Nanometer imitated lipoprotein structure drug carrier, preparation method and application thereof
A lipoprotein and nanotechnology, applied in the direction of drug combination, pharmaceutical formulation, anti-tumor drugs, etc., can solve the problems of off-target cytotoxicity and non-overexpression, and achieve the goal of reducing surface charge, reducing affinity, and increasing in vivo stability Effect
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Embodiment 1
[0030] Example 1 Preparation of Taxol-loaded Lipomimetic Protein Structural Carrier.
[0031] (1) Weigh 60 mg of dioleoylphosphatidylethanolamine (DOPE), 5.7 mg of oleic acid (OA), 12 mg of cholesterol, 6 mg of paclitaxel, and 2 mg of stearylamine, dissolve in 10 mL of chloroform, and place in 100 mL In an eggplant-shaped bottle, evaporate to dryness under reduced pressure at 37 ºC to form a film, add 10 mL of phosphate buffer (pH 7.4, 0.02 mol / L), hydrate at 37 ºC for 30 min; sonicate the probe on an ice bath for 5 min to make lipid core fluid;
[0032] (2) Accurately weigh 8.4 mg bovine serum albumin and dissolve it with 1.68 ml phosphate buffer (pH 7.4, 0.02 mol / L) to form a 5 mg / mL protein solution. In step (2), slowly and stir the lipid core solution Add it to the above-mentioned drug-loaded lipid core solution, and incubate with slow stirring at 37°C for 8 hours to obtain a paclitaxel-loaded lipomimetic protein structure carrier (abbreviated as BSA-LC / DOPE-PTX) solution...
Embodiment 2
[0033] Example 2 Preparation of a structural carrier of a lipo-mimetic protein containing soybean lecithin component loaded with paclitaxel.
[0034] Refer to the preparation method in Example 1 to prepare the control lipid core containing paclitaxel loaded with soybean lecithin (LC / SPC-PTX) and the lipomimetic protein structure carrier containing soybean lecithin loaded with paclitaxel (BSA-LC / SPC-PTX) , the difference is that soybean lecithin (SPC) is used to replace DOPE and OA components in LC / DOPE-PTX, and the dosage of other components remains unchanged.
Embodiment 3
[0035] Example 3 Characterization of drug-loaded lipid cores.
[0036] 3.1 Particle size and Zeta potential of lipid core
[0037] Take an appropriate amount of freshly prepared paclitaxel-loaded lipid core and dilute with distilled water to an appropriate concentration. A Zetasizer-Nano ZS90 particle size and Zeta potential analyzer was used to investigate the particle size and distribution in the diluent, and to measure its Zeta potential. The results are shown in Table 1.
[0038] 3.2 Encapsulation efficiency and drug loading of lipid core
[0039] Adopt the method combining low speed and ultracentrifugation to separate free drug, measure the entrapment efficiency of paclitaxel in the lipid core, the results are shown in Table 1, and the specific steps are as follows:
[0040] (1) Take the sample solution first, dilute it with phosphate buffer (pH 7.4, 0.02 mol / L), put it in a centrifuge tube and centrifuge it at 1000r / min for 10 min to get the supernatant, repeat this op...
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