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Related Experiment Videos

Optimization of topical cidofovir penetration using microparticles.

S Santoyo1, E Ga de Jalón, P Ygartua

  • 1Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31080, Pamplona, Spain.

International Journal of Pharmaceutics
|August 15, 2002
PubMed
Summary

Poly(lactide-co-glycolide) (PLGA) microparticles enhance topical cidofovir delivery by increasing drug retention in the basal epidermis and reducing skin penetration. This offers improved antiviral therapy for herpes viruses.

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Area of Science:

  • Pharmaceutical Sciences
  • Biomaterials Science
  • Dermatology

Background:

  • Cidofovir exhibits broad-spectrum antiviral activity against herpes viruses.
  • Topical delivery of cidofovir aims for prolonged therapeutic effects in the basal epidermis.
  • Developing effective topical formulations is crucial for enhancing cidofovir's therapeutic potential.

Purpose of the Study:

  • To develop and evaluate poly(lactide-co-glycolide) (PLGA) microparticles for prolonged topical delivery of cidofovir.
  • To compare the skin penetration and distribution of cidofovir from microparticle formulations versus a conventional solution.
  • To determine if microparticles can enhance cidofovir retention in the basal epidermis.

Main Methods:

  • PLGA microparticles were prepared using spray-drying and solvent evaporation (W/O/W) methods.

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  • Encapsulation efficiency and drug release profiles were assessed.
  • Skin penetration and distribution studies were conducted using Franz-type diffusion cells and porcine skin.
  • Cidofovir content in skin layers was quantified after 24-hour topical application.

    • Main Results:

    • Spray-dried PLGA microparticles demonstrated high encapsulation efficiency (80%) and suitable characteristics for skin delivery.
    • Topical application of cidofovir-loaded microparticles resulted in significantly higher drug retention in the basal epidermis compared to a cidofovir solution.
    • Microparticle formulations showed reduced skin penetration over 24 hours compared to the drug solution.

    Conclusions:

    • Spray-dried PLGA microparticles are a promising carrier system for improving topical cidofovir delivery.
    • These microparticles enhance drug retention in the target epidermal layer while minimizing systemic penetration.
    • Cidofovir-loaded microparticles represent a viable strategy for advancing topical antiviral therapy against herpes viruses.