Nano-micelle drug carrier based on vitamin E derivative, nano-micelle drug composition as well as preparation method and application of nano-micelle drug composition

A technology of nanomicelles and derivatives, applied in the field of medicine, can solve the problems that the anti-tumor effect cannot be improved, cannot load enough drugs, and the hydrophobic inner core is not strong enough to achieve good P-glycoprotein inhibitory ability, Good anti-tumor effect, good biocompatibility effect

Active Publication Date: 2017-08-08
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, only the combination of TPGS-1K and TPGS-2K, due to the weak hydrophobicity of its hydrophobic core, cannot load enough drugs, and the drug load is small, and the anti-tumor effect cannot be improved

Method used

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  • Nano-micelle drug carrier based on vitamin E derivative, nano-micelle drug composition as well as preparation method and application of nano-micelle drug composition
  • Nano-micelle drug carrier based on vitamin E derivative, nano-micelle drug composition as well as preparation method and application of nano-micelle drug composition
  • Nano-micelle drug carrier based on vitamin E derivative, nano-micelle drug composition as well as preparation method and application of nano-micelle drug composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] In this example, vitamin E derivative nanomicelles (T1k2k-TOS) were prepared by the following method, which specifically included the following steps:

[0038] Weigh 1 mg TPGS 1K, 5 mg TPGS 2K, 3 mg α-TOS, and dissolve them in 15 mL of chloroform, remove the solvent by a rotary evaporator, and form a thin film in 1.5 mL of PBS (pH 7.4) at 45 °C in water 30 minutes, followed by ultrasound for 5 minutes, and filtered with a 0.22 μm filter membrane to obtain the vitamin E derivative nanomicelle system T1k2k-TOS.

[0039] The particle size of the vitamin E derivative nanomicelle was detected with a zetasizer Nano ZS90 laser dynamic light scattering instrument from Malvern Instruments, and the average particle size was 17.2 nm.

Embodiment 2

[0041] In this example, vitamin E derivative nanomicelles (T1k2k-TOS) were prepared by the following method, which specifically included the following steps:

[0042] Weigh 1 mg TPGS 1K, 7 mg TPGS 2K and 3 mg α-TOS, and dissolve them in 20 mL of chloroform, remove the solvent by a rotary evaporator, and hydrate the formed film in 2 mL of PBS (pH 7.4) at 45 °C 30 minutes, followed by ultrasonication for 5 minutes, and filtered through a 0.22 μm filter membrane to obtain the vitamin E derivative nanomicelle system T1k2k-TOS.

[0043] The particle size of the vitamin E derivative nanomicelle was detected with a zetasizer Nano ZS90 laser dynamic light scattering instrument from Malvern Instruments, and the average particle size was 64.3 nm.

Embodiment 3

[0045] In this example, the vitamin E derivative-based nanomicelle pharmaceutical composition T1k2k-TOS-DOX was prepared by the following method, which specifically included the following steps:

[0046] Weigh 1mg TPGS 1K, 5mg TPGS 2K, 2.5mgα-TOS and 0.6mg hydrophobic doxorubicin, and dissolve them in 15mL chloroform, remove the solvent by rotary evaporator, and form a thin film in 1.5mL PBS ( pH 7.4), hydration at 45° C. for 30 minutes, followed by ultrasonication for 5 minutes, and filtration with a 0.22 μm filter membrane to obtain a nanomicelle pharmaceutical composition system.

[0047] The zetasizer Nano ZS90 laser dynamic light scattering instrument of Malvern instrument company is used to detect the particle diameter of the nano-micelle pharmaceutical composition system based on vitamin E derivatives, and the results are as follows: figure 1 As shown, it can be seen that the average particle size is 23.6nm.

[0048] The drug-loaded nanomicelle T1k2k-TOS-DOX prepared i...

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Abstract

The invention provides a nano-micelle drug carrier based on a vitamin E derivative, a nano-micelle drug composition as well as a preparation method and application of the nano-micelle drug composition. The nano-micelle drug carrier based on the vitamin E derivative is a nano-micelle formed by D-alpha-tocopherol polyethylene glycol 1000 succinate, D-alpha-tocopherol polyethylene glycol 2000 succinate and alpha-tocopherol succinate; and the carrier entraps a hydrophobic anti-tumor drug to obtain the nano-micelle drug composition. The D-alpha-tocopherol polyethylene glycol 1000 succinate, D-alpha-tocopherol polyethylene glycol 2000 succinate and alpha-tocopherol succinate are matched with one another and cooperate, so that the formed nano-micelle is good in stability, is small and uniform in grain size, improves drug encapsulation efficiency, has relatively good P-glycoprotein inhibiting ability, has good anti-tumor effect, is small in toxicity to normal cells and has good biocompatibility. The preparation method is simple and is wide in application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a nano-micelle drug carrier based on a vitamin E derivative, a nano-micelle drug composition, a preparation method and an application thereof. Background technique [0002] In the past few decades, nanomedicine has gradually become a new option to improve the efficacy of chemotherapy. However, multidrug resistance remains a major obstacle in the fight against cancer. A major cause of transport-associated multidrug resistance is due to the overexpression of drug efflux pumps, such as P-glycoprotein (P-gp), which expels multiple drugs out of cells. Since currently widely used chemotherapeutic drugs such as doxorubicin, paclitaxel, and vinblastine are all substrates of P-glycoprotein, cancers with overexpression of P-glycoprotein have become a major challenge in clinical chemotherapy. It causes a decrease in intracellular drug accumulation by promoting the extracellular export, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/704A61K47/22A61P35/00
CPCA61K9/1075A61K31/704A61K47/22
Inventor 梁兴杰鲁斯兰·葛那底维奇·塔岗塔伊夫李婵陈士柱闻妍
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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