Lung-targeted medicine carrying precursor liposome for injection and method of use thereof

Abstract

The invention relates to the technical field of medicament delivery by a carrier, in particular to a lung targeting medicament carried proliposome used for injection and an application method thereof. Solid dispersion technology is adopted to obtain solution A by dissolving active medicament, phospholipid liposome, cholesterol liposome, surface active agent and acid type carrier in absolute ethylalcohol or the mixed solvent of absolute ethyl alcohol and absolute ether; active carbon which is used for injection and has the volume being 0.1-1% of the volume of the solution A is added into the solution A; stirring, standing and filtering of the solution by a millipore filter are carried; therefore, aseptic solution B free of pyrogen is obtained; aseptic additives are added into the solutionB under an aseptic condition; organic solvent is removed; and solid granular medicament carried proliposome or powdered medicament carried proliposome are obtained. The invention has the advantages that the preparation process is simple; the cost is low; the quality is controllable; the stability is good; and the invention is suitable for industrial production. The medicament carried proliposome prepared by effervescency dispersion technology has small and uniform particle diameter, the electric charge ranges from -10mv to -30mv, the proliposome can deliver over 90% medicament to a lung, and remarkable lung targeting effect is achieved, and thus being the best preparation delivering medicament by a carrier for treating lung diseases.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical carrier administration, in particular to the lung-targeted drug-loaded proliposome for injection and its application method. Background technique [0002] Liposome refers to a bimolecular vesicle with a structure similar to a biological membrane. It is a multilayered vesicle naturally formed by phospholipids dispersed in water. Each layer is a lipid bilayer. Separated by a water phase, the thickness of the bilayer is about 4 nm. It was first discovered by British Bangham and Standish in the 1960s when phospholipids were dispersed in water and observed with an electron microscope. In 1971, British Liman et al. began to use liposomes as drug carriers. Liposome is the most promising targeted drug delivery carrier in pharmacy. It can embed drug powder or solution in particles with a diameter of nanometer or micrometer. This particle has a cell-like structure and can enter the body to change T...

AI Technical Summary

Problems solved by technology

The disadvantages are: the concentration of surfactant in the preparation is high, the encapsulation rate of water-soluble drugs is low, etc.

Its disadvantage is: the high concentration of organic solvent limits the clinical application of the preparation

Its shortcoming is: except freeze-drying method, its method for preparing solid particle precursor liposome is all difficult to reach the requirement of aseptic and non-pyrogenic; Generally speaking, the particle size of liposome suspension obtained by hydration is difficult to control

Its disadvantages are: the use of highly toxic organic solvents such as chloroform and methanol, the uneven distribution of phospholipids on the surface of the carrier, and the complicated operation

Its disadvantage is that it is often necessary to use highly toxic organic solvents such as chloroform and methanol

Its advantages are: phospholipids and drugs are relatively stable during the preparation process, and are suitable for the preparation of heat-sensitive prodrug liposomes; its disadvantages are: complex process and high cost

[0020] From the above literature, it can be seen that there are some problems in the study of lung-targeted drug delivery system at home and abroad: (1) Because the particle size is too large, the safety of intravenous drug delivery may not be guaranteed; (2) Lung-specific targeting If it is not high enough, it will increase the drug concentration in the liver and spleen while increasing the drug concentration in the lung, which may cause toxic side effects on the liver and spleen; (3) In addition to the classic capillary bed of the lung that is intercepted by mechanical filtration as the target , the rest of the lung targeting mechanism is not yet clear

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