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Plant anti-cancer targeting nano-preparation, and preparation method thereof

A nano-preparation, plant-based technology, applied in the field of medicine, can solve the problems of slow dissociation of complexes, unstable carriers, limited tumor efficacy, etc., and achieve good stability.

Active Publication Date: 2012-09-26
AC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with polyoxyethylene castor oil, although both can increase the solubility of paclitaxel and have similar pharmacokinetics, the toxic and side effects of liposomes are significantly lower than the latter
[0008] As can be seen from the above description, the main disadvantages of the existing anticancer drug drug delivery system are: 1. The carrier is unstable in the body, such as liposomes are dispersed very quickly in the body, and the anticancer drug and the circulatory system in the body Albumin binding, so that the carrier actually only plays the role of anticancer drug solubilization and cannot play the role of drug carrier and carrier targeting in vivo; 2. Passive targeting: due to the size of drug-loaded nanoparticles In the range of 100 to 150 nanometers, most of the drug-loaded nanoparticles are easily swallowed by mononuclear macrophages in the body during circulation in the body, and accumulate in tissues such as liver, spleen, and lung, and have a certain effect on tumors in these tissues. Good curative effect, but limited curative effect on tumors in other parts; 3. The anticancer drug cannot form a stable complex with the carrier, and the drug is easy to dissociate into the blood and bind to the albumin; 4. Nano anticancer drugs are in the The stability in solution in vitro is only a few hours to a day, and the complex formed by anticancer drugs and albumin dissociates slowly

Method used

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  • Plant anti-cancer targeting nano-preparation, and preparation method thereof
  • Plant anti-cancer targeting nano-preparation, and preparation method thereof
  • Plant anti-cancer targeting nano-preparation, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 prepares paclitaxel / TPGS / hyaluronic acid / albumin nano-preparation

[0048] (1) Dissolve 500mg of human serum albumin freeze-dried powder and 500mg of hyaluronic acid with a molecular weight of 5000Da in 20mL of PBS buffer; adjust the pH of the solution to 5.5 to obtain an albumin / hyaluronic acid solution;

[0049] (2) Dissolve 50 mg of paclitaxel and 50 mg of TPGS in 1 mL of chloroform; add the paclitaxel solution to the above albumin / hyaluronic acid solution under stirring conditions to form colostrum;

[0050] (3) The colostrum is processed by a high-pressure homogenizer (9000-40000psi) to obtain a nanoemulsion. The nanoemulsion is transferred to a rotary evaporator and evaporated under reduced pressure at 30-45°C to quickly remove the organic solvent, and freeze-dried under sterile conditions to obtain a freeze-dried product. Powder; lyophilized powder is stable at room temperature for less than 10 hours after resuspended in saline. Measured by a nanome...

Embodiment 2

[0051] Embodiment 2 prepares paclitaxel / TPGS / hyaluronic acid-albumin nano-preparation

[0052] (1) Weigh 500 mg of human serum albumin freeze-dried powder and dissolve it in 20 mL of sterile water; add 400 mg of hyaluronic acid with a molecular weight of 5 KDa to the albumin solution, and dissolve the albumin completely under full stirring; then, use 0.1 N hydrochloric acid to adjust the pH of the solution to 5.5; EDCI, which is twice the number of moles of hyaluronic acid, was added to the above solution, and stirred overnight at room temperature; The reaction product of EDCI and EDCI was then freeze-dried; the above freeze-dried hyaluronic acid-albumin conjugate was dissolved in 20 mL of PBS buffer; the pH of the solution was adjusted to 5.5 to obtain an albumin / hyaluronic acid solution;

[0053] (2) Dissolve 50 mg of paclitaxel and 50 mg of TPGS in 1 mL of chloroform; add the paclitaxel solution to the albumin / hyaluronic acid solution under stirring conditions to form colos...

Embodiment 3

[0055] Example 3 Preparation of paclitaxel / TPGS / hyaluronic acid-albumin nano-preparation

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

[0057] Prepare hyaluronic acid active lipid first: dissolve 400 mg of hyaluronic acid (molecular weight 5KDa) in 10 mL of 0.1M MES buffer, add 1.2 times the molar number of hyaluronic acid EDCI, and 1.2 times the molar number of hyaluronic acid N -Hydroxysulfosuccinimide; stir and react at room temperature for 30 minutes to prepare hyaluronic acid succinimide active lipid;

[0058] Dissolve 500 mg of human serum albumin freeze-dried powder in 10 mL of sterile water, add it to the succinimide active lipid solution of hyaluronic acid; adjust the pH value to 7.0-7.2, and stir and react at room temperature for 60 minutes; after the reaction is completed Add it into a dialysis membrane with a molecular weight of 10,000, dialyze to remove unreacted reagents and reaction by-products; freeze-dry the hyaluronic acid-albumin solution a...

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Abstract

The invention discloses a plant anti-cancer targeting nano-preparation, and a preparation method of the nano-preparation. The nano-preparation comprises (by weight) 43-60% of human blood albumin, 1.5-7.5% of plant anti-cancer drug, 24-40% of hyaluronic acid with molecular weight of 3,000-1,800,000 Da, 3.5-15 % of nanoparticle stabilizer, and the balance of water. The preparation method includes preparation of hyaluronic acid-albumin conjugate; preparation of plant anti-cancer drug solution; and preparation of the targeting nano-preparation. The plant anti-cancer targeting nano-preparation has good stability and bio-targeting function.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a plant-based anti-cancer targeting nano-preparation and a preparation method thereof. Background technique [0002] Paclitaxel and docetaxel in plant drugs belong to broad-spectrum anticancer drugs and have been widely used in the treatment of malignant tumors such as breast cancer, ovarian cancer and non-small cell lung cancer. The main problems faced by this kind of anticancer drugs in the application process include low solubility, high toxicity and side effects, low bioavailability, and easy drug resistance. [0003] In order to solve the problem of low solubility, traditional formulations of this class of drugs require a large amount of solubilizers such as polyoxyethylene castor oil. However, this excipient can not only cause many side effects, such as vasodilation, hypotension, dyspnea, and severe allergies, but also the excipient does not have the targeting of cancer...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K45/00A61K47/42A61P35/00
Inventor 刘锋
Owner AC PHARMA
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