Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug
Abstract
Microemulsion systems composed of water, isopropyl myristate, PEG-8 caprylic/captzc glycerides (Labrasol((R))), and polyglyceryl-6 dioleate (Plurol Oleique((R))), were investigated as potential drug delivery vehicles for an amphiphilic model drug (diclofenac diethylamine). Pseudo-ternary phase diagram of the investigated system, at constant surfactant/cosurfactant mass ratio (Km 4:1) was constructed at room temperature by titration, and the oil-to-surfactant/cosurfactant mass ratios (O/SC) that exhibit the maximum in the solubilization of water were found. This allowed the investigation of the continuous structural inversion from water-in-oil to oil-in-water microemulsions on dilution with water phase. Furthermore, electrical conductivity (sigma) of the system at Km 1:4, and O/SC 0.250 was studied, and the percolation phenomenon was observed. Conductivity and apparent viscosity (eta') measurement results well described colloidal microstructure of the selected formulations, including gr...adual changes during their formation. Moreover, sigma, eta', and pH values of six selected microemulsion vehicles which differ in water phase volume fraction (phi(W)) at the selected Km and O/SC values, were measured. In order to investigate the influence of the amphiphilic drug on the vehicle microstructures, each system was formulated with 1.16% (w/w) diclofenac diethylamine. Electrical conductivity, and eta' of the investigated systems were strongly affected by drug incorporation. The obtained results suggest that diclofenac diethylamine interacts with the specific microstructure of the investigated vehicles, and that the different drug release kinetics from these microemulsions may be expected. The investigated microemulsions should be very interesting as new drug carrier systems for dermal application of diclofenac diethylamine.
Keywords:
microemulsion / caprylocaproyl macrogolglycerides / percolation / drug delivery / diclofenac diethylamineSource:
International Journal of Pharmaceutics, 2004, 271, 1-2, 11-19Publisher:
- Elsevier Science BV, Amsterdam
DOI: 10.1016/j.ijpharm.2003.10.037
ISSN: 0378-5173
PubMed: 15129969
WoS: 000189248000003
Scopus: 2-s2.0-1142297663
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Institution/Community
PharmacyTY - JOUR AU - Đorđević, Ljiljana AU - Primorac, Marija AU - Stupar, Mirjana AU - Krajišnik, Danina PY - 2004 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/529 AB - Microemulsion systems composed of water, isopropyl myristate, PEG-8 caprylic/captzc glycerides (Labrasol((R))), and polyglyceryl-6 dioleate (Plurol Oleique((R))), were investigated as potential drug delivery vehicles for an amphiphilic model drug (diclofenac diethylamine). Pseudo-ternary phase diagram of the investigated system, at constant surfactant/cosurfactant mass ratio (Km 4:1) was constructed at room temperature by titration, and the oil-to-surfactant/cosurfactant mass ratios (O/SC) that exhibit the maximum in the solubilization of water were found. This allowed the investigation of the continuous structural inversion from water-in-oil to oil-in-water microemulsions on dilution with water phase. Furthermore, electrical conductivity (sigma) of the system at Km 1:4, and O/SC 0.250 was studied, and the percolation phenomenon was observed. Conductivity and apparent viscosity (eta') measurement results well described colloidal microstructure of the selected formulations, including gradual changes during their formation. Moreover, sigma, eta', and pH values of six selected microemulsion vehicles which differ in water phase volume fraction (phi(W)) at the selected Km and O/SC values, were measured. In order to investigate the influence of the amphiphilic drug on the vehicle microstructures, each system was formulated with 1.16% (w/w) diclofenac diethylamine. Electrical conductivity, and eta' of the investigated systems were strongly affected by drug incorporation. The obtained results suggest that diclofenac diethylamine interacts with the specific microstructure of the investigated vehicles, and that the different drug release kinetics from these microemulsions may be expected. The investigated microemulsions should be very interesting as new drug carrier systems for dermal application of diclofenac diethylamine. PB - Elsevier Science BV, Amsterdam T2 - International Journal of Pharmaceutics T1 - Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug VL - 271 IS - 1-2 SP - 11 EP - 19 DO - 10.1016/j.ijpharm.2003.10.037 ER -
@article{ author = "Đorđević, Ljiljana and Primorac, Marija and Stupar, Mirjana and Krajišnik, Danina", year = "2004", abstract = "Microemulsion systems composed of water, isopropyl myristate, PEG-8 caprylic/captzc glycerides (Labrasol((R))), and polyglyceryl-6 dioleate (Plurol Oleique((R))), were investigated as potential drug delivery vehicles for an amphiphilic model drug (diclofenac diethylamine). Pseudo-ternary phase diagram of the investigated system, at constant surfactant/cosurfactant mass ratio (Km 4:1) was constructed at room temperature by titration, and the oil-to-surfactant/cosurfactant mass ratios (O/SC) that exhibit the maximum in the solubilization of water were found. This allowed the investigation of the continuous structural inversion from water-in-oil to oil-in-water microemulsions on dilution with water phase. Furthermore, electrical conductivity (sigma) of the system at Km 1:4, and O/SC 0.250 was studied, and the percolation phenomenon was observed. Conductivity and apparent viscosity (eta') measurement results well described colloidal microstructure of the selected formulations, including gradual changes during their formation. Moreover, sigma, eta', and pH values of six selected microemulsion vehicles which differ in water phase volume fraction (phi(W)) at the selected Km and O/SC values, were measured. In order to investigate the influence of the amphiphilic drug on the vehicle microstructures, each system was formulated with 1.16% (w/w) diclofenac diethylamine. Electrical conductivity, and eta' of the investigated systems were strongly affected by drug incorporation. The obtained results suggest that diclofenac diethylamine interacts with the specific microstructure of the investigated vehicles, and that the different drug release kinetics from these microemulsions may be expected. The investigated microemulsions should be very interesting as new drug carrier systems for dermal application of diclofenac diethylamine.", publisher = "Elsevier Science BV, Amsterdam", journal = "International Journal of Pharmaceutics", title = "Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug", volume = "271", number = "1-2", pages = "11-19", doi = "10.1016/j.ijpharm.2003.10.037" }
Đorđević, L., Primorac, M., Stupar, M.,& Krajišnik, D.. (2004). Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug. in International Journal of Pharmaceutics Elsevier Science BV, Amsterdam., 271(1-2), 11-19. https://doi.org/10.1016/j.ijpharm.2003.10.037
Đorđević L, Primorac M, Stupar M, Krajišnik D. Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug. in International Journal of Pharmaceutics. 2004;271(1-2):11-19. doi:10.1016/j.ijpharm.2003.10.037 .
Đorđević, Ljiljana, Primorac, Marija, Stupar, Mirjana, Krajišnik, Danina, "Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug" in International Journal of Pharmaceutics, 271, no. 1-2 (2004):11-19, https://doi.org/10.1016/j.ijpharm.2003.10.037 . .