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Pharmacokinetics of an extended-release human interferon alpha-2b formulation

  • Original Articles
  • Interferon, Pharmacokinetics, Extended-Release
  • Published:
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Abstract

The in vivo half-life of human interferon alpha-2b (hIFN-α-2b) is relatively short, and frequent injections over prolonged periods are required for efficacy. An extended-release formulation of hIFN-α-2b (Depo/IFN) was created by encapsulation into a lipid-based drug-delivery system. The capture efficiency was 51%±13% and the release half-life in human plasma at 37°C was 16 days. The pharmacokinetics of Depo/IFN was compared with that of unencapsulated standard hIFN-α-2b (Std/IFN) in the peritoneal cavity of male BDF1 mice. Depo/IFN exhibited a 13-fold longer intraperitoneal (i.p.) half-life as compared with Std/IFN (20 vs 1.5 h). The release of free hIFN-α-2b from Depo/IFN into the peritoneal cavity was slow and protracted, with a 10-fold lower peak concentration and a 13-fold longer apparent half-life being observed in comparison with Std/IFN. The areas under the curve of free hIFN-α-2b in the peritoneal cavity were comparable for Depo/IFN and Std/IFN. hIFN-α-2b was detectable in plasma only after the i.p. administration of Std/IFN. These data suggest the possibility that Depo/IFN may be useful as an extended-release formulation of hIFN-α-2b.

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  1. UCSD Cancer Center, University of California, San Diego, 9500 Gilman Drive, 92093-0812, La Jolla, CA, USA

    Andrea Bonetti & Sinil Kim

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  1. Andrea Bonetti
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  2. Sinil Kim
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Bonetti, A., Kim, S. Pharmacokinetics of an extended-release human interferon alpha-2b formulation. Cancer Chemother. Pharmacol. 33, 258–261 (1993). https://doi.org/10.1007/BF00686225

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  • DOI: https://doi.org/10.1007/BF00686225

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