Please use this identifier to cite or link to this item:
- Improvement of the oral praziquantel anthelmintic effect by cyclodextrin complexation
- Universidade Estadual de Campinas (UNICAMP)
- Universidade Federal de Lavras (UFLA)
- Universidade Estadual Paulista (UNESP)
- Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
- Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
- FAPESP: 06/03838-1
- FAPESP: 02/04103-4
- Schistosomiasis is a parasitic disease which kills a half million people per year, a I I over the world. Praziquantel (PZQ) is the drug-of-choice for schistosomiasis because of its effectiveness, ease of administration, and low cost. However, poor solubility restricts its delivery, especially via the oral route. In this study, we describe beta-cyclodextrin (beta-CD) complexation as an alternative to improve the PZQ bioavailability. Physicochemical analysis were performed to characterize the inclusion complex formed between PZQ and beta-CD. Differential scanning calorimetry (DSC) thermograms and morphological analysis using scanning electronic microscopy (SEM) gave evidences of the complex formation. Diffusion NMR experiments allowed determination of the fraction of PZQ bound to beta-CD (37%) and the association constant (941 +/- 47 M(-1)). The in vivo evaluation of the complexation on the effect of PZQ was performed on mice infected with Schistosoma mansoni (BH strain); after 15 days of treatment with the PZQ:beta-CD complex the efficacy, evaluated by the number of remaining alive worms, was 99%, against 59% elicited by plain PZQ.
- Journal of Drug Targeting. Abingdon: Taylor & Francis Ltd, v. 18, n. 1, p. 21-26, 2010.
- Taylor & Francis Ltd
- inclusion complex
- Acesso restrito
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.