Pharmacokinetic profile of Oncofid-S after intraperitoneal and intravenous administration in the rat

J Pharm Pharmacol. 2012 Mar;64(3):360-5. doi: 10.1111/j.2042-7158.2011.01417.x.

Abstract

Objectives: Oncofid-S is a bio-conjugate molecule obtained from the binding of campthotecin, SN-38, to hyaluronic acid. In view of a possible clinical development for loco-regional treatment of peritoneal carcinomatosis, this study aimed to establish the pharmacokinetic profile of Oncofid-S after single intraperitoneal or intravenous administration in the rat.

Methods: Single-dose intraperitoneal or intravenous administrations of Oncofid-S were performed. Groups of six rats were sacrificed at various times (up to 24 and 72 h in i.p. and i.v. study, respectively) after drug injection. Trunk blood, livers and spleens were collected for subsequent analysis. Total SN-38 was assayed by HPLC.

Key findings: We found that Oncofid-S was poorly absorbed after intraperitoneal injection, the estimated AUC0–72 being less than 2%. The drug was distributed in liver,but not spleen, and was eliminated with a terminal half-life of 16 h. After intravenous dosing, Oncofid-S was found in liver as well as in spleen.

Conclusions: Here we have demonstrated that Oncofid-S administered intraperitoneally in the rat was poorly absorbed into the systemic circulation, even after the administration of an extremely high dose. This finding reinforces the rationale for developing Oncofid-S in the loco-regional intraperitoneal treatment of peritoneal carcinomatosis in man.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Antineoplastic Agents, Phytogenic / pharmacokinetics*
  • Area Under Curve
  • Camptothecin / administration & dosage
  • Camptothecin / analogs & derivatives*
  • Camptothecin / pharmacokinetics
  • Half-Life
  • Humans
  • Hyaluronic Acid / administration & dosage
  • Hyaluronic Acid / analogs & derivatives*
  • Hyaluronic Acid / pharmacokinetics
  • Infusions, Intravenous
  • Injections, Intraperitoneal
  • Liver / metabolism
  • Male
  • Models, Animal
  • Rats
  • Rats, Wistar
  • Spleen / metabolism
  • Tissue Distribution

Substances

  • Antineoplastic Agents, Phytogenic
  • ONCOFID-S
  • Hyaluronic Acid
  • Camptothecin