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Polymeric drug carrier for image-guided delivery

A polymer, drug technology, applied in or guided delivery, chemical exchange-dependent saturation transfer contrast agent, reagent field of drug carrier

Inactive Publication Date: 2010-11-17
KONINKLIJKE PHILIPS ELECTRONICS NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Polymeric drug carrier for image-guided delivery
  • Polymeric drug carrier for image-guided delivery
  • Polymeric drug carrier for image-guided delivery

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Embodiment Construction

[0106]Abbreviations used in the examples, to the extent not used above: PBD is poly(butadiene), PEO is poly(ethylene oxide), HEPES is (4-(2-hydroxyethyl)-1 -piperazineethanesulfonic acid).

[0107] Polymersomes with an average diameter of 100-150 nm were formed by thin film hydration techniques combined with subsequent extrusion. Briefly, Mn(g / mol): PBD(2500)-b-PEO(1300), PD=1.04 and f EO = 0.34 poly(butadiene (1,2-addition)-b-oxirane) dissolved in CHCl 3 middle. The solvent was gently removed under reduced pressure to obtain a thin polymer film. The membrane contained 65mM [Tm(hpdo3a)(H 2 O)] and 5mM carboxyfluorescein in 20mM HEPES solution for hydration. Sonication at 50°C for 30 minutes followed by three freeze-thaw cycles under vacuum using liquid nitrogen at -177°C and a water bath at 50°C resulted in a monodisperse distribution of polymersomes. Subsequently, the dispersion was extruded several times through polycarbonate filters with pore diameters of 1 μm, 0.4 μm...

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Abstract

Described are Chemical Exchange-dependent Saturation Transfer (CEST) contrast agents for Magnetic Resonance Imaging (MRI) comprising a polymersome provided with a paramagnetic agent. The polymersome preferably comprises a polymeric shell enclosing a cavity, wherein the cavity comprises a pool of proton analytes, and wherein the shell allows diffusion of the proton analytes. The polymersome-based CEST MRI contrast agents are suitable as drug carriers useful in MRI-guided drug release.

Description

field of invention [0001] The present invention relates to image guided drug delivery based on polymersomes as drug carriers. More particularly, the present invention relates to magnetic resonance imaging (MRI) monitored or guided delivery of biologically active agents such as therapeutic or diagnostic agents (hereinafter "drugs"). Furthermore, the present invention relates to a Chemical Exchange-dependent Saturation Transfer (CEST) contrast agent for magnetic resonance imaging (MRI), in particular to an agent suitable for use as a drug carrier. Background of the invention [0002] Many diseases localized primarily in specific tissues are treated with systemically administered drugs. A well-known example of standard cancer therapy is systemic chemotherapy, which is accompanied by significant side effects on the patient due to undesired biodistribution and toxicity. The therapeutic window of these drugs is generally defined by, on the one hand, the minimum required therapeu...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K49/00A61K49/18A61K9/00A61K9/127
CPCA61K41/0028A61K9/1273A61K49/1812A61P35/00
Inventor S·兰格赖斯H·格鲁尔L·L·P·梅萨格J·A·皮克马特D·伯丁斯基
Owner KONINKLIJKE PHILIPS ELECTRONICS NV
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