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Liposome composite phospholipid capable of adjusting phase-transition temperature and application thereof

A technology of phase transition temperature and complex phospholipids, which is applied in liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as drug leakage and increased permeability, and achieve Enhanced stability, reduced leakage, and enhanced targeted delivery effects

Active Publication Date: 2012-08-08
上海洁士宝日化集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, if two or more phospholipid materials are used to prepare liposomes at the same time, in most cases, different phospholipids still maintain their specific phase transition temperature in the liposome membrane. When the phase transition temperature is between, different phases exist in the liposome membrane at the same time, which is called phase separation (phase separations), resulting in the formation of a block structure (domain structure) on the membrane surface, which will increase the permeability of the lipid membrane. large, resulting in drug leakage

Method used

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  • Liposome composite phospholipid capable of adjusting phase-transition temperature and application thereof
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  • Liposome composite phospholipid capable of adjusting phase-transition temperature and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of Calcein Complex Phospholipid Liposome and Test of Release Behavior in Vitro

[0038] According to the molar ratio of DPPC and HSPC of 2:8, 4:6, 5:5, 6:4 and 8:2, weigh 120 mg each of the composite phospholipid materials, dissolve them in 10 mL chloroform, and place them in 50 mL eggplant-shaped bottles for 60 °C to form a thin film by rotary evaporation under reduced pressure, take out the eggplant-shaped bottle, and place it in a vacuum oven at 55 °C for 12 hours. Then, 5 mL of pH 7.4 phosphate buffered saline (PBS) containing 90 mM calcein was added to the eggplant-shaped flasks, and hydrated by rotation at 60 °C for 40 min. , 50 times) to obtain calcein complex phospholipid liposomes with different molar ratios of DPPC and HSPC. Calcein DPPC and HSPC liposomes containing only one phospholipid material of DPPC and HSPC were prepared respectively in the same way.

[0039] Remove the free drug from the above calcein liposomes by gel column chr...

Embodiment 2

[0041] Example 2 Comparison of release behavior of calcein liposomes with different phospholipid compositions at 37°C

[0042] Get the DPPC that embodiment 1 prepares and HSPC mol ratio is the calcein liposome that 2:8, 4:6, 5:5, 6:4 and 8:2 composite phospholipid and single DPPC and HSPC material make, then The release behavior of the above calcein liposomes was compared at 37°C. For specific experimental results, see figure 2 shown. The experimental results show that after adding a certain proportion of HSPC, the stability of the prepared calcein complex phospholipid liposomes at 37 ° C is significantly better than that of single DPPC phospholipid calcein liposomes, and there is an obvious correlation, the ratio of HSPC The higher the value, the more stable the complex phospholipid liposome and the lower the release rate. Therefore this experiment further shows that the liposome that the preferred DPPC of the present invention and HSPC composite phospholipid material are ...

Embodiment 3

[0043] Example 3 Differential Scanning Calorimetry (DSC) Determination of the Correlation Between the Phase Transition Temperature of Liposomes and the Composition of Phospholipids

[0044] 1. Preparation of liposomes: Weigh 120 mg of composite phospholipid materials (the molar ratios of DPPC and HSPC are 2:8, 4:6, 5:5, 6:4, 8:2) and dissolve in 10 mL respectively Chloroform, then placed in a 50 mL eggplant-shaped bottle, 60 ℃ reduced pressure rotary evaporation to form a thin film, take out the eggplant-shaped bottle, and place it in a vacuum drying oven at 55 ℃ for 12h. Add 5 mL of pH 7.4 phosphate buffered saline (PBS) into the eggplant-shaped bottle, and hydrate with rotation at 60 °C for 40 min. Composite phospholipid liposomes made of molar ratios of DPPC and HSPC (2:8, 4:6, 5:5, 6:4, 8:2, respectively).

[0045] DPPC and HSPC liposomes containing only phospholipid materials of DPPC and HSPC were prepared respectively by the same method.

[0046] Get the composite phos...

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Abstract

The invention discloses liposome composite phospholipid capable of adjusting phase-transition temperature and application thereof. The liposome composite phospholipid is prepared from 1-10 molar parts of dipalmitoyl phosphorylcholine (DPPC) and 1-10 molar parts of hydrogenated soya phosphatidylcholine (HSPC), and can be used for preparing thermosensitive target liposome preparation. According to the invention, different phospholipid materials are screened through a large number of experiments, and the experimental result indicates that the liposome composite phospholipid capable of adjusting phase-transition temperature can be obtained by scientifically combining DPPC and HSPC; the composite phospholipid can form a new phase when being prepared into a liposome membrane, avoid phase separation, has a single phase-transition temperature and can overcome the shortcoming of the prior art that two different phospholipid materials have two phase-transition temperatures; and moreover, the composite phospholipid has better stability and target release effect compared with the single-DPPC liposome, has phase-transition temperature with better tolerance to human body compared with the single-HSPC liposome, and has wide application range.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a liposome complex phospholipid capable of adjusting phase transition temperature and its application in pharmaceutical preparations. Background technique [0002] Phase transition temperature (phase transition temperature, T m ) is one of the most important physical and chemical characteristic parameters of the liposome membrane. When the temperature reaches the phase transition temperature, the liposome membrane, that is, the phospholipid bilayer, changes from a solid gel phase to a disordered liquid crystal phase. disordered phase), the C-C single bond in the phospholipid alkyl chain changes from the all-trans conformation to the ortho-cross conformation, resulting in a substantial increase in the total volume occupied by the hydrocarbon chain, which leads to a sharp increase in the permeability of the liposome membrane Increase, the drug is released from ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/24A61K9/127A61K9/19A61K9/10A61K31/475
Inventor 陈军蔡宝昌程冬
Owner 上海洁士宝日化集团有限公司
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