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2013
|
vol. 60
|
issue 4
773-777
EN
Nanostructured lipid carriers (NLC) are stable colloidal formulations with notable advantages for drug delivery systems. Thanks to their physicochemical stability, biocompatibility, biodegradability and controlled drug release, they have received increasing attention for the last several years. The aim of the study was to prepare and characterize nanostructured lipid carriers (NLC). Both, the effect of the process parameters and the effect of the preemulsion composition on the NLC properties were investigated. In the work, different type of surfactants (i.e. decyl glucoside, Poloxamer188, Tween 80, sodium cholate) and their combinations were used to stabilize NLC dispersions. Moreover, several kinds of solid lipids (modified beeswax, gliceryl behenate, cetyl palmitate and berry wax) and liquid lipids (caprilic/capric triglyceride and decyl oleate) were applied. An ultrasonication method using a probe type sonicator was used to obtain NLC, and the time and energy of the process were modified throuhout. The physicochemical properties of the formulations, such as particle size, size distribution, polidispersity index were studied using the dynamic light scattering (DLS) method. The electrophoretic mobility of obtained particles was also measured, using the Zetasizer Nano ZS Malvern Instrument based on the Laser Doppler Velocimetry (LDV) technique. Knowing the value of electrophoretic mobility of particles for given conditions, the zeta potential was determined. The obtained results showed that the process parameters and the composition of the preemulsion had significant impact on the nanoparticles structure. The optimal formulations size ranged between 60 and 80 nm, and the value of their zeta potential was up to -30mV. The stability of these systems was further confirmed by macroscopic observation.
EN
Two O/W forskolin-loaded nano-emulsions (0.075% wt.) based on medium chain triglycerides (MCT) and stabilized by a nonionic surfactant (Polysorbate 80 or Polysorbate 40) were studied as forskolin delivery systems. The nano-emulsions were prepared by the PIC method. The mean droplet size of the nano-emulsions with Polysorbate 80 and Polysorbate 40 with oil/surfactant (O/S) ratios of 20/80 and 80% water concentration, measured by Dynamic Light Scattering (DLS), was of 118 nm and 111 nm, respectively. Stability of the formulations, as assessed by light backscattering for 24 h, showed that both nano-emulsions were stable at 25°C. Studies of forskolin in vitro skin permeation from the nano-emulsions and from a triglyceride solution were carried out at 32°C, using Franz-type diffusion cells. A mixture of PBS/ethanol (60/40 v/v) was used as a receptor solution. The highest flux and permeability coefficient was obtained for the system stabilized with Polysorbate 80 (6.91±0.75 µg · cm-2·h-1 and 9.21 · 10-3±1.00 · 10-3 cm · h-1, respectively) but no significant differences were observed with the flux and permeability coefficient value of forskolin dissolved in oil. The obtained results showed that the nano-emulsions developed in this study could be used as effective carriers for topical administration of forskolin.
EN
Nanostructured lipid carriers (NLC) composed of the substances generally recognized as safe (GRAS) were obtained by using a hot high-pressure homogenization technique (HPH). The influence of the number of homogenization cycles and concentration of a decyl glucoside surfactant on the NLC properties were studied. The system's stability was assessed by macroscopic observation, light backscattering and zeta potential measurements. NLC particle size was measured using dynamic light scattering (DLS). The kinetically stable formulations were loaded with forskolin and selected for in vitro drug permeation study using the Franz cell method. Concentration of forskolin in the receptor solution (i.e. ethanol/PBS mixture) was analyzed with high performance liquid chromatography (HPLC) with UV detection. The obtained results have shown that NLC formulations could be used as effective carriers for forskolin permeation through the skin.
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