| Nowadays most anti - cancer drugs had no specific targeting and poor selectivity which led to weak therapeutic benefit. Developing drugs which could automatically release in schedule time at some speed into function organ or target organ as well as sustain efficiency concentration for long time were the important direction of scientists for the purpose of increasing therapeutic effects and decreasing toxic and side effects of drugs. With the enhancing research level and influences of nanotechnology to the drug research, it is possible to treat cancer with nanotechnology by adopting some specific target release drug system as carriers and then delivery the anticancer drugs or other cytotoxic drug to tumor tissue.Drug - loaded nanoparticles may promote drug absorption, construct new drug release system, improve drug delivery, attenuate the toxic side effects and reverse of multidrug resistance, which has been playing an enormous and unique role in anti - cancer research. Solid lipid nanoparticles ( SLN) combined the advantages and avoided the disadvantages of polymeric nanoparticles. 1 - ( Hex-ylcarbamoyl) -5 - Fluorouacil (HCFU) was the third derivative of 5 ?Fu, which had wide anticancer range, higher lipophil and therapeutic index, non -liver metabolism dependence, as well as no cross - resistance with 5 - Fu and other characteristics. According to the advantages of SLN and the merit of new drug HCFU, the present study was designed to produced HCFU - SLN by the method of solvent emulsification; examined and compared the anticancer activity of HCFU - SLN and free HCFU besides reversion effect of HCFU - SLN to CCL -187/HCFU cell. This study provided new ideas to produce safety, reasona-ble, effective anticancer drugs and research anti - cancer target therapy.Methods1. Preparation and in vitro release of HCFU - SLN1.1 Optimization HCFC - SLN technological processBy the method of uniform design to optimize various kinds of technological conditions and to confine the concentration of HCFC, lecithin, tristearin, Plu-ronic F68, ultrasound emulsification time as examination factors. Five levels were set for each factor according to required manners.1.2. Measurement of Zeta potential, entrapment efficiency and drug loading of HCFU - SLNQuantity of sample solution was moved into dialysis bag, after the conductance reduced to lower 50 μΩ, measured the Zeta potential by electrophoresis method. Separated and purified the nanoparticles by Sephadex G - 50 pillar chromatography. HCFU concentration was examined by reversed - phase HPLC, Chromatogram column; Spherisorb Waters(ODS,250mm x4. 6mm,5um) ;mobile phase; 0. 05 M potassium phosphate - methanol (30;70,v/v); flow rate; 1. 0 ml/min;inspected wave -length; 265 nm; in -sample; 20ul. Entrapment efficiency and drug loading of HCFU - SLN was calculated.1. 3 In vitro release of HCFU - SLNIn vitro release was processed by dialysis method. Quantity of sample solution was put into dialysis bag and moved in measuring flask with suitable phosphate buffer solution ( PBS). The flask was oscillated in constant temperature, extracted releasing solution, and then determined the content of HCFU released from HCFU - SLN in vitro using high performance liquid chromatography, the percentage of accumulative released drug was calculated.2. Anti - cancer activity of HCFU - SLN in vitro 2.1 Cell cultureCCL - 187 and Hela cells were cultured with RPMI1640 medium contained 10% fetal calf serum (contained 100 IU/ml penicillin and 100 ug/ml strepto-mycin) at 37℃ in a humidified atmosphere containing 5% carbon dioxide. The medium was changed after cultured 2 or 3 days and then subculture. The logarithm developing cells were used in present experiments.2. 2 Cytotoxicity comparison of HCFU - SLN and free HCFUA tetrazolium dye ( MTT ) assay was used in cytotoxicity experiments. Cells in different concentration were made into suspension and inoculated in 96- well plates. The cells were cultured for 24h and the comparison study of HCFU and HCFU -...
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