Phospholipid-coated therapeutic agent nanoparticles and related methods

Inactive Publication Date: 2016-12-01
AUTOTELIC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides phospholipid-coated therapeutic agent nanoparticles that can be administered by injection and release the therapeutic agent quickly and effectively under physiological conditions. The nanoparticles are stable in aqueous delivery vehicles and can be made using phospholipids and synthetic polymeric micelles. The phospholipid can be a mono-acylphospholipid or a diacylphospholipid, and the nanoparticle can contain one or more phospholipids. The nanoparticle can also include a combination of a diacylphospholipid and a mono-acylphospholipid. The therapeutic agent can have an X log P greater than 2.0. Overall, the invention provides a new way to deliver therapeutic agents for the treatment of diseases.

Problems solved by technology

The effective delivery of hydrophobic therapeutic agents remains a challenging problem for the pharmaceutical industry.
These challenges relate to the difficulty in formulating these therapeutic agents in vehicles for administration.
Furthermore, serious side effects are occasionally observed associated with the vehicle itself.
Disadvantages and side effects of Taxol® are directly associated this solvent.

Method used

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  • Phospholipid-coated therapeutic agent nanoparticles and related methods
  • Phospholipid-coated therapeutic agent nanoparticles and related methods
  • Phospholipid-coated therapeutic agent nanoparticles and related methods

Examples

Experimental program
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example 1

The Preparation of Representative Paclitaxel Nanoparticles by Microfluidization-Solvent Evaporation

[0231]The PTX-phospholipid NPs were prepared by LV1 low volume Microfluidizer® processor (Microfluidics, Massachusetts, US) microfluidization. The organic solvent (ethanol:chloroform (9:1)) containing PTX and phospholipids were added to an aqueous phase (de-ionized water, DI) and the emulsion was run through the microfluidizer to provide a nanoemulsion. The solvent from the nanoemulsion was removed by rotary evaporation to provide a nanosuspension of phospholipid-coated PTX nanoparticles in the aqueous phase.

[0232]Nanoparticles were prepared by mixing together the organic and aqueous phase. Organic phase consisted of 40 mg of 12:0 PC (DLPC) 1,2-dilauroyl-sn-glycero-3-phosphocholine (Avanti Polar Lipids, Inc., Alabama, US), 10 mg of 12:0 lyso PC 1-lauroyl-2-hydroxy-sn-glycero-3-phosphocholine (Avanti Polar Lipids, Inc., Alabama, US) and 10 mg of paclitaxel (paclitaxel was from Tecoland ...

example 2

The Preparation of Representative Paclitaxel Nanoparticles by Thin-Film Hydration

[0234]A phospholipid film was prepared by dissolving PTX and phospholipids in ethanol. The dry film was hydrated with water for visual, microscopic, size and loading efficiency measurements of the resulting unfiltered formulation.

[0235]Organic phase consisted of 40 mg of 12:0 PC (DLPC) 1,2-dilauroyl-sn-glycero-3-phosphocholine (Avanti Polar Lipids, Inc., Alabama, US), 10 mg of 12:0 lyso PC 1-lauroyl-2-hydroxy-sn-glycero-3-phosphocholine (Avanti Polar Lipids, Inc., Alabama, US) and 10 mg of paclitaxel (paclitaxel was from Tecoland Corporation, Irvine, Calif. (DMF No. 11909)) dissolved in 10 ml of ethanol. Aqueous phase consists of 10 ml DI water. The two phases are mixed in a 250 ml evaporator flask. The solution is completely evaporated using a rotary evaporator at the following conditions: water bath temperature=28° C., pressure <2 mm Hg, chiller temperature=5° C., rotation speed=280 rpm, until a film ...

example 3

Size and Zeta Potential Measurement of Representative Paclitaxel Nanoparticles

[0236]The particle size and the particle size measurements were carried out using Zetasizer Nano-ZS (Malvern Instruments Ltd, Worcestershire, UK) and the Zav hydrodynamic diameter of the samples was determined by cumulative analysis. The particle size and particle size distribution by intensity were measured by photon correlation spectroscopy (PCS) using dynamic laser light scattering (4 mW He—Ne laser with a fixed wavelength of 633 nm, 173° backscatter at 25° C.) in 10 mm diameter cells. The Zav of the particle size, also known as cumulants mean, is defined as harmonic intensity average particle diameter. All measurements were done with six runs. Zeta potential (surface charge) determinations of the NPs in water were based on the electrophoretic mobility of the particles using folded capillary cells in automatic mode of measurement duration using Zetasizer Nano-ZS. The measurements were performed by the l...

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Abstract

Phospholipid-coated nanoparticles containing a therapeutic agent, compositions that include the nanoparticles, and methods for making and using the nanoparticles and compositions.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS[0001]This application is a continuation of PCT / US2016 / 035293, filed Jun. 1, 2016, which claims priority to U.S. Application No. 62 / 169,397, filed Jun. 1, 2015, U.S. Application No. 62 / 263,453, filed Dec. 4, 2015, and U.S. Application No. 62 / 323,335, filed Apr. 15, 2016, each expressly incorporated herein by reference in its entirety.BACKGROUND OF THE INVENTION[0002]The effective delivery of hydrophobic therapeutic agents remains a challenging problem for the pharmaceutical industry. These challenges relate to the difficulty in formulating these therapeutic agents in vehicles for administration. Historically, hydrophobic therapeutic agents are administered in delivery vehicles that are less than advantageous with regard to delivery properties including therapeutic agent dose and bioavailability. Furthermore, serious side effects are occasionally observed associated with the vehicle itself.[0003]The formulation of paclitaxel over the years is a...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/00A61K31/337
CPCA61K9/5123A61K9/0019A61K31/337A61K9/5192A61K9/1075A61K9/1617A61K9/5084
Inventor TRIEU, VUONGDE, TAPAS K.
Owner AUTOTELIC
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