Characterization, in vitro cytotoxicity and cellular accumulation of paclitaxel-loaded lipid nano-emulsions.
Lipid nano-emulsions (LNEs) having a mean droplet size of approximately 50 nm were investigated as drug carriers for paclitaxel (TXL) to achieve its satisfactory loadings and to develop a pharmaceutically acceptable alternative to the current formulation, Taxol. TXL was incorporated into the LNEs at 2.0 mg/ml without changes in particle size or drug precipitation. In the cytotoxicity study, TXL-loaded LNEs had cytotoxicity to HeLa cells equivalent to that of TXL alone; the 50% growth inhibitory concentrations (IC(50)) of TXL-loaded LNEs and TXL alone were 1.53 +/- 0.23 nM and 1.76 +/- 0.08 nM, respectively. However, a cellular accumulation study using 1,6-diphenyl-1,3,5-hexatriene (DPH) as a fluorescent probe showed that the accumulation of DPH-loaded LNEs in HeLa cells was remarkably lower than that of DPH alone. These results indicated that LNEs were a useful vehicle for TXL, even though LNEs themselves could not be efficiently accumulated in HeLa cells.
Takegami
Shigehiko
S
Department of Analytical Chemistry, Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto, Japan. takegami@mb.kyoto-phu.ac.jp
Takara
Kohji
K
Tanaka
Shiori
S
Yamamoto
Kazuhiro
K
Hori
Masahiro
M
Yokoyama
Teruyoshi
T
Kitade
Tatsuya
T
D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000494:pharmacology; D002463:Cell Membrane Permeability; D004161:Diphenylhexatriene / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics; D004655:Emulsions / Q000737:chemistry* / Q000493:pharmacokinetics; D006367:HeLa Cells; D006801:Humans; D008055:Lipids / Q000737:chemistry* / Q000493:pharmacokinetics; D017239:Paclitaxel / Q000008:administration & dosage* / Q000494:pharmacology; D010316:Particle Size; D012995:Solubility
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D004161:Diphenylhexatriene; D017239:Paclitaxel