Quality by design approach for preparation of zolmitriptan/chitosan nanostructured lipid carrier particles – formulation and pharmacodynamic assessment was written by Awadeen, Randa Hanie;Boughdady, Mariza Fouad;Meshali, Mahasen Mohamed. And the article was included in International Journal of Nanomedicine in 2020.Quality Control of (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one This article mentions the following:
Zolmitriptan (ZT) is a selective serotonin agonist that is used for the treatment of migraine. It belongs to BCS class III with high solubility and low permeability. Besides, the drug is subjected to pre-systemic metabolism Accordingly, new Zolmitriptan/chitosan nanostructured lipid carriers (ZT/CT NLCs) coated with Tween 80 (stealthy layer) have been developed to overcome such demerits. The NLCs were developed by combining ultrasonication and double emulsion (w/o/w) techniques. The lipids were Gelucire and Labrasol. Herein, the quality by design (23 full factorial design) was scrupulously followed, where critical process parameters and critical quality attributes were predefined. The optimized formulation (F8) was fully characterized with respect to entrapment efficiency (%EE), percentage yield (% yield), particle size, size distribution (PDI), zeta potential (ZP), morphol. appearance (TEM). In vitro release, stability study and pharmacodynamic evaluations were also assessed. The optimized freeze dried formula was dispensed in in situ gelling hard gelatin capsule encompassing pectin and guar gum for further in vitro and pharmacodynamic evaluations. The optimized spherical nanoparticles experienced high percentage EE and yield (78.14% and 60.19%, resp.), low particle size and PDI (343.87 nm and 0.209, resp.), as well as high neg. ZP (-25.5 mV). It showed good phys. stability at refrigerated conditions. The NLCs dispensed in in situ gelling hard gelatin capsule comprising pectin and guar gum experienced sustained release for 30 h and significantly maintained the pharmacol. effect in mice up to 8 h (p < 0.001). ZT, a BCS class III drug that suffers from poor permeability and pre-systemic metabolism, was successfully maneuvered as nanostructured lipid carrier particles (NLCs). The incorporation of the NLCs in in situ gelling hard gelatin capsules fulfilled a dual function in increasing permeability, as well as sustaining the pharmacodynamic effect. This result would open new vistas in improving the efficacy of other class III drugs. In the experiment, the researchers used many compounds, for example, (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8Quality Control of (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one).
(S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one (cas: 139264-17-8) belongs to oxazolidine derivatives. Oxazolidines that are the precursor to bisoxazolidines are in effect mono-oxazolidines. They are also used as moisture scavengers in polyurethane and other systems. In another report, the incorporation of an additional substituted oxazolidine ring over a range of new biphenylazepinium salt organocatalysts for the asymmetric epoxidation of alkenes improved enantiocontrol over the parent structures.Quality Control of (S)-4-((3-(2-(Dimethylamino)ethyl)-1H-indol-5-yl)methyl)oxazolidin-2-one
Referemce:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem