Ohshima, Hiroyuki and Miyagishima, Atsuo and Kurita, Takurou and Makino, Yuji and Iwao, Yasunori and Sonobe, Takashi and Itai, Shigeru (2009) Freeze-dried nifedipine-lipid nanoparticles with long-term nano-dispersion stability after reconstitution. International Journal of Pharmaceutics, 377 (1-2). 180-184 .
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Official URL: http://www.sciencedirect.com/science/article/B6T7W...
Nifedipine (NI) is a poorly water-soluble drug and its oral bioavailability is very low. To improve the water solubility, NI-lipid nanoparticle suspensions were prepared by a combination of co-grinding by a roll mill and high-pressure homogenization without any organic solvent. The mean particle size and zeta potential of the NI-lipid nanoparticle suspensions were about 52.6 nm and −61.8 mV, respectively, and each parameter remained extremely constant during a period of 4 months under 6 °C and dark conditions, suggesting that the negative charge of the phospholipid, dipalmitoyl phosphatidylglycerol, is very effective in preventing coagulation of the particles. In order to assure the nano-order particle size of the suspensions in view of long-term stability, a freeze-drying technique was applied to the NI-lipid nanoparticle suspensions. The mean particle size of freeze-dried NI-lipid nanoparticles after reconstitution was significantly increased in comparison to that of the preparations before freeze-drying. It was found, however, that the addition of sugars (glucose, fructose, maltose or sucrose) to the suspensions before freeze-drying inhibited the aggregation of nanoparticles, suggesting that the long-term stability storage of freeze-dried NI-lipid nanoparticles after reconstitution would be overcome. In addition, freeze-dried nanoparticles with 100 mg sugar (glucose, fructose, maltose or sucrose) showed excellent solubility (>80%), whereas without sugar, as a control, showed low solubility (<20%). It was found that negatively charged phospholipids and sugars prevent coagulation of NI nanoparticle suspensions, and reproduce the nanoparticle dispersion after reconstitution; and remarkably increase the apparent solubility of nifedipine.
|Uncontrolled Keywords:||Nanoparticles; Long-term nano-dispersion stability; Freeze-dry; Sugar; Water solubility|
|Subjects:||Biomedical Science > Nanomedicine|
|Deposited On:||04 Aug 2009 10:34|
|Last Modified:||04 Aug 2009 10:34|
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