Enhanced bioavailability and anthelmintic efficacy of mebendazole in redispersible microparticles with low-substituted hydroxypropylcellulose

We investigated the microparticulate structures that emerge spontaneously upon dispersion of an redispersible microparticles in aqueous medium and elucidated their influence on dissolution, and on their oral bioavailability and therapeutic efficiency using a murine model of infection with the nematode parasite Trichinella spiralis

Torrado-Santiago

2014

Scholarcy highlights

  • Mebendazole, methyl-5-benzoyl benzimidazole-2-carbamate, a broad-spectrum anthelmintic drug of the benzimidazole class effective against a number of nematodal and cestodal species under oral administration as tablets or suspension, is recommended for the treatment of non-surgical cases and as a supplementary treatment prior to and post-surgery in hydatid disease patients.1MBZ has limited water solubility
  • In the current work we have developed low-substituted hydroxypropylcellulose redispersible microparticles which would allow us to achieve similar anthelmintic effects with lower doses
  • scanning electron microscopy was used to determine the morphology of different samples, all of them at the same magnification
  • This medium allows a good dispersion of particles avoiding swelling of carrier
  • At a higher magnification most of the microaggregates are formed by clusters of small rounded MBZ particles
  • MBZ raw material registered 10% higher activity in relation to untreated control whereas the RDM-1:5 was significantly more active as compared with pure MBZ
  • Microparticles RDM-1:5 and the blank formulation containing only L-HPC show large swollen translucent particles with attenuated non-rounded edges, which can be attributed to the carrier, and small particles of less than 1 μm which can be attributed to MBZ or L-HPC
  • Dovepress these redispersible microparticles may provide a more secure drug system for oral poorly water soluble drugs in the clinical treatment of systemic helminthic infections with low drug doses

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