Bioavailability enhancement of vitamin E TPGS liposomes of nintedanib esylate: formulation optimization, cytotoxicity and pharmacokinetic studies was written by Kala, Shabari Girinath;Chinni, Santhivardhan. And the article was included in Drug Delivery and Translational Research in 2022.Related Products of 656247-18-6 The following contents are mentioned in the article:
Abstract: Nintedanib esylate is a kinase inhibitor designated for the cure of non-small cell lung cancer suffered from first-pass metabolism which resulted in low oral bioavailability (∼ 4.7). The exploration intended to increase the oral bioavailability of drug by means of D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) liposomes. The nintedanib esylate-loaded TPGS liposomes were prepared by thin-film hydration method by optimizing process parameters like phospholipids:cholesterol ratio, drug loading and sonication time through the design of experiments The drug′s behavior was studied using a variety of techniques, including physicochem. characterization and in vitro and in vivo studies. TPGS liposomes had a particle size of 125 ± 6.7 nm, entrapment efficiency of 88.6 ± 4.1and zeta potential of + 46 ± 2.8 mV. X-ray diffraction anal. revealed the drug was converted to partially amorphous state, while transmission electron microscope images showed the spherical shape with TPGS on the surface of liposomes. The formulation showed Higuchi kinetics with sustained drug release of 92in 36 h. Cellular uptake of C-6-labeled liposomes was observed in A-549 cells and cytotoxicity testing revealed that liposomes were more effective than marketed formulation. The preparation was found stable in stability chamber and simulated fluids. Liposomal oral bioavailability was ∼ 6.23 times greater in Sprague-Dawley male rats compared to marketed formulation, according to in vivo pharmacokinetic data. Liposomes performed better than marketed capsules upon oral administration because of the prolonged drug release and increased oral bioavailability; as a result, the developed formulation can become a successful strategy in cancer chemotherapy. This study involved multiple reactions and reactants, such as (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6Related Products of 656247-18-6).
(Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate (cas: 656247-18-6) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Related Products of 656247-18-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics