Nanoparticle formulation

A technology of nanoparticles and preparations, applied in the field of nanoparticle preparations, to achieve the effect of reducing cancer growth rate and body fat deposition

Active Publication Date: 2015-08-12
英国研究与创新署
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of these prior art examples are able to deliver the therapeutic agent in its native form to the selected target organ with efficient release and distribution to the desired desired site

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Embodiment 1: Preparation of liposomal nanoparticles

[0082] Take an appropriate volume of N 1 -cholesteryloxy-carbonyl-3,7-diaza-1,9-nonanediamine (CDAN), 1,2-distearoylglycerol-3-phosphatidylcholine (DSPC), cholesterol and 1, Organic solvent (usually CHCl 3 ) stock solution, mixed in a 5 mL round bottom flask at a molar ratio of 32:32:35:1 to form a thin film. The film was then rehydrated with an amount of 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) (4 mM, NaCl 135 mM, pH 6.5) and sonicated to generate lipid Dispersions, buffered to pH 7, and purified by diafiltration to obtain liposome suspensions at predetermined total lipid concentrations.

Embodiment 2

[0083] Example 2: Preparation of liposomes encapsulating short-chain fatty acids.

[0084] Take an appropriate volume of N 1 -cholesteryloxy-carbonyl-3,7-diaza-1,9-nonanediamine (CDAN), 1,2-distearoylglycerol-3-phosphatidylcholine (DSPC), cholesterol and 1, Organic solvent (usually CHCl 3 ) stock solution, mixed in a 5 mL round bottom flask at a molar ratio of 32:32:35:1 to form a thin film. The film was then washed with a certain amount of acetic acid solution (1M, CH 3 CO 2 H, pH 2.0) and sonicated to generate a lipid dispersion, buffered to pH 7, and purified by diafiltration to obtain a liposome suspension of predetermined total lipid concentration.

[0085] Liposome-encapsulated acetate nanoparticles (also called "LITA") were prepared in which 1 mL of solution contained approximately 10 11 Nanoparticles / ml. To measure the particle size, such as figure 1 shown.

Embodiment 3

[0086] Example 3: Preparation of fluorescently labeled liposomes.

[0087] Take an appropriate volume of N 1 -cholesteryloxy-carbonyl-3,7-diaza-1,9-nonanediamine (CDAN), 1,2-distearoylglycerol-3-phosphatidylcholine (DSPC), cholesterol, 1, 2-Distearoylglycerol-3-phosphatidylethanolamine-N-(Lissamine Rhodamine B Sulfonyl) (DOPE-rhodamine) and 1,2-Distearoylglycerol-3-phosphatidylethanolamine-N - Organic solvent of methoxy(polyethylene glycol)-2000 (DSPE-PEG2000) (usually CHCl 3 ) stock solution, mixed in a 5 mL round bottom flask at a molar ratio of 32:32:35:1 to form a thin film. The film was then rehydrated with an amount of 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) (4 mM, NaCl 135 mM, pH 6.5) and sonicated to generate lipid Dispersions, buffered to pH 7, and purified by diafiltration to obtain liposome suspensions at predetermined total lipid concentrations.

[0088] To prepare liposomes containing encapsulated short-chain fatty acids, the lipid compositi...

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Abstract

The present invention concerns nanoparticle formulations suitable for the delivery of one or more therapeutic agents, the formulations comprising: a cationic cholesterol derivative; a neutral phospholipid; cholesterol or a neutral cholesterol derivative; and a saturated fatty acid, PEGylated neutral derivative of phosphatidylethanolamine or phosphatidylcholine.

Description

technical field [0001] The present invention relates to nanoparticle formulations. In particular, it relates to, but is not limited to, nanoparticle-assisted delivery of therapeutic agents for the treatment of metabolism and cancer. Background technique [0002] Dysregulation of cellular metabolism is a central prerequisite for many chronic disease processes, including cancer. Recently, there has been renewed interest in the potential of metabolic engineering to retransform abnormal cells and tissues through the use of small molecules. However, achieving sufficient and sustained metabolic effects by such methods can be difficult due to the need to identify suitable small molecules and develop suitable modes of administration. [0003] Metabolic engineering provides a powerful and efficient tool as it allows the systematic manipulation and fine-tuning of cellular metabolic activity. Methods to reengineer metabolism in dysregulated or oncogenic states are needed. The metho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
CPCA61K9/127A61K47/24A61K31/19A61K47/28A61K9/1271A61K9/1277Y10S977/906Y10S977/773Y10S977/907A61P25/08A61P3/04A61P35/00A61P9/00A61P9/10A61P3/10
Inventor 吉米·贝尔伊丽莎白-路易丝·托马斯利·布罗迪迈利兹-萨胡里·阿里索鲁安德鲁·米勒加里·佛洛斯特
Owner 英国研究与创新署
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