A kind of liposome drug carrier and its preparation method and application

A liposome and pharmaceutical preparation technology, applied in the field of liposome drug carrier and its preparation, can solve the problems of poor liposome stability, liposome instability, and low encapsulation efficiency, and achieve uniform particle size , Improve the ability to enter the cell, good effect of encapsulation rate

Active Publication Date: 2019-08-27
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the application of liposomes as a drug carrier has many advantages and characteristics, at present, there are also certain limitations: the stability of liposomes is not good, and during the preservation process of liposomes, or when encountering Temperature changes and adding different additives or excipients may cause liposomes to adsorb, aggregate and fuse with each other, resulting in instability of liposomes; the encapsulation efficiency is low. Low, especially for some water-soluble drugs, the entrapment rate is lower, and the drug is easy to leak from the liposome

Method used

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  • A kind of liposome drug carrier and its preparation method and application
  • A kind of liposome drug carrier and its preparation method and application
  • A kind of liposome drug carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Example 1 Preparation of phospholipid liposomes loaded with bisphosphonates

[0081] 1.1 Preparation of reagents and stock solutions

[0082] Chloroform (analytical grade);

[0083] Phosphate buffer: Take 12.2mM disodium hydrogen phosphate and 8.2g / l NaCl in ultrapure water, adjust the pH to 7.40;

[0084] Stock solution: 100mg / ml EPC / HSPC, take 100mg EPC / HSPC and dissolve in chloroform;

[0085] 20mg / ml Chol, take 20mg Chol and dissolve in chloroform;

[0086] Dissolve an appropriate amount of bisphosphonate solution in ultrapure water, and adjust to pH 7.4 with 5N NaOH.

[0087] 1.2 Preparation method - thin film dispersion method

[0088] a) Take the stock solution egg yolk lecithin EPC or hydrogenated soybean lecithin HSPC and cholesterol in an eggplant-shaped bottle in a molar ratio of 2:1;

[0089] b) Slowly blow dry with nitrogen gas or evaporate chloroform with low-pressure rotation in a water bath to form a thin film in the eggplant-shaped bottle;

[0090...

Embodiment 2

[0096] Example 2 Preparation of Palmitic Acid and Cholesterol Liposome Loaded Bisphosphonates

[0097] 2.1 Preparation of reagents and stock solutions

[0098] Chloroform (analytical grade);

[0099] tert-butanol (analytical grade);

[0100] Phosphate buffer: take 12.2mM disodium hydrogen phosphate and 8.2g / l NaCl in ultrapure water, adjust the pH to 7.40;

[0101] Stock solution: 100mg / ml PA, take 100mgPA and dissolve in chloroform or tert-butanol;

[0102] 20mg / ml Chol, take 20mg Chol and dissolve in chloroform;

[0103] Dissolve an appropriate amount of bisphosphonate solution in ultrapure water, and adjust the pH to 7.60 with 5N NaOH.

[0104] 2.2 Preparation method 1 - thin film dispersion method

[0105] a) Take the stock solution palmitic acid PA and cholesterol in eggplant-shaped bottles in molar ratios of 3:5, 3:7, and 3:8;

[0106] b) Slowly blow dry with nitrogen gas or evaporate chloroform with low-pressure rotation in a water bath to form a thin film in the ...

Embodiment 3

[0118] Example 3 Evaluation and comparison of the above-mentioned liposome-loaded bisphosphonate drugs

[0119] 3.1 Particle size, PDI, potentiometric determination

[0120] Instrument: dynamic light scattering laser particle size analyzer and zeta potential analyzer (zetasizer3000);

[0121] Conditions: The refractive index of the sample is set to that of silica (1.59), the dispersed phase is water (refractive index 1.36, viscosity 0.8cp), the detection temperature is 25 degrees, and the sample is equilibrated in the temperature of the detection chamber for 60 seconds before detection. The laser wavelength is 633nm, and the refraction angle is 90°;

[0122] Particle size and PDI measurement: 50 μl of sample was taken, diluted 10 times with pure water, transferred to the particle size cell, and each sample was measured in parallel three times.

[0123] Potentiometric measurement: 50 μl of sample was taken, diluted 10 times with 10% Hepes solution, transferred to a potential ce...

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Abstract

The invention belongs to the technical field of drug preparation development, in particular to a liposome drug carrier and a preparation method and application thereof. The liposome drug carrier includes the following ingredients: cetylic acid and cholesterol. By freeze drying or rotary drying the ingredients transform into membranes. Through the subsequent hydration and filming the final products are acquired. The liposome drug carrier can automatically form lipid microspheres which are quite stable. At the same time the drug carrier preserves the advantages of traditional liposome, namely, the drug carrier has a structure similarity to the bimolecular lamellar membrane structure of biological plasma membrane. The drug carrier has the advantages of excellent biological adaptability, stability, simple production and high encapsulation efficiency and the like. The liposome drug carrier can be used to carry biphosphonate drugs with a consistent and unified particle diameter, high encapsulation efficiency and high stability. The carrier has negative charges and can further enhance the ability that the drug enters cells. Compared with traditional lecithin liposome the carrier enhances the effects on macrophages.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a liposome drug carrier and its preparation method and application. Background technique [0002] Liposome is a directional drug carrier formed by wrapping drug molecules with vesicles formed by phospholipid bilayer membranes, and is a new dosage form of targeted drug delivery system. It is to embed the solution or the active substance in the solution in the particles with a diameter of nanometer. At present, the main raw material of liposome is phospholipid, which is the main chemical component of liposome, and the most representative one is lecithin. Cholesterol is also another important component of liposomes. It does not form a membrane structure itself, but can be inserted into the phospholipid membrane at a certain molar ratio. Adding cholesterol can change the phase transition temperature of the lipid membrane, thereby affecting the permeability and fluidity of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/12A61K47/28A61K31/663
Inventor 徐宇虹李琳琳
Owner SHANGHAI JIAO TONG UNIV
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