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Cephradin-plaga microspheres for sustained delivery to cattle.

C Ustariz-Peyret1, J Coudane, M Vert

  • 1CRBA-URA CNRS 1465, Faculty of Pharmacy, University Montpellier 1, France.

Journal of Microencapsulation
|March 18, 1999
PubMed
Summary
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Researchers developed novel microspheres for sustained delivery of cephradin (an antibiotic) to cattle. These poly(lactic-co-glycolic acid) microspheres achieved high encapsulation and extended drug presence in blood circulation.

Area of Science:

  • Pharmaceutical Sciences
  • Veterinary Medicine
  • Materials Science

Background:

  • Controlled drug delivery systems are crucial for therapeutic efficacy and patient compliance.
  • Sustained-release formulations present unique challenges, especially for veterinary applications requiring specific release profiles.
  • Poly(alpha-hydroxy acid)s are FDA-approved biodegradable polymers suitable for drug matrices.

Purpose of the Study:

  • To develop and optimize poly(lactic-co-glycolic acid) (PLGA) microspheres for sustained delivery of cephradin to cattle.
  • To achieve a targeted release rate of 4-5 mg/kg/day over 3-4 days via intramuscular injection.
  • To investigate factors influencing encapsulation yield and drug release characteristics.

Main Methods:

  • Solvent evaporation technique using poly(vinyl alcohol) (PVA) as an emulsion stabilizer.

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  • Optimization of experimental conditions, including aqueous phase volume, addition of organic solvents/non-solvents, and sodium chloride concentration.
  • Modification of temperature and pressure to enhance drug entrapment.
  • In vivo studies in dogs to assess pharmacokinetic profiles.

    • Main Results:

    • Microspheres containing up to 30% cephradin were successfully prepared by adding sodium chloride to the aqueous phase.
    • Drug entrapment was increased to 40% by decreasing temperature and pressure.
    • Preliminary canine studies showed 20% cephradin microspheres extended drug presence in blood circulation up to 48 hours.
    • Higher drug loading resulted in increased blood concentrations but reduced sustained release duration.

    Conclusions:

    • Optimized PLGA microspheres can effectively encapsulate and provide sustained release of cephradin for veterinary applications.
    • The developed microsphere formulation shows promise for extended antibiotic delivery in cattle.
    • Further optimization is needed to balance drug load, release duration, and injection volume constraints for cattle.