPbetaCD is a promising excipient for improving the oral bioavailability of bropirimine.