Study of Physico-Chemical Properties and Morphology of Phospholipid Composition of Indomethacin

Abstract

Nonsteroidal anti-inflammatory drugs (NSAIDs), inhibitors of cyclooxygenase-2, an enzyme involved in the formation of anti-inflammatory prostaglandin PGE2, are the most common treatment for chronic inflammatory diseases, such as, for example, arthritis. One of the most commonly used drugs of this class is indomethacin, a derivative of indolylacetic acid. In this work, we studied the physicochemical properties of the phospholipid composition of indomethacin obtained earlier (codenamed “Indolip”) and the effect of freeze drying on its parameters. It was shown that the properties such as particle size, light transmission, phospholipid oxidation index did not change significantly, which indicated the stability of the drug after lyophilization. Measurement of the spectra of small-angle neutron scattering has shown that morphologically, Indolip is a vesicle whose radius is five times greater than the value of the bilayer thickness.

Effect of an NGR Peptide on the Efficacy of the Doxorubicin Phospholipid Delivery System

“…The data obtained indicate a more stable state of the composition without the targeted component (more than 15 mV); the introduction of the NGR-containing peptide lowered the value of this parameter. In this regard, the further use of this composition in this form is advisable immediately after preparation; for long-term storage, it requires additional processing, for example, lyophilization, as has been done for a number of other drugs [47,48].…”

Nanoencapsulation and Nanocoating of Bioactives of Application Interest in Food, Nutraceuticals and Pharma

“…This is very interesting, since a large proportion of the novel drug candidates present low water solubility or a strong first-pass effect, which reduce their bioavailability [6]. In this regard, Tikhonova et al [7] studied the nanoencapsulation of indomethacin into phospholipid nanoparticles by means of lyophilization. The encapsulation of this drug will help to avoid side effects, such as cardiovascular and gastrointestinal disorders, as well as enhance bioavailability, consequently increasing bioactivity.…”