Abstract | PURPOSE: METHODS: The levels of RS-1541 in the plasma and tissues including tumor, were determined by HPLC. The maximum tolerated dose (MTD) was estimated by toxic death and change in body weight. The decrease in tumor diameter was measured for antitumor activity. RESULTS: There existed large variations in pharmacokinetics of RS-1541, depending on the size of emulsion particles. Compared with a colloidal solution (reference solution), the small (110nm) and medium (230nm) size emulsions showed high concentrations of RS-1541 in the tumor, while the large emulsions (350nm-630nm) exhibited low concentrations. The MTD of RS-1541 was reduced, when incorporated in the emulsions larger than 220nm in size. At MTD, each size of emulsions (70nm-380nm) effectively retarded the tumor growth and increased survival time. The maximum effect was achieved for the 220 nm emulsions. CONCLUSIONS: When particle size is properly selected, these emulsions could be promising and effective as an injectable carrier for lipophilic antitumor agents in order to enhance the tumor delivery and efficacies while reducing toxicities.
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Authors | A Kurihara, Y Shibayama, A Mizota, A Yasuno, M Ikeda, K Sasagawa, T Kobayashi, M Hisaoka |
Journal | Pharmaceutical research
(Pharm Res)
Vol. 13
Issue 2
Pg. 305-10
(Feb 1996)
ISSN: 0724-8741 [Print] United States |
PMID | 8932454
(Publication Type: Journal Article)
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Chemical References |
- Antibiotics, Antineoplastic
- Emulsions
- Lactones
- Surface-Active Agents
- Triglycerides
- palmitoyl rhizoxin
- polyethoxylated castor oil
- Castor Oil
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Topics |
- Animals
- Antibiotics, Antineoplastic
(administration & dosage, pharmacokinetics, pharmacology)
- Castor Oil
(administration & dosage, analogs & derivatives, pharmacology, toxicity)
- Chemistry, Pharmaceutical
- Drug Screening Assays, Antitumor
- Drug Synergism
- Emulsions
- Female
- Lactones
(administration & dosage, toxicity)
- Lymphoma, Large B-Cell, Diffuse
(drug therapy, metabolism)
- Mice
- Mice, Inbred Strains
- Neoplasm Transplantation
- Surface-Active Agents
(administration & dosage, pharmacology, toxicity)
- Triglycerides
(administration & dosage, pharmacology)
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