Erbulozole (P.I.N.N.) (R 55 104) encapsulated into cyclodextrins: has it a combined antitumoral and radioprotective potential?

Abstract

The clinically applicable formulation of the microtubule inhibitor erbulozole (R 55 104), dissolved into an aqueous hydroxypropyl-beta-cyclodextrin solution (designated as R 55 104-CYCLO), exerts a similar effect on growth delay of subcutaneous MO4 fibrosarcomas in mice, with or without 10 Gy gamma-irradiation given locally to the tumors 2 h later, compared to R 55 104 in water. The drug concentration can be reduced from 80 mg/kg to 5 mg/kg without affecting the activity of this particular drug-radiation combination. Furthermore, 80 mg/kg R 55 104-CYCLO show a radioprotective effect when given 2 h before total body irradiation of non-tumor bearing mice. A radiation dose of 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 Gy respectively was given resulting in a LD50(30) of 5.97 Gy for the irradiated mice and 7.65 Gy for the drug-radiation treated animals (Dose Effect Factor = 0.78). Therapeutic implications of both observations are discussed.

• Authors: W Distelmans, R Van Ginckel, W Vanherck, R Willebrords, L Wouters, M De Brabander, J Mesens
• Journal: Anticancer research (Anticancer Res) 1991 Jan-Feb Vol. 11 Issue 1 Pg. 253-6 ISSN: 0250-7005 [Print] GREECE
• PMID: 2018359 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Capsules
• Dioxolanes
• Radiation-Protective Agents
• erbulozole

Topics

• Animals
• Antineoplastic Agents (therapeutic use)
• Capsules
• Cell Division (drug effects)
• Dioxolanes (therapeutic use)
• Fibrosarcoma (drug therapy, pathology, radiotherapy)
• Gamma Rays
• Mice
• Mice, Inbred Strains
• Radiation-Protective Agents (therapeutic use)
• Sarcoma, Experimental (drug therapy, pathology, radiotherapy)