In vitro evaluation of viability, integrity, and inflammation in genital epithelia upon exposure to pharmaceutical excipients and candidate microbicides was written by Gali, Youssef;Delezay, Olivier;Brouwers, Joachim;Addad, Noura;Augustijns, Patrick;Bourlet, Thomas;Hamzeh-Cognasse, Hind;Arien, Kevin K.;Pozzetto, Bruno;Vanham, Guido. And the article was included in Antimicrobial Agents and Chemotherapy in 2010.Safety of 纬-Cyclodextrin xhydrate This article mentions the following:
The use of microbicides is a promising approach for the prevention of HIV-1 transmission. Unfortunately, various candidates failed in clin. trials. In some cases, the candidate microbicide even resulted in enhanced virus transmission. Therefore, there is an urgent need to develop more predictive preclin. strategies to anticipate the in vivo efficiency/toxicity rate, including in vitro assays that evaluate effects on epithelial integrity and inflammation. The present study aims to identify potential safety issues concerning the use of microbicides and excipients commonly used in vaginal microbicide preparations The toxicities of various active pharmaceutical ingredients (APIs; TMC-120, UC-781, tenofovir [PMPA], PRO-2000, and glycerol monolaurate [GML]) and excipients (preservatives, cosolvents, surfactants, and cyclodextrins) were evaluated using an in vitro dual-chamber model and uterine cervical explants. Epithelial viability and permeation of fluorescent virus-sized beads, as well as induction of interleukin-8 (IL-8; as a sensitive marker of an inflammatory response), were assessed. Surprisingly, cell viability and epithelial layer integrity were compromised by most excipients at concentrations near the typical concentration used in vaginal gels, and a significant increase in the production of IL-8 was observed at subtoxic concentrations Within the APIs, TMC-120, UC-781, and PMPA showed higher selectivity indexes than PRO-2000 and GML. In conclusion, identification of safety issues concerning the use of pharmaceutical excipients could help to formulate less toxic vaginal microbicide preparations In the experiment, the researchers used many compounds, for example, 纬-Cyclodextrin xhydrate (cas: 91464-90-3Safety of 纬-Cyclodextrin xhydrate).
纬-Cyclodextrin xhydrate (cas: 91464-90-3) belongs to tetrahydropyran derivatives. Tetrahydropyrans are useful synthons for biologically important compounds. There is large number of marine macrolide natural products that contain tetrahydropyran and tetrahydrofuran ring together. For instance, goniodomin A (actin targeting polyether), prorocentrolide (toxin halistatins), and percentotoxineSafety of 纬-Cyclodextrin xhydrate
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics