Folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation and preparation method thereof

A technology of nanostructured lipids and doxorubicin hydrochloride, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of the lack of specific selectivity of tumor cells and the difficulty in obtaining therapeutic effects. , tumor targeting is not obvious and other problems, to achieve the effect of improving bioavailability, improving water insolubility, and prolonging residence time

Active Publication Date: 2018-11-23
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, commonly used chemotherapeutic drugs such as antibiotics doxorubicin and daunorubicin, anti-metabolite drugs methotrexate, 5-fluorouracil, anti-tumor animal and plant components paclitaxel, hydroxycamptothecin, etc., have significant anti-tumor activity, but Due to the lack of specific selectivity for tumor cells, the tumor targeting is not obvious. While killing tumor cells, it will cause irreversible damage to normal tissues and organs of the body and reduce the body's immunity. Therefore, it is difficult to achieve ideal therapeutic effects.

Method used

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  • Folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation and preparation method thereof
  • Folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation and preparation method thereof
  • Folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0047] The invention provides a nanostructured lipid carrier preparation co-loaded with doxorubicin hydrochloride and gambogic acid for targeted modification of folic acid, comprising the following components:

[0048]

[0049] Preferably, the weight part of the doxorubicin hydrochloride is 0.05-0.5 part.

[0050] Preferably, the weight part of the gambogic acid is: 0.05-0.5 part.

[0051] Preferably, the weight portion of the phospholipid-polyethylene glycol-folic acid is 0.01-0.48 parts.

[0052] Preferably, the solid lipids are stearic acid, behenic acid, glyceryl behenate, glyceryl monostearate, glyceryl palmitostearate, glyceryl myristate, glyceryl monopalmitate and lauryl One or more of glycerides.

[0053] Preferably, the liquid lipid is one or more of caprylic capric macrogol glyceride, caprylic capric triglyceride, isopropyl palmitate, isopropyl myristate, soybean oil and oleic acid kind.

[0054]Preferably, the fat-soluble emulsifier is soybean lecithin and / or...

Embodiment 2

[0072] Accurately weigh a certain amount of doxorubicin hydrochloride, add 2 mL of deionized water to dissolve, and weigh 2 parts by weight of poloxamer, add it to 9 mL of deionized water, and dissolve in a water bath at 74°C. Under magnetic stirring, 0.01 parts by weight of fully dissolved doxorubicin hydrochloride aqueous solution was added to the poloxamer, and mixed uniformly to form an aqueous phase together. Weigh 0.01 parts by weight of gambogic acid and dissolve it in 2mL of absolute ethanol. After the dissolution is complete, add 0.1 parts by weight of soybean lecithin to mix the two evenly; weigh 0.01 parts by weight of DSPE-PEG-FA and dissolve them in In DMSO, add preparation simultaneously as organic phase; In addition, take 0.1 weight part of stearic acid as solid lipid, 0.1 weight part of isopropyl palmitate as liquid lipid, add 1mL chloroform to make it dissolve, and ethanol solution and The chloroform solutions were combined and mixed to form an oil phase. Kee...

Embodiment 3-11

[0074] Examples 3-11 prepared formulations according to the components in Table 2.

[0075] Table 2 each component of preparation and parts by weight thereof

[0076]

[0077]

[0078] In order to further understand the medicine, the inventors also conducted studies on the antitumor activity and tumor targeting properties of the preparation prepared by the present invention. The test methods and evaluations are as follows:

[0079] 1. Determination of particle size, polydispersity index (PDI) and zeta potential of nanostructured lipid carriers

[0080] Take an appropriate amount of the prepared doxorubicin hydrochloride / gambogic acid nano-structured lipid carrier and folic acid targeted modified doxorubicin hydrochloride / gambogic acid nano-lipid carrier solution, dilute to a suitable concentration with deionized water, and place in In the laser particle size analyzer, the particle size, distribution and Zeta potential value were measured at 25°C. The results are shown ...

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Abstract

The invention discloses a folic acid targeted modified co-loaded doxorubicin hydrochloride and gambogic acid nanostructure lipid carrier preparation. In the embodiment, the preparation is prepared from 0.01 to 1 part of doxorubicin hydrochloride, 0.01 to 1 part of gambogic acid, 0.01 to 2 parts of phospholipid-polyethylene glycol-folic acid, 0.1 to 10 parts of solid lipid, 0.1 to 5 parts of liquidlipid, 0.1 to 3 parts of a lipid-soluble emulsifier and 1 to 10 parts of a water-soluble emulsifier. The invention further discloses a preparation method of the preparation. The nano preparation prepared by the method has the advantages of smaller particle size, even distribution, good stability and higher encapsulation efficiency; furthermore, the nano preparation improves water insolubility ofgambogic acid, prolongs drug residence time and has better active targeting; two drugs synergistically play curative effects, so that antineoplastic activity is enhanced, chemotherapeutic medicine dosage is reduced, and bioavailability is improved; meanwhile, multidrug resistance generated by the doxorubicin hydrochloride is inverted.

Description

technical field [0001] The invention relates to the field of pharmaceutical technology, in particular to a folic acid targeted modification co-carrying doxorubicin hydrochloride and gambogic acid nanostructured lipid carrier preparation and a preparation method thereof. Background technique [0002] According to the 2017 American Cancer Annual Report recently released by the American Cancer Society (ACS), for women, breast cancer, lung cancer and colorectal cancer will become the three most common cancers in 2017, and breast cancer will account for new 30% of cancer cases. At present, the clinical treatment of breast cancer is mainly based on chemotherapy, combined with targeted therapy, endocrine therapy and immunotherapy to reduce tumor metastasis and recurrence after mastectomy and improve the survival rate of patients. However, commonly used chemotherapeutic drugs such as antibiotics doxorubicin and daunorubicin, anti-metabolite drugs methotrexate, 5-fluorouracil, anti-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/352A61K31/704A61K47/54A61P35/00
CPCA61K9/5123A61K31/352A61K31/704A61K47/545A61P35/00A61K2300/00
Inventor 刘志东庞晓晨李楠李佳玮刘媛媛吴玉梅张兵卢鹏郭盼皮佳鑫祁东利
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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