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Placenta microenvironment targeted delivery probe as well as preparation method and application thereof

A microenvironment and placenta technology, applied in the fields of biomedical engineering and chemistry, can solve problems such as deficiency, and achieve the effects of reducing distribution and release, stabilizing structure, and reducing toxic and side effects

Active Publication Date: 2022-03-25
THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009]In summary, there is currently a lack of nanocarriers that can effectively avoid non-specific drug absorption by mothers and fetuses, and then achieve specific drug delivery and functional regulation of TB cells in the placenta system

Method used

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  • Placenta microenvironment targeted delivery probe as well as preparation method and application thereof
  • Placenta microenvironment targeted delivery probe as well as preparation method and application thereof
  • Placenta microenvironment targeted delivery probe as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Synthesis of S1, polyacetylimide grafted polyethylene glycol (PEG-PEI)

[0048] Polyethyleneimine-grafted polyethylene glycol (PEG-PEI) was synthesized by a two-step method. First, the terminal hydroxyl groups of monomethyl ether polyglycol were activated with carbonyldiimidazole, and then reacted with the amino groups of polyethyleneimine to generate PEG. -PEI. The specific operation is as follows: weigh monomethyl ether glycol (8.0 g, Mn=2 kDa) into a reaction flask, dry it in vacuum at 80° C. for 6 h, and add THF (60 mL) under an argon atmosphere to dissolve it. Weigh carbonyldiimidazole (CDI, 6.4g) and another reaction bottle, then slowly drop THF dissolved in mPEG-OH into the CDI bottle with a constant pressure dropping funnel, and stir the reaction overnight at room temperature. Distilled water (0.648 mL) was added to inactivate excess CDI, and stirring was continued for 30 min. Precipitate the solution into a large amount of cold ether, filter and dry in vacuo ...

Embodiment 2-4, comparative example 1-6

[0069] Compared with Example 1, Example 2-4 or Comparative Example 1-6 can be prepared by changing the dosage of polymer, drug and SPIO in Step S3 or omitting a certain step in Steps S3, S4, S5, S6, and S7 , see Table 1 below for details:

[0070] Table 1: Examples and comparative examples

[0071]

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Abstract

The invention discloses a placenta microenvironment targeted delivery probe as well as a preparation method and application thereof. A) a shell is a lipid bimolecular membrane which is modified by enzyme substrate polypeptide-PEG and is subjected to targeted disintegration under the action of an enzyme which is in contact with placenta tissue interstitial fluid and is highly expressed, and B) an inner core is a drug carrier which is modified by a marker antibody which is specifically and highly expressed on the surface of placenta trophoblast; and C) loading superparamagnetic ferroferric oxide SPIO nanoparticles, a small molecule drug for regulating and controlling the functions of placental trophoblasts, a therapeutic gene or a combination thereof in the drug carrier. The placenta microenvironment targeted delivery probe disclosed by the invention can effectively avoid non-specific drug absorption of other organs outside the placenta of a maternal body and a fetus, so that delivery and function regulation and control of a trophoblast specific drug in the placenta are realized.

Description

technical field [0001] The invention relates to the fields of chemistry and biomedical engineering, in particular to a placental microenvironment targeted delivery probe and its preparation method and application. Background technique [0002] Fetal growth restriction (FGR) refers to the failure of the fetus to achieve the maximum growth potential determined by its genetic factors under the influence of various harmful factors in utero. The main manifestation is that the fetal weight is lower than the tenth percentile of the average weight for gestational age, or two standard deviations lower than the average weight, which is one of the important causes of perinatal morbidity and death. The perinatal death rate of infants with FGR is 4-6 times that of infants with normal weight. Even if they survive, their physical and mental development will be hindered to varying degrees. The causes of IUGR are many and complex, but in various pathogenic models, it is believed that the oc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/42A61K47/10A61K47/34A61K47/68A61K31/7105A61K31/23A61P15/00B82Y5/00B82Y40/00G01N21/31
CPCA61K9/5169A61K9/5146A61K47/6843A61K31/7105A61K31/23A61P15/00B82Y5/00B82Y40/00G01N21/3103
Inventor 郭宇王伟伟华赟鹏颜彦青王晶
Owner THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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