TY - JOUR
T1 - Phosphatidylcholine embedded microemulsions
T2 - Physical properties and improved Caco-2 cell permeability
AU - Spernath, Aviram
AU - Aserin, Abraham
AU - Ziserman, Lior
AU - Danino, Dganit
AU - Garti, Nissim
N1 - Funding Information:
The authors wish to thank NutraLease Ltd. and the BSF (grant number 2003260) for their financial support.
PY - 2007/6/22
Y1 - 2007/6/22
N2 - The present study evaluates the effect of a solubilized model drug, diclofenac sodium salt (diclofenac), in our unique new U-type microemulsion system embedded with phosphatidylcholine (PC) in terms of microstructure transformations, physical properties of the system (viscosity, electrical conductivity), droplet sizes and shapes, and nucleation and growth of the droplets. The physical properties are correlated to the permeability of diclofenac through Caco-2 monolayer cells. The major findings reported are: (1) systems that are rich in surfactant and contain minimal oil phase form a microemulsion that enables high solubilization of diclofenac (20 wt.% diclofenac in the oil and surfactant concentrate can be fully diluted with water); (2) PC presence at the interface does not affect the size of the O/W droplets, while the presence of diclofenac at the interface decreases the O/W droplet size by an average of 50%; (3) diclofenac seems to increase incorporation of PC into the W/O interface; (4) diclofenac affects the physical properties of the microemulsion increasing the viscosity of the W/O microemulsion system and completely changing the conductivity profile of the system upon water dilution; (5) cryo-TEM images indicate that above 70 wt.% water the droplets are spherical; (6) diclofenac permeability through Caco-2 monolayer cells increases when PC is embedded into the interface.
AB - The present study evaluates the effect of a solubilized model drug, diclofenac sodium salt (diclofenac), in our unique new U-type microemulsion system embedded with phosphatidylcholine (PC) in terms of microstructure transformations, physical properties of the system (viscosity, electrical conductivity), droplet sizes and shapes, and nucleation and growth of the droplets. The physical properties are correlated to the permeability of diclofenac through Caco-2 monolayer cells. The major findings reported are: (1) systems that are rich in surfactant and contain minimal oil phase form a microemulsion that enables high solubilization of diclofenac (20 wt.% diclofenac in the oil and surfactant concentrate can be fully diluted with water); (2) PC presence at the interface does not affect the size of the O/W droplets, while the presence of diclofenac at the interface decreases the O/W droplet size by an average of 50%; (3) diclofenac seems to increase incorporation of PC into the W/O interface; (4) diclofenac affects the physical properties of the microemulsion increasing the viscosity of the W/O microemulsion system and completely changing the conductivity profile of the system upon water dilution; (5) cryo-TEM images indicate that above 70 wt.% water the droplets are spherical; (6) diclofenac permeability through Caco-2 monolayer cells increases when PC is embedded into the interface.
KW - Caco-2 monolayer cells
KW - Diclofenac
KW - Microemulsions
KW - Permeability
KW - Phosphatidylcholine
UR - http://www.scopus.com/inward/record.url?scp=34248651228&partnerID=8YFLogxK
U2 - 10.1016/j.jconrel.2007.02.014
DO - 10.1016/j.jconrel.2007.02.014
M3 - 文章
C2 - 17475359
AN - SCOPUS:34248651228
SN - 0168-3659
VL - 119
SP - 279
EP - 290
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 3
ER -