A preparation method of amphiphilic pectin-dihydroartemisinin nanoparticles
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A technology of dihydroartemisinin and nanoparticles, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, etc. problem, to achieve the effect of good biocompatibility, simple preparation method and small particle size
Inactive Publication Date: 2018-11-30
BEIJING FORESTRY UNIVERSITY
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[0005] The purpose of the present invention is to address the deficiencies in the prior art and provide a method for preparing novel amphiphilic pectin-dihydroartemisinin nanoparticles. PET-DHA can self-assemble into nanoparticles in an aqueous medium to solve the problem of DHA The problem of poor water solubility and low bioavailability, and avoiding the use of a large amount of chemical reagents, resulting in difficulties in reagent recovery, using pectin as a drug carrier, good targeting, high drug loading, and avoiding incomplete release and burst release of drugs toxic side effects on patients
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Embodiment 1
[0029] Example 1. Preparation of a new type of amphiphilic pectin-dihydroartemisinin nanoparticles:
[0030] (1) Acetylation of PET
[0031] Take a certain amount of PET (50%~80% esterification degree), slowly add glacial acetic acid, acetic anhydride and sulfuric acid, react for a period of time in an ice bath, then heat up to 50℃, stir until the solution is clear, the mixture is rotary evaporated, and washed with ethanol To neutrality, freeze-dry to obtain acetylated pectin powder A.
[0032] (2) Synthesis of PET-DHA
[0033] Take 0.1g of PET from (1), slowly add it to a 25ml round bottom flask containing 4ml of pyridine, and sonicate for 10min, stir to dissolve for 20min, then add 0.1g of activator 1-(3-dimethylaminopropyl)- to the solution 3-Ethylcarbodiimide hydrochloride (EDC), 0.02g catalyst 4-dimethylaminopyridine (DMAP), stirred for 30min, added 0.1g dihydroartemisinin, and reacted in water bath for 36h to obtain PET-DHA polymerization Things.
[0034] (3) Purification of PE...
Embodiment 2
[0038] Example 2. Preparation of a new type of amphiphilic pectin-dihydroartemisinin nanoparticles:
[0039] In this example, through the same synthesis method and steps as in Example 1, the esterification degree of pectin is (20%-50%), the dihydroartemisinin is 0.1g, and the measured particle size is 30-80nm.
Embodiment 3
[0040] Example 3. Preparation of a new type of amphiphilic pectin-dihydroartemisinin nanoparticles:
[0041] In this example, through the same synthesis method and steps as in Example 1, the esterification degree of pectin is (20%-50%), the dihydroartemisinin is 0.3g, and the measured particle size is 20-60nm.
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Abstract
The invention discloses preparation of novel amphipathic pectin-dihydroartemisinin nano particles, and belongs to the field of bio-pharmaceuticals and nano technologies. Pectin (PET) is adopted as a carrier, carboxyl (-COOH) of the pectin is combined with hydroxyl (-OH) of dihydroartemisinin through an ester bond, the mixture and 10-hydroxycamptothecine (HCPT) are dissolved in an organic solvent together through purification, and polymeric micelle is obtained; nano particles are prepared, and the hydrophobic drug entrapped pectin-dihydroartemisinin / 10-hydroxycamptothecine nano particles (PET-DHA / HCPT NPS) are prepared through the steps of ultrasonic treatment, centrifugation, washing, dialysis, freeze drying and the like. Compared with existing research, the pectin is converted into the nano drug carrier from a single auxiliary material or cross-linking agent, the nano particles with the pectin loaded with a hydrophobic drug are transmitted, targeting is good, good dispersity is achieved, the drug loading capacity is high, high stability and good biodegradability are achieved, toxicity is low, and the novel amphipathic nano drug has a slow release function and can inhibit growth of multiple cancer cells, and cancer cell apoptosis is achieved. The preparation technology and process are short in period, cost is low, operation is convenient, and wide industrial prospects are achieved.
Description
Technical field [0001] The invention belongs to the field of biopharmaceuticals and nanotechnology, and relates to a drug delivery system, in particular to the preparation of a novel amphiphilic pectin-dihydroartemisinin nanoparticle. Background technique [0002] Cancer of colon is the most common malignant tumor in Western Europe, North America and other developed countries, and it is also one of the nine common malignant tumors in my country. In the past 30 years, colon cancer in most countries or regions including my country The incidence rate is on the rise. In my country, males rank the fifth in deaths from malignant tumors and females rank the sixth in deaths from colon cancer. Colon cancer is the same as other cancers. It is a systemic disease with local manifestations. The 5-year survival rate is still hovering at 50%. Comprehensive treatment or appropriate adjuvant radiotherapy and chemotherapy are the most important clinical treatments, but not Can see exciting result...
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