Lipid vesicles penetrate into intact skin owing to the transdermal osmotic gradients and hydration force

Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: the state of the art

“…In the process, transfersomes go through a series of stress-dependent adjustments of the local carrier symphony to minimize the struggle of motion through the otherwise confining channels.​ This process allows transfersomes to convey the drugs associated into and diagonally across the skin easily and very reproducibly.​ This happens at a rate largely higher than that achieved by more predictable formulations and offers an excellent means for controlling drug distribution in the skin [19,20]. Transfersomes have been used as carriers for different therapeutic agents, including proteins, insulin [21,22], DNA [23], gap junction protein [24], peptides [25], albumin [15], nutraceuticals [26], corticosteroids [27], antigens [28], analgesics [29], sex hormones [30], and anesthetics [31], and have been proven to augment significantly the amount of drug permeated through the skin [10]. The topical application of transfersome-entrapped anticancer drug is described by a few research groups.…”

“…It is believed that the unimpeded passage of such carriers is based on two key factors: the high elasticity (deformability) of the vesicle bilayers and the reality of an osmotic gradient across the skin. Because of their high deformability, transfersomes with the help of EAs generate a transepidermal osmotic gradient; and further squeeze among the stratum corneum cells and carry drug across the whole skin [10]. The transpore hydrostatic force difference is liable for the penetration or passage of transfersomes intact throughout the stratum corneum, i.e.…”

“…The osmotic gradient is caused by the difference in water concentration between the skin surface and skin interiors. Transfersomes are highly deformable, and this property assists in their quick penetration through the intercellular lipid pathway of the subcutaneous tissue.​ Some of the exploratory findings reported on the existence of misdeeds inside the intercellular lipid packing of murine subcutaneous tissue, which acts as the virtual channel through which transfersomes can penetrate [6,10]. Transfersomes have been defined as specially designed vesicular particles consisting of at least one inner aqueous compartment enclosed by lipid vesicles; liposomes in morphology, but, functionally, transfersomes are suitably deformable to go through pores much smaller than their own size.…”

“…Introduced in 1992, Cevc and Blume second-generation vesicular carriers, named Ultradeformable liposomes or Transfersomes®, possess slighter vesicular size (typically <300 nm) and higher elasticity (typically five–eight times higher compared with conventional liposomes) [10–12]. …”

“…The transfersome term was first introduced by Cevc [10] and has been the subject of several patents and literature information since the 1990s (Transfersomes, a trademark of IDEA AG, Munich, Germany), and it represents the first generation of ultradeformable vesicles. The skin permeation and penetration of these elastic vesicles result from a synergic mechanism among the carrier properties and the access enrichment ability.​ Transfersomes are ultradeformable lipid bundles of aggregates in supramolecular form constructed with a minimum of one interior aqueous segment encircled by a lipid bilayer exhibiting adapted properties, which are appropriate under the presence of surfactants in the vesicular membrane (edge activator (EA)) [13–18].…”