摘要:
A method for measuring tumor response to a cancer therapy is provided. The method comprises the steps of injecting a polymeric contrast agent in a subject; obtaining a series of magnetic resonance image signals of the contrast agent in the tumor for up to about 60 minutes; and determining a slope of the magnetic resonance image signal as a function of time.
摘要:
A method for synthesizing extended poly(amino acids) conjugated to imaging agents, such as DTPA, is disclosed. The amino acid is initially conjugated to the imaging agent at the monomer stage, followed by formation of the corresponding N-carboxyanhydride. The method utilizes catalyzed ring opening polymerization of the N-carboxyanhydride of the amino acid-imaging agent monomer allowing the formation of a poly(amino acid) backbone having 100% imaging agent conjugation if desired. However, the present method also permits the degree of conjugation to be controlled by copolymerizing the N-carboxyanhydride of the amino acid-imaging agent monomer with one or more unconjugated monomers, i.e. N-carboxyanhydrides of the same or of other amino acids. Various imaging agents may be employed, and new hybrid random, block, and mixed copolymers may be prepared.
摘要:
Novel degradable macromolecular magnetic resonance imaging contrast agents for use in various diagnostic procedures, and methods for synthesizing, using and degrading these agents, are disclosed. The macromolecule contrast agents disclosed in various aspects of this invention are degradable gadolinium compounds which show prolonged plasma retention, and enhanced permeability and retention in solid tumors, but are still capable of being rapidly cleared from the body.
摘要:
Magnetic resonance (nullMRnull) contrast-enhancing agents comprise poly(amino acid) backbone chain conjugated to chelating moieties that comprise a plurality of carboxylic acid groups that form coordination complexes with paramagnetic ions. A method for detecting atherosclerotic plaque areas comprises administering at least one of these contrast agents into a subject; and obtaining and comparing MR images of and MR signals from the plaque areas before and after administering the contrast agent. The method can be used to assess an effectiveness of a prescribed course of treatment for atherosclerosis.
摘要:
This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.
摘要:
Linear extended polymeric paramagnetic chelates for use as MRI contrast agents are synthesized by conjugating DTPA chelator moieties to higher than 90% of the monomer residues of the polyamino acid backbone chain. The resulting polymer can be labeled with Gd, since each chelator moiety holds a Gd ion, and the resulting conformation is of an unfolded, extended linear type, capable of entering small pores and moving around obstacles in the extracellular space of tissues. The efficient production of these extended polymers is critical for the application of such contrast agents to medical imaging. One such agent is a reptating polymer containing technetium-99.
摘要:
Linear extended polymeric paramagnetic chelates for use as MRI contrast agents are synthesized by conjugating DTPA chelator moieties to higher than 90% of the monomer residues of the polyamino acid backbone chain. The resulting polymer can be labeled with Gd, since each chelator moiety holds a Gd ion, and the resulting conformation is of an unfolded, extended linear type, capable of entering small pores and moving around obstacles in the extracellular space of tissues. The efficient production of these extended polymers is critical for the application of such contrast agents to medical imaging. One such agent is a reptating polymer containing technetium-99.
摘要:
This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).
摘要翻译:本发明提供用于增强药物和其它药物穿过上皮组织(包括皮肤,胃肠道,肺上皮等)的递送的组合物和方法。 组合物和方法也可用于穿过内皮组织,包括血脑屏障。 与非共轭化合物相比,组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白,以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6至25个残基之间的聚精氨酸分子(SEQ ID NO:50)。
摘要:
Improved methods for forming substituted polymers having a high degree of conjugation include the steps of activating a steric hindrance molecule under conditions that ensure substantially all the steric hindrance molecules are mono-activated and then reacting with a polymer. An improved method for recovering polypeptides substituted with steric hindrance molecules and having an elongate configuration removes impurities and volatiles without achieving complete dryness of the copolymer.
摘要:
Sequential injections of contrast agents are employed for assessing angiogenic activity. At least one of the injections is of a polymeric contrast agent which binds to angiogenic microvasculature.