A kind of multivesicular liposome for eye vitreous injection and preparation method thereof

A technology of multivesicular liposomes and vitreous bodies, which is applied in the direction of liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., to achieve good sustained release, reduce the number of administrations, and prolong release the effect of time

Active Publication Date: 2020-07-17
YANTAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] There is no report on the application of multivesicular liposomes in the vitreous of the eye

Method used

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  • A kind of multivesicular liposome for eye vitreous injection and preparation method thereof

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Embodiment 1

[0041] A preparation method of multivesicular liposome for eye vitreous injection, comprising the steps of:

[0042] Accurately weigh 22 mg, 6 mg, 18 mg, and 6 mg of dioleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, cholesterol, and triolein respectively in a 10ml beaker, add 3ml of chloroform to dissolve, and obtain the lipid phase;

[0043] The lipid phase obtained above was combined with 4 ml of 25 mg / ml bevacizumab solution containing 7% sucrose, and vortexed to form W / O colostrum;

[0044] Inject the colostrum obtained above into 10ml of 4% glucose and 60mmol / L lysine aqueous solution, vortex and mix to form W / O / W type double emulsion;

[0045] Quickly pour the double emulsion obtained above into 20ml of the external water phase, carry out rotary evaporation at about 37°C, remove the organic solvent chloroform, centrifuge at 1000r / min, discard the supernatant, add an appropriate amount of physiological saline to the lower part of the precipitate, and obtain th...

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Abstract

The invention relates to a multivesicular liposome for ocular vitreous injection. The multivesicular liposome is prepared from the following components in parts by weight: 1 part of bevacizumab, 0.2-150 parts of lipid, 5-500 parts of an osmotic pressure regulator and 6-200 parts of a co-emulsifier. A preparation method of the multivesicular liposome for ocular vitreous injection comprises the steps of dispersing an inner water phase into a lipid phase according to the volume ratio of the inner water phase to the lipid phase of (1:1) to (1:10) to form a W / O primary emulsion; dispersing the W / O primary emulsion into an outer water phase according to the volume ratio of the W / O primary emulsion to the outer water phase of (1:1) to (1:5) to form a W / O / W compound emulsion; transferring the W / O / W compound emulsion to the outer water phase and removing an organic solvent in the compound emulsion; and centrifuging the obtained solution at 500-3,000rpm, taking lower sediments and adding normal saline for dispersion again to obtain the multivesicular liposome. According to the method provided by the invention, the prepared multivesicular liposome is high in encapsulation efficiency and has a good slow release effect, the particle sizes are 10-50 microns, the administration times are reduced and the compliance of a patient is improved.

Description

technical field [0001] The invention relates to a multivesicular liposome for eye vitreous injection, and also relates to a preparation method of the multivesicular liposome for eye vitreous injection, which belongs to the field of pharmaceutical preparations. Background technique [0002] Age-related macular degeneration (hereinafter referred to as AMD) is the primary cause of irreversible visual impairment in the elderly, mainly due to aging changes in the structure of the macular area. Age-related macular degeneration mostly occurs in people over 45 years old, and its prevalence increases with age. It is currently an important disease that causes blindness in the elderly. AMD is divided into dry (non-neovascular) and wet (neovascular) forms. Dry AMD is the atrophy and degeneration of the macular area caused by retinal pigment epithelial cells and photoreceptor cell atrophy; wet AMD mainly manifests as glass membrane destruction, choroidal blood vessel invasion and subret...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/14A61K39/395A61P27/02A61P27/06A61P9/10
CPCA61K9/0002A61K9/0019A61K9/127A61K39/3955A61K47/14A61K47/24A61K47/28
Inventor 慕宏杰孙考祥王毅云
Owner YANTAI UNIV
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