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Drug-loaded mixed micelle

A technology of mixing micelles and loading drugs, which can be applied in drug combinations, pharmaceutical formulations, antineoplastic drugs, etc., can solve the problems of immature paclitaxel nanomicelle technology and the lack of ideal long-term stable nanomicelles. Affinity and endocytosis, easy quality control, good stability

Inactive Publication Date: 2013-03-13
HANGZHOU PUSH KANG BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the technology of paclitaxel nano-micelle is still immature, and there is no ideal long-acting and stable nano-micelle.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the synthesis of chitosan-cholic acid copolymer

[0030] As indicated by the synthesis figure 1 As shown, take chitosan (average molecular weight is 5000) 160mg (0.032mol), carbodiimide (EDC) 194.7mg, N-hydroxysuccinimide 116.3mg and deoxycholic acid 32mg (0.082mol) add 100mL In the reactor, add 40mL methanol and water mixed solution with a volume ratio of 1:1 in the reactor, stir for 24 hours, dialyze and freeze-dry the reaction solution to obtain the chitosan-cholic acid copolymer. The Fourier transform infrared spectrum (FTIR) of chitosan, deoxycholic acid and their graft copolymers are as follows: figure 2 shown. The results showed that cholic acid was successfully attached to the end group of chitosan.

Embodiment 2

[0031] Embodiment 2: the synthesis of chitosan-cholic acid copolymer

[0032] As indicated by the synthesis figure 1 As shown, take chitosan (average molecular weight is 10000) 300mg (0.03mol), carbodiimide (EDC) 180mg, N-hydroxysuccinimide 105mg and deoxycholic acid 11.8mg (0.03mol) add 100mL reaction In the reactor, add 40mL of methanol and water into the reactor with a volume ratio of 1:1 mixed solution, stir for 24 hours, dialyze and freeze-dry the reaction solution to obtain the chitosan-cholic acid copolymer.

Embodiment 3

[0033] Example 3: Preparation of single-component mPEG-PDLLA nanomicelles containing paclitaxel

[0034] Dissolve 100mg of mPEG-PDLLA (molecular weight: 4000) and 20mg of paclitaxel in 4mL of methanol, and rotate under reduced pressure at 60°C to form a film. After the film is formed, continue to rotate under vacuum for 1 hour, and then transfer to a vacuum drying oven to continue drying. After 12 hours of vacuum drying, add water and hydrate at 60° C. for 20 minutes in a rotary evaporator under normal pressure to obtain nanomicelles. The encapsulation efficiency of the micelles is 90.4%, the particle size is 32nm, and the surface charge is -8.9mV.

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Abstract

The invention discloses a drug-loaded mixed micelle comprising taxane medicaments, amphiphilic chitosan derivatives and polyethylene glycol polyester block copolymer. The invention further discloses a preparation method of the drug-loaded mixed micelle. The product does not contain polyoxyethylene castor oil and ethanol, reduces adverse drug reactions, increases security of drug clinic application; by adding the amphiphilic chitosan derivatives and the polyethylene glycol polyester block copolymer, the stability of the preparation is enhanced and drug loading and drug efficacy are increased; and the preparation process is simple and controllable, and the production can be expanded easily.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to polymer micelles carrying insoluble antitumor drugs, in particular to a polymer mixed micelles freeze-dried powder containing taxane-type insoluble antitumor drugs and a preparation method thereof. Background technique [0002] Taxane drugs (such as paclitaxel, docetaxel, etc.) are currently one of the most effective anti-tumor drugs clinically, and are widely used in the treatment of various tumors such as ovarian cancer, breast cancer, and lung cancer. Paclitaxel is a natural anti-tumor drug isolated from the bark of Taxus brevifolia. It was used in clinical research on ovarian cancer and breast cancer in 1983, and was approved by the US FDA in 1992. Docetaxel (docetaxel, docetaxel) is a taxane compound, which can be obtained by semi-synthesis from the non-cytotoxic precursor compound 10-deacylated baccatin II extracted from Taxus chinensis, 1998 Approved by the US FDA...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/36A61P35/00
Inventor 余波王丰王国营张晓敏孙之彬袁媛杨艳
Owner HANGZHOU PUSH KANG BIOTECH CO LTD
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