Polydithiothreitol nano system for antitumor drug delivery and preparation method and application of polydithiothreitol nano system for antitumor drug delivery

A technology of polydithiothreitol and dithiothreitol, which is applied in the field of polydithiothreitol nanosystems for anti-tumor drug delivery and its preparation, and can solve the problem of low water solubility of camptothecin and difficulty in preparing preparations, etc. problems, to achieve the effect of improving targeted delivery efficiency, stable properties, and improving bioavailability

Active Publication Date: 2019-03-08
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low water solubility of camptothecin

Method used

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  • Polydithiothreitol nano system for antitumor drug delivery and preparation method and application of polydithiothreitol nano system for antitumor drug delivery
  • Polydithiothreitol nano system for antitumor drug delivery and preparation method and application of polydithiothreitol nano system for antitumor drug delivery
  • Polydithiothreitol nano system for antitumor drug delivery and preparation method and application of polydithiothreitol nano system for antitumor drug delivery

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105]The synthesis of embodiment 1 polydithiothreitol

[0106] 1. Prepare polymer polydithiothreitol (PDTT) as drug carrier by the following method, comprising the following steps:

[0107] (1) Weigh 4.62g of dithiothreitol, dissolve it with 11mL of dried dimethyl sulfoxide, and keep a high vacuum inside the reaction vessel by freezing with liquid nitrogen;

[0108] (2) After returning to room temperature, raise the temperature to 90°C while keeping stirring, and after 10 hours of reaction, remove residual dimethyl sulfoxide and product water;

[0109] (3) Add ethyl acetate, heat to dissolve the solid crude product, and then cool and precipitate the solid at room temperature. After repeated repetitions, a white solid is obtained, which is polydithiothreitol.

[0110] 2. Results

[0111] The NMR spectrum of polymer PDTT is as follows figure 2 shown by figure 2 It can be seen that the signal at ~5.17ppm is the absorption peak of solvent heavy water, the signal at ~3.34ppm...

Embodiment 2

[0113] The synthesis of embodiment 2 polydithiothreitol

[0114] 1. Prepare polymer polydithiothreitol (PDTT) as drug carrier by the following method, comprising the following steps:

[0115] (1) Weigh 2.31g of dithiothreitol, dissolve it with 5.5mL of dried dimethyl sulfoxide, and keep a high vacuum inside the reaction vessel by freezing with liquid nitrogen;

[0116] (2) After returning to room temperature, raise the temperature to 100°C while keeping stirring, and after 20 hours of reaction, remove residual dimethyl sulfoxide and product water;

[0117] (3) Add ethyl acetate, heat to dissolve the solid crude product, and then cool and precipitate the solid at room temperature. After repeated repetitions, a white solid is obtained, which is polydithiothreitol.

[0118] 2. Results

[0119] The prepared polydithiothreitol has a stable structure, good biocompatibility, and can carry hydrophobic antitumor drugs, and a large number of disulfide bonds in the polymer make the sys...

Embodiment 3

[0120] The preparation of embodiment 3 graft medicine (polydithiothreitol grafted camptothecin)

[0121] 1. Prepare the graft drug by the following method, comprising the following steps:

[0122] (1) Take a clean and dry 250mL round bottom flask, weigh 2g of camptothecin, 2.11g of 4-dimethylaminopyridine (DMAP) and dissolve in 100mL of dichloromethane, and place it on a magnetic stirrer under the protection of argon. Stir for 10 minutes;

[0123] (2) Weigh phosgene 0.57g, quickly join in the round-bottomed flask, and the system continues to stir for 30min to carry out the acylation reaction;

[0124] (3) 0.9 g of polydithiothreitol was dissolved in 30 mL of tetrahydrofuran, placed in a constant pressure funnel, dropped into a round bottom flask under the protection of argon, and grafted at room temperature for 24 hours;

[0125] (4) Concentrate the solvent to 30mL by rotary evaporation, then drop into ethyl acetate, put it in a refrigerator at 20°C overnight, filter, rinse ...

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Abstract

The invention discloses a polydithiothreitol based drug-loading nano system and a preparation method and application thereof. A disulfide-bond-containing novel polymer namely polydithiothreitol controllable in composition and structure is prepared, and a nano carrier for targeted delivery of antitumor drugs is successfully created. Different antitumor drugs are grafted to hydroxide radicals of polydithiothreitol to form nanoparticle solution with particle size uniformity and stability through a nanoparticle preparation process such as a single-emulsion method and a nano precipitation method. The novel polymer namely polydithiothreitol is stable in property after drug grafting and high in biocompatibility and degradability and has GSH fast reduction responsiveness, targeted delivery efficiency of the nano carrier is improved, positioning controlled release of drugs in tumor cells is realized, bioavailability of hydrophobic drugs is improved, and a promising application prospect and a wide development space in the field of medicines are realized.

Description

technical field [0001] The invention belongs to the technical fields of functional polymer materials and biomedicine. More specifically, it relates to a polydithiothreitol nanosystem for antitumor drug delivery and its preparation method and application. Background technique [0002] Malignant tumors have become one of the major diseases that threaten human life and health. Although there are more than 90 kinds of anti-tumor drugs clinically, most anti-tumor drugs have disadvantages such as poor water solubility, poor controlled release effect, poor targeting, and strong tumor resistance. At the same time, these drugs can also bring serious toxic side effects to normal tissues and organs and reduce human immunity. [0003] Stimuli-responsive polymer systems have been widely used in the field of nanomedicine because they can respond to external environments such as temperature, light, enzymes, and pH. Among them, the reduction-response controlled release method has been re...

Claims

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Application Information

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IPC IPC(8): C08G75/0268A61K31/4745A61K31/519A61K31/56A61K45/00A61K47/69A61P35/00
CPCA61K31/4745A61K31/519A61K31/56A61K45/00A61K47/6935A61P35/00C08G75/0268
Inventor 吴钧康洋张鑫宇易恬琦
Owner SUN YAT SEN UNIV
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