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A kind of pH-sensitive drug-loaded particle and its preparation method and application

A drug-loading and particle technology, applied in the field of medicine, can solve problems such as low anticoagulant heparin modifiers

Active Publication Date: 2018-03-13
BENGBU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The low anticoagulant heparin modification has the activity of anti-tumor cell invasion and metastasis. Using this low anticoagulant heparin modification alone to prepare the drug-loaded microemulsion can not only target drug delivery, but also play a role in combined drug delivery. , this kind of drug-loaded microparticles has not yet been documented

Method used

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  • A kind of pH-sensitive drug-loaded particle and its preparation method and application
  • A kind of pH-sensitive drug-loaded particle and its preparation method and application
  • A kind of pH-sensitive drug-loaded particle and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 Preparation of low anticoagulant heparin

[0030] Dissolve 20 g of heparin sodium (molecular weight 1.2 to 2.8 Daltons) in 175 ml of deionized water, adjust the pH of the solution to 5 with 1N HCl, add sodium periodate (NaIO 4 ) 15g, the solution was adjusted to 500ml with deionized water, and the pH of the solution was adjusted to 5 with 1N HCl. Reaction at 4°C for 24h. Dialyze in deionized water to obtain 1.5 L of dialysate, add 32 ml of 10N NaOH aqueous solution, and react in the dark at room temperature for 3 h. Then sodium borohydride (NaBH 4 ) 1 g, after reacting at room temperature for 4 h, the solution was neutralized to pH 7.0. Add 2.54 L of ethanol, let it stand for 3 hours, precipitate out, and re-purify with ethanol, and dry the precipitated solid under reduced pressure to obtain 9.8 g of low anticoagulant heparin, with a yield of 49%. 1 HNMR such as figure 2 shown.

Embodiment 2

[0031] Embodiment 2 Preparation of low anticoagulant heparin modification

[0032] Pass 10 g of low anticoagulant heparin prepared in Example 1 through a resin column, add 20 mg of tributylamine to form a salt, evaporate under reduced pressure to obtain 13 g of heparin salt, add the salt-formed substance to 110 mL of DMF solvent, add 0.1 mL of acetic anhydride and 0.7 g dicyclohexylcarbodiimide (DCC), stirred and reacted at room temperature for 48 hours, added 30 mL of alkaline aqueous solution to terminate the reaction and hydrolyzed the product, filtered to remove solids, dialyzed to remove impurities, added 5 L of ethanol to the dialysate, and obtained a precipitate. The above precipitate is low anticoagulant heparin modification, 1 HNMR such as image 3 shown.

[0033] The low anticoagulant heparin modification (hereinafter referred to as heparin modification) involved in the following examples all use the product of Example 2.

Embodiment 3

[0034] The preparation of embodiment 3 camptothecin nanoparticles freeze-dried powder

[0035] Dissolve 4mg of camptothecin in 1mL of 0.00004% NaOH aqueous solution, add 8mg of modified heparin, and ultrasonically emulsify for 10min at 25°C and 20KHz ultrasonic conditions to obtain a mixed solution; pass the mixed solution through a 0.22μm microporous membrane to obtain a microemulsion with a particle size of 60-200nm; freeze-dry the microemulsion at -20°C to obtain a freeze-dried powder of camptothecin nanoparticles.

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Abstract

The invention relates to a pH-sensitive drug-loaded particle as well as a preparation method and application thereof. The drug-loaded particle is prepared by the following steps: dissolving camptothecin or a camptothecin derivative in an alkaline aqueous solution, adding a low-anticoagulant heparin modifier and ultrasonically processing so as to obtain a mixed solution; and conducting millipore filtration on the mixed solution, so that the drug-loaded particle is obtained. The drug-loaded particle, under slightly acid conditions, such as at pH value of 1.5-6.0, is under a gel state; the grain size of the gel is 1-3 [mu]m; and the gel, in the acid tissues of a human body, can be degraded to release the camptothecin or the camptothecin derivative, so that an anti-tumor effect is achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pH-sensitive drug-loaded particle and a preparation method and application thereof. Background technique [0002] Many insoluble drugs have significant pharmacological activity clinically, but due to poor water solubility, their bioavailability into the human body is low, and at the same time, they produce high toxicity and side effects. Nanoscale drug-loaded microemulsions can change the absorption and distribution of drugs in the human body, and control the release rate of drugs, making them ideal drug delivery carriers today. The emulsifiers used as carriers are mostly endogenous compounds in the human body, such as lecithin, bile acid; or artificially synthesized biodegradable polymer emulsifiers. Heparin belongs to sulfated glycosaminoglycans, which can be widely modified by hydrophobicity. This polysaccharide emulsifier can be used as a carrier for insoluble...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K31/4745A61K9/19A61P35/04A61P35/00A61P17/06A61P17/00A61K47/36
CPCA61K9/0019A61K9/0021A61K9/0043A61K9/0078A61K9/19A61K31/4745
Inventor 梁颖
Owner BENGBU MEDICAL COLLEGE
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