Enhancement and modification of etoposide release from crospovidone particles loaded with oil-surfactant blends

Pharmaceutical Development and Technology
L BoltriP Esposito

Abstract

A novel solid formulation for oral delivery of pH-sensitive, scarcely water-soluble etoposide has been designed, characterized, and tested in vitro. The purpose of this study was to assess the performance of the new dosage forms, in comparison to marketed, liquid-filled capsules. The solid formulation was developed by grinding the drug with a cross-linked polymeric carrier (crospovidone) under controlled process conditions (mechano-physical drug activation), and subsequently incorporating selected oil/surfactant (o/s) blends into the polymer particles. Physicochemical characterization (thermal analysis, drug dissolution kinetics, drug o/w partition studies) provided information on drug-polymer interaction at the solid state, and on the formulation performance in vitro, resulting in the enhancement and modification of the etoposide solubilization process. DSC thermograms showed the amorphous or nanocrystalline state of etoposide within the carrier, as indicated by the shifting of DSC peaks (delta T > -10 degrees C). Solubility kinetics of etoposide in oversaturation conditions were strongly affected by the chemical nature of the vehicle used: short-chain triglycerides afforded drug concentrations well above 600 micrograms ml-1 f...Continue Reading

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Citations

Jan 15, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Tamara IosioFrancesca Serdoz
May 18, 2020·Current Drug Delivery·Nandini ChaudharyAwani K Rai
Apr 15, 2004·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·R Neslihan Gursoy, Simon Benita

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