Polycystic liposome gel capable of overcoming burst release and maintaining antibody activity and preparation method thereof

A technology of multivesicular liposomes and antibody activity, which is applied in the direction of liposome delivery, antibodies, medical preparations of non-active ingredients, etc. It can solve problems such as inflammation and irritation, and achieve improved compliance, prolonged release time, Reduce the effect of drug burst release phenomenon

Active Publication Date: 2019-07-09
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

(2) Although polymer materials such as PLGA or PLA are biodegradable and have good biocompatibility, their degradation products are highly acidic substances such as lactic acid, which can cause irritation or even inflammation to the injection site or tissue
[0006] In the prior art, the use of intravitreal injection for the treatment of ocular neovascular diseases has long been reported

Method used

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  • Polycystic liposome gel capable of overcoming burst release and maintaining antibody activity and preparation method thereof
  • Polycystic liposome gel capable of overcoming burst release and maintaining antibody activity and preparation method thereof
  • Polycystic liposome gel capable of overcoming burst release and maintaining antibody activity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Preparation of multivesicular liposome gel sustained-release preparation loaded with bevacizumab (LG1):

[0053] Bevacizumab multivesicular liposome (Bev-MVLs) preparation: the bevacizumab solution of 25mg / mL that contains 3mL 6% sucrose and 10% (w / v) HSA is used as internal aqueous phase; Accurately weigh Dioleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, cholesterol, triolein 23mg, 7mg, 19mg, 7mg respectively in 10ml beaker, add 3ml chloroform to dissolve, obtain lipid phase; 10000rpm high-speed shearing conditions were added dropwise to the lipid phase, and sheared for 5min to form w / o type colostrum; the colostrum was added dropwise to 12mL of 4% glucose and 60mmol under 4000rpm high-speed shearing conditions. / L of lysine in the external aqueous phase solution, keep for 1min to form a w / o / w type double emulsion; 37°C rotary evaporation to obtain multivesicular liposome suspension;

[0054] Preparation of multivesicular liposome gel sustained-release pre...

Embodiment 2

[0056] Preparation of multivesicular liposome gel sustained-release formulation loaded with ramuzumab:

[0057] Rabluzumab multivesicular liposomes (Ran-MVLs) preparation: 2 mL of 25 mg / mL of Rabluzumab solution containing 6% sucrose and 10% (w / v) HSA was used as the internal aqueous phase; Oleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, cholesterol, triolein 14mg, 5mg, 13mg, 5mg respectively in a 10ml beaker, add 2ml chloroform and ether mixed solution (1:1, v / v) Dissolve to obtain a lipid phase; add the inner water phase dropwise to the lipid phase under 10000rpm high-speed shear conditions, and shear for 5min to form w / o type colostrum; put the colostrum under 4000rpm high-speed shear conditions Add dropwise to 9mL of 5% glucose and 40mmol / L lysine in the external aqueous phase solution, keep for 1min to form w / o / w type double emulsion; 37°C rotary evaporation to obtain multivesicular liposome suspension liquid;

[0058] Preparation of multivesicular liposome ...

Embodiment 3

[0060] Preparation of multivesicular liposome gel sustained-release formulation loaded with aflibercept:

[0061] Preparation of aflibercept multivesicular liposomes (Afl-MVLs): 2 mL of 10 mg / mL aflibercept solution containing 5% sucrose and 10% (w / v) HSA was used as the internal aqueous phase; Oleoylphosphatidylcholine, dipalmitoylphosphatidylglycerol, cholesterol, triolein 15mg, 6mg, 15mg, 6mg respectively in a 10ml beaker, add 2ml chloroform and ether mixed solution (1:1, v / v) Dissolve to obtain a lipid phase; add the inner water phase dropwise to the lipid phase under 11000rpm high-speed shear conditions, and shear for 6min to form w / o type colostrum; put the colostrum under 6000rpm high-speed shear conditions Add dropwise to 8mL of 4% glucose and 40mmol / L lysine in the external aqueous phase solution, keep for 1min to form a w / o / w type double emulsion; 37°C rotary evaporation to obtain multivesicular liposome suspension liquid;

[0062] Preparation of multivesicular lip...

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Abstract

The invention discloses a polycystic liposome gel capable of overcoming burst release and maintaining antibody activity, and belongs to the field of eye sustained and controlled release preparations of biological macromolecular drugs. A monoclonal antibody clone antibody drug is wrapped in the polycystic liposome with good biocompatibility and biodegradability, and then the polycysticliposome is dispersed in sol formed by a temperature-sensitive polymer material, and after the sol is injected through a vitreous cavity, the sol is solidified into semi-solid gel at the body temperature to form apolycysticliposome-temperature-sensitive hydrogel composite preparation, so that release of the antibody drug is controlled. By the adoption of the polycystic liposome gel capable of overcoming burstrelease and maintaining antibody activity, the advantages of the polycystic liposome and the hydrogel preparation are utilized, in-vitro release of the antibody drug can be kept for about 60 days, the burst release problem of a general dosage form of the antibody drug is reduced, the activity of the antibody drug is greatly maintained, retention time of the antibody drug in eyes after vitreous injection is prolonged to a greater extent, injection frequency is reduced, and compliance of patients is improved.

Description

technical field [0001] The invention relates to a multivesicular liposome gel capable of overcoming sudden release and maintaining antibody activity and a preparation method thereof. Background technique [0002] As we all know, sustained-release preparations have the characteristics of delaying drug release, which can greatly reduce the speed of drug absorption by the body, and reduce the peak and valley phenomenon of blood drug concentration in the administration of common preparations, so as to keep the blood drug concentration at a relatively stable level. Within the effective range, better therapeutic effect can be achieved while improving drug safety. It is mainly suitable for chronic diseases that require long-term administration, especially for drugs with short half-lives that require frequent administration, which can effectively improve patient compliance. [0003] At present, sustained-release preparations with polyester or polyanhydride as the skeleton material ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/395A61K9/127A61K9/06A61K47/34A61K47/18A61K47/26A61K47/42A61K47/32A61P9/10
CPCC07K16/22A61K9/1277A61K9/06A61K47/34A61K47/183A61K47/26A61K47/42A61K47/32A61P9/10A61K2039/505
Inventor 慕宏杰王毅云孙考祥
Owner YANTAI UNIV
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