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Oral sustained-release cisplatin capsule

T Houjou1, K Nakano, O Ike

  • 1Department of Pharmaceutics and Pharmacokinetics, Kyoto Pharmaceutical University, Japan.

The Journal of Pharmacy and Pharmacology
|May 1, 1996
PubMed
Summary
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Developing an oral sustained-release cisplatin capsule using ethylcellulose and Carbopol shows promise. This formulation controls drug release, offering a feasible alternative to traditional cisplatin administration.

Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Oncology Therapeutics

Background:

  • Cisplatin is a potent chemotherapy drug with challenges in oral administration due to its hydrophilic nature.
  • Controlling the release rate of hydrophilic drugs from oral dosage forms is complex.
  • Ethylcellulose capsules alone are insufficient for controlled cisplatin release.

Purpose of the Study:

  • To develop and evaluate an oral sustained-release cisplatin preparation.
  • To investigate the combined effect of micropores and Carbopol on cisplatin release kinetics.
  • To assess the in vivo performance of the sustained-release formulation.

Main Methods:

  • Formulation of sustained-release cisplatin capsules using ethylcellulose and varying amounts of Carbopol (15-100 mg) and micropore numbers (20, 30, 60).

Related Experiment Videos

  • In vitro release studies to determine drug release profiles under different formulation parameters.
  • In vivo pharmacokinetic studies in rabbits comparing the sustained-release capsule with oral cisplatin solution.

    • Main Results:

    • In vitro release rate decreased with increasing Carbopol amounts for 60 and 30 micropores.
    • In vivo studies in rabbits demonstrated sustained release patterns with 30 micropores and 15 mg Carbopol.
    • Achieved prolonged serum cisplatin levels, with Cmax of 0.41 µg/mL at 3.33 h and 0.23 µg/mL at 24 h.

    Conclusions:

    • An oral sustained-release cisplatin preparation is feasible using a combination of ethylcellulose and Carbopol.
    • The number of micropores and the amount of Carbopol significantly influence cisplatin release.
    • This formulation offers a potential improvement for oral cisplatin therapy.