Targeted amphipathic nano-drug microcapsule

A nano-drug and amphiphilic technology, applied in the direction of nano-drugs, microcapsules, nanocapsules, etc., can solve the problems of reduced water solubility of drug molecules, high synthesis cost, poor biocompatibility, etc., to achieve good biocompatibility, The effect of reducing toxic and side effects and stabilizing the structure

Inactive Publication Date: 2015-03-18
CHENGDU LVKE HUATONG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, due to the complex structure of the polymer in the star polymer, the prepared drug carrier has problems such as poor biocompatibility, decreased drug loading capacity, and reduced water solub

Method used

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  • Targeted amphipathic nano-drug microcapsule
  • Targeted amphipathic nano-drug microcapsule
  • Targeted amphipathic nano-drug microcapsule

Examples

Experimental program
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Embodiment 1

[0044] ① Preparation of azide small molecule initiator

[0045]Step 1: Dissolve 5 mL of 2-chloroethoxyethanol in 25 mL of butanone, and add 4.5 g of NaN to the solution 3 , 2.5gBu 4 NI, 10 mg of dicyclohexane-18-crown-6, the mixture was heated to boiling and stirred for 24 hours. The mixture was filtered and the precipitate was rinsed thoroughly with acetone. The resulting mixed solution is the crude product of the product, after the mixed solution was concentrated, at 90 o C was distilled to obtain the pure product. The resulting 2-azidoethoxyethanol 1 H NMR (CDCl 3 ): 3.70 (t, 2 H, C H 2 OH), 3.65 (t, 2 H, HOCH 2 C H 2 O), 3.56 (t, 2H, N 3 CH 2 C H 2 O), 3.37 (t, 2H, C H 2 N 3 ), and 2.56 (s, 1H, OH).

[0046] Step 2: Dissolve 2g of 2-azidoethoxyethanol and 5.09g of α-chloroacyl chloride in 30mL of dichloromethane prepared in step 1, transfer the reaction system to ice, and dissolve 6.8g of dicyclohexyl The carbodiimide was slowly added to the reaction ...

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Abstract

The invention discloses a targeted amphipathic nano-drug microcapsule which is prepared through following steps: (1) polymerizing phosphatidylcholine through an atom transfer radical polymerization method to obtain poly-phosphatidylcholine; (2) modifying the poly-phosphatidylcholine with a folic acid molecule; (3) polymerizing octadecyl glutamate carboxylic acid anhydride through a ring-opening polymerization method to obtain poly-octadecyl glutamate; (4) performing stem-grafting to the poly-octadecyl glutamate with adriamycin through a hydrazone bond; (5) performing a bond-connecting process to the poly-phosphatidylcholine and the poly-octadecyl glutamate in a click chemical manner to obtain a segmented copolymer; (6) dissolving the segmented copolymer in tetrahydrofuran and moving the solution to a dialysis bag, performing dialysis with pure water, and filtering a dialyzate through a filter membrane; and (7) freeze-drying a solution after filtration to obtain a medicine carrying micelle. The medicine carrying micelle has a double-layer core-shell structure of which an outer layer is hydrophilic poly-phosphatidylcholine and an inner layer is a drug molecule wrapping layer. The microcapsule belongs to nano-particles, can achieve targeted transmission of the drug and pH-sensitive releasing in cancer cells, is large in drug carrying amount and is good in stability. The targeted function can reduce toxic and side effects of the drug on normal tissue and organ.

Description

technical field [0001] The invention relates to a targeting amphiphilic nano drug microcapsule, in particular to a preparation method of a block polymer material drug carrier microcapsule with cancer cell targeting. The invention belongs to the field of polymer chemistry and polymer technology. Background technique [0002] Cancer has become the most important disease that endangers human health. One of the important methods to treat cancer is drug therapy. However, many anticancer drugs have defects such as insoluble in water and poor stability. For example, camptothecin, paclitaxel, doxorubicin, and 5-fluorouracil are difficult to be well utilized by organisms due to their poor solubility. Solving the problem of their water solubility is the key to the clinical application of such pharmaceutical preparations. In addition, most of the tumor treatment and diagnostic drugs have non-selective effects, and are often distributed in some normal tissues and organs, and the therap...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/48A61K31/704B82Y5/00C08G81/02A61P35/00
Inventor 不公告发明人
Owner CHENGDU LVKE HUATONG TECH
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