Aripiprazole Nanocrystal Impregnated Buccoadhesive Films for Schizophrenia

J Nanosci Nanotechnol. 2017 Apr;17(4):2345-352. doi: 10.1166/jnn.2017.12588.

Abstract

Aripiprazole is an atypical antipsychotic drug approved worldwide for treatment of acute and long term schizophrenia in adults. Increasingly atypical antipsychotics are playing a key role in the management of schizophrenia. The aim of the present study was to design a mucoadhesive dosage form for buccal delivery of aripiprazole which could provide a rapid drug delivery to the systemic circulation. Nanocrystals of aripiprazole were prepared by nano-precipitation using acid-base neutralization. These nanocrystals were then incorporated into buccoadhesive chitosan films. All the drug loaded films were found to smooth, non-tacky possessing high mechanical strength. Films were characterized for crystallinity of drug, surface pH, thickness, folding endurance, swelling behavior, mucoadhesive strength, drug release and ex-vivo permeation across rabbit cheek mucosa. In-vitro drug release studies indicated distinctly higher drug release from nanocrystal loaded films, FAPZ 13 and FAPZ 14. Permeation studies indicated a higher flux from films FAPZ 14 (442.34 ± 51.08 μg/cm2/h, P < 0.0001) when compared to film FAPZ 12. These promising results indicate that the developed nanocrystal loaded buccal films FAPZ 14 have the potential to provide a faster availability of aripiprazole and the buccoadhesive films offer promising option to patients with schizophrenia especially for geriatric patients.

Keywords: Buccal Film; Aripiprazole; Chitosan; Nanocrystals.

MeSH terms

  • Animals
  • Antipsychotic Agents* / chemistry
  • Antipsychotic Agents* / pharmacokinetics
  • Aripiprazole* / chemistry
  • Aripiprazole* / pharmacokinetics
  • Chitosan / chemistry
  • Drug Delivery Systems
  • Drug Liberation
  • Mouth Mucosa* / chemistry
  • Mouth Mucosa* / metabolism
  • Nanoparticles / chemistry*
  • Rabbits
  • Schizophrenia

Substances

  • Antipsychotic Agents
  • Aripiprazole
  • Chitosan