Document Detail

Haloperidol-loaded polysorbate-coated polymeric nanocapsules increase its efficacy in the antipsychotic treatment in rats.
MedLine Citation:
PMID:  21168486     Owner:  NLM     Status:  In-Data-Review    
Haloperidol is an antipsychotic drug associated with the development of movement disorders. We evaluated the effect of its nanoencapsulation on its pharmacological activity and motor side effects. Haloperidol-loaded polysorbate-coated nanocapsules (H-NC) showed nanometric size, negative zeta potential and low polydispersity indices and high encapsulation efficiency (>95%). Rats received a single dose of H-NC (0.2mg/kgip) and four doses of d,l-amphetamine, AMPH (8.0mg/kgip), injected every 3h (0, 3, 6 and 9h). The AMPH-induced stereotyped movements were quantified in the intervals of 15min after each of four doses of AMPH, demonstrating greater pharmacological efficacy of the H-NC over free haloperidol (FH). The acute motor side effects were evaluated 1h after a single dose of H-NC or its free solution (0.2mg/kgip). The group treated with H-NC presented lower extrapyramidal effects (catalepsy and oral dyskinesia) than those treated with FH. In the last experimental set, rats sub-chronically treated with a daily dose of H-NC (0.2mg/kgip) for 28days showed a lower incidence of extrapyramidal effects than those treated with the free drug (0.2mg/kgip). Our findings showed the potential of using H-NC in the development of a nanomedicine aimed at increasing the efficacy of this antipsychotic drug and reducing its side effects.
Dalila M Benvegnú; Raquel C S Barcelos; Nardeli Boufleur; Patrícia Reckziegel; Camila S Pase; Aline F Ourique; Ruy Carlos R Beck; Marilise E Bürger
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Publication Detail:
Type:  Journal Article     Date:  2010-12-17
Journal Detail:
Title:  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V     Volume:  77     ISSN:  1873-3441     ISO Abbreviation:  Eur J Pharm Biopharm     Publication Date:  2011 Feb 
Date Detail:
Created Date:  2011-01-31     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9109778     Medline TA:  Eur J Pharm Biopharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  332-6     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Elsevier B.V. All rights reserved.
Programa de Pós-Graduação em Farmacologia, Universidade Federal de Santa Maria-UFSM, Santa Maria-RS, Brazil.
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