Bufalin micellar nano-preparation and preparation method thereof
A technology of micellar nanometer and bufalin, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The screening conditions, cytotoxicity and other issues of new cancer drug candidate compounds, to achieve the effect of facilitating binding and drug release, improving bioavailability, and increasing water solubility
Active Publication Date: 2020-04-07
THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST +1
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[0004] The object of the present invention is to provide a kind of bufalin micellar nano-preparation and its preparation method, aiming to solve the problem that bufalin used alone does not meet the screening conditions of anticancer new drug candidate compounds, while the existing non-polypeptide PAMAM dendrimers Cytotoxicity induced by drug carriers and difficulty in adding functional groups
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[0020] In order to make the technical problems, technical solutions and beneficial effects to be solved by the present invention clearer, the present invention will be further described in detail below in conjunction with the embodiments. It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.
[0021] Due to poor water solubility, high toxicity, short half-life in vivo, and poor bioavailability, bufalin alone is difficult to use as a drug. However, conventional non-peptide dendrimer drug carriers are too cytotoxic, have high potential risks, and are not conducive to structural modification. Therefore, after a long-term research and development process, the inventors of the present invention have proposed a technical solution that bufalin is expected to be used in clinical medicine.
[0022] combine Figure 1-6 , an embodiment of the present invention provides a bufalin micelle n...
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Abstract
The invention provides a bufalin micelle nano-preparation. The bufalin micelle nano-preparation comprises bufalin, and a lipidized polypeptide micelle carrier which wraps the bufalin, and one moleculeof the lipidized polypeptide micelle carrier comprises one molecule of a hydrophilic unit and one molecule of a hydrophobic unit connected with the hydrophilic unit, wherein the hydrophilic unit is an asymmetric dendritic polypeptide polymer unit, the hydrophobic unit is a lipid unit, and the end of the dendritic polypeptide polymer unit carries a positive charge.
Description
technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a bufalin micellar nano-preparation and a preparation method thereof. Background technique [0002] Bufalin is a compound that has a good therapeutic effect on a variety of tumors. However, due to poor water solubility, high toxicity, short half-life in vivo, and poor bioavailability, bufalin alone cannot meet the screening requirements for new anticancer drug candidates. conditions, thus greatly limiting the clinical application of bufalin. [0003] Dendrimers (Dendrimers) are a new class of artificial macromolecules, which have great advantages as carriers for drug / gene delivery, such as extremely low polydispersity, regular high branching, multipotentialization, nanoparticle size , globular structure and definite molecular weight, etc. Most of the current literature reports use non-peptide PAMAM dendrimers as drug carriers. Although it shows great adva...
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IPC IPC(8): A61K9/107A61K31/585A61K47/18A61P35/00
CPCA61K9/1075A61K31/585A61K47/42
Inventor 陈四保哈兰德·帕勒荆晶
Owner THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST