Hypocrellin nanometer preparation for actively targeting specific tumor cells as well as preparation method and application thereof

A technology of oleocanthal and tumor cells, applied in the field of nano-medicine, can solve the problems of poor metabolism, lack of biocompatibility, metabolic burden, etc., to improve encapsulation efficiency, increase targeting and success The effect of high rate and encapsulation rate

Active Publication Date: 2018-03-20
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Utilizing the above-mentioned carriers to wrap hypocrellin, although a nano-drug with good water solubility has been obtained, there are still defects. For example, the material of this type of drug carrier is an inorganic material. Capacitance, cannot be metabolized well in the body, may bring metabolic burden to the body
However, there is no public report on the use of transferrin-targeted modification of polylactic acid-glycolic acid / carboxymethyl chitosan nanoparticles for delivery of hypocretin photosensitizers for photodynamic therapy.
At the same time, polylactic acid-glycolic acid and carboxymethyl chitosan were used in the targeted nanoparticles to prepare nanoparticles to encapsulate hypocretin to improve the encapsulation efficiency. There is no public document

Method used

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  • Hypocrellin nanometer preparation for actively targeting specific tumor cells as well as preparation method and application thereof
  • Hypocrellin nanometer preparation for actively targeting specific tumor cells as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] The carboxymethyl chitosan (CMC) that takes 300mg, the polyvinyl alcohol (PVA) of 500mg is dissolved in 50mL ultrapure water, makes aqueous phase; Hypocretin A (HA) was dissolved in 5 mL of acetone as the organic phase, and the organic phase was added dropwise to the aqueous phase stirred at a high speed of 10000 rpm / min. After the dropwise addition, 50W ultrasonic dispersion was performed for 10min, and then placed on a magnetic stirrer and stirred at 1000rpm / min for 12h to evaporate the organic solvent. The remaining solvent is centrifuged at 13000rpm / min to remove unencapsulated HA, unreacted PLGA and CMC, and excess emulsifier, and the resulting precipitate is polylactic acid-glycolic acid / carboxymethyl chitosan encapsulated Hypocretin nanoparticles. Wash the nanoparticles, resuspend them in 50 mL of 0.5M NaCl activation buffer, add 20 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 30 mg of N-hydroxybutyl Imide was activated for 15 minutes, ...

Embodiment 2

[0035] Example 2 has the same raw materials and preparation method as Example 1, except that 100 mg of CMC, 300 mg of PVA, 100 mg of PLGA, 12 mg of hypocrellin and 125 mg of transferrin are used.

[0036] Hypocretin B, 2 mg / mL transferrin, and 0.2 mg / mL hypocretin B in the hypocretin nanoparticles actively targeting specific tumor cells obtained in this example, the solvent is water, and the encapsulation efficiency of hypocretin is 83%. %, the loading of transferrin was 80%.

Embodiment 3

[0038] Example 3 has the same raw materials and preparation method as Example 1, except that 500 mg of CMC, 100 mg of PVA, 500 mg of PLGA, 37.5 mg of Hypocretin C and 25 mg of transferrin are used.

[0039] The hypocretin nano-preparation actively targeting specific tumor cells obtained in this example contains 0.6 mg / mL hypocretin C, 0.5 mg / mL transferrin, and water as a solvent. The encapsulation efficiency of hypocrellin was 82%.

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Abstract

The invention discloses a hypocrellin nanometer preparation for actively targeting specific tumor cells as well as a preparation method and application thereof. The preparation is a transferrin modified polylactic acid-glycolic acid / carboxymethyl chitosan enveloped hypocrellin preparation; the final mass volume ratio of the active ingredients of hypocrellin in the preparation is 0.2 to 0.6mg / mL; the final mass volume ratio of the transferrin is 0.5 to 2mg / mL; the solvent is ultrapure water. The hypocrellin nanometer preparation for actively targeting specific tumor cells has the functions of actively targeting excessive expression transferrin receptor tumor cells, and has the advantages of good water dispersion effect, uniform particle diameter, good enveloping rate, high stability, high material safety performance and the like. Meanwhile, the preparation process is simple and convenient; the prepared nanometer preparation is a medicine preparation for actively targeting and transmitting hypocrellin type photosencitizers to various tumor cells.

Description

technical field [0001] The invention belongs to the technical field of nanomedicine, and in particular relates to a transferrin-modified hypocretin nano-preparation granule capable of targeting tumor cells overexpressing transferrin receptors, and a preparation method and application thereof. Background technique [0002] Photodynamic therapy (PDT) is a new type of medical technology, mainly used in the treatment of tumors and other diseases. Photodynamic therapy is considered to be the fourth cancer treatment after surgery, radiotherapy and chemotherapy. Since Dousherty et al. pushed photodynamic therapy into clinical research in the 1970s, photodynamic therapy has achieved remarkable results. At present, domestic and foreign research on photodynamic therapy is still focused on its anti-tumor application. In addition, photodynamic therapy has been further studied in the treatment of rheumatoid arthritis, macular degeneration, antibacterial, antiviral, etc. The three indi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/51A61K47/69A61K47/62A61K47/34A61K47/36A61P35/00
CPCA61K9/5146A61K9/5161A61K41/0057
Inventor 陈双林林羲闫淑珍
Owner NANJING NORMAL UNIVERSITY
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