Targeted hydrophobic antitumor drug nano preparation and preparation method thereof

A technology of anti-tumor drugs and nano preparations, applied in the field of medicine, can solve the problems of reduced drug content in filtrate, reduced product yield, large particle size distribution coefficient, etc., to achieve enhanced inhibitory effect, ensure blood drug concentration, and good stability Effect

Active Publication Date: 2016-03-23
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, the nano-preparation particles of CN201210142991 have a large particle size distribution coefficient and a wide particle size distribution, and after freeze-drying and reconstitution, due to the entanglement between the hyaluronic acid molecular chains of the modified human serum albumin, the particles are mutually aggregated, Adhesion, resulting in an in

Method used

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  • Targeted hydrophobic antitumor drug nano preparation and preparation method thereof
  • Targeted hydrophobic antitumor drug nano preparation and preparation method thereof
  • Targeted hydrophobic antitumor drug nano preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Preparation of paclitaxel-targeted anti-tumor nano-preparation

[0047] (1) Preparation of hyaluronic acid-albumin conjugate:

[0048] Add 2.7042g of hyaluronic acid (molecular weight 2kDa) and 4.4958g of human serum albumin (the molar number is 1 / 20 times of hyaluronic acid) into 27.0mL of sterile water to dissolve, adjust the pH of the solution to 5.5, then mix 12.9600g of EDCI and 29. Add 3584g Sulfo-NHS to the above solution to react for 15min, adjust the pH of the solution to 7.4, continue to stir and react at room temperature for 5h, after the reaction is completed, dialyze to remove unbonded hyaluronic acid, unreacted EDCI, Sulfo-NHS and other By-products, hyaluronic acid-albumin conjugates were obtained after freeze-drying;

[0049] (2) Preparation of carrier solution:

[0050] Dissolve 0.9720g of human serum albumin and 0.1080g of hyaluronic acid-albumin conjugate in 216.0mL of sterile water to obtain a carrier solution;

[0051] (3) Preparation of...

Embodiment 2

[0055] Example 2 Preparation of paclitaxel-targeted anti-tumor nano-preparation

[0056] (1) Preparation of hyaluronic acid-albumin conjugate:

[0057] Add 2.4575g of hyaluronic acid (molecular weight 3kDa) and 8.1711g of human serum albumin (3 / 20 times the molarity of hyaluronic acid) into 27.0mL0.01MMES solution to dissolve, adjust the pH of the solution to 5.5, and then add 6.2813g of EDCI Add 14.2291g of Sulfo-NHS to the above solution to react for 15min, adjust the pH of the solution to 7.4, continue to stir and react at room temperature for 4h, after the reaction is completed, dialyze to remove unbonded hyaluronic acid, unreacted EDCI, Sulfo-NHS and Other by-products, hyaluronic acid-albumin conjugates are obtained after freeze-drying;

[0058] (2) Preparation of carrier solution:

[0059] Dissolve 1.2754g of human serum albumin and 0.3189g of hyaluronic acid-albumin conjugate in 213.0mL of sterile water to obtain a carrier solution;

[0060] (3) Preparation of drug s...

Embodiment 3

[0064] Example 3 Preparation of paclitaxel-targeted anti-tumor nano-preparation

[0065] (1) Preparation of hyaluronic acid-albumin conjugate:

[0066] Add 1.4319g of hyaluronic acid (molecular weight 5kDa) and 3.1741g of human serum albumin (1 / 6 times the molarity of hyaluronic acid) into 18.0mL0.01MPBS to dissolve, adjust the pH of the solution to 5.4, then mix 1.6470g of EDCI and 3. Add 3579g Sulfo-NHS to the above solution to react for 15min, adjust the pH of the solution to 7.5, continue to stir and react at room temperature for 4h, after the reaction is completed, dialyze to remove unbonded hyaluronic acid, unreacted EDCI, Sulfo-NHS and other By-products, hyaluronic acid-albumin conjugates were obtained after freeze-drying;

[0067] (2) Preparation of carrier solution:

[0068] Dissolve 1.0594g of human serum albumin and 0.4606g of hyaluronic acid-albumin conjugate in 150.0mL of sterile water to obtain a carrier solution;

[0069] (3) Preparation of drug solution:

...

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Abstract

The invention relates to a targeted hydrophobic antitumor drug nano preparation. The nano preparation comprises a hydrophobic antitumor drug and a carrier in a mass ratio being 1: (4-32.5), wherein the carrier comprises 37.5wt%-95.3wt% of albumin and 4.7wt%-62.5wt% of a hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared from albumin and hyaluronic acid in a mole ratio being 1: (1-20). The preparation method of the nano preparation comprises steps as follows: preparing the hyaluronic acid-albumin conjugate; preparing a carrier solution; preparing a drug solution; preparing the nano preparation. The nano preparation has more uniform particle size distribution and good dispersability, is stable and avoids agglomeration, the particle size is nearly unchanged after freeze-drying and redissolving, and the yield is high after the nano preparation is filtered by a millipore filter (0.22 mu m), and the pharmacological function is good.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a targeted hydrophobic antitumor drug nano-preparation and a preparation method thereof. Background technique [0002] In most tumors, blood vessels grow rapidly and irregularly, and the internal lymphatic system clears slowly. There are tumor penetration enhancing factors, which make macromolecules and nanoparticles easy to stay inside the tumor, which is called "enhanced permeability and retention effect" (Enhanced Permeability and Retention, EPR). Due to the EPR effect, nano drug delivery system can be passively targeted to tumors, and has received more and more attention in the application of tumor targeted therapy. Ordinary nano dosage forms, such as liposomes, nanoparticles, etc., will be recognized by the human reticuloendothelial system in the plasma, which will speed up the plasma clearance of nano preparations and reduce their therapeutic effect. Therefore, surface-...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K47/42A61K31/337A61K31/4745A61K31/675A61K31/704A61K38/14A61P35/00
CPCA61K9/19A61K31/337A61K31/4745A61K31/675A61K31/704A61K38/14A61K47/42A61K38/13A61K31/436A61K9/0019A61K9/1075A61K47/22A61K47/26A61K47/02A61K47/10A61K47/24A61K47/36A61K9/5161A61K9/5169A61K9/5192
Inventor 刘锋赖树挺曹付春郑阳连远发
Owner AC PHARMA CO LTD
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