Paclitaxel drug delivery carrier and preparation method thereof
A delivery carrier, paclitaxel technology, applied in the preparation method of peptides, drug combinations, pharmaceutical formulations, etc., can solve the problems of limited paclitaxel effect, little development, and limited application of paclitaxel, so as to improve water solubility, solve poor water solubility, contain good sealing effect
Active Publication Date: 2021-06-08
INST OF URBAN AGRI CHINESE ACADEMY OF AGRI SCI
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Problems solved by technology
[0004] However, the existing technology has limited effect on enhancing the water solubility of paclitaxel, and few preparations similar to water-soluble drugs have been developed, which limits the application of paclitaxel
Method used
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Embodiment 1
[0044] 1. Raw materials and reagents
[0045] 1. Glyceryl monostearate, Kolliphor EL (polyoxyethylene (35) castor oil), lecithin, propanol, methylene chloride, 2nd generation polyamide-amine dendrimer, 3rd generation polyamide-amine Dendrimer, fluorenylmethoxycarbonyl-aspartic acid-4-tert-butyl ester, N,N-diisopropylethylamine, methanol, piperidine, ninhydrin, glycine, 1-hydroxybenzotriazole , N,N-diisopropylcarbodiimide, arginine, glycine, alanine and other organic reagents and materials are all commercially available products;
[0046] 2. The glass microspheres are owned by the inventor's laboratory, and the particle size distribution is 100-200 μm;
[0047] 3. DGRGGGAAAA is prepared by referring to the method of Example 1 of Chinese Patent CN 107365354 A. For the convenience of public reading, the present invention quotes it as follows:
[0048] Preparation of the amphiphilic polypeptide DGRGGGAAAA:
[0049] a. Weigh 1g of 2-cl resin (the degree of substitution of resin ...
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Abstract
The invention provides a paclitaxel drug delivery carrier and a preparation method thereof. The preparation method comprises the following steps of (1) dissolving glycerin monostearate, Kolliphor EL and lecithin in an organic solvent, adding glass microspheres, evaporating the organic solvent to dryness, and performing freeze drying to obtain film-formed glass microspheres; (2) dissolving paclitaxel in the organic solvent, then adding a mixed aqueous solution of polypeptide DGRGGGAAAAA and polyamide-amine dendrimers, performing uniform mixing and oscillation, evaporating the organic solvent to dryness, then performing freeze drying and resuspension by using a phosphate buffer solution; and (3) adding the product obtained in the step (2) into the product obtained in the step (1), performing ultrasonic treatment in a water bath, and then separating out the glass microspheres. The water solubility of the paclitaxel is obviously improved, the liposome with good encapsulation efficiency is prepared, the problem that in the prior art, the application of the paclitaxel is limited due to poor water solubility of the paclitaxel is solved, treatment of related tumors is facilitated, and wide application prospects are realized.
Description
technical field [0001] The invention belongs to the technical field of pharmacy and relates to the preparation of a drug carrier, in particular to a paclitaxel drug delivery carrier and a preparation method thereof. Background technique [0002] Paclitaxel is a natural terpenoid with the molecular formula C 47 h 51 NO 14 , which is extracted from the bark of the yew tree, has the advantages of broad anti-tumor spectrum and high therapeutic index, and is widely used in the treatment of various cancers. However, paclitaxel has poor water solubility, and its solubility in water is about 0.7mg / L [1] ; meanwhile, its oral bioavailability is low [2] , less than 2%, resulting in its clinical use only through intravenous injection. [0003] At present, paclitaxel preparations include liposomes, microspheres, microemulsions, nanoparticles and micelles, etc. These preparations address the defect of paclitaxel's low water solubility and improve the clinical application effect of p...
Claims
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IPC IPC(8): A61K9/127A61K47/42A61K47/34A61K31/337A61P35/00C07K7/06C07K1/14C07K1/06C07K1/04
CPCA61K9/1277A61K47/42A61K47/34A61K31/337A61P35/00C07K7/06
Inventor 王涛甘人友任茂智刘宏艳夏宇
Owner INST OF URBAN AGRI CHINESE ACADEMY OF AGRI SCI