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Novel ?2-1,3-D-glucan porous microcapsule enveloped folate-functionalized liposomes as a Trojan horse for facilitated oral tumor-targeted co-delivery of chemotherapeutic drugs and quantum dot
摘要： In this study, a new type of β-1,3-D-glucan porous microcapsule (GPM)-enveloped and folate conjugated chitosan-functional liposome (FCL), FCL@GPM, was developed for the potential oral co-delivery of chemotherapeutic drugs and quantum dots (QDs) with facilitated drug absorption and antitumor efficacy. In this dual-particulate system, multiple FCLs serve as the cores for effective loading, folate-mediated tumor-targeting, facilitated intracellular accumulation, and pH-responsive controlled release of chemotherapeutic agents, while a GPM acts as the shell for affording macrophage-mediated tumor selectivity. Gefitinib (GEF) was selected as a chemotherapeutic agent, while acid degradable ZnO QDs were selected due to its dual role both as an anticancer agent for synergistic chemotherapy and as a fluorescent probe for potential cancer cellular imaging. The GEF and ZnO QDs co-loaded FCL@GPMs (GEF/ZnO-FCL@GPMs) have a prolonged release manner with limited release before uptake by intestinal cells. Furthermore, the Peyer’s patches uptake, macrophages uptake, cytotoxicity, and biodistribution of FCL@GPMs were tested. In addition, GEF and ZnO QDs co-loaded FCLs (GEF/ZnO-FCLs) not only have a tumor acidity responsive release property, but also induce a superior cytotoxicity on cancer cells as compared to GEF. Moreover, a 1.75-fold increase in the bioavailability of GEF delivered from GEF/ZnO-FCL@GPMs as compared to its trademarked drug (Iressa?). As a result, GEF/ZnO-FCL@GPMs exerted a superior antitumor efficacy (1.47-fold) as compared to its trademarked drug in mice. Considered together, the developed FCL@GPMs, combining the unique physicochemical and biological benefits of FCLs and GPMs, possess a great potential as an efficient delivery system for the co-delivery of chemotherapeutic agents and quantum dots.
关键词： chemotherapeutic drugs,pH-responsive controlled release,tumor-targeting,oral co-delivery,macrophage-mediated tumor selectivity,β-1,3-D-glucan porous microcapsule,folate conjugated chitosan-functional liposome,quantum dots
更新于2025-09-23 15:19:57
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New 55Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging
摘要： Overexpression of folate receptors (FRs) on di?erent tumor types (e.g., ovarian, lung) make FRs attractive in vivo targets for directed diagnostic/therapeutic agents. Currently, no diagnostic agent suitable for positron emission tomography (PET) has been adopted for clinical FR imaging. In this work, two 55Co-labeled albumin-binding folate derivatives-[55Co]Co-cm10 and [55Co]Co-rf42-with characteristics suitable for PET imaging have been developed and evaluated. High radiochemical yields (≥95%) and in vitro stabilities (≥93%) were achieved for both compounds, and cell assays demonstrated FR-mediated uptake. Both 55Co-labeled folate conjugates demonstrated high tumor uptake of 17% injected activity per gram of tissue (IA/g) at 4 h in biodistribution studies performed in KB tumor-bearing mice. Renal uptake was similar to other albumin-binding folate derivatives, and liver uptake was lower than that of previously reported [64Cu]Cu-rf42. Small animal PET/CT images con?rmed the biodistribution results and showed the clear delineation of FR-expressing tumors.
关键词： folate receptors,cobalt-55,PET imaging,albumin binder,ovarian cancer,folic acid
更新于2025-09-12 10:27:22
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[IEEE 2018 40th Annual International Conference of the IEEE Engineering in Medicine and Biology Society (EMBC) - Honolulu, HI, USA (2018.7.18-2018.7.21)] 2018 40th Annual International Conference of the IEEE Engineering in Medicine and Biology Society (EMBC) - Point-of-Care Assessment of Folate Status in Women of Reproductive Age Using a Fluorescence Lateral Flow Assay <sup>*</sup>
摘要： Folate is an essential vitamin to the development of a fetus in early pregnancy. Maternal folate supplementation around the time of conception has been shown to decrease the risk of neural tube defects (NTDs), a class of serious birth defects. The closure of the neural tube before the 28th day after conception necessitates that the folate intake must take place before most women know that they are pregnant. Therefore, screening women of reproductive age for folate status would allow for an improved understanding of the need for supplementation in women who could become pregnant as well as the effectiveness of current supplementation and fortification recommendations. Current folate assessment is limited to lab-based assays which require expensive equipment, trained personnel, and are time-intensive. Our point-of-care diagnostic test quantifies levels of folate in human serum with the use of a lateral flow assay and a portable imaging device. We have designed an assay which uses fluorescent particles, folate binding protein, and antibodies to measure serum folate. This test could be used in resource-limited settings, where access to laboratory infrastructure is limited and where knowledge of folate status in women of reproductive age is lacking. By increasing our understanding of folate status around the world, we can improve implementation of folic acid supplementation and fortification and therefore reduce the risk of NTDs.
关键词： portable imaging device,neural tube defects,point-of-care diagnostic,Folate,lateral flow assay
更新于2025-09-10 09:29:36
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Association between seasonal serum folate levels and ultraviolet radiation
摘要： UV radiation has been consistently reported to cause folate photodegradation in vitro and in human skin. Seasonal variations in UV radiation might explain seasonal changes in folate levels in blood. Yet, few studies have addressed this phenomenon. The main objective of this study was to investigate whether a relationship exists between seasonal variations in serum folate levels in a population of Spain (Latitude: 36° 41' 6.88''; Longitude: 4° 30' 0.64'') and the annual variations of solar ultraviolet reached in the localization. From a sample of 118831 serum folate determinations, two studies were performed. The first one, which included all subjects, showed a decreased in mean folate concentrations in all seasons with respect to winter with lower values in summer. The risk of folate deficiency was 1.37 times greater in summer than in winter (95%CI: 1.29-1.46). In the second study, subjects with a first folate determination in winter and a second one in summer were 3.32 more likely to develop folate deficiency than those with a first folate determination in summer and a second one in winter (95%CI: 1.55 to 7.11). Folate levels showed a seasonal variation inversely related to solar total UV radiation reached in our location, with maximum daily doses of 5000 J m-2 reached in June. A gradual increase in percentage of folate deficiency is observed since spring. So, patients with folate levels close to deficiency are at a higher risk of having folate deficiency in summer.
关键词： folic acid,solar ultraviolet radiation,seasonal variation,folate deficiency,folate,photodegradation,population study
更新于2025-09-09 09:28:46