Liver-targeting high-density lipoprotein analogue nano-particles, preparation method thereof, and application thereof
A high-density lipoprotein and nanoparticle technology, applied in the field of liver-targeted high-density lipoprotein analog nanoparticles and their preparation, can solve the problems of blood pollution, high cost of ultracentrifugation to separate HDL, difficult plasma source, etc. Injury, prolong dosing interval, overcome the effect of source difficulty
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Embodiment 1
[0030] The preparation of embodiment 1HDL analog
[0031] 1.1 Preparation of blank complex
[0032] Put 40 mg of lecithin in a round-bottomed flask, dissolve it with 5 ml of dichloroethane and methanol (V:V=1:1), and after rotary evaporation at 37°C to form a film, add 2 ml of 250 mmol ammonium sulfate solution, dissolve in water and sonicate for 10 minutes, and then Incubate at 28°C for 1 hour, and sonicate the probe for 10 minutes. Finally, the suspension was passed through a Sephadex G-50 column, and the eluent was 50 mM PBS solution with pH=7.4, and the white part was collected to obtain a blank HDL complex.
[0033] 1.2 Preparation of drug complex
[0034] Dissolve 4mg of doxorubicin hydrochloride in 1ml of deionized water, slowly add it into the blank complex at a water bath temperature of 50°C, keep it for 30min, and then take it out. Add 2ml of PBS dissolved in 2mg of apolipoprotein A-I at room temperature, mix well, incubate at 37°C for 12h, then sonicate in a wate...
Embodiment 2
[0037] Embodiment 2HDL analog character
[0038] 2.1 Investigation on particle size and morphology of HDL analogues.
[0039] Measure the particle size with a particle size analyzer, the results are as follows figure 1 and figure 2 As shown, the average density diameter is 100nm, and the average number diameter is about 20nm, which is consistent with the size displayed by the transmission electron microscope.
[0040] 2.2 Investigation of encapsulation efficiency of HDL analogs
[0041] Take 500ul of the particle solution of Example 2.1 in a 10ml volumetric flask, add 100ul TritonX-100, constant volume, and then treat the blank HDL complex prepared in Example 2.2 in the same way at a wavelength of 480nm in a UV spectrophotometer as a control to measure its absorbance. Encapsulation efficiency and drug loading efficiency are calculated by formulas (1) and (2)
[0042]
[0043]
[0044] The results showed that the encapsulation rate of the drug complex was 80.5%, and th...
Embodiment 3
[0060] Embodiment 3 HDL analog antitumor activity
[0061] Experimental animals: Male BALB / c nu / nu male nude mice (Department of Experimental Animals, Shanghai Institute of Materia Medica, Chinese Academy of Sciences), week age: 6 weeks old, average 15-20 grams. They were raised in a constant temperature SPF laminar flow room at 25°C, with 12 hours of light and 12 hours of darkness alternately, free access to standard pelleted feed and drinking water.
[0062] Establishment of orthotopic implantation model of human liver cancer in nude mice:
[0063] The MHC97L tumor source of the human liver cancer model with high metastatic potential established by the Liver Cancer Research Institute was taken, immersed in normal saline, and cut into 2mm×1mm×1mm size for later use. Nude mice were anesthetized by intraperitoneal injection of 2.5 mg / kg pentobarbital, the surgical field was disinfected, the left costal margin was cut obliquely about 8 mm into the abdomen, the liver lobe was ta...
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