Statins used in the treatment of dyslipidemias are top-selling drugs in the world. Economical production of statins in industrial scale is challenging, because the side chain of statins is a 3,5-dihydroxyacid derivative consisting of two asymmetric centers. The most prominent methods for the preparation of the side chain are based on biocatalysis and surveyed in this review.
The use of nanoparticle carriers for the sustained release of cytotoxic drugs in cancer therapy can result in fewer adverse effects and can thus be of great benefit for the patient. Recently, a novel nanocomposite, prepared by the encapsulation of THCPSi nanoparticles within solid lipids (SLN), was developed and characterized as a promising drug delivery carrier in vitro. The present study describes the in vivo evaluation of unmodified THCPSi nanoparticles and THCPSi-solid lipid nanocomposites (THCPSi-SLNCs) as potential drug delivery carriers for cancer therapy by using (18)F radiolabeling for the detection of the particle biodistribution in mice. Passive tumor targeting of (18)F-THCPSis and (18)F-THCPSi-SLNCs by the enhanced permeation and retention effect was investigated in a murine breast cancer model. Encapsulation of THCPSi nanoparticles with solid lipids improved their accumulation in tumors at a 7 week time point (tumor-to-liver ratio 0.10 ± 0.08 and 0.24 ± 0.09% for (18)F-THCPSis and (18)F-THCPSi-SLNCs, respectively).
The [ 18 F]radiolabelling of the melanin-targeting positron-emission tomography radiotracer [ 18 F]MEL050 was rapidly optimised using a commercial continuous-flow microfluidic system. The optimal [ 18 F]fluorination incorporation conditions were then translated to production-scale experiments (35-150 GBq) suitable for preclinical imaging, complete with automated HPLC-solid phase extraction purification and formulation. [ 18 F]MEL050 was obtained in 43 AE 10 % radiochemical yield in ,50 min.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.