Encapsulation of isorhamnetin glycosides from opuntia ficus-indica through a liposomal delivery system and its anti-aging effect

Abstract

Introduction. Opuntia ficus-indica, known as prickly pear, has multiple biological applications, many of them attributed to its phenolic compounds: isorhamnetin glycosides. In addition to having these advantages, these compounds have limitations characterized by their high polarity that limits their permeability through skin layers for use in topical formulations, bioavailability due to the size of the structures, the rapid metabolization and thermosensitive feature. In order to increase their stability and solubility, the compounds were encapsulated through a liposomal delivery system. Methods. The extraction of the compound was carried out by means of ethanolic extraction in a 50:50 ethanol:water ratio. The isorhamnetin glycosides were identified by a high pressure liquid chromatograph equipped with a photodiode array detector and quantified as milligrams of total isorhamnetin glycosides per extract gram by a high-pressure liquid chromatograph equipped with a UV-Vis detector. The liposomes were synthesized by the thin-film layer evaporation and extrusion technique through a mixture of lipids (phosphatidylcholine and cholesterol in the following ratios: 7:3 and 10:1) using chloroform and methanol as solvents. Diameter size, polydispersity index, zeta potential, and stability studies were evaluated through dynamic light scattering (DLS) measurements in a zetasizer instrument. Encapsulation efficiency and release percentage analysis were also evaluated through a high-pressure liquid chromatograph equipped with a UV-Vis detector. Results. Liposomes of nanometric size were obtained consisting of a combination of cholesterol and phosphatidylcholine (70:30) ranging from 77.68 ± 10.76 nm to 297.20 ± 33.79 nm. The encapsulation efficiency of the liposomes is on a range from 87.85% ± 13.49 to 98.61% ± 0.93. More stable smaller particle size values were achieved when using a 7:3 lipid ratio in the liposomal synthesis. Also, these liposomes demonstrated an anti-elastase activity of 21.72% and a 15.83% of anti-collagenase activity. After the 72 h isorhamnetin glycosides release analysis, the results indicate around a 50% release rate. Conclusions. Encapsulation of isorhamnetin by liposomes improves the stability and solubility of the compounds, making it a more effective delivery system. The usage of a cosmetic formulation including isorhamnetin glycosides loaded liposomes can prevent skin aging based on a controlled delivery system technology. This product will be preferred by customers which tend to buy natural cosmetic products.