Sustained release of hydrophilic drug from polyphosphazenes/poly(methyl methacrylate) based microspheres and their degradation study

Mater Sci Eng C Mater Biol Appl. 2016 Jan 1:58:169-79. doi: 10.1016/j.msec.2015.08.010. Epub 2015 Aug 12.

Abstract

Drug delivery system is referred as an approach to deliver the therapeutic agents to the target site safely in order to achieve the maximum therapeutic effects. In this perspective, synthesis of three new polyphosphazenes and their blend fabrication system with poly(methyl methacrylate) is described and characterized with (1)H NMR, (31)P NMR, GPC and DSC. Furthermore, these novel blends were used to fabricate microspheres and evaluated for sustain release of hydrophilic drug (aspirin as model drug). Microspheres of the two blends showed excellent encapsulation efficacy (about 93%), controlled burst release (2.3% to 7.93%) and exhibited sustain in vitro drug release (13.44% to 32.77%) up to 218 h. At physiological conditions, the surface degradation of microspheres and diffusion process controlled the drug release sustainability. Furthermore, it was found that the degree of porosity was increased with degradation and the resulting porous network was responsible for water retention inside the microspheres. The percentage water retention was found to be interrelated with degradation time and percentage drug release.

Keywords: Blends; Drug release behavior; Hydrolytic degradation; Microspheres; Polyphosphazenes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aspirin / chemistry*
  • Aspirin / metabolism
  • Calorimetry, Differential Scanning
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Hydrophobic and Hydrophilic Interactions
  • Microspheres*
  • Organophosphorus Compounds / chemical synthesis
  • Organophosphorus Compounds / chemistry*
  • Particle Size
  • Polymers / chemical synthesis
  • Polymers / chemistry*
  • Polymethyl Methacrylate / chemical synthesis
  • Polymethyl Methacrylate / chemistry*
  • Porosity
  • Temperature

Substances

  • Drug Carriers
  • Organophosphorus Compounds
  • Polymers
  • poly(phosphazene)
  • Polymethyl Methacrylate
  • Aspirin