Characterization, in vitro cytotoxicity and cellular accumulation of paclitaxel-loaded lipid nano-emulsions

Lipid nano-emulsions (LNEs) having a mean droplet size of ∼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 w...

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Bibliographic Details
Published in:Journal of microencapsulation 2010-08, Vol.27 (5), p.453-459
Main Authors: Takegami, Shigehiko, Takara, Kohji, Tanaka, Shiori, Yamamoto, Kazuhiro, Hori, Masahiro, Yokoyama, Teruyoshi, Kitade, Tatsuya
Format: Article
Language:English
Subjects:
Antineoplastic Agents, Phytogenic - administration & dosage
Antineoplastic Agents, Phytogenic - pharmacology
Biological and medical sciences
Cell Membrane Permeability
cellular accumulation
cytotoxicity
Diphenylhexatriene - pharmacokinetics
Drug Carriers - chemistry
Drug Carriers - pharmacokinetics
Emulsions - chemistry
Emulsions - pharmacokinetics
General pharmacology
HeLa Cells
Humans
Lipid nano-emulsion
Lipids - chemistry
Lipids - pharmacokinetics
Medical sciences
paclitaxel
Paclitaxel - administration & dosage
Paclitaxel - pharmacology
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Solubility
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Summary:Lipid nano-emulsions (LNEs) having a mean droplet size of ∼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 (IC50) 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.
ISSN:0265-2048
1464-5246
DOI:10.3109/02652040903515482