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 t...

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
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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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