Grafted retinol polymer and camptothecin compound adopting grafted retinol polymer as carrier
A retinol and polymer technology, applied in the field of preparation of camptothecin compounds, can solve the problems of large toxic and side effects, limited application, insoluble in water, etc., and achieve the goal of reducing toxic and side effects, reducing toxic and side effects, and improving enrichment Effect
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[0040] A preparation method of a camptothecin compound using a grafted retinol polymer as a carrier, comprising the following steps:
[0041] (1) dissolving camptothecin and grafted retinol polymer in dimethyl sulfoxide at a mass ratio of 1:5, 1:10 or 1:20;
[0042] (2) Put the solution obtained in step (1) into a dialysis bag, and after dialysis for 48 hours, freeze-dry the collected micellar solution to obtain the desired compound; wherein the molecular weight cut-off of the dialysis bag is 3500.
[0043] An application of a camptothecin compound grafted with a retinol polymer as a carrier, and the micelles can reduce the expression of protein hypoxia factor HIF-1-α in fibrotic liver tissue.
[0044] The application of a camptothecin compound grafted with a retinol polymer as a carrier, and the micelles can reduce the expression of the rate-limiting enzyme gene of the glycolysis pathway in fibrotic liver tissue.
[0045] Application of a camptothecin compound grafted with a...
Embodiment 1
[0067] Example 1 In vitro targeting experiment of grafted retinol polymer micelles
[0068] The rat liver was digested by in situ perfusion, and the primary rat hepatic stellate cells (HSC) and hepatocytes (HC) obtained by digestion were inoculated on 24-well plates, and high-glucose DMEM medium (containing 15%- 20% FBS, 1% double antibody P / S) at 37°C, 5% CO 2 Culture in the cell incubator; after 2 days of HC growth and 7 days of HSC growth, add Nile Red polymer nanomicelles and continue to culture for 2 hours, wash twice with phosphate buffered saline (PBS), add 2.5% glutaraldehyde Fix for 0.5h, wash twice with PBS, add 4',6-diamidino-2-phenylindole DAPI (1:600, V / V) for about 5min, then discard DAPI, wash twice, add appropriate amount of PBS Protected from light, use a fluorescence microscope to observe the uptake of retinol-targeted nanomicelles coated with Nile red (VA-PEG-PCL) and non-targeted nanomicelles coated with Nile red (PEG-PCL) by HSC cells and HC cells -PCL) ...
Embodiment 2
[0070] Example 2 Targeting experiment of grafted retinol polymer micelles in mice
[0071] Get 16 mice, 8 in each group are randomly divided into 2 groups; inject olive oil (control group) or 20% CCl into the mice through the abdominal cavity respectively 4 - olive oil (dose 2ml / kg) for acute liver injury; after two days of administration, the animals in each group were randomly divided into two groups, and the mice were injected with Nile Red VA-PEG-PCL and PEG through the tail vein respectively. -PCL micellar solution; the mice were killed three hours later, and the heart, liver, spleen, lung, and kidney tissues of each mouse were collected, and after homogenization, the fluorescence intensity of Nile Red in the tissue samples was detected to analyze the micellar drug in vivo Biological distribution, the results are as follows Figure 6 shown.
[0072] The mice used are male ICR mice of SPF level, weighing 20-25g, provided by Chengdu Dashuo Animal Co., Ltd.; CCl 4 It is a...
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