Comparative study of liposomes, transfersomes and ethosomes as carriers for improving topical delivery of celecoxib

Abstract

Topical administration of celecoxib proved to be an effective mean of preventing skin cancer development and improving anticancer drugs effectiveness in skin tumors treatment. The aim of this study was the development of an effective topical formulation of celecoxib, able to promote drug skin delivery, providing its in depth penetration through the skin layers. Three kinds of vesicular formulations have been investigated as drug carriers: liposomes containing a surfactant, or transfersomes and ethosomes, containing suitable edge activators. Firstly, the effect of membrane composition variations on the system performance has been evaluated for each vesicle type. Selected formulations were characterized for particle size, polydispersity index and encapsulation efficiency. The best formulations were subjected to ex vivo permeation studies through excised human skin. All vesicular formulations markedly (p < 0.001) improved the drug amount penetrated into the skin with respect to an aqueous suspension, from 2.0 to 6.5, up to 9.0 folds for liposomes, transfersomes and ethosomes, respectively. In particular, ethosomes containing Tween 20 as edge activator not only showed the best vesicle dimensions and homogeneity, and the highest encapsulation efficacy (54.4%), but also enabled the highest increase in drug penetration through the skin, probably due to the simultaneous presence in their composition of ethanol and Tween 20, both acting as permeation enhancers. Therefore, among the various vesicular formulations examined in the study, Tween 20-ethosomes can be considered the most promising one as carrier for topical celecoxib applications aimed to prevent skin cancer development and increase the anticancer drugs effectiveness against skin tumors.

Development, characterization, and skin delivery studies of related ultradeformable vesicles: transfersomes, ethosomes, and transethosomes

“…This may be attributed to the fusion of these vesicles with skin lipids and the active release along the penetration pathway, resulting in a depot effect. In particular, this effect could be higher in the presence of ethanol 22,23,[37][38][39] which increases the skin permeability by intercalation into the polar head group of skin lipids. The synergistic mechanism between ethanol, surfactant, vesicles, and skin lipids is responsible for a higher skin penetration of transethosomes.…”

“…In fact, most studies are limited to lipophilic actives and to the comparison between elastic and rigid vesicles. 2,23 To the best of our knowledge, there is only one comparative study between transfersomes, ethosomes, and transethosomes. 22 Charge interaction between actives and vesicles are also determinant for incorporation in vesicles.…”

Bile salts-containing vesicles: promising pharmaceutical carriers for oral delivery of poorly water-soluble drugs and peptide/protein-based therapeutics or vaccines

“…Broadly, vesicular carriers are divided into two main classes: liposomes, which represent the groundbreaking discovery of Alec Bangham in the 1960s and are composed mainly of phosphatidylcholine (PC) and cholesterol (CH) bilayers, and niosomes that were revealed later in 1970, by L'Oreal, and denote non-ionic surfactant vesicles (Torchilin, 2005). Following that, newer forms of lipid vesicles were presented by various researchers and includes tranferosomes (Bragagni et al, 2012), emulsomes (Vyas et al, 2006), enzymosomes (Gaspar et al, 2003), ethosomes (Pandey et al, 2014) and pharmacosomes (Semalty et al, 2009).…”

Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

“…Many researchers have reported superior properties of transethosomes over classical ethosomes. [17][18][19][20][21][22][23][24][25][26][27][28][29][30] Different types of edge activators and penetration enhancers have been investigated to produce ethosomal systems with better characteristics. Transethosomes were reported to entrap drugs with molecular weights ranging from 130.077 Da to 200-325 kDa.…”