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PD-L1 targeted sorafenib-loaded PLGA nano preparation and preparation method thereof

A PD-L1, nano-formulation technology, applied in the field of biomedicine, can solve the problem of not being able to further promote the absorption of cancer cells

Pending Publication Date: 2021-05-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, passive targeting can only facilitate efficient localization of nanocarriers in the tumor stroma and cannot further facilitate their uptake by cancer cells

Method used

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  • PD-L1 targeted sorafenib-loaded PLGA nano preparation and preparation method thereof
  • PD-L1 targeted sorafenib-loaded PLGA nano preparation and preparation method thereof
  • PD-L1 targeted sorafenib-loaded PLGA nano preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of PD-L1 Targeted Loaded Sorafenib PLGA Nano-Preparation (referred to as PDL1-SRF-PLGA NPs)

[0043] 1. Weigh Sorafenib (SRF), dissolve in DMSO, and configure a concentration of 20mg / ml, weigh PLGA, dissolve in dichloromethane, and configure a concentration of 20mg / mL, vortex mix the SRF solution and the PLGA solution (volume Ratio 1:20), to obtain the organic phase.

[0044] 2. Weigh PVA and dissolve it in deionized water to obtain an aqueous phase with a concentration of 10 mg / ml.

[0045] 3. Take the organic phase with a pipette gun, quickly add it to the water phase (the volume ratio of the organic phase to the water phase is 1:15), ultrasonicate for 15 minutes to obtain an emulsion, stir with a magnetic stirrer for 4 hours, remove the organic phase, and the carrier material is precipitated Solidification forms nanoparticles.

[0046] 4. Centrifuge at 3000rpm to remove large-particle nano-preparation and unencapsulated Sorafenib to obtain Sor...

Embodiment 2

[0061] Example 2 Expression of PD-L1 in the tumor microenvironment of the human liver cancer cell line BEL-7402

[0062] 1. Dissect the BEL-7402 tumor-bearing mice, take out the tumor mass, remove blood clots, mucous membranes and vacuolar necrotic tissue, cut into small pieces, place them in a 70 μm sieve, dilute with 5% FBS-PBS, and place on ice Gently grind and sieve to make a single cell suspension.

[0063] 2. Collect the single-cell suspension in a sterile centrifuge tube, centrifuge at 500g at 4°C for 10 minutes, discard the upper turbid solution, resuspend the cell pellet with diluent, and wash twice by centrifugation;

[0064] 3. Resuspend the cell pellet in 100 μl of diluent, add 0.5 μl of rabbit anti-human PD-L1 antibody, mix well, and incubate at 4°C for 1 hour.

[0065] 4. Centrifuge and wash twice.

[0066] 5. Resuspend the cell pellet in 100 μl of diluent, add 0.5 μl of fluorescently labeled goat anti-rabbit secondary antibody, mix well, and incubate at 4°C fo...

Embodiment 3

[0069] Example 3 Performance testing of PD-L1 targeting loaded Sorafenib PLGA nano-preparation

[0070] The medicine was prepared with reference to Example 1.

[0071] 1. The particle size and polydispersity coefficient of PDL1-SRF-PLGA NPs were measured by laser particle size analyzer.

[0072] The results showed that the size of PDL1-SRF-PLGA NPs was 145.4±1.6nm, suitable for gathering in the tumor; the polydispersity coefficient was 0.120±0.006, and the distribution was relatively uniform.

[0073] 2. The morphology of PDL1-SRF-PLGA NPs was observed by counterstaining with transmission electron microscope.

[0074] Such as figure 2 As shown, the transmission electron microscope (TEM) image shows that the PDL1-SRF-PLGA NPs have a clear spherical structure, which is consistent with the particle size determined by the laser particle size analyzer.

[0075] 3. The encapsulation efficiency and drug loading of PDL1-SRF-PLGA NPs were detected by HPLC.

[0076] The encapsulati...

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Abstract

The invention relates to the technical field of biological medicines, and discloses a PD-L1 targeted sorafenib-loaded PLGA nano preparation and a preparation method thereof. The PD-L1 targeted sorafenib-loaded PLGA nano preparation comprises PLGA, sorafenib and an anti-PD-L1 single-chain antibody. The preparation method comprises the following steps of: preparing a sorafenib-loaded PLGA nano preparation, activating the tail end of PLGA, adding the anti-PD-L1 single-chain antibody for coupling, and freeze-drying the obtained PD-L1 targeted sorafenib-loaded PLGA nano preparation to obtain PD-L1 targeted sorafenib-loaded PLGA nano preparation freeze-dried powder. The PD-L1 targeted sorafenib-loaded PLGA nano preparation has the advantages that the insoluble small-molecular drug sorafenib is loaded into a macromolecular hydrophobic core, so that the water solubility of sorafenib is greatly improved. The anti-PD-L1 single-chain antibody is coupled on a shell, so that nanoparticles are delivered to tumors through active targeting and passive targeting. The PD-L1 targeted sorafenib-loaded PLGA nano preparation prepared by the method has an obvious anti-liver tumor effect.

Description

Technical field: [0001] The present invention relates to the technical field of biomedicine, in particular to a PD-L1 targeting loading sorafenib PLGA nano-preparation and its preparation method and application. Background technique: [0002] Primary liver cancer (PLC) is one of the most common malignancies, and the majority (70% to 90%) of primary liver cancers occurring worldwide are hepatocellular carcinoma (HCC) . The early symptoms of liver cancer are hidden, and most patients are already in the middle and late stages when they are diagnosed, and surgical intervention is not possible. According to statistics, 90% of patients with liver cancer need to receive drug treatment. In stark contrast to other cancers, HCC is resistant to systemic chemotherapy. Therefore, until 2007, there were no effective systemic treatments for these patients. Sorafenib becomes the first systemic therapy proven to improve survival in advanced HCC. [0003] Sorafenib is a tyrosine kinase i...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/68A61K31/44A61K9/19A61P35/00B82Y5/00B82Y40/00B82Y30/00
CPCA61K31/44A61K47/6937A61K47/6849A61K9/19A61P35/00B82Y5/00B82Y40/00B82Y30/00
Inventor 邱郑王旻程露刘利华费欢
Owner CHINA PHARM UNIV
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