Bionic high-density lipoprotein nanoparticles and preparation and application thereof
A high-density lipoprotein, bionic technology, applied in the field of bionic high-density lipoprotein nanoparticles and its preparation and application, can solve the problems of natural HDL particle size composition, difficulty in mass production, and restrictions on wide application, etc. Achieve the effect of synthesis and easy acquisition, simple process and efficient treatment
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Embodiment 1
[0050] Example 1: Preparation of biomimetic high-density lipoprotein (rHDL) nanoparticles
[0051] 1.1 Screening of biomimetic nanocarriers
[0052] Dissolve phospholipids in a 1:1 mixed solution of chloroform and methanol, ultrasonically disperse, add docetaxel acetonitrile solution dropwise, mix well, rotate at 37°C to form a film, and put it into a vacuum drying oven for 12 hours to remove excess The organic solvent was hydrated in PBS, the probe was sonicated, the 5A solution dissolved in PBS was dropped, vortexed to mix, heated for 10 min, cooled for 10 min, and circulated 3 times to obtain biomimetic high-density lipoprotein nanoparticles.
[0053] Due to the different binding abilities of different phospholipids (DMPC, DPPC, HSPC, POPC) and 5A peptidomimetics, the stability of the formed nanoparticles may be different. Therefore, different phospholipids were changed according to the above method. Molecular simulations and thermodynamic studies were used to screen out t...
Embodiment 2
[0077] Example 2: Properties of rHDL drug-loaded nanoparticles
[0078] The optimal formulation for encapsulated docetaxel is: DMPC 15mg, 5A 5mg, DTX 0.6mg, PBS 1mL. Preparation process: Dissolve 15mg DMPC in a mixed solvent solvent of methanol:chloroform (1:1), disperse by ultrasonic, add 0.6mg DTX solution dropwise, mix uniformly and rotate to evaporate to form a film, put it in a vacuum drying box to remove excess organic matter. Solvent, PBS with pH 7.4 was hydrated and sonicated for 10 minutes, 5 mg of 5A solution dissolved in PBS was added dropwise, vortexed to mix, and the DTX-sHDL nanoparticles were obtained by heating and cooling for 10 minutes for 3 times.
[0079] Optimal formulation for encapsulation of 10-hydroxycamptothecin (10-HCPT): 15 mg DPPC, 5 mg 22A, 0.6 mg 10-HCPT, PBS 1 mL. The preparation process is as follows: dissolving 15 mg of SM in a mixed solvent solvent of methanol: chloroform (1:1), ultrasonically dispersing it, adding 0.6 mg of 10-HCPT solution...
Embodiment 3
[0082] Embodiment 3: use high performance liquid chromatography, GPC gel chromatography column to measure rHDL
[0083] Using TSK-GEL SW gel column (300×7.5mm, 10μm); detection at 220nm, pH 7.4 PBS mobile phase at 0.7mL·min -1 At the flow rate, 20 μL of the nanoparticle solution was injected at room temperature. GPC gel chromatography analysis was performed on free 5A mimetic peptide, blank HDL and drug-loaded HDL, respectively. The results showed that the chromatographic peak when the retention time was about 10.6min was HDL. Compared with blank HDL, drug-loaded HDL retained a The time and peak area did not change significantly, which further indicated that the encapsulation of the drug did not change the structure of HDL and could still exist stably.
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