Provided herein are nanoparticle-lipid composite carriers as theranostic agents, particularly for diagnosis and/or treatment of cancers and related diseases and conditions. In particular embodiments, the carrier composites comprise a lipid core and an outer shell of functionalized nanoparticles (fNPs).

The present invention provides nanoparticles comprising a) a micelle comprising an amphiphilic polymer with a number average molecular weight (Mn) of 20,000 g/mol or less, and b) at least one peptide comprising at least one T cell epitope. The present invention further provides pharmaceutical compositions comprising these nanoparticles and the use of the compositions for suppressing specific immune responses.

There is provided a microparticle composition suitable for molecular imaging, the composition comprising microparticles, wherein the microparticles comprise: a core microparticle structure having a central area and a shell, and wherein the core microparticle structure comprises (i) a phosphatidylcholine lipid: (ii) a phosphatidylethanolamine lipid comprising at least one maleimide moiety; and (iii) an alkoxylated fatty acid.

After a stroke the temporal course of microglial/macrophage activation is biphasic. The initial phase promotes neuroinflammation, while the later phase aids neurovascular recovery. Therefore the dynamics of stroke-induced cerebral microglial/macrophage activation are of substantial interest. In one embodiment, the present invention is directed to the use of novel anti-Iba-1-targeted superparamagnetic FePt nanoparticles immunocelles in conjunction with magnetic resonance imaging (MRI) to measure the spatiotemporal course of the activation of microglia/macrophages in brain tissue at 7, 14, and 28 days post-stroke. Ischemic cerebral lesion areas are identified using T.sub.2-weighted MR images. After injection of FePt nanoparticles as immunocelles, quantitative contrast changes in T.sub.2*-weighted MR images showed that the nanoparticles were taken up solely in brain regions that coincided with areas of microglial/macrophage activation detected by post-mortem immunohistochemistry. There was observed good agreement between the locations of the Fe.sup.+-cells, as shown by Perl's staining for iron, and the Iba-V-microgiia/macrophages, The time course of nanoparticle uptake paralleled the changes of microglial/macrophage activation and phenotypes measured by immunohistochemistry over the four week period post-stroke. Maximum microglial/macrophage activation occurred seven days post-stroke for both measures, and the diminished activation found after two weeks continued to four weeks. The results evidence that nanoparticle-enhanced MRI constitute a novel approach for monitoring the dynamic development of neuroinflammation in living animals during the progression and treatment of stroke and neurodegenerative diseases. The implications and methods for diagnosis and monitoring therapy of stroke and other disease states and conditions are presented.

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

Disclosed are compositions that contain a plurality of biocompatible self-assembling molecules that transform from isolated molecules or spherical micelles while in blood serum into cylindrical nanofibers in the acidic extracellular environment of tumors, which can be used to achieve a higher relative concentration of imaging drug delivery, or radiotherapeutic agents at the tumor site compared to non-tumor tissues. This transition is rapid and reversible, indicating the system is in thermodynamic equilibrium.

The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising: an aqueous phase, representing 70% to 90% by weight of the composition, advantageously 75% to 85% and more advantageously from 78% to 82% a lipid phase comprising an oil, representing 9.5% to 29.5% by weight of the composition, advantageously 14% to 25% and more advantageously 17% to 21%, a surfactant at the interface between the aqueous and lipid phases, the surfactant comprising at least one amphiphilic paramagnetic metal chelate and optionally an amphiphilic lipid; the total content of surfactant by weight relative to the oil being between 4% and 10% and advantageously between 5% and 8%; the total content of surfactant by weight relative to the composition being between 0.35% and 2.95% and advantageously between 0.5% and 2%; the oil comprising at least 70%, advantageously at least 80%, advantageously at least 95% by weight and especially at least 97% of saturated C6-C18, advantageously C6-C14 and more advantageously C6-C10 fatty acids.

Provided herein are phospholipid-free small unilamellar vesicle (PFSUV) compositions, including a steroid and a non-ionic surfactant wherein the molar ratio of steroid:nonionic surfactant is between 3:1 to 5:1. Furthermore, the compositions described herein were found to useful for drug loading, drug delivery where preferential targeting of drugs to the liver is of interest.

The present invention provides an alginic acid-based injectable hydrogel system for labeling an accurate position of a disease lesion and effectively delivering a drug to a target region. The formulation of the present invention can make it easy to locally inject a contrast agent and a drug into a target region while controlling the release rate of the contrast agent or the drug, with the formation of the hydrogel in the injected region. Through the advantages, the labeled position can be accurately determined from images, thereby enhancing the precision of surgical operation, with a minimal incision formed therefor. In addition, when used, the alginic acid-based injectable hydrogel system allows the effective local delivery of a drug to a target region while increasing the long-acting effect of the drug.