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

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 ...

AI Technical Summary

Problems solved by technology

[0006] In addition, DPPC thermosensitive liposomes have limited stability at a body temperature of 37°C, and some drugs will leak at a body temperature of 37°C, thereby reducing the efficacy of the drug. Liposome phospholipids that can increase the stability of thermosensitive liposomes at body temperature without affecting their release at phase transition temperatures, while significantly reducing the cost of thermosensitive liposomes

[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

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