Development of Ultradeformable Liposomes with Fatty Acids for Enhanced Dermal Rosmarinic Acid Delivery

Abstract

This study aimed to develop ultradeformable liposomes (ULs) with fatty acids, namely, oleic, linoleic, and linolenic acid, to improve the skin penetration of rosmarinic acid. This study also investigated the vesicle-skin interaction and skin penetration pathway of ULs with fatty acids using the co-localization technique of multifluorescently labeled particles. The prepared ULs were characterized in terms of size, surface charge, size distribution, shape, % entrapment efficiency (% EE), and % loading efficiency (% LE). The prepared ULs with fatty acids had an average particle size between 50.37 ± 0.3 and 59.82 ± 17.3 nm with a size distribution within an acceptable range and exhibited a negative surface charge. The average % EE and % LE were 9 and 24.02, respectively. The in vitro skin penetration study found that ULs with oleic acid could significantly increase the skin penetration of rosmarinic acid compared to ULs. According to confocal laser scanning microscopy observations, this study suggested that UL vesicles attach to the skin before releasing the entrapped drug to penetrate the skin. These findings suggested that ULs with oleic acid penetrated the skin via the transfollicular pathway as a major penetration pathway.

Advances in Nanomaterials Used in Co-Delivery of siRNA and Small Molecule Drugs for Cancer Treatment

“…The upper stratum corneum layer is the most penetrated layer while dioleoyl-phosphatidylethanolamine (DOPE)-based liposomes are able to achieve a deeper penetration [78]. Liposomes have been modified to improve their skin penetration ability for dermal drug delivery [79]. Deep penetration in the skin membrane is achievable via the use of transferosomes (liposomes with edge activators) or ethosomes (liposomes comprised of ethanol) [73].…”

Rosmarinic Acid and Ulvan from Terrestrial and Marine Sources in Anti-Microbial Bionanosystems and Biomaterials

“…Lipid nanotechnology-based systems are another interesting route to encapsulate RA and other plant extracts for drug delivery. For example, RA, due to its physicochemical properties, has low skin penetration efficiency, but its encapsulation in liposomes [118], ethosomes [119] and ultra-deformable liposomes containing fatty acids [120] can increase its transdermal penetration. Liposomes are micro or nanosized spherical vesicles composed of one or more lipid layers containing an aqueous phase.…”

Micron and nano hybrid ufasomes from conjugated linoleic acid, their vesiculation and encapsulation of ginsenoside Rg3

“…[4][5][6][7] Compared with ordinary liposomes, ufasomes that are composed of unsaturated fatty acid vesicles (FAVs) possess unique advantages such as natural abundance, biodegradability, stimulus-responsive morphological transformation, and high bioavailability, [8][9][10] could be used for encapsulating bioactive ingredients in aqueous solution. [11][12][13][14][15] In general, ufasomes are colloidal suspensions with hollow core-shell structure. 16 The main difference in the vesiculation mechanism between ufasome and ordinary liposome is that, in addition to hydrogen bond and hydrophobic interaction that drive the self-assembly of conventional liposome, 17 formation of ufasome also involves countra-ionic interaction or ionic pairs, which is not often found in ordinary liposome.…”

“…Compared with ordinary liposomes, ufasomes that are composed of unsaturated fatty acid vesicles (FAVs) possess unique advantages such as natural abundance, biodegradability, stimulus‐responsive morphological transformation, and high bioavailability, 8‐10 could be used for encapsulating bioactive ingredients in aqueous solution 11‐15 . In general, ufasomes are colloidal suspensions with hollow core‐shell structure 16 .…”