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Vesicle-type medication system containing metformin, and application thereof

A drug delivery system, metformin technology, applied in the field of pharmaceutical preparations, can solve the problems of low solubility, difficult loading into liposomes, etc., and achieve the effects of prolonging survival time, wide drug loading range, and less leakage

Inactive Publication Date: 2014-04-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ciprofloxacin is charged and soluble in an acidic or alkaline environment, but is neutral and has low solubility in the external aqueous phase of the drug-loading technology in the physiological pH range. Therefore, it is difficult to use citric acid Gradient method for loading into liposomes (encapsulation efficiency is usually less than 20%)

Method used

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  • Vesicle-type medication system containing metformin, and application thereof
  • Vesicle-type medication system containing metformin, and application thereof
  • Vesicle-type medication system containing metformin, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Choice of phospholipid and cholesterol ratio

[0054] The ratio of phospholipids to cholesterol can significantly affect liposome membrane stability and drug loading efficiency. at 200 mmol·L -1 (MetH) 4 EDTA (i.e. metformin ethylenediaminetetraacetic acid) was used as a hydration medium to prepare blank liposomes, establish a transmembrane gradient, and load epirubicin hydrochloride. The average particle size and encapsulation efficiency of the preparation were measured, and the results are shown in Table 1.

[0055] Table 1 Effect of different ratios of phospholipids and cholesterol

[0056]

[0057] Note: The concentration of metformin in the hydration medium is 600 mmol L -1 (HSPC is hydrogenated soybean lecithin; CH is cholesterol; PEG2000-CHS is the reaction product of polyethylene glycol monomethyl ether with a molecular weight of 2000 and cholesterol hemisuccinate, that is, cholesterol hemisuccinate polyethylene glycol ester).

[0058] I...

Embodiment 2

[0059] Example 2 pH effect

[0060] Prepare 200 mmol L -1 (MetH) 4 EDTA solution was used as a hydration medium, and epirubicin hydrochloride liposomes were prepared according to the method in Experimental Example 1, and the encapsulation efficiency was investigated. The results are shown in Table 2.

[0061] Table 2 Effect of pH value of hydration medium on encapsulation efficiency of epirubicin hydrochloride liposomes

[0062]

[0063] According to Table 2, it can be seen that the encapsulation efficiency increases with the increase of the pH value of the hydration medium. When the pH value of the hydration medium is 6-9, the encapsulation efficiency is greater than 80%.

Embodiment 3

[0064] Example 3 Effect of hydration medium concentration

[0065] The preparation concentrations were 100, 200, 300, 400 mmol·L -1 (MetH) 4 EDTA solution (pH 7.0) was used as a hydration medium, and doxorubicin hydrochloride liposomes were prepared according to the optimized prescription, and the changes in drug loading and encapsulation efficiency of preparations with different concentrations at different times were investigated. The results are shown in Table 3.

[0066] Table 3 Effect of hydration medium concentration on encapsulation efficiency of epirubicin hydrochloride liposomes

[0067]

[0068] As can be seen from Table 3, 100 mmol L -1 and 400 mmol·L -1 (MetH) 4 The encapsulation efficiency of EDTA liposomes did not reach more than 90% in 120 min, 300 mmol·L -1 (MetH) 4 EDTA liposomes had the highest encapsulation efficiency at 80 min, while 200 mmol·L -1 (MetH) 4 The encapsulation efficiency of EDTA was maximum at 60 min.

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Abstract

The invention belongs to the field of pharmaceutical preparation, and specifically discloses a vesicle-type medication system containing metformin, and an application thereof. According to the invention, metformin is used for replacing part of ammonium in a classic ammonium ion gradient, and an ammonium gradient and / or metformin gradient in water phase inside and outside liposome is established. A novel vesicle-type medication system (comprising various liposomes) is prepared. With the trans-membrane gradient, an anti-tumor drug is actively loaded into liposome. The metformin is still retained in water phase in liposome. Therefore, the two are both encapsulated in liposome. According to the invention, a surface active substance is adopted as a basic membrane material; a solution of a guanidine-containing cationic compound is adopted as a hydration medium, and blank vesicles are prepared; and trans-membrane gradient is established upon the blank vesicles, so that the medication system is prepared. The vesicle-type medication system is characterized by wide drug loading range, high drug encapsulation efficiency, and good stability. With the vesicle-type medication system, drug toxicity can be reduced, and tumor reoccurrence can be inhibited.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a vesicle drug delivery system which contains metformin and can utilize gradients to realize active drug loading and application thereof. Background technique [0002] Tumor recurrence and metastasis have always been two major problems that cannot be completely solved in the treatment of malignant tumors. In the process of tumor research in the past, the traditional theory believed that the occurrence and development of tumors were the result of the joint proliferation of all tumor cells, so research has been devoted to how to kill a large number of tumor cell populations. However, studies in recent years have found that not all tumor cells have the potential for unlimited proliferation, and only a small number of stem cell-like cell populations, namely tumor stem cells, have the potential for self-renewal and unlimited proliferation. [0003] The tumor ste...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/16A61K31/155A61P35/00
Inventor 邓意辉杨强张小飞
Owner SHENYANG PHARMA UNIVERSITY