title: Highly efficient and lowly toxic docetaxel nanoemulsions for intravenous injection to animals.
abstract: Hypersensitivity many occur with commercial docetaxel injections containing Tween 80 and ethanol. An alternative formulation of docetaxel, an oil-in-water nanoemulsion was prepared using the high-pressure homogenization method. It was composed of medium-chain triglyceride, oleic acid, egg lecithin, and poloxamer. These ingredients are known as safe agents for intravenous (i.v.) injection. The nanoemulsion had a small size of 169 nm, and a high surface charge with the zeta potential of -33.9 mV. It maintained well stable even under high centrifugation. Acute toxicity of i.v. injection, erythrocyte hemolysis experiment, and rabbit ear vein irritation test showed no toxicity for the docetaxel nanoemulsion. The docetaxel nanoemulsion led to a larger apparent distribution volume and area under curve than the docetaxel injection after i.v. administration to rats. The histopathological test of tumor further demonstrated the highly anticancer efficiency of the docetaxel nanoemulsion. Thus, the nanoemulsion is a promising delivery system for docetaxel with highly anticancer efficiency and low toxicity.
authors.affiliation: Department of Pharmacy, Chinese PLA General Hospital, Beijing, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Li
authors.forename: Lina
authors.initials: L
authors.lastname: Du
authors.forename: Chenyun
authors.initials: C
authors.lastname: Wang
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
authors.forename: Xingguo
authors.initials: X
authors.lastname: Mei
authors.forename: Yiguang
authors.initials: Y
authors.lastname: Jin
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity*; D019540:Area Under Curve; D001672:Biocompatible Materials; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy / Q000473:pathology; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D000077143:Docetaxel; D016503:Drug Delivery Systems; D004355:Drug Stability; D005079:Excipients; D006207:Half-Life; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D053758:Nanoparticles; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000473:pathology; D010316:Particle Size; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000633:toxicity*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001672:Biocompatible Materials; D005079:Excipients; D043823:Taxoids; D000077143:Docetaxel