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Formulation of delivery systems with risperidone based on biodegradable terpolymers.

Artur Turek1, Aleksandra Borecka2, Henryk Janeczek2

  • 1School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia, Katowice, Chair and Department of Biopharmacy, Jedności 8, 41-200 Sosnowiec, Poland.

International Journal of Pharmaceutics
|June 29, 2018
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Summary

New risperidone delivery systems using terpolymers were developed for treating mental diseases. Both solution casting and hot melt extrusion are suitable for creating long-acting wafers and rods.

Keywords:
FormulationHot melt extrusionRisperidoneSolution castingTerpolymers

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Area of Science:

  • * Pharmaceutical Sciences
  • * Polymer Chemistry

Background:

  • * Risperidone is an oral medication for mental health conditions.
  • * Parenteral delivery systems offer advantages over oral formulations, with wafers and rods being promising alternatives to microparticle suspensions.
  • * Poly(lactide-co-glycolide) (PLGA) based systems are gaining traction for sustained drug delivery.

Purpose of the Study:

  • * To evaluate solution casting and hot melt extrusion for formulating risperidone-loaded wafers and rods.
  • * To investigate the use of novel terpolymers: poly(lactide-co-glycolide-co-trimethylene carbonate) and poly(lactide-co-glycolide-co-ε-caprolactone).
  • * To analyze the impact of formulation methods and terpolymer composition on risperidone release profiles.

Main Methods:

  • * Terpolymer synthesis using zirconium initiators and different lactide forms.
  • * Formulation of delivery systems via solution casting and hot melt extrusion.
  • * Characterization using NMR, DSC, GPC, SEM, and release studies via HPLC.

Main Results:

  • * Formulated terpolymers maintained their microstructure, glass transition temperature, and morphology.
  • * Solution casting caused a lesser decrease in molecular weight compared to hot melt extrusion.
  • * Risperidone incorporation further reduced molecular weight; release occurred in three phases, with an initial burst effect noted for poly(L-lactide-co-glycolide-co-ε-caprolactone).

Conclusions:

  • * Both solution casting and hot melt extrusion are viable methods for creating risperidone-loaded terpolymer delivery systems.
  • * Terpolymer composition can be adjusted to control the drug release duration.
  • * These novel systems offer potential for prolonged risperidone delivery.