Development of nonionic surfactant/phospholipid o/w emulsion as a paclitaxel delivery system.
Paclitaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated paclitaxel in the triacylglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 0.75 mg/ml paclitaxel, 10% (w/v) oil blend, 4% (w/v) EPC, 3% (w/v) Tween 80 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at 4 degrees C, and the paclitaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around 150 nm for at least 3 months. Paclitaxel-emulsion displayed cytotoxicity against HeLa cells with IC50 at 30 nM. The average life span of ascitic-tumor-bearing mice was prolonged significantly by the treatment of paclitaxel-emulsion (P<0.05). The formulated emulsion is a promising carrier for paclitaxel and other lipophilic drugs.
Kan
P
P
Department of Chemical Engineering, National Tsing Hua University, Hsinchu, Taiwan 300, ROC.
Chen
Z B
ZB
Lee
C J
CJ
Chu
I M
IM
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D004655:Emulsions; D005990:Glycerol / Q000737:chemistry; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D008813:Mice, Inbred ICR; D009821:Oils / Q000737:chemistry; D017239:Paclitaxel / Q000737:chemistry* / Q000633:toxicity; D010316:Particle Size; D010743:Phospholipids / Q000737:chemistry*; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D014280:Triglycerides / Q000737:chemistry
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D004655:Emulsions; D009821:Oils; D010743:Phospholipids; D011136:Polysorbates; D013501:Surface-Active Agents; D014280:Triglycerides; D010767:Phosphorylcholine; C075010:erucylphosphocholine; D017239:Paclitaxel; D005990:Glycerol