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Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis

Identifieur interne : 001508 ( Istex/Corpus ); précédent : 001507; suivant : 001509

Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis

Auteurs : R. L. Gaur ; S. Dixit ; M. K. Sahoo ; M. Khanna ; S. Singh ; P. K. Murthy

Source :

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Abstract

The study was aimed at developing better orally active albendazole (ALB) formulations. Six formulations (ALB-1 to ALB-6) were prepared and tested against Brugia malayi in Mastomys coucha and jird (Meriones unguiculatus) at 200 mg/kg, orally, for 5 consecutive days. The anti-filarial efficacy was assessed against microfilariae (mf), adult worms and female reproductive potential. Three of the 6 ALB formulations showed greatly improved female worm sterilizing potential (ALB-1: 90%; ALB-3: 63%; ALB-4: 77% of untreated control) in B. malayi – M. coucha model. Sterilization efficacy of ALB-1 was also better than that shown by pure-ALB (P<0·001) or its marketed tablet formulation, Zentel (P<0·01), while that of ALB-4 was better than pure-ALB (P<0·05). The activity of ALB-3, pure-ALB and Zentel was, however, comparable. ALB-1 also showed late microfilaricidal activity with a maximum of 78% fall in microfilarial count. In contrast, neither the pure ALB nor Zentel showed any microfilaricidal activity. In the jird – B. malayi model, ALB-1 and ALB-4 showed marginal sterilizing efficacy whereas pure ALB or Zentel were ineffective. In conclusion the anti-filarial efficacy of ALB-1 was found to be superior to pure-ALB or Zentel.

Url:
DOI: 10.1017/S0031182006001612

Links to Exploration step

ISTEX:2DAAB185C3A67EBDE8249801F078556D38F461D9

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<aff>Division of Parasitology,
<institution>Central Drug Research Institute</institution>
, Lucknow, 226001,
<country>India</country>
</aff>
</contrib>
</contrib-group>
<pub-date pub-type="epub">
<day>2</day>
<month>11</month>
<year>2006</year>
</pub-date>
<pub-date pub-type="ppub">
<month>4</month>
<year>2007</year>
</pub-date>
<volume>134</volume>
<issue>4</issue>
<fpage>537</fpage>
<lpage>544</lpage>
<history>
<date date-type="accepted">
<day>3</day>
<month>10</month>
<year>2006</year>
</date>
<date date-type="received">
<day>5</day>
<month>5</month>
<year>2006</year>
</date>
<date date-type="rev-recd">
<day>28</day>
<month>9</month>
<year>2006</year>
</date>
</history>
<permissions>
<copyright-statement>© 2006 Cambridge University Press</copyright-statement>
</permissions>
<abstract abstract-type="normal">
<p>The study was aimed at developing better orally active albendazole (ALB) formulations. Six formulations (ALB-1 to ALB-6) were prepared and tested against
<italic>Brugia malayi</italic>
in
<italic>Mastomys coucha</italic>
and jird (
<italic>Meriones unguiculatus</italic>
) at 200 mg/kg, orally, for 5 consecutive days. The anti-filarial efficacy was assessed against microfilariae (mf), adult worms and female reproductive potential. Three of the 6 ALB formulations showed greatly improved female worm sterilizing potential (ALB-1: 90%; ALB-3: 63%; ALB-4: 77% of untreated control) in
<italic>B. malayi</italic>
<italic>M. coucha</italic>
model. Sterilization efficacy of ALB-1 was also better than that shown by pure-ALB (
<italic>P</italic>
<0·001) or its marketed tablet formulation, Zentel (
<italic>P</italic>
<0·01), while that of ALB-4 was better than pure-ALB (
<italic>P</italic>
<0·05). The activity of ALB-3, pure-ALB and Zentel was, however, comparable. ALB-1 also showed late microfilaricidal activity with a maximum of 78% fall in microfilarial count. In contrast, neither the pure ALB nor Zentel showed any microfilaricidal activity. In the jird –
<italic>B. malayi</italic>
model, ALB-1 and ALB-4 showed marginal sterilizing efficacy whereas pure ALB or Zentel were ineffective. In conclusion the anti-filarial efficacy of ALB-1 was found to be superior to pure-ALB or Zentel.</p>
</abstract>
<kwd-group>
<kwd>albendazole</kwd>
<kwd>formulation</kwd>
<kwd>filariasis</kwd>
<kwd>
<italic>Brugia malayi</italic>
</kwd>
<kwd>
<italic>Meriones unguiculatus</italic>
</kwd>
<kwd>
<italic>Mastomys coucha</italic>
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<page-count count="8"></page-count>
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<title>Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis</title>
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<title>Anti-filarial activity of novel formulations of albendazole against experimental brugian filariasis</title>
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<name type="personal">
<namePart type="given">R. L.</namePart>
<namePart type="family">GAUR</namePart>
<affiliation>Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India</affiliation>
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<namePart type="given">M. K.</namePart>
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<affiliation>Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India</affiliation>
<role>
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</role>
</name>
<name type="personal">
<namePart type="given">M.</namePart>
<namePart type="family">KHANNA</namePart>
<affiliation>Division of Pharmaceutics, Central Drug Research Institute, Lucknow, 226001, India</affiliation>
<role>
<roleTerm type="text">author</roleTerm>
</role>
</name>
<name type="personal">
<namePart type="given">S.</namePart>
<namePart type="family">SINGH</namePart>
<affiliation>Division of Pharmaceutics, Central Drug Research Institute, Lucknow, 226001, India</affiliation>
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</name>
<name type="personal">
<namePart type="given">P. K.</namePart>
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<affiliation>Division of Parasitology, Central Drug Research Institute, Lucknow, 226001, India</affiliation>
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<abstract type="normal">The study was aimed at developing better orally active albendazole (ALB) formulations. Six formulations (ALB-1 to ALB-6) were prepared and tested against Brugia malayi in Mastomys coucha and jird (Meriones unguiculatus) at 200 mg/kg, orally, for 5 consecutive days. The anti-filarial efficacy was assessed against microfilariae (mf), adult worms and female reproductive potential. Three of the 6 ALB formulations showed greatly improved female worm sterilizing potential (ALB-1: 90%; ALB-3: 63%; ALB-4: 77% of untreated control) in B. malayi – M. coucha model. Sterilization efficacy of ALB-1 was also better than that shown by pure-ALB (P<0·001) or its marketed tablet formulation, Zentel (P<0·01), while that of ALB-4 was better than pure-ALB (P<0·05). The activity of ALB-3, pure-ALB and Zentel was, however, comparable. ALB-1 also showed late microfilaricidal activity with a maximum of 78% fall in microfilarial count. In contrast, neither the pure ALB nor Zentel showed any microfilaricidal activity. In the jird – B. malayi model, ALB-1 and ALB-4 showed marginal sterilizing efficacy whereas pure ALB or Zentel were ineffective. In conclusion the anti-filarial efficacy of ALB-1 was found to be superior to pure-ALB or Zentel.</abstract>
<subject>
<genre>keywords</genre>
<topic>albendazole</topic>
<topic>formulation</topic>
<topic>filariasis</topic>
<topic>Brugia malayi</topic>
<topic>Meriones unguiculatus</topic>
<topic>Mastomys coucha</topic>
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<identifier type="eISSN">1469-8161</identifier>
<identifier type="PublisherID">PAR</identifier>
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<date>2007</date>
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