PH/ROS response type nano-drug delivery system and preparation method

A nano-drug and delivery system technology, applied in drug delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of poor tumor permeability, uncontrolled release rate, low targeting, etc., achieve high-efficiency tumor killing effect, achieve target The effect of tropic drug release and cell uptake promotion

Pending Publication Date: 2021-07-30
NANCHANG UNIV
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0003] However, to date, most nanomedicines still face many challenges and are difficult to achieve satisfactory therapeutic effects
For example, low targeting, poor tumor penetration, non-selective drug release location, uncontrolled release rate, etc., hinder the further development and application of nanocarriers in the field of anti-tumor

Method used

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  • PH/ROS response type nano-drug delivery system and preparation method
  • PH/ROS response type nano-drug delivery system and preparation method
  • PH/ROS response type nano-drug delivery system and preparation method

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Embodiment 1

[0035] (1) First, Lys(Z)-NCA dissolved in DMF was dissolved in mPEG-NH 2 The benzyl group was deprotected by ring-opening polymerization as an initiator. Dried mPEG-NH 2 (1.0 g, 0.2 mmol) and Cbz-Lys-NCA (1.8 g, 6.0 mmol) were placed in a dry 50 ml glass reactor and 30 mL DMF was added. After stirring at 25° C. for 3 days, the reaction system was poured into 150.0 mL glacial ether three times to obtain pure mPEG-b-PLL(Z) precipitate (yield 88.6%). The degree of polymerization measured by 1H-NMR is 30, and the average molar mass of mPEG-b-PBLG is 12870 (mPEG5000-b-PLL(Z)7870). 1.6 g of the obtained mPEG-b-PLL(Z) was added to 10.0 mL of TFA and 0.8 mL of HBr / HOAc solution to remove its Cbz group. After stirring in an ice bath for 1 hour, the system was poured into 150.0 mL of ice ether and dialyzed against distilled water. The dialysis product was freeze-dried to obtain the mPEG-b-PLL product. After purification, the product was dried under vacuum at room temperature.

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Abstract

The invention discloses a pH / ROS responsive nano-drug delivery system and a preparation method thereof. MPEG-NH2 and Cbz-Lys-NCA are mainly used as raw materials for polymerization to form a prodrug skeleton, alpha-TOS and D (Boc) are used as carriers for synthesis of a polymer, DMA and the skeleton are conjugated, the polymer skeleton is modified by pHLIP, DOX is entrapped, pHLIP is modified on the polymer skeleton, and an anti-cancer drug is entrapped in the polymer skeleton. By integrating DMA and pHLIP, pH responsiveness and charge reversal to a tumor microenvironment are realized, and cellular uptake is promoted. The TOS is combined to a polymer, so that a mitochondrial electron transport chain is blocked, rapid generation of ROS is achieved, release of drugs and more TOS is promoted, and positive feedback release of the drugs is formed; and therefore, the killing effect on tumors is realized by releasing the wrapped anti-cancer drug; moreover, through the unique pH / ROS double-response type characteristic, stability can be kept in the blood circulation environment, drug release is increased in the tumor microenvironment, targeted drug release is achieved, targeted uptake of tumor cells to drugs can be improved, and the more efficient tumor killing effect is achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug carrier, a micelle and a preparation method and application thereof, in particular to a pH / ROS responsive nano drug delivery system and a preparation method. Background technique [0002] Malignant tumors are a common disease that seriously threatens human life and health. Drug therapy is one of the common means of anti-tumor treatment, and the types of drugs used and the routes of administration are constantly being updated. With the rise and development of nanotechnology in recent years, nanoparticle (NP)-mediated drug delivery has been widely pursued to develop safer and more effective treatments for many important diseases, especially in the research and development of nano-anticancer drugs. field plays a huge role. [0003] However, to date, most nanomedicines still face many challenges and are difficult to achieve satisfactory therapeutic effects. For examp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/62A61K47/54A61K47/69A61K31/704A61K41/00A61P35/00
CPCA61K47/62A61K47/545A61K47/6935A61K31/704A61K41/0004A61P35/00
Inventor 周陆苗雅昕张心怡张卫芳
Owner NANCHANG UNIV
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