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Capecitabine polymer-lipid hybrid nanoparticle capable of utilizing micro-mixing and amphiphilic properties of capecitabine

A nanoparticle, capecitabine technology, applied in the field of nanoparticles, can solve problems such as delivery

Active Publication Date: 2021-11-09
JINGJIE PTM BIOLAB HANGZHOU CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although many US patent publications claim to provide nanoparticle formulations of cancer chemotherapeutic drugs, none of them have lipid or polymer delivery with capecitabine, especially polymer-lipid of capecitabine or its metabolites Promiscuous delivery direct association

Method used

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  • Capecitabine polymer-lipid hybrid nanoparticle capable of utilizing micro-mixing and amphiphilic properties of capecitabine
  • Capecitabine polymer-lipid hybrid nanoparticle capable of utilizing micro-mixing and amphiphilic properties of capecitabine
  • Capecitabine polymer-lipid hybrid nanoparticle capable of utilizing micro-mixing and amphiphilic properties of capecitabine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0134] Example 1: Preparation of CAP nanoparticles

[0135] Structure of polymer-lipid nanoparticles of CAP

[0136] Capecitabine and phospholipid form micelles (see figure 1 ). The micelles are encapsulated by electrostatic interactions using oppositely charged polymers. Multiple layers of alternating charge polymers can be deposited on the particles if desired. Finally, the outermost layer of polyethylene glycol (PEG) provides steric stability and longer blood circulation time.

[0137] particle formation process

[0138] First, lipid-capecitabine micelles were generated by a rapid solvent exchange method using a multi-inlet vortex mixer (MIVM), followed by spray-drying or freeze-drying with leucine and trehalose. Specifically, MIVM is set as figure 2shown. The micellar suspension was lyophilized for 48 hours. Resuspend the dried powder in aqueous solution by vigorous mixing or sonication. The oppositely charged polymers were added to the lipid-CAP micelles. If mu...

Embodiment 2

[0144] Example 2: Formation of lipid-CAP micelles with neutral surfaces.

[0145] Two treatments have been used to generate micelles-film hydration and continuous mixing. To 215.6 μL of CAP (5 mg / ml), add 117.4 μL of DPPC (1,2-dipalmitoyl-sn-glycerol-3-phosphorylcholine) (25 mg / ml) and 329.9 μL of DPPE-PEG (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] (25 mg / ml). Mix the mixture well and evaporated under a stream of argon and placed under vacuum for at least 2 h. Then, the mixture was rehydrated with water and sonicated for 10 min. CAP, DPPC, and PEGylated lipid DPPE-PEG were dissolved in ethanol by continuous mixing , and rapidly mixed with DI water in MIVM in different volumes depending on the molar ratio. Fill the solution into a 5 mL gas-tight syringe and rapidly mix with the other three streams that are DI water. Mix the CAP / phospholipid solution stream and one of the water streams Pump at 6ml / min. Pump the other two streams at 5...

Embodiment 3

[0153] Example 3: Formation of lipid-CAP micelles with positively charged surfaces.

[0154] Two treatments have been used to create micelles – film rehydration and continuous mixing. By film hydration, both DOTAP (1,2-dioleoyl-3-trimethylammonium-propane) and CAP were dissolved in chloroform at a concentration of 10 mM. Equal volumes of DOTAP and CAP (500ul) solutions were mixed together and the mixture was evaporated under argon flow and then placed under vacuum for at least 2 hours to ensure complete solvent evaporation. The dried film was then rehydrated with 1 ml of DI water and sonicated for 10 min. Cationic phospholipids such as DOTAP are used to prepare micelles with CAP by continuous mixing. CAP (2mM) and DOTAP (2mM) were dissolved in ethanol. The solution was filled into a 5 mL gas-tight syringe and mixed rapidly in the MIVM with the other three streams being DI water. One of the streams of the CAP / phospholipid solution and the water stream was pumped at a rate o...

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Abstract

The invention includes a composition and a method for preparing a nanoparticle composition. The nanoparticle composition comprises a phospholipid core comprising one or more lipids and one or more active agents, and at least one layer of one or more polymers on the surface of the phospholipid core. More specifically, the invention relates to the purpose of the capecitabine (N4-pentyloxycarbonyl-5-deoxy-5-fluoro-cytidine, CAP) in the category of lipid polymer nanoparticle preparations for optimizing the pharmaceutical properties of the capecitabine for treating cancer.

Description

[0001] This application is a divisional application of application number 201880061265.9, titled polymer-lipid hybrid nanoparticles of capecitabine using micro-mixing and amphiphilic properties of capecitabine, filing date 2018.09.20. [0002] Cross References to Related Applications [0003] This disclosure claims the benefit of priority to US Provisional Patent Application No. 62 / 561,744, filed September 22, 2017, the disclosure of which is incorporated herein by reference in its entirety. technical field [0004] The present disclosure generally relates to nanoparticles comprising a phospholipid core comprising one or more lipids and one or more polymers on the surface of the phospholipid core and at least one layer of one or more polymers on the surface of the phospholipid core Various active agents. More specifically, the present disclosure relates to the use of capecitabine (N4-pentyloxycarbonyl-5-deoxy-5-fluoro-cytidine, CAP) within such lipopolymer nanoparticle formul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/36A61K47/32A61K47/24A61K31/7068A61K45/06A61K9/00A61P35/00A61P1/08A61P17/00A61P37/04A61P9/00A61P1/12A61P7/00
CPCA61K9/5123A61K9/5146A61K9/5192A61K9/5161A61K9/5138A61K9/0019A61K47/6909A61K31/7068A61K45/06A61P35/00A61P1/08A61P17/00A61P37/04A61P9/00A61P1/12A61P7/00A61K2300/00
Inventor 程仲毅
Owner JINGJIE PTM BIOLAB HANGZHOU CO LTD
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