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Medicament carrying nano particles and preparation method and application thereof

A nanoparticle and drug technology, which is applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of filter clogging, patient drug administration impact, nanoparticle precipitation reduces drug stability and drug efficacy, etc., and achieves good water dispersion sexual effect

Inactive Publication Date: 2012-03-14
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The industrial scale preparation method described in these patents will cause filter clogging and the yield of paclitaxel is always lower than 30%. At the same time, it also faces the immunogenicity of HSA and the precipitation of nanoparticles during the injection process reduces drug stability and drug efficacy. The problem of making it have a certain impact on the patient's drug administration

Method used

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  • Medicament carrying nano particles and preparation method and application thereof
  • Medicament carrying nano particles and preparation method and application thereof
  • Medicament carrying nano particles and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: Preparation of polylactic acid-polyethylene glycol diblock copolymer blank nanoparticles

[0051] Accurately weigh 20mg of PLGA-mPEG into a 5mL tube, dissolve in 2mL of acetone, and slowly drop the acetone solution of the polymer into the aqueous solution at room temperature under a magnetic stirrer (1 drop / 10s, emulsifier A is added to the solution). After stirring for 24 hours, the organic solvent was evaporated and removed. With the volatilization of the organic solvent, the inner core solidified into balls to form polymer nanoparticles, which were filtered through a 0.22 μm aqueous phase filter to obtain a transparent blank nanoparticle solution, which was stored at 4°C.

Embodiment 2

[0052] Embodiment 2: Preparation of paclitaxel-loaded polymer nanoparticles

[0053] 8.0mg paclitaxel and 85.1mg polylactic acid-polyethylene glycol diblock copolymer, diblock molecular weight are 60,000 and 5,000 respectively, dissolve in 5mL acetone; Add acetone solution in the TPGS solution of 40mL 0.08%, then The mixture was processed under high pressure (30,000 psi) in a homogenizer (suitably sterilized) until a nanoemulsion was obtained; aseptically frozen to -30°C and lyophilized for 57 hours while warming to 35°C. The obtained powder containing 8.59% (w / w) paclitaxel was reconstituted with 0.9% sodium chloride aqueous solution to obtain a paclitaxel concentration of 2 mg / mL.

[0054] The obtained paclitaxel-encapsulated nano drug loading is 8.59 (w / w)%, the obtained preparation has an average value of 0.17 microns, pH 7.2-7.6, and stability greater than 24 hours.

Embodiment 3

[0055] Embodiment 3: Preparation of paclitaxel-loaded polymer nanoparticles

[0056] 10.1mg of paclitaxel and 67.8mg of poly(lactic acid-polyethylene glycol) diblock copolymer, the diblock molecular weights are 30,000 and 5,000 were dissolved in 4mL of acetone; acetone was added to 40mL of 0.05% TPGS solution, the mixture was under high pressure (30,000 psi) in a homogenizer (appropriately sterilized) until a nanoemulsion is obtained; freeze to -30°C under aseptic conditions and lyophilize for 57 hours while warming to 35°C. The obtained powder containing 12.96% (w / w) paclitaxel was reconstituted with 0.9% aqueous sodium chloride solution to obtain a paclitaxel concentration of 2 mg / mL.

[0057] The drug-loading capacity of the obtained paclitaxel-coated nanoparticles is 12.96%, and the obtained preparation has an average value of 0.16 microns, a pH of 7.2-7.6, and a stability of more than 24 hours.

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Abstract

The invention discloses medicament carrying polymer nano particles and a preparation method thereof in the technical field of pharmacy. The medicament carrying polymer nano particles contain medicaments and polylactic acid-methoxy polyethylene glycol (PLA-mPEG) or poly (lactic-co-glycolic acid)-methoxy polyethylene glycol (PLGA-mPEG). The molecular weight of the block polylactic acid (PLA) or the poly (lactic-co-glycolic acid) (PLGA) is 10,000 to 60,000, the molecular weight of the block methoxy polyethylene glycol (mPEG) is 2,000 to 5,000, and the block ratio of the PLA or the PLGA to the mPEG is (60:40)-(90:10). The preparation method of the nano particles avoids the defects of low medicament nano particle entrapment rate and serious burst release caused by using the conventional surfactant, complex removing steps and the like; and the medicament carrying polymer nano particles with high quality are synthesized by simplified processes and with relatively low cost.

Description

technical field [0001] The invention relates to a nano drug and a preparation method thereof, in particular to a biodegradable nano particle containing a diblock copolymer and a preparation method thereof. Background technique [0002] Paclitaxel is a diterpene component extracted and isolated from yew or short leaves. It has important broad-spectrum anti-tumor activity and can be used to treat ovarian cancer, breast cancer, non-small cell lung cancer, malignant black solid tumors and some other solid tumors. It is especially effective in the treatment of metastatic ovarian cancer and breast cancer, and is recognized as a very promising anticancer drug. At present, more than 50 countries have approved the sale of synthetic paclitaxel. According to the forecast of the National Cancer Institute (NCI), paclitaxel will become one of the first-choice anticancer drugs in the next 10-15 years. [0003] The chemical structure of paclitaxel is highly fat-soluble, soluble in organic ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/19A61K47/34A61K47/36A61K31/337A61P35/00
Inventor 程立华林标扬
Owner ZHEJIANG UNIV
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