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Sustained-release genistein from nanostructured lipid carrier suppresses human lens epithelial cell growth

International Journal of Ophthalmology(English edition) 2016年第5期9卷 643-649页

作者： Jin-Lu Liu Wen-Ji Zhang Xue-Dong Li Na Yang Wei-San Pan Jun Kong Jin-Song Zhang Department of Ophthalmology the Fourth Affiliated Hospital of China Medical UniversityEye Hospital of China Medical UniversityKey Lens Research Laboratory of Liaoning Province Department of Pharmaceutics School of PharmacyShenyang Pharmaceutical University

AIM： To design and investigate the efficacy of a modified nanostructured lipid carrier loaded with genistein（Gen-NLC） to inhibit human lens epithelial cells（HLECs） proliferation.·METHODS： Gen-NLC was made by melt emulsification method. The morphology, particle size（PS）, zeta potentials（ZP）, encapsulation efficiency（EE） and in vitro release were characterized. The inhibition effect of nanostructured lipid carrier（NLC）, genistein（Gen） and Gen-NLC on HLECs proliferation was evaluated by cell counting kit-8（CCK-8） assay, gene and protein expression of the proliferation marker Ki67 were evaluated with real-time quantitative polymerase chain reaction（RT-q PCR） and immunofluorescence analyses.·RESULTS： The mean PS of Gen-NLC was 80.12±1.55 nm with a mean polydispersity index of 0.11±0.02. The mean ZP was-7.14 ±0.38 m V and the EE of Gen in the nanoparticles was 92.3% ±0.73%. Transmission electron microscopy showed that Gen-NLC displayed spherical-shaped particles covered by an outer-layer structure. In vitro release experiments demonstrated a prolonged drug release for 72 h. The CCK-8 assay results showed the NLC had no inhibitory effect on HLECs and Gen-NLC displayed a much more prominent inhibitory effect on cellular growth compared to Gen of the same concentration. The m RNA and protein expression of Ki67 in LECs decreased significantly in Gen-NLC group.·CONCLUSION： Sustained drug release by Gen-NLCs may impede HLEC growth.

关键词： posterior capsular opacification genistein nanostructured lipid carrier human lens epithelial cells

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Solidification of nanostructured lipid carrier onto pellets by fluid-bed coating:preparation,in vitro characterization and bioavailability in dogs

Solidification of nanostructured lipid carrier onto pellets ...

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2012年中国药物制剂大会——中国药学会药剂专业委员会年会、亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Zhiqiang Tian.Jianping Qi,Wei Wu~* Department of pharmaceutics,school of pharmacy,Fudan University,Shanghai 201201,P.R.China

Previous studies have demonstrated that nanostructured lipid carrier(NLC)is a promising system for poorly water-soluble drugs delivery with improved *** NLC,however,is mostly prepared in a liquid form,which has some disadvantages:drug expulsion during storage,thermodynamic instability and high water content of NLC suspension. Therefore,the conversion of the NLC suspension into a dry product is necessary. The present work investigates fluid-bed coating as a new technique to prepare a pellet-based NLC of *** suspension was prepared by high pressure homogenization and the physicochemical properties of nanocarriers were *** were selected to entrap NLC as the matrix of coating *** electron microscopic was used to characterize the morphology of both the surface and cross-section of the solidified NLC pellets and using powder x-ray diffraction analysis and differential scanning calorimeter(DSC)identify the physical state of fenofibrate in solidified NLC *** capacity of the coating layer to entrap NLC and the redispersion of NLC from solidified NLC pellets were also ***,in vivo absorption of both solidified NLC pellets and NLC suspension in dogs was evaluated. Solidified NLC pellets were successfully prepared by a fluid-bed coating technique with good surface properties observing by scanning electron ***,obtained with small particle size and good size distribution,can be entrapped with PVP-K17 to get good quality of solidified NLC pellets in *** optimized solidified NLC pellets was prepared by single factor test,in which the coated weight was 100%,drug loading 5.6%in NLC,and NLC suspension agent 67%.Powder x-ray diffraction analysis and DSC confirmed nonexistence of crystalline fenofibrate in the *** redispersed readily from solidified NLC pellets at high rate within about 15 min to arrive high cumulative redispersion extent achieving over 90%.The particl

关键词： solidification nanostructured lipid carrier fluid-bed coating poorly water-soluble drugs bioavailability

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Antitumor activity and biodistribution of DHA-NLC formulation in sarcoma 180-bearing mice

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Journal of Chinese Pharmaceutical Sciences 2013年第4期22卷 348-354页

作者：张晓云乔华赵鹏倪京满史彦斌兰州大学药学院甘肃兰州730000 兰州大学第一医院药剂科甘肃兰州730000 兰州大学第一医院肿瘤科甘肃兰州730000

lipid nanoparticles have become attractive for its prominent properties recent years. In this paper, in vivo anti-tumor efficacy of nanostructured lipid carrier of dihydroartemisinin （DHA-NLC） were evaluated in sarcoma 180-bearing mice model through intraperitoneal （i.p.） administration. In vivo biodistribution was also investigated in Kunming mice bearing S180. Results demonstrated that the intraperitoneally injected DHA-NLC could significantly inhibit tumor growth at the dose levels of 20, 40 and 80 mg/kg, and their inhibition rates were 71.24%, 79.20% and 85.74%, respectively. The biodistribution of DHA after intraperitoneal injection of DHA-NLC in S180-bearing mice is remarkably different from the DHA solution. Therefore, DHA encapsulated in NLC does demonstrate superior anticancer effect to DHA suspension on S 180-bearing mice at the same dose and displayed a dose-dependent antitumor efficacy.

关键词： nanostructured lipid carrier Antitumor Sarcoma 180 Biodistribution

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