Nanomedicine: Nanotechnology, Biology and Medicine
Volume 5, Issue 3 , Pages 323-333, September 2009

PLGA nanoparticle formulations of risperidone: preparation and neuropharmacological evaluation

  • Madaswamy S. Muthu, MPharm

      Affiliations

    • Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, India
    • ,
  • Manoj K. Rawat, MPharm

      Affiliations

    • Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India
    • ,
  • Amit Mishra, MPharm

      Affiliations

    • Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India
    • ,
  • Sanjay Singh, PhD

      Affiliations

    • Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India
    • Corresponding Author InformationCorresponding author. Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi – 221005, India.

Received 9 May 2008; accepted 24 December 2008. published online 20 January 2009.

Abstract 

The aim of this work was to develop extended-release poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles of risperidone and thermal-responsive in situ gel containing risperidone nanoparticles for parenteral (subcutaneous) delivery and to reduce the dose-dependent extrapyramidal side effects of risperidone. PLGA nanoparticles of risperidone were designed by nanoprecipitation method using polymeric stabilizer (Poloxamer 407). The prepared nanoparticles were characterized for particle size by photon correlation spectroscopy and atomic force microscopy. Poloxamer 407–based in situ gel containing PLGA nanoparticles of risperidone was prepared by modified cold method to control the initial rapid release from the nanoparticles. The in vivo efficacy (antipsychotic effect) of prepared formulations (nanoparticles and in situ gel containing nanoparticles) was studied by administering them subcutaneously to mice. Extrapyramidal side effects of the formulations were also studied. The particle size of the prepared nanoparticles ranged between 85 and 219 nm. About 89% to 95% drug encapsulation efficiency was achieved when risperidone was loaded at 1.7% to 8.3% by weight of the polymer. During in vivo studies prepared risperidone formulations showed an antipsychotic effect that was significantly prolonged over that of risperidone solution for up to 72 hours with fewer extrapyramidal side effects. The prolonged effect of risperidone was obtained from the risperidone formulations administered subcutaneously, and this may improve the treatment of psychotic disorders by dose reduction.

From the Clinical Editor

The development of extended-release poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles of risperidone is reported in this paper, along with the development of thermal-responsive in situ gel containing risperidone nanoparticles for parenteral (subcutaneous) delivery and to reduce the dose-dependent extrapyramidal side effects. In vivo studies showed a significantly prolonged antipsychotic effect with fewer extrapyramidal side effects.

Key words: Atomic force microscopy, Psychopharmacology, Photon correlation spectroscopy, Poloxamer 407, Poly(d,l-lactide-co-glycolide) nanoparticles, Risperidone

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 This research was supported by University Grant Commission, New Delhi, India in terms of a Senior Research Fellowship.

PII: S1549-9634(09)00003-3

doi:10.1016/j.nano.2008.12.003

Nanomedicine: Nanotechnology, Biology and Medicine
Volume 5, Issue 3 , Pages 323-333, September 2009

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