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Mucoadhesive microspheres prepared by interpolymer complexation and solvent diffusion method.

Myung-Kwan Chun1, Chong-Su Cho, Hoo-Kyun Choi

  • 1College of Pharmacy, Chosun University, 375 Seoseok-dong, Dong-gu, Gwangju 501-759, Republic of Korea.

International Journal of Pharmaceutics
|December 29, 2004
PubMed
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Mucoadhesive microspheres were developed using poly(acrylic acid) and poly(vinyl pyrrolidone) to extend drug release in the stomach. These novel microspheres demonstrated controlled acetaminophen release, offering potential for improved oral drug delivery.

Area of Science:

  • Pharmaceutics
  • Polymer Science

Background:

  • Mucoadhesive microspheres enhance gastric residence time for improved oral drug delivery.
  • Interpolymer complexation offers a novel approach to microsphere formulation.

Purpose of the Study:

  • To prepare mucoadhesive microspheres using poly(acrylic acid) (PAA) and poly(vinyl pyrrolidone) (PVP) via interpolymer complexation.
  • To investigate the effect of formulation parameters on microsphere characteristics and drug release.

Main Methods:

  • Microspheres were prepared using a solvent diffusion method with PAA-PVP complexation.
  • Fourier Transform Infrared (FT-IR) spectroscopy confirmed hydrogen bonding between PAA and PVP.
  • Particle size, morphology, and adhesive force were evaluated.
  • Acetaminophen release studies were conducted at pH 2.0 and 6.8.

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Main Results:

  • Spherical microspheres with complete internal filling were successfully prepared.
  • Optimal ethanol/water ratios (8/2 and 7/3) were determined for microsphere formation.
  • Increased water content and polymer concentration led to larger particle sizes.
  • Microsphere adhesive force was comparable to Carbopol.
  • Complex microspheres exhibited slower acetaminophen release than PVP microspheres at both pH levels.

Conclusions:

  • PAA-PVP interpolymer complexation is effective for creating mucoadhesive microspheres.
  • Formulation parameters significantly influence microsphere size and drug release characteristics.
  • These mucoadhesive microspheres show promise for sustained drug delivery in the gastric environment.