Controlled release formulations of risperidone antipsychotic drug in novel aliphatic polyester carriers: Data analysis and modelling

Eur J Pharm Biopharm. 2015 Aug:94:473-84. doi: 10.1016/j.ejpb.2015.06.027. Epub 2015 Jul 6.

Abstract

In the present study a series of biodegradable and biocompatible poly(ε-caprolactone)/poly(propylene glutarate) (PCL/PPGlu) polymer blends were investigated as controlled release carriers of Risperidone drug (RISP), appropriate for transdermal drug delivery. The PCL/PPGlu carriers were prepared in different weight ratios. Miscibility studies of blends were evaluated through differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Hydrolysis studies were performed at 37°C using a phosphate buffered saline solution. The prepared blends have been used for the preparation of RISP patches via solvent evaporation method, containing 5, 10 and 15wt% RISP. These formulations were characterized using FT-IR spectroscopy, DSC and WAXD in order to evaluate interactions taking place between polymer matrix and drug, as well as the dispersion and the physical state of the drug inside the polymer matrix. In vitro drug release studies were performed using as dissolution medium phosphate buffered saline simulating body fluids. It was found that in all cases controlled release formulations were obtained, while the RISP release varies due to the properties of the used polymer blend and the different levels of drug loading. Artificial Neural Networks (ANNs) were used for dissolution behaviour modelling showing increased correlation efficacy compared to Multi-Linear-Regression (MLR).

Keywords: Blends; Controlled release; Modelling; Poly(propylene glutarate); Poly(ε-caprolactone); Risperidone drug.

MeSH terms

  • Antipsychotic Agents / administration & dosage*
  • Antipsychotic Agents / chemistry
  • Calorimetry, Differential Scanning
  • Cell Survival / drug effects
  • Chemistry, Pharmaceutical
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Drug Liberation
  • Glutarates / chemistry
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Models, Chemical*
  • Neural Networks, Computer
  • Polyesters / chemical synthesis
  • Polyesters / chemistry*
  • Polyesters / toxicity
  • Polypropylenes / chemistry
  • Risperidone / administration & dosage*
  • Risperidone / chemistry
  • Spectroscopy, Fourier Transform Infrared
  • X-Ray Diffraction

Substances

  • Antipsychotic Agents
  • Drug Carriers
  • Glutarates
  • Polyesters
  • Polypropylenes
  • polycaprolactone
  • Risperidone