Liposomal-praziquantel: Efficacy against Schistosoma mansoni in a preclinical assay

Frezza, Tarsila Ferraz; Gremião, Maria Palmira Daflon; Zanotti-Magalhães, Eliana Maria; Magalhães, Luiz Augusto; Souza, Ana Luiza Ribeiro de; Allegretti, Silmara Marques

doi:10.1016/j.actatropica.2013.06.011

Cited by 54 publications

(22 citation statements)

References 33 publications

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“…Moreover, liposome‐entrapped drugs provided protection over a much broader time window . Similar effects were also confirmed with other drugs, including PZQ and DEC, in later studies . Here the observed improvement in therapeutic efficacy using liposome encapsulated drugs can be explained by greater bioavailability and longer circulation of the drugs as they are loaded in liposomes.…”

Section: How Can Nanodelivery Systems Transform the Treatment Of Helmsupporting

confidence: 69%

“…Here the observed improvement in therapeutic efficacy using liposome encapsulated drugs can be explained by greater bioavailability and longer circulation of the drugs as they are loaded in liposomes. It has been also speculated that the drug molecules may be absorbed more effectively by parasites, as liposomes dock on and fuse with worms' outermost surface, but further investigation of the idea may be required.…”

Section: How Can Nanodelivery Systems Transform the Treatment Of Helmmentioning

confidence: 99%

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Nanomedicine Approaches Against Parasitic Worm Infections

Coronado

Longstaff

et al. 2018

Adv Healthcare Materials

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Nanomedicine approaches have the potential to transform the battle against parasitic worm (helminth) infections, a major global health scourge from which billions are currently suffering. It is anticipated that the intersection of two currently disparate fields, nanomedicine and helminth biology, will constitute a new frontier in science and technology. This progress report surveys current innovations in these research fields and discusses research opportunities. In particular, the focus is on: (1) major challenges that helminth infections impose on mankind; (2) key aspects of helminth biology that inform future research directions; (3) efforts to construct nanodelivery platforms to target drugs and genes to helminths hidden in their hosts; (4) attempts in applying nanotechnology to enable vaccination against helminth infections; (5) outlooks in utilizing nanoparticles to enhance immunomodulatory activities of worm-derived factors to cure allergy and autoimmune diseases. In each section, achievements are summarized, limitations are explored, and future directions are assessed.

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Section: How Can Nanodelivery Systems Transform the Treatment Of Helmsupporting

confidence: 69%

Section: How Can Nanodelivery Systems Transform the Treatment Of Helmmentioning

confidence: 99%

Nanomedicine Approaches Against Parasitic Worm Infections

Coronado

Longstaff

et al. 2018

Adv Healthcare Materials

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“…An increase of 2 to 4 times the concentration of PZQ in the incubation medium did not change the amount of absorbed PZQ, indicating an increased saturation concentration gradient. Frezza et al 17 observed that the PZQ dose previously tested for the LE strain (Mourão et al 2005) did not show the same activity when employed in mice infected with the S. Mansoni BH strain. Increasing the dose of PZQ improved schistosomicidal activity, and PZQ encapsulated in liposomes was more effective than an equivalent dose of free PZQ, inhibiting oviposition and hepatic granuloma formation.…”

Section: Introductionmentioning

confidence: 90%

“…These drugs may have greater bioavailability in the host, and they may be better absorbed by the tegument of S. mansoni, which has an affinity for phospholipids. 17 Campos et al 18 developed a Dextran-70 hydrogel for the controlled release of PZQ and performed in vitro release assays. They observed that the release profile of PZQ was prolonged by incorporation into dextran molecules.…”

Section: Introductionmentioning

confidence: 99%

Nanostructured Lipid Carriers as a Strategy to Improve the <I>In Vitro</I> Schistosomiasis Activity of Praziquantel

Kolenyak-Santos¹,

Garnero²,

Oliveira³

et al. 2015

j nanosci nanotechnol

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Praziquantel (PZQ) is a pyrazinoisoquinoline anthelmintic that was discovered in 1972 by Bayer Germany. Currently, due to its efficacy, PZQ is the drug of choice against all species of Schistosoma. Although widely used, PZQ exhibits low and erratic bioavailability because of its poor water solubility. Nanostructured lipid carriers (NLC), second-generation solid lipid nanoparticles, were developed in the 1990s to improve the bioavailability of poorly water soluble drugs. The aim of this study was to investigate nanostructured lipid carriers as a strategy to improve the efficacy of PZQ in S. mansoni treatment. We prepared NLC2 and NLC4 by adding seventy percent glycerol monostearate (GMS) as the solid lipid, 30% oleic acid (OA) as the liquid lipid and two surfactant systems containing either soybean phosphatidylcholine/poloxamer (PC/P-407) or phosphatidylcholine/Tween 60 (PC/T60), respectively. The carriers were characterized by nuclear magnetic resonance, differential scanning calorimetry, thermogravimetric analysis and Fourier transform-infrared spectroscopy. The safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. The results showed that the encapsulation of PZQ in NLC2 or NLC4 improved the safety profile of the drug. Treatment efficacy was evaluated on the S. mansoni BH strain. PZQ-NLC2 and PZQ-NLC4 demonstrated an improved efficacy in comparison with free PZQ. The results showed that the intestinal transport of free PZQ and PZQ-NLC2 was similar. However, we observed that the concentration of PZQ absorbed was smaller when PZQ was loaded in NLC4. The difference between the amounts of absorbed PZQ could indicate that the presence of T60 in the nanoparticles (NLC4) increased the rigid lipid matrix, prolonging release of the drug. Both systems showed considerable in vitro activity against S. mansoni, suggesting that these systems may be a promising platform for the administration of PZQ for treating schistosomiasis.

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“…These formulations have gained significance as nanocarriers in helminthic infection due to their ability to diffuse through the intestinal mucosal layers. In schistosomiasis, liposome encapsulated praziquantel has shown significant reductions in parasitic burdens and hepatic granulomas due to increased affinity for parasite phospholipids [130]. Liposome based nanocapsules of praziquantel (PZQ-LNCs) improved the drug efficacy and ameliorated disease pathology [131].…”

Section: Nano-medicinal Approachmentioning

confidence: 99%

Molecular Medicines for Parasitic Diseases

Singh¹

2021

Methods in Molecular Medicine

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Being the cause for significant amount of morbidities and mortalities, parasitic diseases remain the major challenge for the healthcare community due to the limitations associated with the current chemotherapeutics. Drug discovery/invention can be achieved by collaborative efforts of biotechnologists and pharmacists for identifying potential candidates and successfully turn them into medicine for improving the healthcare system. Although molecular medicine for disease intervention is still in its infancy, however, significant research works and successful trials in short span of time have made it broadly accepted among the scientific community. This chapter identifies different molecular medicine approaches for dealing with parasites that have been coming up on the horizon with the new technological advances in bioinformatics and in the field of omics. With the better understanding of the genomics, molecular medicine field has not only raised hopes to deal with parasitic infections but also accelerated the development of personalized medicine. This will provide a targeted approach for identifying the druggable targets and their pathophysiological importance for disease intervention.

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Liposomal-praziquantel: Efficacy against Schistosoma mansoni in a preclinical assay

Cited by 54 publications

References 33 publications

Nanomedicine Approaches Against Parasitic Worm Infections

Nanomedicine Approaches Against Parasitic Worm Infections

Nanostructured Lipid Carriers as a Strategy to Improve the <I>In Vitro</I> Schistosomiasis Activity of Praziquantel

Molecular Medicines for Parasitic Diseases

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