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Tumor targeted sericin micelle, and preparation method and application thereof

A sericin protein and tumor-targeting technology, which can be used in anti-tumor drugs, pharmaceutical formulations, preparations for in vivo experiments, etc., can solve the problems of IR780 photofading, low quantum yield, poor photostability, etc., and achieve excellent performance , excellent biocompatibility, non-toxic effect of degradation products

Active Publication Date: 2017-05-31
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, IR780 also has many defects in application, such as poor hydrophilicity, easy aggregation and quenching in aqueous solution, resulting in low quantum yield, and poor photostability, and free IR780 is prone to photofading (Jiang C, ActaBiomaterialia, 2015, 14 ,61-69)

Method used

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  • Tumor targeted sericin micelle, and preparation method and application thereof
  • Tumor targeted sericin micelle, and preparation method and application thereof
  • Tumor targeted sericin micelle, and preparation method and application thereof

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Embodiment 1

[0038] (1) Extraction of sericin: sterilize the shredded silkworm cocoons by ultraviolet light, add them to 0.02M sodium bicarbonate solution and boil for 30 minutes, filter to remove insoluble silk fibroin and other insoluble substances, and put the filtrate into the retentate A cellulose dialysis bag with a molecular weight of 8,000-14,000 Da is dialyzed in pure water for three days to remove ion salts, and then freeze-dried to obtain sericin.

[0039] (2) Preparation of sericin-cholesterol derivatives: Dissolve 1.5g sericin in 20mL dry DMSO, dissolve at 50°C for 2h, cool to 25°C; dissolve 0.3g cholesterol formyl chloride in 5mL dichloromethane, Add dropwise to the DMSO solution of sericin protein, use 0.3mL of anhydrous triethylamine as an acid-binding agent, react at 30°C for 24h under the protection of argon, remove methylene chloride by rotary evaporation, and first use 500mL of ethanol to precipitate to obtain silk Collin-cholesterol derivatives were redispersed in 200 mL...

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Abstract

The invention belongs to the technical field of biological medicine materials, and discloses a tumor targeted sericin micelle, and a preparation method and an application thereof. According to the method provided by the invention, with water soluble natural protein sericin having good biocompatibility and biodegradability as a raw material, an amphiphilic sericin derivative containing a hydrophobic cholesterol group is synthesized under a room temperature condition, folic acid is further coupled by a chemical reaction to prepare a targeted amphiphilic sericin derivative, and a drug-loaded nanometer micelle can be formed with a hydrophobic drug IR780 in an aqueous solution by means of the self assembly. The nanometer micelle system can effectively improve the stability of the drug in the blood circulation and reduce the toxic and side effects of the drug, thereby having a very good research value and application prospect in the preparation of tumor diagnostic agents or treatment drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and in particular relates to a tumor-targeted sericin micelle and a preparation method and application thereof. Background technique [0002] As a water-soluble glycoprotein, sericin is one of the important components of silk fibroin, which plays a role in binding silk fibroin fibers. Traditionally, sericin is often regarded as a waste product of the silk industry. In recent years, with the in-depth research on sericin, this former silk industrial waste has been widely used because of its antioxidant properties, excellent moisturizing properties, promoting mammalian cell mitosis and low immunogenicity. It is used in the fields of pharmaceuticals, cosmetics, food and biotechnology (David L. Kaplan, et al, Progress in Polymer Science, 2008, 33, 998-1012). [0003] The molecular structure of sericin contains polar side chains and hydrophobic regions, has amphiphilic properties, and ca...

Claims

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Application Information

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IPC IPC(8): A61K47/66A61K47/54A61K31/404A61K9/107A61K41/00A61K49/00A61P35/00
CPCA61K41/0052A61K49/0021A61K49/0056A61K9/107A61K31/404A61K41/17
Inventor 张黎明邓立志杨立群郭伟洪胡彦锋李国新
Owner SUN YAT SEN UNIV
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