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Liposome, a pharmaceutical composition comprising the liposome, and a method of delivering active agents to a target site using the liposome

A technology of liposomes and active agents, applied in drug combination, liposome delivery, drug delivery, etc., can solve problems such as limitations

Inactive Publication Date: 2013-05-15
SAMSUNG ELECTRONICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this technique is limited in cases where the phase transition temperature of liposomes is significantly higher than normal tissue temperature

Method used

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  • Liposome, a pharmaceutical composition comprising the liposome, and a method of delivering active agents to a target site using the liposome
  • Liposome, a pharmaceutical composition comprising the liposome, and a method of delivering active agents to a target site using the liposome
  • Liposome, a pharmaceutical composition comprising the liposome, and a method of delivering active agents to a target site using the liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1: Preparation of liposomes and measurement of thermal sensitivity

[0080] Use stearoyl-VPGVG VPGVG VPGVG VPGVG VPGVG VPGVG-NH at a molar ratio of 0.55:55:2:20 or 0.55:55:2:40 2 (SEQ NO:6, hereinafter referred to as "SA-V6-NH 2 ”), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), [1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy( Polyethylene glycol)-2000] (ammonium salt)] (DSPE-PEG-2000) and cholesterol to prepare liposomes in the form of unilamellar vesicles.

[0081] In detail, the SA-V6-NH 2 Dissolve in methanol, and dissolve DPPC, DSPE-PEG and cholesterol in chloroform. After mixing the methanol and chloroform solutions in a round bottom flask, a lipid thin layer was formed on the inner wall of the flask by evaporating the solvent at room temperature using a rotary evaporator.

[0082] Next, the liquid thin layer was hydrated by adding physiological saline in which 200 mM calcein was dissolved to the flask at room temperature. Calcein is ...

Embodiment 2

[0089] Liposomes were prepared according to the same method used in Example 1, except that 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) was added to DPPC as the main lipid component, and DPPC / DSPC was mixed in molar ratios of 0 / 100, 25 / 75, 50 / 50, 75 / 25, 100 / 0 and used mainly lipid molecules. Then, the heat sensitivity of the liposomes was assessed. The prepared liposomes had a similar mean diameter and distribution to the liposomes prepared in Example 1.

[0090] figure 2 It is to show that calcein passes through according to embodiment 2 with the molar ratio of about 0.55:about 55 (0 / 100,25 / 75,50 / 50,75 / 25,100 / 0 (by molar ratio)):about 2:about 20 Use SA-V6-NH 2 , graphs of temperature release profiles in liposomes prepared from major lipid molecules (DPPC / DSPC), DSPE-PEG and cholesterol. Such as figure 2 As shown in , the onset temperature of calcein release increases as the amount of DSPC of the main lipid molecule increases. When DSPC 100 was used as the main l...

Embodiment 3

[0091] Example 3: Preparation and Thermosensitivity Measurement of Doxorubicin-Containing Liposomes Using the Ammonium Sulfate Gradient Method

[0092] DSPC and DPPC were used as the main lipid components at a mixing ratio of 25:75 and SA-V3-NH at a molar ratio of 0.55:55:2:20 2 , DSPC+DPPC, DSPE-PEG, and cholesterol, and use the ammonium sulfate gradient method (J. Control. Release 2009, 139, 73-80) to prepare doxorubicin-encapsulated unilamellar vesicular liposomes.

[0093] In detail, stearoyl-VPGVG VPGVG VPGVG-NH 2 (SEQ NO:7, hereinafter referred to as "SA-V3-NH 2 ”) was dissolved in methanol, and DSPC, DPPC, DSPE-PEG and cholesterol were dissolved in chloroform. After mixing the methanol and chloroform solutions in a round bottom flask, evaporate the solvent in the flask by using a rotary evaporator at room temperature A thin layer of lipids forms on the inner wall.

[0094] Next, the lipid lamella was hydrated by adding a 250 mM ammonium sulfate solution to the flask ...

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Abstract

A liposome comprising elastin-like polypeptides, a pharmaceutical composition comprising the liposome, and a method of delivering active agents to a target site using the liposome.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of Korean Patent Application No. 10-2011-107055 filed with the Korean Intellectual Property Office on Oct. 19, 2011, the disclosure of which is incorporated herein by reference in its entirety. technical field [0003] The present disclosure relates to liposomes comprising elastin-like polypeptide (ELP), pharmaceutical compositions comprising the liposomes, and methods of delivering active agents to target sites by using the liposomes. Background technique [0004] Liposomes consist of at least one lipid bilayer membrane enclosing an aqueous interior compartment. Liposomes can be characterized by membrane type and size. Small unilamellar vesicles (SUVs) have a single membrane and are typically in the range of 20-50 nm in diameter. Large unilamellar vesicles (LUV) are typically larger than 50 nm. Oligolamellar large vesicles and multilamellar vesicles have multiple, usually concent...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K49/18A61K47/42
CPCA61K47/48815A61K47/48238A61K41/0028A61K41/0052A61K47/62A61K47/6911A61P1/04A61P21/02A61P23/00A61P25/08A61P29/00A61P3/02A61P31/00A61P35/00A61P37/06A61P37/08A61K47/50A61K9/127A61K31/56A61K38/08
Inventor 金旻相金泫伶朴宣玟朴在钻蔡洙荣
Owner SAMSUNG ELECTRONICS CO LTD
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