Synthesis and Assessment of Lipid Nanovesicles for Efficient Transdermal Delivery of Hydrophilic Molecules

Abstract

The transdermal delivery of hydrophilic molecules through the dermis is a challenging task because of the various skin barriers. Thus, lipid nanovesicles, including liposomes, ethosomes and transethosomes, are advantageous to transdermal drug delivery. This study was designed to develop nanovesicles like liposomes (LF1), ethosomes (EF1) and transethosomes (TF1) containing hydrophilic agents such as Rhodamine B (RB) as a model compound. Nanovesicles loaded with RB were synthesized using an ethanol injection method followed by probe sonication (hot method). The nonsonicated nanovesicles had vesicle sizes ranging from [Formula: see text] to [Formula: see text][Formula: see text]nm, while sonicated nanovesicles sizes ranged from [Formula: see text] to [Formula: see text][Formula: see text]nm. In addition, the nonsonicated nanovesicles had polydispersity index (PdI) ranging from [Formula: see text] to [Formula: see text], whereas the PdI of the sonicated nanovesicles ranged from [Formula: see text] to [Formula: see text]. Transmission electron microscopy revealed the distinguishable features of the sonicated nanovesicles depending on the compositions. The entrapment efficiency of RB was observed in the order of [Formula: see text]. At the end of 10[Formula: see text]h, RB permeated through the Strat-M[Formula: see text] membrane at [Formula: see text], [Formula: see text] and [Formula: see text]g/cm2 from the LF1, EF1 and TF1 containing RB, respectively. The flux ([Formula: see text]) of TF1 was obtained 5.53 times higher than RB itself. Therefore, the TF1 nanovesicle allowed the highly efficient permeation and entrapment of hydrophilic RB compared to LF1 and EF1 nanovesicles. Hence, it can be concluded that transethosomes would be a better choice for hydrophilic compounds to cross the skin barriers via the transdermal route.