SN-38-PLGA sustained release microsphere for intratumoral injection and preparation method and application thereof

A technology of intratumoral injection and sustained-release microspheres, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, microcapsules, etc. Poor drug resistance, loss of anti-tumor activity, etc., to achieve good application prospects, improve drug utilization, and reduce the number of administrations

Inactive Publication Date: 2019-10-08
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] As a broad-spectrum anticancer drug, irinotecan has a strong inhibitory effect on a variety of cancer cells, but it must be converted into 7-ethyl-10-hydroxycamptothecin (SN -38) to show anti-tumor effect, unfortunately, the conversion efficiency is only 2% to 8%, can not be efficiently utilized to a certain extent, resulting in great waste
[0005] Moreover, although the activity of SN-38 is very high (studies have pointed out that the therapeutic effect of SN-38 is about 1000 times that of its prodrug irinotecan), some chemical and pharmacological characteristics of itself limit its clinical application. A

Method used

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  • SN-38-PLGA sustained release microsphere for intratumoral injection and preparation method and application thereof
  • SN-38-PLGA sustained release microsphere for intratumoral injection and preparation method and application thereof
  • SN-38-PLGA sustained release microsphere for intratumoral injection and preparation method and application thereof

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specific Embodiment approach

[0058] Another specific embodiment of the present invention, in the step (1),

[0059] The mass ratio of SN-38 to PLGA (i.e. drug-to-lipid ratio, w / w) is 1:5-20 (preferably 1:10);

[0060] The concentration of the PLGA is 40~160mg / mL (preferably 80mg / mL);

[0061] Another specific embodiment of the present invention, in the step (2),

[0062] The volume ratio of the oil phase to the water phase in the colostrum is 1:1 to 8 (preferably 1:3);

[0063] The polyvinyl alcohol concentration in the water phase is 0.5-2% (preferably 1.5%);

[0064] The shear rate is controlled to be 5000~20000r / min (preferably 5000r / min);

[0065] Shearing time is 0.5~2min (preferably 1min);

[0066] Another specific embodiment of the present invention, in the step (3),

[0067] The volume ratio of the aqueous phase to the dispersed phase in the colostrum is 1:3 to 10 (preferably 1:5);

[0068] The polyvinyl alcohol concentration in the dispersed phase is 0.1 to 1.0% (preferably 0.5%),

[0069]...

Embodiment 1

[0078] 1 Experimental materials

[0079] 1.1 Drugs and reagents

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Abstract

The invention provides an SN-38-PLGA sustained release microsphere for intratumoral injection and a preparation method and application thereof. SN-38 is used as a model drug, PLGA is used as a carriermaterial, the SN-38-PLGA sustained release microsphere capable of being available for intratumoral injection dose is successfully built by adopting an emulsification-solvent evaporation method, and the SN-38-PLGA sustained release microsphere has the advantages of smooth and rounded surface, moderate particle size and high encapsulation efficiency and drug-loading capacity and the like; and meanwhile, the SN-38-PLGA sustained release microsphere for the intratumoral injection can enable the SN-38 to maintain effective high concentration for a long time in a tumor area, inactivation of the SN-38 drug is effectively avoided, and thus good practical application value is achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to SN-38-PLGA sustained-release microspheres for intratumoral injection and a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] At present, the morbidity and mortality of cancer are increasing year by year, posing serious threats and challenges to human health and life. Its pathogenesis is extremely complicated, and factors such as genetics, environment, even eating habits and psychological burden all play a very important role in it. In recent years, with the development of pharmacology, pharmacy, molecul...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K9/52A61K31/4745A61P35/00
CPCA61K9/0019A61K9/5031A61K31/4745A61P35/00
Inventor 黄桂华郝燕云席延卫冯瑞华
Owner SHANDONG UNIV
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