Princeton University

Chester E Markwalter

Robert K Prud'homme

Robert F Pagels

Hydrophilic molecules such as biologics, which can include peptides, proteins, and other biologically-derived materials, can be used as therapeutic agents in medical applications. They can face administration challenges because of poor membrane permeability and rapid clearance from the blood stream. Methods for the formation of a core-shell-brush nanoparticle from an A-B-C triblock copolymer are set forth. A hydrophilic core can contain the biologic and the C Block of the copolymer. The shell can be comprised of the precipitated B Block, and the A Block can form a stabilizing brush layer. The particles can be assembled by sequential precipitations under defined mixing conditions. Presented herein are methods to tune release based on process parameters during particle assembly and triblock characteristics.

Triblock copolymer stabilizers for the formation of nanoparticles encapsulating soluble biologics, therapeutics, and imaging agents

A method for controlling the encapsulation efficiency and burst release of water soluble molecules from nanoparticle and microparticle formulations produced by the inverted Flash NanoPrecipitation (iFNP) process and subsequent processing steps is presented. The processing steps and materials used can be adjusted to tune the encapsulation efficiency and burst release of the encapsulated water-soluble material. The encapsulation efficiency of the soluble agent in the particles and the burst release of the soluble agent from the particles can be controlled by: (1) the copolymers used in the assembly or coating process, (2) the degree of crosslinking of the nanoparticle core, (3) the incorporation of small molecule or polymeric additives, and/or (4) the processing and release conditions employed.

Method for controlling encapsulation efficiency and burst release of water soluble molecules from nanoparticles and microparticles produced by inverse flash nanoprecipitation

An 'inverse' precipitation route to precipitate aqueous soluble species with copolymers as nanoparticles having a hydrophilic, polar core and a less polar shell is described. The aggregation of these nanoparticles to form larger microparticles and monoliths provides a highly loaded construct (e.g., a depot) for the sustained and controlled release of actives.

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Princeton, NJ, United States of America

Chester E Markwalter