Targeted delivery of therapeutics possesses the potential to localize therapeutic agents to a specific tissue as a mechanism to enhance treatment efficacy and abrogate side effects. Antibodies have been used clinically as therapeutic agents and are currently being explored for targeting drug-loaded nanoparticles. Peptides such as RGD peptides are also being developed as an inexpensive and stable alternative to antibodies. In this study, cyclo(1,12)PenITDGEATDSGC (cLABL) peptide was used to target nanoparticles to human umbilical cord vascular endothelial cells (HUVEC) monolayers that have upregulated intercellular cell-adhesion molecule-1 (ICAM-1) expression. The cLABL peptide has been previously demonstrated to possess high avidity for ICAM-1 receptors on the cell surface. Poly(DL-lactic-co-glycolic acid) nanoparticles conjugated with polyethylene glycol and cLABL demonstrated rapid binding to HUVEC with upregulated ICAM-1, which was induced by treating cells with the proinflammatory cytokine, interferon-γ. Binding of the nanoparticles could be efficiently blocked by pre-incubating cells with free peptide suggesting that the binding of the nanoparticles is specifically mediated by surface peptide binding to ICAM-1 on HUVEC. The targeted nanoparticles were rapidly endocytosed and trafficked to lysosomes to a greater extent than the untargeted PLGA-PEG nanoparticles. Verification of peptide-mediated nanoparticle targeting to ICAM-1 may ultimately lead to targeting therapeutic agents to inflammatory sites expressing upregulated ICAM-1.
Pure curcumin, an excellent curcuminoid derivative, decreased WT1 gene expression in both transcriptional and translational levels. Thus, pure curcumin is one of a potential chemotherapeutic agent used for treatment of human leukemia. However, its chemotherapeutic property will need to be studied more in future.
The aim of this research was to develop and validate a spectrofluorimetric method for determination of tranexamic acid in hydrogel patch formulations. Tranexamic acid (trans‐4‐aminomethylcyclohexanecarboxylic acid, trans‐AMCHA) is an antifibrinolytic drug that recently gained attention as a skin‐whitening agent due to its inhibitory effect on ultraviolet (UV)‐induced pigmentation in vivo. Derivatization with naphthalene‐2, 3‐dicarboxaldehyde (NDA) in the presence of cyanide ion (CN‐) to produce a fluorescent 1‐cyanobenz[f]isoindole (CBI) product (?ex = 420 nm, ?em = 480 nm) [[Au: Please check the symbol.]] is for the first time reported for the determination of tranexamic acid in hydrogel patch formulations. Other separation techniques were not used in the analysis of the CBI‐fluorescent product as required in the previous studies. The developed method was proven to be precise and accurate with percent recoveries ranging between 98.0% and 101.8% at the concentration range of 8.4–84.0 μg/ml (R2 > 0.999). The intra‐and inter‐day precisions as expressed by the relative standard deviations (RSD) were below 1.85%. Derivatization of tranexamic acid with NDA/CN‐was completed within 5 min and was stable for at least 30 min. The method has been applied to the analysis of drug content and release profiles in tranexamic hydrogel patch formulations.
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