FRET imaging revealed that nanocrystals enhanced drug oral absorption by dissolution rather than endocytosis: A case study of coumarin 6 was written by Zhang, Guangshuai;Wang, Yunzhi;Zhang, Zuopeng;He, Zhonggui;Liu, Yang;Fu, Qiang. And the article was included in Journal of Controlled Release in 2021.Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:
Nanocrystals (NCs) exhibit potential in improving oral bioavailability for poorly water-soluble drugs. However, whether NCs improve oral absorption by quick dissolution or by endocytosis remains inconclusive because tracking of dissolved drugs and NCs particles cannot occur simultaneously. In this study, we aim to elucidate how NCs improve oral absorption by using coumarin 6 (C6), an aggregation-caused quenching fluorophore, and 2-((5-(4-(dip-tolylamino)phenyl)thiophen-2-yl)methylene)malononitrile (MeTTMN), an aggregation-induced emission fluorophore. C6 was used as a model drug to prepare NCs and MeTTMN was incorporated to construct fluorescence resonance energy transfer (FRET) pairs. Thus, the mol. absorption can be detected using the fluorescence signal of dissolved C6 and the NCs particles can be tracked simultaneously by monitoring FRET signals. The reliability of this tracking method was validated. Accordingly, in vitro dissolution, gastrointestinal traffic, and biodistribution studies were conducted. The results showed that dissolved C6 mols. were the main absorption mode of C6 NCs. Identification of such pathways bears considerable significance for the broad application of drug NCs in improving the druggability of insoluble drugs. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one).
3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Name: 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica