John Garner

PLGA-NHS from PolySciTech used in development of Prodrug Nanoparticles for drug delivery to cancer

Blog Post created by John Garner on May 3, 2019

Langecker, 2018 prodrug nanoparticles polyscitech.jpg

One method of loading drugs into a polymer, beyond simple encapsulation, is to actively conjugate the drug to the end or side-chains of the polymer so that it is bound by a cleavable linkage. Such a design is called a ‘prodrug’ in that it breaks down to release the drug in the human body. In organic chemistry, N-hydroxysuccinimide ester serves as an effective ‘leaving group’ when enables these kinds of attachments to occur between a carboxylic acid and a nucleophile (typically an amine). One of the products PolySciTech Provides is PLGA-NHS, this is a degradable PLGA chain with the acid endcap activated into the NHS-ester form such that it is ready to conjugate to a nucleophile. Recently, researchers at Los Gatos Pharmaceuticals, Inc Used PLGA-NHS (AI096) from PolySciTech (www.polyscitech.com) to create drug-conjugate (Prodrug) and form this into nanoparticles. This research holds promise to provide for superior drug delivery formulations which may be effective for cancer therapy. Read more: Langecker, Peter, Matthias Steiert, Toshiaki Hino, Jan Scicinski, and Kumarapandian Paulvannan. "Composite Nanoparticles And Uses Thereof." U.S. Patent Application 16/026,446, filed December 27, 2018. https://patents.google.com/patent/US20180369232A1/en

“Abstract: Provided herein are composite nanoparticles, methods of making composite nanoparticles and methods of using composite nanoparticles to treat or ameliorate various diseases, such as, for example, cancer. (Synopsis from Background/Summary): What is needed are nanoparticles large enough for selective tumor tissue penetration (diameter of between 60 and 400 nm) which can decompose within the tissue to a size amenable for cellular uptake (diameter of less than about 20 nm) by tumor cells. The above concept may have broad applicability beyond selective delivery of active ingredients to tumor tissues. The present invention satisfies these and other needs by providing in one aspect, a composite nanoparticle. The composite nanoparticle includes subunit nanoparticles of between about 10 nm and about 20 nm diameter which contain an active ingredient, wherein the composite nanoparticle has a diameter of between about 60 nm and about 400 nm. In another aspect, a method for forming composite nanoparticles is provided. Subunit nanoparticles of diameter between about 10 nm and about 20 nm which include an active ingredient are synthesized and assembled into composite nanoparticles of diameter between about 60 nm and about 400 nm.”

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