Sonodynamic sensitive liposome, pharmaceutical composition and use thereof
A technology of sonodynamics and liposomes, which is applied in drug combination, liposome delivery, antineoplastic drugs, etc., can solve the problems of short lifespan and short diffusion range, reduce toxic and side effects, facilitate industrial production, and simple preparation methods Effect
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Embodiment 1
[0110] Example 1: Preparation of doxorubicin sonodynamically sensitive liposomes
[0111] (1) Materials and dosage: (the dosage of 100ml liposome, the following table 1)
[0112] [Table 1]
[0113]
[0114] (2) Preparation method
[0115] Weigh various lipid materials, materials with long cycle characteristics and sound sensitizers according to the dosage in Table 1, dissolve in 200ml of chloroform:methanol (4:1) solution, and remove the organic solvent by rotary evaporation at 50-60°C , to obtain a film that is dry and evenly adhered to the bottom of the glass bottle. The obtained film was hydrated at 50-60° C. for 30 minutes with 220 ml of citric acid solution with pH=4.0 to form a uniform liposome solution. Then, extrude through a polycarbonate membrane, first through a polycarbonate membrane with a pore diameter of 200 nm, and then through a polycarbonate membrane with a pore diameter of 100 nm. The obtained liposomes were adjusted with an appropriate amount of sodi...
Embodiment 2
[0116] Example 2: Determination of Encapsulation Efficiency of Doxorubicin Sonodynamically Sensitive Liposomes
[0117] Take 1 ml of adriamycin sonodynamically sensitive liposome prepared in Example 1 in a 1.5 ml EP tube, centrifuge at 10000 r / min for 10 min. Take 0.2ml of the supernatant in a 10ml volumetric flask, permeate the membrane with methanol solution to make up the volume, and inject into high performance liquid chromatography (HPLC) for analysis (C18 column, Agilent SB-C18, 4.6×150mm, 1.8μm, methanol-acetonitrile - Phosphate buffer (25mM NH 4 h 2 PO 4 -30mM H 3 PO 4 ,pH 5.0) (5:2:3) as the mobile phase, 1.0ml min -1 , the detection wavelength is 233nm, the same below), and the drug content (C1) of adriamycin loaded in the liposome is 0.211mg; another 0.2ml of the non-centrifuged sonodynamic sensitive liposome sample of adriamycin is put in a 10ml volumetric flask , permeate the membrane with methanol solution and dilute to the scale mark, high performance liqu...
Embodiment 3
[0118] Example 3: In vitro sonodynamic sensitivity test of doxorubicin sonodynamically sensitive liposomes
[0119] Take 0.5ml of the doxorubicin sonodynamically sensitive liposomes prepared in Example 1 and put them into a cellulose acetate dialysis bag (cellulose acetate dialysis bag, MWCO 8-14kDa) (BioVision, Inc., batch number C413103001), and soak in 30ml The HEPES solution was magnetically stirred at 60r / min. Ultrasound therapy ( 2776, Chattanooge, USA) using ultrasound (1MHz, 1W / cm 2 ) irradiation, after 2 minutes of ultrasonication, take out 0.5ml of the release liquid and pass it through a 0.22μm filter membrane to determine the drug content in the release liquid by HPLC (C18 column, Agilent SB-C18, 4.6×150mm, 1.8μm, methanol- Acetonitrile-phosphate buffer (25mM NH 4 h 2 PO 4 -30mM H 3 PO 4 ,pH 5.0) (5:2:3) as the mobile phase, 1.0ml min -1 , detection wavelength 233nm). Samples not irradiated by ultrasound were used as controls, and the drug content was det...
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