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Liposome compositions for improved drugretention

A liposome composition and liposome technology, applied in the direction of liposome delivery, active ingredients of heterocyclic compounds, antibacterial drugs, etc., can solve problems such as high liposome leakage rate and release

Inactive Publication Date: 2002-05-29
ALZA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Another problem is that some agents that do accumulate in liposomes are released immediately after accumulation
There is also the problem that some agents that are successfully loaded and retained in liposomes in vitro have a high leakage rate from liposomes in vivo, thus losing The advantages

Method used

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  • Liposome compositions for improved drugretention
  • Liposome compositions for improved drugretention
  • Liposome compositions for improved drugretention

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0095] Preparation of liposomes containing dextran sulfate-ciprofloxacin

[0096] A, the preparation of dextran sulfate ammonium salt

[0097] Dextran sulfate, sodium salt, molecular weight 8,000 Daltons (Dextran Product Limited (Ontario, Canada)) was converted to dextran sulfate ammonium salt as follows. An ion exchange column with a bed volume of 400 mL was packed with DOWEX 50X8-100 ion exchange resin (Aldrich Chemical Co, Milwaukee, WI). The packed column was flushed with 2L of 1N HCl at a flow rate of 3-4mL / min until the pH of the elution was about 1-2. Excess HCl was washed off the column with 2-3 L of deionized water until the pH of the elution water was approximately 5.5.

[0098] 300 mL of dextran sulfate sodium salt (50 mg / mL in water) was added to the resin and twelve 50 mL fractions were collected. Fractions containing dextran sulfate (fractions 3-12) were combined and the pH was adjusted from 1.29 to 5.5 with 5M ammonium hydroxide (approximately 25 mL).

[0...

Embodiment 3

[0108] Diafiltration of Dextran Sulfate against Saline Solutions

[0109] Dextran sulfate sodium salt (molecular weight 8,000 Daltons, Dextran Products Limited, Scarborough, Ontario, Canada) was dissolved in distilled water at a concentration of 100 mg / ml. Features a 300,000 molecular weight shut-off valve and a 0.79 ft 2 Surface area diafiltration cartridges (A / G / Technology Corporation, Needham, MA) were washed with 2 liters of distilled water. 90 mL of dextran sulfate was diafiltered against 1000 mL (approximately 10 volumes exchanged) of distilled water. The volume exchange liquid (each 100mL) was collected separately, and each 1mL was used for the quantification of dextran sulfate. The final residue was adjusted to the same initial volume (90 mL) with water, and then the content of dextran sulfate was determined.

[0110] The same diafiltration procedure was repeated using 0.15M NaCl, 0.35M NaCl, 0.45M NaCl and 1.0M NaCl. The permeate was collected and analyzed fo...

Embodiment 4

[0112] Liposome formulation with polyacrylic acid

[0113] An aqueous solution of 250 mM polyacrylic acid (Aldrich Chemicals, Milwaukee, WI) with a molecular weight of 2,000 Daltons and 50 mM ammonium sulfate in water was prepared and the pH of the solution was adjusted to 5.5 with 5M NaOH.

[0114] Liposomes were prepared as described in Example 2 by hydrating dissolved HSPC, cholesterol and mPEG-DSPE with an aqueous ammonium polyacrylate / ammonium sulfate solution in a molar ratio of 50:45.2:4.8. Unentrapped polymer was removed and ciprofloxacin was loaded into liposomes as in Example 2.

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Abstract

The invention describes a liposome composition for enhanced retention of a quinolone compound, and in particular of a fluoroquinolone compound. Entrapped in the liposomes is a polyanionic polymer effective to form a complex with the fluoroquinolone. A method of preparing the liposomes which includes a process for removal of unentrapped polyanionic polymer is also described.

Description

field of invention [0001] The present invention relates to liposome compositions which provide improved retention of drugs in liposomes. In particular, the invention relates to liposomes comprising fluoroquinolone antibiotic compounds. Background of the invention [0002] Liposomes, or lipid vesicles, are recognized drug delivery systems that improve the therapeutic activity and increase safety of various pharmaceutical agents. For use as in vivo carriers of diagnostic or therapeutic compounds, liposomes are generally prepared to contain the compound entrapped within the liposomes. For use in medical therapy, liposome formulations should have a high loading efficiency, i.e., a high drug-to-lipid ratio, to reduce the patient's load of non-therapeutic lipids, and should have a practical shelf life, allowing the The loaded compounds show little leakage or loss of activity. [0003] There are two general approaches to the preparation of liposome formulations: passive loading,...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/127A61K31/47A61K31/496A61K31/5383A61K47/24A61K47/32A61K47/34A61K47/36A61K47/48A61P31/04
CPCA61K47/48176A61K31/5383A61K9/1271A61K47/4823A61K47/48215A61K9/127A61K31/496A61K9/1278A61K47/60A61K47/58A61K47/61A61P31/04A61K31/47
Inventor L·S·S·郭R·基万
Owner ALZA CORP
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