Rheological behavior study and its significance in the assessment of application properties and physical stability of phytosome loaded hydrogels

Abstract

Phytosomes are amphiphilic molecular complexes of substances of plant origin and phospholipids that are considered as active ingredients of dermopharmaceutical and cosmetic formulations of potentially improved efficiency. The study aim was the formulation of carbomer hydrogels with commercially available phytosomes of escin (Escin ß-Sitosterol Phytosome®) (EP) and 18-ß glycyrrhetinic acid (18-ß Glycyrrhetinic Acid Phytosome®) (GP) and evaluation of their application properties and real-time physical stability. Phytosomes incorporation did not significantly affect pH of the hydrogels, which was acceptable for cutaneous application. However, these hydrogels had significantly different organoleptic properties (opaque and softer consistency) compared to the hydrogel without active substance (C) and the hydrogels with pure active substances (E and G) used for comparison. The values of maximum and minimum apparent viscosity and yield stress were significantly lower in phytosome-loaded hydrogels. The results of oscillatory rheological analysis indicated that viscous character prevails in EP and GP hydrogels (elastic modulus (G')˂viscous modulus (G")), while in hydrogels C, E and G elastic properties were more pronounced (G'˃G"). Escin phytosome had greater influence on carbomer gel network strength. Phytosome-loaded hydrogels were physically stable during 24 months of storage under ambient conditions, although the rheological analysis also indicated a potential risk of sedimentation.

Fitosomi su amfifilni molekulski kompleksi supstanci biljnog porekla i fosfolipida koji se razmatraju kao aktivni sastojci dermofarmaceutskih i kozmetičkih formulacija potencijalno unapređene efikasnosti. Cilj studije bio je formulacija karbomernih hidrogelova sa komercijalno dostupnim fitosomima escina (Escin ß-Sitosterol Phytosome®) (EP) i 18-ß gliciretinske kiseline (18-ß Glycyrrhetinic Acid Phytosome®) (GP) i njihova karakterizacija u cilju procene aplikativnih svojstava i fizičke stabilnosti u realnom vremenu. Inkorporiranje fitosoma nije značajno uticalo na pH hidrogelova, koji je bio prihvatljiv za primenu na koži. Međutim, ovi hidrogelovi imali su značajno različite organoleptičke osobine (neprozirni i mekše konzistencije) u poređenju sa hidrogelom bez aktivne supstance (C) i odgovarajućim hidrogelovima sa čistim aktivnim supstancama (E i G) koji su upotrebljeni za poređenje. Vrednosti maksimalnog i minimalnog prividnog viskoziteta i napon popuštanja bili su značajno niži kod hidrogelova sa fitosomima. Rezultati oscilatorne reološke analize ukazali su da kod hidrogelova EP i GP preovlađuje viskozni karakter (elastični modul (G')˂viskozni modul (G")), dok su kod hidrogelova C, E i G bila izraženija elastična svojstva (G'˃G"). Fitosom escina je imao veći uticaj na jačinu karbomerne gelske mreže. Hidrogelovi sa fitosomima bili su fizički stabilni tokom 24 meseca čuvanja pod ambijentalnim uslovima, mada su rezultati reološke analize ukazali na potencijalni rizik od sedimentacije.