Dennis E. Discher - Philadelphia PA, US Shenshen Cai - Morgan Town WV, US Yan Geng - Langhorne PA, US Paul Dalhaimer - Sheboygan WI, US
International Classification:
A61K 31/337 C12N 5/02 A61P 35/00
US Classification:
514449, 435375
Abstract:
Provided are filomicelle nanocarrier systems for the controlled transport and bioselective delivery of encapsulatable, cytotoxic active agents contained therein, particularly anticancer agents. Further provided are methods for controlling destabilization of the filomicelle membrane and the resulting hydrolysis-triggered, controlled release of the active agent(s) encapsulated therein by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s), wherein bioselective release of the encapsulated cytotoxic agents is distributed intracellularly, and wherein lowered dosage of the drug was delivered to the non-tumor organs. Thus, the filomicelle system offers enhanced tumor-selective biodistribution of a drug, and a reduced toxicity of the encapsulated drug to other organs.
Block Co-Polymer Worm Micelles And Methods Of Use Therefor
Dennis Discher - Philadelphia PA, US Paul Dalhaimer - Sheboygan WI, US
International Classification:
A61K048/00 A61K049/00 A61K009/127
US Classification:
424009520, 424450000, 514044000, 514002000
Abstract:
Provided are worm-like micelles, capable of encapsulating at least one encapsulant, wherein each worm-like micelle comprises one or more wholly synthetic, polymeric, super-amphiphilic molecules that self assemble in aqueous solution, without organic solvent or post assembly polymerization; and wherein at least one of said super-amphiphilic molecules is a hydrophilic block copolymer, the weight fraction (w) of which, relative to total copolymer molecular weight, directs assembly of the amphiphilic molecules into the worm-like micelle of up to one or more microns in length, and determines its stability, flexibility and convective responsiveness. Also provide are methods of preparing and methods of using the worm-like micelles, particularly when loaded with one or more encapsulants. The loaded worm-like micelles of the present invention are particularly suited for the stable and controlled transport, delivery and storage of materials, either in vivo or in vitro.