Improvement of the oral praziquantel anthelmintic effect by cyclodextrin complexation

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.

Parasitology of juvenile mullet (Mugil liza) and effect of formaldehyde on parasites and host

Few studies have been performed with parasites of marine and estuarine fish in southern Brazil. In the present study, unpublished results show the ways of parasitism of juvenile mullet by parasites. The toxicity of formaldehyde and the effectiveness of this chemotherapy in controlling parasites in reared juvenile mullet Mugil liza were also studied. Juvenile mullets (1 +/- 0.26 g; 4.1 +/- 0.4 cm) were exposed to different concentrations of 37% formaldehyde: control group and five formaldehyde concentrations which were tested: T1 (13.5), T2 (21.6), T3 (40.5), T4 (81) and T5 (135) mg L-1 with 8 fish per repetition in triplicate. To verify the drug effectiveness in parasitic control, juvenile mullets were exposed to 1 h prophylactic bath of 37% formaldehyde with a control group and five formaldehyde concentrations: T1 (67.5), T2 (135), T3 (270), T4 (405) and T5 (540) mg L-1, 8 fish per repetition in triplicate. Ligophorus cf. uruguayensis (Monogenoidea: Ancyrocephalidae) and Solostamenides cf. platyorchis (Monogenoidea: Microcotylidae) were identified in the gills. Digenea and Nematoda were observed in the intestines. This is the first occurrence of S. cf. platyorchis in Brazil. During the toxicity test, the LC50-96 h was estimated at 20.77 mg L-1 of formaldehyde. During the 1 h formaldehyde prophylactic bath, all parasites were eliminated in formaldehyde concentrations between 135 and 540 mg L-1. High survival rate was observed in all treatments. Values of prevalence and intensity of infestation observed in this study showed the potential damage caused by Monogenoidea to mullet. Formaldehyde baths with 135 mg L-1 are recommended to control Monogenoidea in mullet and the safe limits for formaldehyde use were presented. Besides, the endoparasites were tolerant to formaldehyde exposure. (C) 2012 Elsevier B.V. All rights reserved.