Studies on Biodegradable Polymeric Nanoparticles of Risperidone: In Vitro and in Vivo Evaluation

Madaswamy S Muthu, Sanjay Singh

Nanomedicine (Lond). 2008 Jun;3(3):305-19.

PMID: 18510426

Abstract:

Aim:




The aim of this work was to develop extended-release risperidone nanoparticles for parenteral delivery (intravenous) and to reduce the dose-dependent extrapyramidal side effects of risperidone.













Methods:




Polymeric nanoparticles containing risperidone made of poly (epsilon-caprolactone) were designed by the nanoprecipitation method using polymeric stabilizers (poloxamers). The in vivo efficacy of prepared formulations and the risperidone solution was studied by administering them intravenously to apomorphine-treated mice. Extrapyramidal side effects of the risperidone and its formulations were also studied.













Results:




The particle size of the prepared nanoparticles ranged between 99 and 304 nm. Approximately 78-85% drug-encapsulation efficiency was achieved when risperidone was loaded at 1.7-4.1% by weight of the polymer. During in vivo studies, prepared risperidone-containing formulations showed a significant prolonged antipsychotic effect than that of risperidone solution, also having less extrapyramidal side effects.













Conclusion:




The prolonged effect of risperidone was obtained from the nanoparticles of risperidone administered by the intravenous route and this may improve the treatment of psychotic disorders by dose reduction.