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Nanoliposomes comprising corticosteroid as medicaments and methods to prepare them

A nano-liposome and corticosteroid technology, applied in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve problems such as short plasma half-life, limited therapeutic efficacy, and increased plasma clearance rate

Inactive Publication Date: 2018-08-21
NANYANG TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, current therapeutic strategies are limited in that the activity of these drugs is not restricted to the site of action (i.e., in atherosclerotic lesions), and additionally, these drugs show limited therapeutic efficacy due to short plasma half-lives and increased plasma clearance
Most drugs exhibit moderate to severe systemic side effects such as uncontrolled bleeding with antiplatelet agents and rapid degradation and washout of fibrinolytic agents such as tissue plasminogen activator (tPA) and streptokinase reduced efficacy of

Method used

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  • Nanoliposomes comprising corticosteroid as medicaments and methods to prepare them
  • Nanoliposomes comprising corticosteroid as medicaments and methods to prepare them
  • Nanoliposomes comprising corticosteroid as medicaments and methods to prepare them

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Embodiment 1: Fluoxinolone acetone (FA)

[0068] This is the first study showing encapsulation of fluoxinolone acetonide into nanoliposomes at high loading concentrations. Different drug / lipid molar ratios (D / L ratios up to 0.2) were tested in normal and pegylated liposomes containing saturated and unsaturated lipids.

[0069] Sample 1: drug / lipid ratio of 0.15

[0070] Preparation of Large Unilamellar Vesicles (LUVs)

[0071] Liposome formulations were prepared by thin film hydration technique. Weigh out DPPC and DSPE-PEG 2K and dissolve in a chloroform:methanol (2:1 v / v) solvent mixture in a round bottom flask. To this lipid-solvent mixture was added fluoxanolone acetone at a drug:lipid molar ratio of 0.15:1. The solvent mixture was removed using a rotary evaporator connected to a water bath maintained at 40 °C. The flask was spun at 150 rpm for 1 hour to completely remove the solvent, resulting in a thin drug-loaded lipid film. Isotonic phosphate-buffered salin...

Embodiment 2

[0092] Embodiment 2: triamcinolone acetonide (TA)

[0093] Another corticosteroid drug, triamcinolone acetonide (TA), also demonstrated sustained release from nanoliposomes, and this is the first study to show high drug loading and sustained release of this drug from nanoliposomes. Preparation and release are completely analogous to the methods described previously. Image 6 and Figure 7 The results of TA loading and release from PEGylated liposomes are shown, respectively.

Embodiment 3

[0094] Example 3: Nanoliposomes comprising sphingolipids

[0095] The experimental process is similar to the previous method. An initial drug / lipid molar ratio of 0.15 was tested. Figure 8 and Figure 9 Results for loading and releasing FA from sphingolipid-containing nanosomes are shown, respectively.

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Abstract

This invention relates to a nanoliposome comprising at least one outer lipid bilayer and at least one corticosteroid encapsulated bythe at leastone lipid bilayer, wherein the ratio of the corticosteroid and lipids forming the lipid bilayer is preferably between 0.01 - 0.5, 0.1 - 0.3 or 0.12 - 0.18. The corticosteroid may be a group B corticosteroid, including triamcinolone acetonide, fluocinoloneacetonide, triamcinolone alcohol, mometasone, amcinonide, budesonide, desonide, fluocinonide and halcinonide. Preferably, the size of the nanoliposome is between 1 0 - 1 000 nm or 50 - 150 nm. The present invention also relates to the use of the nanoliposome of the invention for use as a medicam ent and for use in the treatment of a cardiovascular disease. Further, the invention is directed to a method to prepare the nanoliposome of the invention, which may further include an extruding step.

Description

field of invention [0001] The present invention belongs to the field of biopharmaceutical chemistry and relates to nanoliposomes comprising at least one outer lipid bilayer and at least one corticosteroid encapsulated by said at least one lipid bilayer. The invention also relates to the use of the nanoliposomes of the invention as medicine and for treating cardiovascular diseases. Furthermore, the present invention relates to a method for preparing the nanoliposomes of the invention. Background of the invention [0002] Atherosclerosis is a systemic vascular disease often grouped under the broad term of cardiovascular disease. Cardiovascular disease accounts for approximately 30% of total global mortality and is an important medical problem requiring viable treatment options. Atherosclerosis is considered a global socioeconomic problem with a large economic burden due to changes in demographics and urban lifestyles, regardless of geography, gender or ethnicity. Current tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/56A61P9/10
CPCA61K31/58A61K9/1271A61K31/57A61P9/10A61K38/08
Inventor S·文卡特拉曼J·V·纳塔拉詹A·达尔维塔恩
Owner NANYANG TECH UNIV
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