The aim of this study is to obtain “giant” liposomes by lipid film hydration using a preparation formula with two different phospholipids, phosphatidylcholine (PC) and phosphatidylserine (PS).Firstly, the macro- and microscopic characterization, total phenols content and antioxidant capacity of the plant Stellaria media (L.) Vill. were assessed. Then, Stellaria media (L.) Vill. extract was encapsulated in both formulations (PCE and PSE) and the liposomes were characterized according to their morphology, size distribution and Zeta potential using optical microscopy and dynamic light scattering. The encapsulation efficiency (EE%) was determined using the Folin–Ciocalteu method and the values of both formulations were compared. PC and PCE liposomes with a diameter between 712 and 1000 nm and PS and PSE liposomes with a diameter between 58 and 1000 nm were obtained. The values EE% of Stellaria media (L.) Vill. extract for PCE and PSE were 92.09% and 84.25%, respectively.
Both PC and PS liposomes and their homologues with encapsulated plant extract were “giant” multilamellar liposomes. In the case of PC and PCE liposomes, around 50–80% presented dimensions between 712 and 1000 nm, while more than 90% of PS and PSE liposomes were in the range of 58–1000 nm. The larger diameter of the PC and PCE liposomes confirmed that the type of phospholipids used in the preparation significantly influenced the size and electrical charge of the formulation. The phosphatidylserine-based formulations showed smaller diameters and a negative Zeta potential, meaning they had better stability compared to phosphatidylcholine-based ones. We also demonstrated a high inclusion percentage of the Stellaria media (L.) Vill. extract in both formulations—more than 90% for PCE and more than 80% for PSE. (Copyright F. Miere (Groza), Simona Cavalu et al.
By H.I. Kutbi, H.Z. Asfour, A. K. Kammoun, A. Sirwi, H. A. Gad and Simona Cavalu
Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine
To improve Brb permeability and bioavailability, this study presents a newly developed formulation, namely Brb hyaluronate-based liposomes, prepared by using film hydration method and characterized by dynamic light scattering measurements, entrapment efficiency percentage (EE%), transmission electron microscope (TEM), in vitro drug release and physical stability. Results of pharmacokinetics studies indicated the potential of the liposomal formulation to increase the oral bioavailability of Brb and to accelerate its entry into the bloodstream. The obtained results are accredited to the lipophilic nature of the prepared system, resembling the structural features of bio-membrane, in addition to their small size that enhances intestinal penetration.
Different formulation variables (lipid, drug and hyaluronic acid amounts) have a significant effect on the physicochemical characteristics of the prepared system using film hydration method. The presence of hyaluronic acid as a main component in liposomes preparation was able to slow berberine diffusion from the vesicles.Oral administration of Brb hyaluronate-based liposomes to rats could improve lipophilicity and bioavailability of the investigated system compared to Brb solution and Brb liposomes prepared without hyaluronic acid. Copyright H.A. Gad and Simona Cavalu