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All-trans retinoic acid nano pharmaceutical preparation as well as preparation method and application thereof

A technology of all-trans retinoic acid and nano-medicine, applied in the field of medicine, can solve the problems of low biocompatibility, large side effects, and poor stability, and achieve the effect of low biocompatibility, large side effects, and poor stability

Active Publication Date: 2019-12-31
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] One of the objectives of the present invention is to provide a nano drug preparation of all-trans retinoic acid, which self-assembles the drug through the nano-carrier, and attaches the PD-1 monoclonal antibody to the outside of the nano-carrier, so that the drug can accurately reach the tumor site and reduce the risk of drug loss. Toxicity to organs, overcoming the shortcomings of all-trans retinoic acid, such as low biocompatibility, poor stability, large side effects, and poor targeting

Method used

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  • All-trans retinoic acid nano pharmaceutical preparation as well as preparation method and application thereof
  • All-trans retinoic acid nano pharmaceutical preparation as well as preparation method and application thereof
  • All-trans retinoic acid nano pharmaceutical preparation as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] An all-trans retinoic acid nanomedicine preparation, comprising: all-trans retinoic acid, PLGA-PEG loaded with all-trans retinoic acid, and PD-L1 monoclonal antibody attached to the surface of the PLGA-PEG.

[0046] Wherein, the all-trans retinoic acid is a hydrophobic drug, which is a derivative of vitamin A, and its structural formula is shown in formula I:

[0047]

[0048] The structural formula of PLGA-PEG is shown in formula II,

[0049]

[0050] The preparation method of the all-trans retinoic acid nano drug preparation comprises the following steps:

[0051] Step 1: preparing amphiphilic block polymer PLGA-PEG;

[0052] Step 2: Dissolve the block polymer PLGA-PEG and all-trans retinoic acid obtained in step 1 in an organic solvent and mix them uniformly, add water, centrifuge to remove unencapsulated all-trans retinoic acid, freeze-dry, that is Nanoparticles loaded with all-trans retinoic acid were obtained;

[0053] Step 3: dissolving, activating, dialyz...

Embodiment 2

[0070] The difference between this example and Example 1 is that the all-trans retinoic acid nano-pharmaceutical preparation is prepared with a feed ratio of 1:12.

[0071] image 3 A is the transmission electron micrograph of the all-trans retinoic acid nanomedicine not connected to the PD-L1 monoclonal antibody in this example; image 3 B is the transmission electron micrograph of the all-trans retinoic acid nano drug preparation in this example. It can be seen from the figure that the particles of all-trans retinoic acid nanodrugs and all-trans retinoic acid nanodrug preparations not connected to PD-L1 monoclonal antibody are spherical and have good dispersion.

[0072] Weigh 10 mg of freeze-dried nanoparticles, dissolve them in 50 mL of PBS solution with pH 7.4, measure their absorbance with a UV spectrophotometer, substitute into the corresponding standard curve, and calculate the corresponding encapsulation efficiency and drug loading. Weigh the freeze-dried powder of ...

Embodiment 3

[0082] (1) Investigate the cytotoxic effect of the all-trans retinoic acid nano drug preparation of the present invention.

[0083] DOK, CAL27 and KC cells were divided into 4×10 3 / hole, 4×10 3 / hole and 10×10 3 The density per well was seeded in a 96-well plate at 37°C with 5% CO 2 cultured in an incubator for 24 hours. After 24 hours, PLGA-PEG was added to the cell culture medium with a concentration gradient of 0 μm, 50 μm, 250 μm, 500 μm, and 750 μm, as well as all-trans retinoic acid (ATRA) and all-trans retinoic acid not linked to PD-L1 monoclonal antibody. Formic acid nanomedicine (ATRA-PLGA-PEG) and all-trans retinoic acid nanomedicine preparation (ATRA-PLGA-PEG-PD-L1), the concentration gradient is 0 μm, 5 μm, 25 μm, 50 μm, 75 μm. Subsequently, the cell viability was measured by the CCK8 (Cell Counting Kit-8) method with a time gradient of 24 hours, 48 ​​hours and 72 hours. Add 10% CCK8 to each well, incubate the culture plate in the incubator for 2 h, and measure...

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Abstract

The invention belongs to the medical field and particularly relates to an all-trans retinoic acid nano pharmaceutical preparation as well as a preparation method and application thereof. The all-transretinoic acid nano pharmaceutical preparation comprises an all-trans retinoic acid medicine molecule shown in a formula I, a nanocarrier entrapping the all-trans retinoic acid medicine molecule and aPD-L1 monoclonal antibody attached to the surface of the nanocarrier. According to the all-trans retinoic acid pharmaceutical preparation, on one hand, all-trans retinoic acid can inhibit oral dysplasia or oral squamous carcinoma cell proliferation and promote apoptosis; and on the other hand, nanoparticles have high permeability and a retention effect, the all-trans retinoic acid can be targetedat tumor parts through entrapment by the nanocarrier. Compared with all-trans retinoic acid technical, the nano pharmaceutical preparation takes effects quickly, has smaller toxic and side effects and has better effects.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an all-trans retinoic acid nano drug preparation, its preparation method and application. [0002] technical background [0003] Oral squamous cell carcinoma (OSCC), which can develop from oral dysplasia, is a common head and neck cancer with a 5-year survival rate of less than 60%. Traditional treatment methods such as surgery, radiotherapy and chemotherapy have brought great pain to patients. Therefore, it is urgent to develop safe and effective targeted therapy drugs. All trans retinoic acid (ATRA) is an effective anticancer drug for the treatment of various cancers such as acute promyelocytic leukemia, glioblastoma, and skin cancer. Our previous studies have found that all-trans retinoic acid plays an anti-tumor role in oral dysplasia and oral squamous cell carcinoma tissues, and can down-regulate the expression of programmed death-ligand 1 (PD-L1) protein; local Topical...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/34A61K47/68A61K31/203A61P35/00A61P1/02
CPCA61K9/5153A61K31/203A61K47/68A61P1/02A61P35/00
Inventor 陈潇婕周刚张雪琼汤明秀王欣
Owner WUHAN UNIV
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