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A kind of core-shell sustained-release nanosphere and its preparation method

A nanosphere and slow-release technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of wide particle size distribution, poor slow-release effect, and difficulty in organic solvents, etc. problems, to achieve the effect of reducing the frequency of medication and side effects, solving the unsatisfactory sustained release effect, and maintaining effective drug concentration

Inactive Publication Date: 2020-11-06
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, in order to solve the above problems, many researchers have prepared paclitaxel into different sustained-release dosage forms, such as liposomes, microemulsions, microspheres, nanospheres, etc., which can effectively avoid the formation of polyoxyethylene castor oil and absolute ethanol mixed solvents. Allergenicity, reduce the autotoxicity of paclitaxel, and prolong the action time of the drug in the body, but there are still some shortcomings and problems that need to be solved urgently in the current research: ①Most paclitaxel sustained-release dosage forms use traditional polylactic acid (without functionalization) Or poly(lactic-co-glycolic acid) (PLGA) is used as a carrier, and paclitaxel is prepared into microspheres by emulsification method and precipitation method. Due to the autocatalytic effect (degradation is too fast), the drug release is too fast, the slow-release effect is not good and it is difficult to control; ②Due to the physical and chemical properties of traditional polylactic acid, slow-release microspheres / particles can only be prepared by methods such as emulsification, precipitation, and spray technology. The organic solvent in the preparation process is difficult to remove, and the particle size is large, difficult to control, and the particle size distribution is relatively large. Wide, it is difficult to enter the tumor tissue through blood vessels after injection; ③ Some dosage forms also use non-degradable carrier materials (such as non-degradable chitosan), which is difficult to remove in vivo after use, which brings safety hazards; ④ Currently public In the reported research on sustained-release nanoparticles or microparticles, since there is no surface treatment of the microparticles, there is an obvious burst release effect, which may cause the blood drug concentration in the human body to approach or exceed the poisoning level, resulting in obvious toxic and side effects, poor system stability, and easy to release. gather

Method used

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  • A kind of core-shell sustained-release nanosphere and its preparation method
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  • A kind of core-shell sustained-release nanosphere and its preparation method

Examples

Experimental program
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Embodiment 1

[0026] Example 1 Preparation of core-shell paclitaxel sustained-release nanospheres

[0027] 1. Weigh 60mg of lecithin, dissolve it in 20ml of chloroform, put it in a round bottom flask, and evaporate it on a rotary evaporator at a speed of 100rpm for 60min to obtain a uniform lipid dry film, add distilled water, and hydrate at 40°C 60 min, and ultrasonication in a water bath for 30 min to obtain a lecithin suspension (lecithin concentration in water is 0.1%, w / v), which is used as the water phase.

[0028] 2. Weigh 1.5 mg of paclitaxel and 15 mg of star-shaped cholic acid-functionalized polylactic acid, add 15 ml of acetone, stir to dissolve, and use it as the organic phase.

[0029] The star-shaped cholic acid functionalized polylactic acid can be synthesized according to the method reported in the literature, and the synthesis method used in this example is:

[0030] ① Weigh 0.8g (1.96mmol) of cholic acid and 4.2g (29.4mmol) of DL-lactide (molar ratio is 1:15), and put the...

Embodiment 2

[0044] 1. Weigh 60mg of lecithin and disperse it in water by thin film dispersion method as the water phase.

[0045] 2. Weigh 1 mg of paclitaxel and 15 mg of star-shaped cholic acid-functionalized polylactic acid, add 15 ml of acetone, stir to dissolve, and use it as the organic phase.

[0046] 3. Add the organic phase dropwise to the water phase, then perform stirring and intermittent ultrasonic treatment in a water bath (100 s each time, 60 s intermittent, 3 cycles), stop the ultrasonic and continue magnetic stirring for 12 h, and pass through a 0.45 μm microporous membrane , centrifuged at high speed for 20min, discarded the supernatant, washed the precipitate three times with distilled water, and freeze-dried to obtain core-shell paclitaxel sustained-release nanospheres. The order is 60:15:1.

[0047] The determination methods of average particle size, polydispersity coefficient, surface morphology, drug loading and encapsulation efficiency are the same as in Example 1. ...

Embodiment 3

[0051] 1. Weigh 60mg of lecithin and distribute it in water by film dispersion method as the water phase.

[0052] 2. Weigh 0.8 mg of paclitaxel and 15 mg of star-shaped cholic acid-functionalized polylactic acid, add 15 ml of acetone, stir to dissolve, and use it as the organic phase.

[0053] 3. Add the organic phase dropwise to the water phase, then perform stirring and intermittent ultrasonic treatment in a water bath (each ultrasonic 60s, intermittent 30s, cycle 4 times), stop the ultrasonic and continue magnetic stirring for 12h, pass through a 0.45μm microporous filter membrane, centrifuged at high speed for 20min, discarded the supernatant, washed the precipitate three times with distilled water, and freeze-dried to obtain core-shell paclitaxel sustained-release nanospheres. The ratio is 75:18.75:1 in turn.

[0054] The determination methods of average particle size, polydispersity coefficient, surface morphology, drug loading and encapsulation efficiency are the same...

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Abstract

The invention discloses a core-shell sustained release nanosphere, which consists of a hydrophobic drug carrier, a hydrophobic core constituted by hydrophobic drugs adsorbed on the hydrophobic drug carrier and lecithin covering the hydrophobic core, wherein the hydrophobic drug carrier is star cholic acid functional polylactic acid; and the mass ratio of the lecithin to the star cholic acid functional polylactic acid to the hydrophobic drugs is (30-80) to (10-20) to 1. The core-shell sustained release nanosphere disclosed by the invention, by taking the star cholic acid functional polylactic acid as the hydrophobic drug carrier and covering the core with the lipidosome (the lecithin), has the advantages of being excellent in sustained release effect, biodegradable, good in biocompatibility, narrow in particle size distribution, stable in property, applicable to injection to parenteral drug delivery and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a core-shell sustained-release nanosphere and a preparation method thereof. The invention also relates to the use of star-shaped cholic acid-functionalized polylactic acid as a hydrophobic drug carrier in the core-shell sustained-release nanosphere new use. Background technique [0002] Paclitaxel is a diterpenoid compound isolated from Taxus genus Taxus. It has a unique anti-microtubule mechanism, which can induce and promote tubulin polymerization, microtubule assembly and microtubule stabilization, thereby preventing tumor cell growth. Growth, a broad-spectrum anticancer drug, can be used for the treatment of ovarian cancer, breast cancer, lung cancer, colorectal cancer, head and neck cancer, lymphoma, and brain tumor. [0003] Due to the low solubility of paclitaxel in water and many pharmaceutical solvents, currently commercially available paclitaxel i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K9/52A61K31/337A61P35/00
CPCA61K9/0002A61K9/5146A61K31/337
Inventor 刘红曾少奇陈勇
Owner HUBEI UNIV