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Related Experiment Videos

Ultrathin antibiotic walled microcapsules.

Ajay J Khopade1, N Arulsudar, Surekha A Khopade

  • 1Max Planck Institute of Colloids and Interfaces, Am Mühlenberg 1, D-14476 Golm, Germany. ajkhopade@sunpharma.com

Biomacromolecules
|January 11, 2005
PubMed
Summary

Ultrathin antibiotic microcapsules were developed using layer-by-layer assembly for sustained ophthalmic drug delivery. These polyelectrolyte/aminoglycoside capsules demonstrate safety and efficacy in vivo.

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A Comparative Preclinical Evaluation of a Novel Difluprednate 0.04% BID Ophthalmic Solution and Marketed 0.05% QID Ophthalmic Emulsion.

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Area of Science:

  • Materials Science
  • Nanotechnology
  • Pharmaceutical Science

Background:

  • Developing novel drug delivery systems is crucial for improving therapeutic outcomes.
  • Ultrathin microcapsules offer potential for targeted and sustained drug release.
  • Aminoglycoside antibiotics are vital for treating bacterial infections, but require effective delivery methods.

Purpose of the Study:

  • To prepare and characterize ultrathin microcapsules composed of polyelectrolytes and an aminoglycoside antibiotic.
  • To evaluate the stability, drug loading, and decomposition kinetics of these microcapsules.
  • To assess the in vivo safety and sustained drug delivery potential of the microcapsules for ophthalmic applications.

Main Methods:

  • Layer-by-layer self-assembly of anionic polyelectrolytes (dextran sulfate sodium or poly(styrenesulfonate)) and tobramycin sulfate on zinc oxide cores.

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  • Dissolution of zinc oxide cores to yield hollow microcapsules.
  • Characterization using zeta potential measurements, transmission and scanning electron microscopy, quartz crystal microbalance, and high-performance liquid chromatography.
  • In vivo studies in rabbits to evaluate safety and drug delivery.
  • Main Results:

    • Successfully fabricated ultrathin polyelectrolyte/tobramycin sulfate microcapsules via layer-by-layer assembly on ZnO templates.
    • Microcapsule yield varied based on polyelectrolyte choice (PSS/TbS higher than DxS/TbS).
    • Decomposition rates differed in various media, with physiological buffer showing the fastest breakdown; stability was influenced by hydrogen bonding and hydrophobic interactions.
    • In vivo studies confirmed the safety and sustained drug delivery capabilities of the microcapsules.

    Conclusions:

    • Ultrathin polyelectrolyte/aminoglycoside microcapsules can be effectively prepared using layer-by-layer assembly and ZnO templating.
    • The physicochemical properties of the polyelectrolytes influence capsule formation and stability.
    • These microcapsules show promise for sustained ophthalmic antibiotic delivery due to their safety and controlled release characteristics.