Effects of sub-micro emulsion composition on cellular disposition of incorporated lipophilic drug / 浙江大学学报·医学版
Journal of Zhejiang University. Medical sciences
; (6): 523-529, 2013.
Article
en Zh
| WPRIM
| ID: wpr-252595
Biblioteca responsable:
WPRO
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the effects of sub-micro emulsion composition on cellular uptake and disposition of incorporated lipophilic drug.</p><p><b>METHODS</b>Sub-micro emulsions containing 10 % oil, 1.2 % lecithin and 2.25 % glycerol were prepared, and the fluorescent agent coumarin 6 was used as a model drug. The effects of oil types, co-surfactants and cationic lipid on uptake and elimination kinetics of 6-coumarin in HeLa cells were studied. The uptake mechanism of sub-micro emulsions was further investigated.</p><p><b>RESULTS</b>Oil type and Tweens had no influence on the cellular uptake. Modifications of surfactants with Span series increased the cellular influx, among which Span 20 with hydrophilic-lipophilic balance (HLB) value of 8.6 was the best enhancer. The intracellular drug level reached up to (46.09 ± 1.98)ng/μg protein which had significant difference with control group [(38.54 ± 0.34)ng/μg protein]. The positively charged emulsions significantly increased the uptake rate constant and elimination rate constant which were 4 times and 1.5 times of those in anionic groups, respectively. The uptake enhancement was also observed in cationic emulsions, cellular concentrations at plateau were (42.73 ± 0.84)ng/μg protein, which was about 3 times of that in anionic emulsions [(15.71 ± 0.74)ng/μg protein], when extracellular drug concentration kept at 100 ng/ml. Cationic emulsions delivered the payload mainly by direct drug transfer to contacted cells, while the negative ones depended on both drug passive diffusion and clathrin-mediated endocytosis of drug containing oil droplets which accounted for 20% of the intracellular drug.</p><p><b>CONCLUSION</b>Interfacial characteristic of sub-micro emulsions such as co-surfactants HLB as well as zeta potentials can influence lipophilic drug both in cellular uptake and elimination.</p>
Texto completo:
1
Base de datos:
WPRIM
Asunto principal:
Tensoactivos
/
Tiazoles
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Farmacocinética
/
Células HeLa
/
Cationes
/
Cumarinas
/
Emulsiones
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Endocitosis
/
Aniones
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
Zh
Revista:
Journal of Zhejiang University. Medical sciences
Año:
2013
Tipo del documento:
Article