Extended release microparticles and suspensions thereof for medical therapy
Inventors
Yang, Ming • Cleland, Jeffrey L. • Yu, Yun • Yu, Weiling • Kays, Joshua
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11160870-B2
Publication Date
2021-11-02
Expiration Date
Abstract
An improved microparticle or lyophilized or otherwise reconstitutable microparticle composition thereof for medical therapy, including ocular therapy.
Core Innovation
The invention relates to a solid aggregating biodegradable microparticle comprising a prodrug of a therapeutically active compound. The microparticle includes encapsulation in poly(lactic-co-glycolic acid) (PLGA) and/or polylactic acid (PLA), and PLGA and/or PLA covalently bound to polyethylene glycol (PEG), together with a surfactant. The prodrug is defined by a formula, or a pharmaceutically acceptable salt thereof, wherein y and yb2 each take values from 1 to 10.
The microparticle has a mean diameter between 20 b5m and 40 b5m and is surface-modified with a surface-treatment agent to partially degrade surface polymer at a temperature less than about 18b0 C. The surface-treatment agent is selected from an aqueous base/alcohol, an aqueous acid/alcohol, phosphate buffered saline/alcohol, or water/alcohol. The solid aggregating biodegradable microparticle is configured to aggregate in vivo.
In vivo, the microparticle aggregates to form at least one pellet of at least 500 b5m, and the resulting pellet provides sustained drug delivery in vivo for at least three months. The claim framework ties the prodrug structure, polymer encapsulation and covalent PEG binding, surfactant inclusion, particulate size, and specific surface-treatment selection to long-duration in vivo sustained delivery.
Claims Coverage
The provided material includes one independent claim. The claim centers on a solid aggregating biodegradable microparticle with five inventive features covering prodrug structure, polymer encapsulation and PEG covalent binding, surfactant inclusion, particle size, surface polymer partial degradation under low temperature with selected surface-treatment agents, and in vivo aggregation to pellets providing sustained drug delivery.
Solid aggregating biodegradable microparticle with prodrug of formula
A solid aggregating biodegradable microparticle comprising a prodrug of a therapeutically active compound, wherein the prodrug is of the formula with y and yb2 each selected from 1 to 10, or a pharmaceutically acceptable salt thereof.
Polymer encapsulation and covalent PEG binding with surfactant
The microparticle includes the prodrug and is encapsulated in poly(lactic-co-glycolic acid) (PLGA) and/or polylactic acid (PLA) and includes PLGA and/or PLA covalently bound to polyethylene glycol (PEG), together with a surfactant.
Specific mean diameter range for the microparticle
The microparticle has a mean diameter between 20 b5m and 40 b5m.
Surface-modification to partially degrade surface polymer at less than about 18b0 C
The microparticle has been surface-modified with a surface-treatment agent to partially degrade surface polymer at a temperature less than about 18b0 C, wherein the surface-treatment agent is selected from an aqueous base/alcohol, an aqueous acid/alcohol, phosphate buffered saline/alcohol, or water/alcohol.
In vivo aggregation to pellet and sustained drug delivery duration
The microparticle aggregates in vivo to form at least one pellet of at least 500 b5m that provides sustained drug delivery in vivo for at least three months.
Overall, the claim coverage centers on a prodrug-defined biodegradable microparticle that combines PLGA/PLA encapsulation and PEG covalent binding with a surfactant, enforces a specific microparticle mean diameter, applies selected low-temperature surface-treatment conditions to partially degrade surface polymer, and requires in vivo aggregation into sufficiently large pellets that sustain drug delivery for at least three months.
Stated Advantages
Provides sustained drug delivery in vivo for at least three months.
Aggregates in vivo to form at least one pellet of at least 500 b5m in vivo.
Partially degrades surface polymer at a temperature less than about 18b0 C.
Documented Applications
In vivo sustained drug delivery using a solid aggregating biodegradable microparticle that aggregates to form at least one pellet.
Interested in licensing this patent?