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Preparation method and product of multi-layer composite dual-drug-loaded microsphere having pH responsivity

A multi-layer composite and dual-drug loading technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, can solve problems that are difficult to meet clinical requirements and achieve good sustained release effect, improve the therapeutic effect, reduce the effect of side effects

Active Publication Date: 2017-02-22
NANJING FORESTRY UNIV
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  • Claims
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Problems solved by technology

However, most traditional drug delivery systems can only deliver one drug. In recent years, although some drug delivery systems (such as nanoparticles, liposomes) have been able to successfully release more than one therapeutic drug, such as some small molecule drugs, such as siRNA , DNA and peptides, but due to the existence of complex auxiliary agents in the preparation process and the disadvantages of hydrophilic drugs adsorbed on the surface are easy to release quickly, there are some shortcomings in maintaining the co-delivery of these drugs, and it is difficult to meet clinical requirements

Method used

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  • Preparation method and product of multi-layer composite dual-drug-loaded microsphere having pH responsivity
  • Preparation method and product of multi-layer composite dual-drug-loaded microsphere having pH responsivity
  • Preparation method and product of multi-layer composite dual-drug-loaded microsphere having pH responsivity

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preparation example Construction

[0035] The invention provides a preparation method of a multi-layer double-loaded composite microsphere with pH response and a microsphere preparation thereof. Due to the distinguishable characteristics of the multilayer polymer microspheres, different drugs can be encapsulated (different drugs are selectively encapsulated between different polymer layers) and drug release can be controlled.

[0036] The self-assembly template of the drug-loaded microspheres is chitosan microspheres, and chitosan microspheres have become a drug-loaded microsphere preparation because of their characteristics such as targeting, sustained release, biodegradability and surface modification. Research hotspot, but because chitosan is a kind of natural degradable material with bioadhesiveness, the traditional preparation method has defects such as large size, poor dispersion of microspheres, and low encapsulation efficiency, so further improvement is needed. The present invention adopts A simple and ...

Embodiment 1

[0040] Weigh 0.12g chitosan and dissolve in 1% (v / v) acetic acid solution, stir and dissolve to obtain chitosan acetic acid solution. Tween-80 was added to the chitosan-acetic acid solution as the water phase. Dissolve 50 mg of paclitaxel in dichloromethane and add chitosan acetic acid solution and stir for 30 min to form oil-in-water (O / W) emulsion I. Add 0.1 mL of glutaraldehyde (concentration 25%) into liquid paraffin and drop into Span 80, stir for 30 min to form water-in-oil W / O emulsion II. After emulsion I and emulsion II were ultrasonically emulsified for 3 minutes, they were mixed and stirred for 40 minutes, and then heated to 40°C for 2 hours to crosslink and solidify.

[0041] Add 10 mL of a dextran-sodium hydroxide (sodium hydroxide concentration of 5 mg / mL) solution with a dextran concentration of 6 mg / mL dropwise into the chitosan microsphere suspension, and form a dextran / chitosan solution after 1 h of reaction. Sugar-loaded paclitaxel microsphere solution (DE...

Embodiment 2

[0044] Weigh 0.12g chitosan and dissolve in 1% (v / v) acetic acid solution, stir and dissolve to obtain chitosan acetic acid solution. Tween-80 was added to the chitosan-acetic acid solution as the water phase. An appropriate amount of 40 mg paclitaxel was dissolved in dichloromethane and added to chitosan acetic acid solution and stirred for 30 min to form oil-in-water (O / W) emulsion I. Add 0.1 mL of glutaraldehyde (concentration: 25%) into liquid paraffin and drop into Span 80, stir for 30 min to form water-in-oil W / O emulsion II. After emulsion I and emulsion II were ultrasonically emulsified for 3 minutes, the two were mixed and stirred for 40 minutes, then the temperature was raised to 40°C, and the cross-linking and curing were performed for 2 hours.

[0045] Add 12 mL of dextran-sodium hydroxide (sodium hydroxide concentration 5 mg / mL) solution with a dextran concentration of 6 mg / mL dropwise into the chitosan microsphere suspension, and form dextran / chitosan after 1 h ...

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Abstract

The invention relates to a multi-layer composite dual-drug-loaded microsphere as well as a preparation method and an application thereof in preparing antineoplastic drugs. In a preferred preparation method, the multi-layer composite dual-drug-loaded microsphere is mainly composed of two model drugs, chitosan and glucan; according to the preparation method, a chitosan microsphere self-assembled template is prepared by virtue of a double-emulsification-crosslinking method, then on the basis of an electrostatic interaction between polyelectrolytes having different charges, the glucan is adsorbed on the surface of the chitosan microsphere so as to form a glucan / chitosan dual-layer composite drug-loaded microsphere, and based on an electrostatic adsorption interaction between the chitosan and the glucan on the surface of the dual-layer composite drug-loaded microsphere, the chitosan / glucan / chitosan multi-layer composite dual-drug-loaded microsphere is formed. An in vitro release test on the multi-layer composite dual-drug-loaded microsphere having pH responsivity provided by the invention shows that the multi-layer composite dual-drug-loaded microsphere has a good sustained-release effect, and an in vitro antineoplastic cell activity test shows that the multi-layer composite dual-drug-loaded microsphere has a good inhibitory effect.

Description

technical field [0001] The invention relates to a biodegradable drug-loaded microsphere, in particular to a preparation method and a product of a multilayer composite chitosan-based double-drug microsphere with pH response. Background technique [0002] Cancer is one of the serious diseases that endanger human health, affecting human life everywhere. There are usually three approaches to cancer treatment: surgical resection, radiation therapy and chemotherapy, while the treatment of localized and spread cancer mainly relies on chemotherapy. Chemotherapy has played an important role in cancer treatment in recent years. However, the chemotherapy drugs currently used in the treatment of cancer generally have the following limitations: (1) Lack of targeting: commonly used anticancer drugs have universal cytotoxicity and lack of anticancer effects on cancer cells. The selectivity and targeting of normal cells lead to non-specific endocytosis in normal cells, which damages the pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/513A61K47/36A61P35/00A61K31/337
Inventor 王芳杨思倩袁健蒯君涛黄超伯高勤卫
Owner NANJING FORESTRY UNIV
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