Effect of Quercetin, Caffeic Acid and Caffeic Acid Phenylethyl Ester, Solubilized in Non-ionic Surfactants, on Histamine Release in vivo and in vitro

Abstract

Summary A practical hindrance in using many therapeutic agents is their limited solubility in aqueous matrixes. This is usually overcome by incorporating the active compounds in a matrix, with the aid of a non-ionic surfactant. Three water-insoluble natural polyphenols with inherent biological activity, quercetin (CAS 117-39-5), caffeic acid and caffeic acid phenylethyl ester, were solubilized in water, with the aid of Tween?. 80 (an esterified and polyethoxylated derivative of sorbitan), Solutol?. HS15 (a polyethoxylated derivative of 12-hydroxy-stearic acid), Cremophor?. RH40 (a ricinoleic acid derivative) or Cremophor?. EL and the effect of the solubilized polyphenols on histamine release was studied in vitro (mast cells) and in vivo in the rat. In vivo Cremophor EL alone increased, and Tween 80 decreased histamine plasma levels. All four groups injected with solubilized quercetin exhibited a decrease in their plasma histamine levels. Caffeic acid solubilized in Cremophor RH40 decreased histamine levels, too. In vitro Tween 80 increased histamine release in a dose-dependent mode. Quercetin in vitro inhibited histamine release in all solubilizers used. It is concluded that the ability of the studied polyphenols to release histamine is not only depending on the condition of the storage vesicles in the mast cells, but also on the surfactant used to solubilize them.

Anti-Apoptotic and Anti-Oxidant Effects of Caffeic Acid Phenethyl Ester on Cadmium-Induced Testicular Toxicity in Rats

“…In our study, to induce toxicity, 1 mg/kg of Cd was injected into rats for 30 days [13,23]. This study confirmed the results of recent studies [39,40] that suggest CAPE also has in vivo effects, besides its proven in vitro effect [41]. As shown in our previous studies, these results also indicated that CAPE has a well-distributed systemic circulation and an easy passage from the serous membranes [42].…”

Preparation of Caffeic Acid Phenethyl Ester-Incorporated Nanoparticles and Their Biological Activity

“…However, poor aqueous solubility of CAPE is a limiting factor in the actual application in cancer chemotherapy. Scheller et al used surfactant such as Tween ® 80, Solutol ® HS15, Cremophor ® RH40, or Cremophor ® EL to solubilize CAPE in the aqueous solution. We fabricated CAPE‐incorporated nanoparticles using CE diblock copolymer by nanoprecipitation/diafiltration method and then these aqueous nanoparticle solutions were lyophilized to store in the refrigerator.…”

Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems

“…The lower the CMC, the more easily micelles are formed. The first study of a CAPE micelle formulation was on non-ionic surfactant dispersions at concentrations close to their CMCs (CMCs in the range of 0.1 mM to 1 mM or 0.01% to 0.05% w/v) and higher, which aimed at studying their histamine-releasing potential (Scheller et al 2000). CAPE was formulated in Tween 80, Solutol HS15, Cremophor RH40 or Cremophor EL.…”