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Synthesis of HSA-Biotin-DDA-TCPP molecule and application of HSA-Biotin-DDA-TCPP molecule as photodynamic therapeutic agent and nano-drug

A biotin-hsa-dda-tcpp and biotin-hsa-dda-tcpp-dox technology, applied in the field of medicine, can solve the problems of poor non-specific distribution, bioavailability, normal cells and tissue side effects, and achieve low cytotoxicity , good anticancer effect

Pending Publication Date: 2021-06-18
BINZHOU MEDICAL COLLEGE
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Problems solved by technology

Among them, chemotherapy is the main treatment method. Doxorubicin (Dox) is one of the most widely used chemotherapeutic drugs at this stage, but due to its non-specific distribution and poor bioavailability, it causes serious damage to normal cells and tissues. Toxic effects, especially to the heart, bone marrow, gastrointestinal tract, and nervous system

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  • Synthesis of HSA-Biotin-DDA-TCPP molecule and application of HSA-Biotin-DDA-TCPP molecule as photodynamic therapeutic agent and nano-drug
  • Synthesis of HSA-Biotin-DDA-TCPP molecule and application of HSA-Biotin-DDA-TCPP molecule as photodynamic therapeutic agent and nano-drug
  • Synthesis of HSA-Biotin-DDA-TCPP molecule and application of HSA-Biotin-DDA-TCPP molecule as photodynamic therapeutic agent and nano-drug

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Embodiment Construction

[0025] Specific embodiments of the present invention are given below to further describe the structure of the present invention, but it is not considered that the present invention is limited to the following embodiments.

[0026] The preparation method of the Biotin-HSA-DDA-TCPP aggregate of the present invention and the application as a drug carrier are realized through the following technical scheme:

[0027] (1) The synthetic method of Biotin-HSA-DDA-TCPP molecule of the present invention:

[0028] Synthesis of S1 molecule: Purify 1g HSA by dialysis to obtain 0.91g pure HSA, select a 250mL round bottom flask, add 17mg Biotin, 15mg EDC·HCl, 10mg NHS, add 100mL water for ultrasonic dissolution, and place in a 60°C oil bath Heating and stirring for 48 hours, observe whether there is precipitation, if there is no precipitation, add HSA. Accurately weigh 0.45 g of HSA and add it into a round-bottomed flask. After ultrasonic dissolution, continue to heat and stir in an oil bath...

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Abstract

The invention relates to synthesis of a Biotin-HSA-DDA-TCPP molecule, an aggregate of the Biotin-HSA-DDA-TCPP molecule, preparation of a Biotin-HSA-DDA-TCPP-Dox nano-drug and an in-vivo and in-vitro activity evaluation method, and belongs to the field of medicines. The preparation method comprises the following steps: firstly, synthesizing the Biotin-HSA-DDA-TCPP molecule from human serum albumin (HSA), biotin, 1, 12-diaminododecane (DDA) and TCPP through a three-step amidation reaction. The molecule is self-assembled in an aqueous solution to form the aggregate. A lipophilic anti-cancer drug adriamycin is entrapped by an organic solvent volatilization method to form the Biotin-HSA-DDA-TCPP-Dox nano-drug. The Biotin-HSA-DDA-TCPP aggregate has advantages of good biocompatibility, good stability and good photodynamic effect. The Biotin-HSA-DDA-TCPP-Dox nano-drug has the advantages of slow release with pH responsiveness and capability of well inducing apoptosis of cancer cells. Meanwhile, the Biotin-HSA-DDA-TCPP-Dox nano-drug can achieve the synergistic effect of the nano-drug and a photodynamic therapeutic agent, has good anti-tumor effects, and has very good application prospects.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the preparation of an aggregate with good biocompatibility, good stability and photodynamic therapy effect, and a stable drug-loaded aggregate and an in vivo and in vitro biological evaluation method. Background technique [0002] Cancer has always been a global public health problem that threatens the safety of human life. Traditional cancer treatment methods include radiotherapy, surgery and chemotherapy. Among them, chemotherapy is the main treatment method. Doxorubicin (Dox) is one of the most widely used chemotherapeutic drugs at this stage, but due to its non-specific distribution and poor bioavailability, it causes serious damage to normal cells and tissues. Toxic side effects, especially to the heart, bone marrow, gastrointestinal tract and nervous system. Therefore, targeted delivery of Dox to solid tumors is very important. Targeted drug delivery systems such as nan...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/42A61K47/64A61P35/00A61K31/704
CPCA61K31/704A61K41/0071A61K47/42A61K47/643A61P35/00A61K2300/00
Inventor 魏光成闫苗苗辛美秀
Owner BINZHOU MEDICAL COLLEGE
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