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Aggregate microparticles for therapy

A technology of aggregation and particles, applied in microcapsules, organic active ingredients, medical preparations of non-active ingredients, etc., can solve problems such as difficult to achieve

Inactive Publication Date: 2022-05-13
GRAYBUG VISION INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This seemingly simple goal is difficult to achieve in practice

Method used

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  • Aggregate microparticles for therapy
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  • Aggregate microparticles for therapy

Examples

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preparation example Construction

[0317] VIII. Methods of Preparation of Surface-Treated Microparticles

[0318] Acronym

[0319] DCM,CH 2 Cl 2 Dichloromethane

[0320] DL drug load

[0321] DMSO Dimethyl Sulfoxide

[0322] EtOH ethanol

[0323] HA sodium hyaluronate

[0324] hr, h hour

[0325] min minutes

[0326] NaOH sodium hydroxide

[0327] NSTMP non-surface treated particles

[0328] PBS Dulbecco's Phosphate Buffered Saline

[0329] PCL polycaprolactone

[0330] PEG polyethylene glycol

[0331] PLA poly(lactic acid)

[0332] PLGA poly(lactic-co-glycolic acid)

[0333] PVA polyvinyl alcohol

[0334] Rpm revolutions per minute

[0335] RT, r.t. room temperature

[0336] SD standard deviation

[0337] Particles with STMP Surface Treatment

[0338] UV ultraviolet

[0339] general method

[0340] All non-aqueous reactions were performed under an atmosphere of dry argon or nitrogen using anhydrous solvents. The structures of starting materials, intermediates and final products were conf...

Embodiment 1

[0344] Example 1. Preparation of biodegradable non-surface treated microparticles (NSTMP) comprising PLGA

[0345]Polymer particles comprising PLGA and diblock copolymers of PLGA and PEG, with or without sunitinib malate, were prepared using a single emulsion solvent evaporation method. Briefly, PLGA (560 mg) and PLGA-PEG (5.6 mg) were co-dissolved in dichloromethane (DCM) (4 mL). Sunitinib malate (90 mg) was dissolved in dimethylsulfoxide (DMSO) (2 mL). The polymer solution and the drug solution are mixed to form a homogeneous solution (organic phase). For empty NSTMP, drug-free DMSO (2 mL) was used. For drug-loaded NSTMP, the organic phase was added to 1% aqueous PVA in PBS (200 mL) and homogenized using a L5M-A laboratory mixer (SilversonMachines Inc., East Longmeadow, MA) at 5,000 rpm for 1 min to obtain an emulsion . For empty NSTMP, 1% PVA in water (200 mL) was used.

[0346] The emulsion (solvent-loaded microparticles) was then hardened by stirring at room temperat...

Embodiment 2

[0347] Example 2. Surface treatment of non-surface treated microparticles (NSTMP) using NaOH(aq) / EtOH

[0348] A pre-chilled solution containing a predetermined ratio of 0.25M NaOH (aqueous) and ethanol was added to the microparticles in a glass vial at about 4°C with stirring in an ice bath to form a 100 mg / mL suspension. The suspension is then stirred on ice for a predetermined time (e.g., 3, 6 or 10 minutes) and poured into a pre-chilled filter unit to remove the NaOH(aq) / ethanol solution. The microparticles were further rinsed with chilled water and transferred to a 50 mL centrifuge tube. The particles were then suspended in pre-cooled water and kept in the refrigerator for 30 minutes to allow the particles to settle. After removing the supernatant, the pellet was resuspended and filtered through a 40 micron cell strainer to remove large aggregates. Subsequently, the particles were washed twice with water at room temperature and lyophilized overnight. Table 1 lists the ...

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Abstract

The present invention is a surface-treated drug-loaded solid (e.g., non-porous) microparticle that aggregates in vivo to form consolidated large particles for drug therapy. In one embodiment, the particles are used for ocular treatment. Methods of producing the surface-treated microparticles and injectable formulations comprising the surface-treated microparticles are also provided. When used in the eye, long-term consistent intraocular delivery can be achieved without impairing vision and minimizing undesired inflammatory responses.

Description

[0001] This application is a divisional application of an invention patent application with an application date of November 11, 2016, an application number of 201680066275.2, and an invention title of "aggregated microparticles for treatment". [0002] Cross References to Related Applications [0003] This application claims priority to U.S. Application No. 62 / 254,707, filed November 12, 2015, U.S. Application No. 62 / 257,608, filed November 19, 2015, and U.S. Application No. 62 / 276,530, filed January 8, 2016 , which is incorporated herein by reference for all purposes. technical field [0004] The present invention is a surface-treated drug-loaded solid (e.g., non-porous) microparticle that aggregates in vivo to form consolidated macroparticles for drug therapy. In one embodiment, the particles are used in ocular therapy. Also provided are methods of producing the surface-treated microparticles and injectable formulations comprising the surface-treated microparticles. When...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/50A61K47/10A61K47/32A61K47/59A61K47/69A61K31/404A61P9/10A61P27/02A61P27/06A61P31/22
CPCA61K9/0019A61K9/0048A61K9/1641A61K31/404A61K47/6927A61K47/593A61K9/1635A61K9/5031A61K9/5026A61P27/02A61P27/06A61P31/22A61P9/10A61K47/26A61K9/1647A61K31/382A61K31/5377A61K31/542A61K47/36A61K9/1623A61K9/1652A61K9/5089A61K47/10
Inventor 余韵J·凯斯杨明J·L·克兰德
Owner GRAYBUG VISION INC