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A kind of microcapsule embedding multivesicular liposome drug carrier and preparation method thereof

A multivesicular liposome and microcapsule technology, applied in the directions of microcapsules, capsule delivery, etc., can solve the problems of general biocompatibility, cross-contamination of drugs, differences in physical and chemical properties, etc., achieve smooth surface of microcapsules, reduce toxic and side effects , the effect of convenient operation

Active Publication Date: 2018-01-16
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, due to the differences in physical and chemical properties between different drugs, they may face problems such as drug cross-contamination when mixed in drug carriers
[0003] In addition, liposome-based drug carriers usually have good biocompatibility but are not very stable, while polymer-based drug carriers usually have good stability but poor biocompatibility.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0022] The present invention also relates to a preparation method of the above-mentioned microcapsule-embedded polyvesicular liposome drug carrier, the steps of the preparation method are as follows:

[0023] Step 10, using sucrose solution as the inner water phase, glucose and L-lysine solution as the outer water phase, and lipid-dissolved dichloromethane solution as the oil phase, high-speed homogenizing and emulsifying the inner water phase and the oil phase to form an initial phase After milking, add the external water phase, vortex emulsify to form a double emulsion, and then rotate to evaporate the dichloromethane to obtain the multivesicular liposome suspension;

[0024] Step 20, take quantitative multivesicular liposomes and disperse them in the sodium alginate solution, disperse evenly with the aid of ultrasonic waves, and then drop the sodium alginate solution dispersed in multivesicular liposomes into the chlorine Calcium alginate beads embedded with multivesicular ...

Embodiment 1

[0030] Example 1: prepare 7.5% (w / v) sucrose solution as the inner aqueous phase; prepare a solution containing 5% (w / v) glucose and 30mM L-lysine as the outer aqueous phase; prepare a solution containing 16.5mg / mL Soybean lecithin, 8mg / mL cholesterol, 8mg / mL triolein and 1mg / mL oleic acid in dichloromethane are used as the oil phase; mix the same volume of the internal water phase and oil phase, and stir on a high-speed homogenizer for 10min , with a rotating speed of 14,000 rpm, to prepare colostrum; add 9 mL of external aqueous phase solution to the colostrum, emulsify on a vortex suspension apparatus for 10 seconds, and prepare double milk. Subsequently, the double emulsion was transferred to a rotary evaporator, and the organic solvent was removed by rotary evaporation at 35° C. and 10 rpm. After centrifugation at 3500 rpm for 5 minutes, the multivesicular liposome suspension was obtained. The microsphere has a smooth surface, good dispersibility, good sphericity, an aver...

Embodiment 2

[0032] Embodiment 2: This embodiment is basically the same as Embodiment 1, except that the sodium alginate solution in the syringe pump is mixed with 2 mg / mL insulin solution. A microcapsule-embedded multivesicular liposome drug carrier system that distributes different drugs in different spaces is prepared, that is, MET is embedded inside the multivesicular liposome, and insulin is embedded outside the multivesicular liposome and inside the microcapsule. The drug loading capacity of MET and insulin in the multivesicular liposome drug carrier system embedded in microcapsules was 0.39% and 1.91%, respectively, and the encapsulation efficiency was 57.10% and 11.41%, respectively. The cumulative release of MET was 18.97% and 0% of insulin when the system was simulated in vitro for 4 hours; the cumulative release of MET and INS was close to 22% at 8 hours. It shows a sequential release phenomenon within a certain period of time.

[0033]The invention adopts the double emulsifica...

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Abstract

The invention provides a microcapsule-embedded multivesicle liposome drug carrier and a preparation method thereof, using sucrose solution as the inner water phase, glucose and L-lysine solution as the outer water phase, and lipid-dissolved methylene chloride solution For the oil phase, the inner water phase and the oil phase are homogenized and emulsified at high speed to form colostrum, then the outer water phase is added, vortex emulsified to form a double emulsion, and then the dichloromethane is evaporated by rotary evaporation to obtain a multivesicular liposome suspension; Multivesicular liposomes are dispersed into sodium alginate solution, dispersed evenly, and then dripped into calcium chloride solution through a high-pressure microcapsule forming device and a syringe pump to prepare calcium alginate embedded with multivesicular liposomes Glue beads. Finally, the gel beads and cationic polymer solution are formed into a film to obtain the sample; at least one of the multivesicular liposomes or the multivesicular liposomes in the microcapsules is loaded with drugs. The invention ensures the spatial distribution of different medicines, improves the long-term release and absorption of medicines, and reduces the toxic and side effects of simple use of medicines.

Description

【Technical field】 [0001] The invention relates to a microcapsule-embedded multivesicle liposome drug carrier and a preparation method thereof. 【Background technique】 [0002] In recent years, microcapsules / spheres and other particulate drug sustained-release systems have developed rapidly and have been widely used clinically. In addition, for many diseases, such as cancer, AIDS, malaria, multiple sclerosis, hypertension, etc., single drug therapy and drug sustained release system often cannot achieve the desired therapeutic effect, and drug combination therapy can pass through the diseased cells. Modulate different signaling pathways to maximize therapeutic effect. Therefore, combined with drug combination therapy and drug carrier system to achieve slow / controlled release of drugs, it can reduce the frequency of drug application and alleviate the suffering of patients. However, at present, drug sustained-release microcapsules / spheres often face problems such as drug burst ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/34
Inventor 刘源岗王士斌吴柯静陈莉李腾腾陈爱政吴文果
Owner HUAQIAO UNIVERSITY
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