Eco-scalable baicalin loaded vesicles developed by combining phospholipid with ethanol, glycerol, and propylene glycol to enhance skin permeation and protection

A new class of biocompatible and scalable phospholipid vesicles was developed, aiming at improving the efficacy of baicalin on the skin. Phosphatidylcholine and baicalin (a natural polyphenol) were hydrated in two steps with a mixture of ethanol, glycerol, and propylene glycol at different ratios, and a low amount of water (4%). Hence, water was almost completely replaced by the co-solvents, which were never used before as predominant dispersing medium of phospholipid vesicles. The vesicles appeared three-dimensionally structured, forming a network that conferred a high viscosity to the dispersions. The vesicles were unilamellar, small in size (∼100 nm), and stable during 12 months of storage. They disclosed optimal performances in the transdermal delivery of baicalin, and high biocompatibility with skin cells (i.e., keratinocytes and fibroblasts). Furthermore, the vesicles promoted the efficacy of baicalin in protecting skin cells against oxidative stress in vitro and injured skin in vivo.