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Drug nano- and microparticles processed into solid dosage forms: physical properties.

Jonghwi Lee1

  • 1Pharmaceutical Research and Development, Merck Research Laboratories, Merck & Co., West Point, Pennsylvania 19486, USA. jlee@sejong.ac.kr

Journal of Pharmaceutical Sciences
|September 23, 2003
PubMed
Summary

Nanoparticle drug formulations offer improved pharmacokinetics. While nanoparticulate systems show slightly increased stress to break and hardness, their aggregates can be redispersed, aiding drug delivery.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Nanoparticles significantly enhance pharmacokinetic performance for insoluble drugs.
  • Understanding nanoparticle characteristics is crucial for successful drug development.
  • This study compares nanoparticulate and microparticulate solid dosage performance.

Purpose of the Study:

  • To compare the processability and solid dosage performance of nanoparticulates versus microparticulates.
  • To investigate the impact of particle size on the mechanical properties of drug compacts.

Main Methods:

  • Nanoparticle suspensions prepared via wet comminution with stabilizers.
  • Spray drying used to convert suspensions into dried particles.
  • Compacts formed from dried particles for performance evaluation.

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Main Results:

  • Nanoparticles tend to aggregate during spray drying.
  • Aggregates demonstrate slow redispersion into nanoparticles in aqueous media.
  • Compacts exhibit structural and micromechanical differences based on primary particle size.
  • Nanoparticulate systems show only slightly higher stress to break and indentation hardness.

Conclusions:

  • Nanoparticulate drug systems offer potential for enhanced drug delivery.
  • Processability challenges like aggregation during spray drying can be managed through redispersion.
  • Mechanical properties of solid dosage forms are influenced by primary particle size.