Ultradeformable liposomes with terpenes for delivery of hydrophilic compound

Abstract

Ultradeformable liposomes containing penetration enhancers were created to deliver NaFl. Vesicles were investigated for their particle size, zeta potential, NaFl entrapment efficiency (%EE), loading efficiency, and in vitro skin penetration. The vesicles obtained were spherical in shape, with a particle size of less than 100 nm and a negative surface charge (-6 to -11 mV). The %EE of NaFl loaded in vesicles ranged from 37 to 48%. Ultradeformable liposomes with monoterpenes (d-limonene, 1,8-cineole and geraniol) significantly improved NaFl penetration through the skin. Confocal laser scanning microscopy analysis confirmed skin-penetration results and was used to evaluate the behavior of hydrophilic compounds penetrating through the skin.

Essential oils and their constituents as skin penetration enhancer for transdermal drug delivery: a review

“…Ultradeformable liposomes with monoterpenes (d-limonene, 1,8-cineole, geraniol) significantly improved fluorescein sodium penetration through the skin. [68] Invasomes could be use to increase the permeation of the active substances encapsulated in these vesicles. The effectiveness of invasomes as drug carriers was reported for ferulic acid loaded into invasomes composed of phosphatidylcholine from soybean lecithin, ethanol and terpenes (limonene, citral, cineole), [69] meloxicam encapsulated into menthosomes consisting of phospholipids, cholesterol, cetylpyridinium chloride, L-menthol [70] and temoporfin loaded into invasomes comprising of phosphatidylcholine from soybean lecithin, ethanol and terpenes (D-limonene, citral, 1,8-cineole).…”

Liposomes for (trans)dermal drug delivery: the skin-PVPA as a novelin vitro stratum corneummodel in formulation development

“…Different strategies have been used to improve transdermal delivery, including the optimization of the drug and vehicle properties, the modification of stratum corneum by chemical penetration enhancers, and electrical/external force methods such as iontophoresis, electroporation and sonophoresis (Delgado-Charro and Guy, 2001). Considerable research has focused on developing nanopharmaceuticals, including nanoparticles (nanospheres, nanocapsules) derived from natural or synthetic polymers, nanoemulsions, solid lipid nanoparticles, nanostructured lipid carriers, dendrimers and vesicular nanosystems, such as niosomes and liposomes, to enhance the transport of drugs through the skin (Cereda et al, 2013;Cevc and Vierl, 2010;Prow et al, 2011;Subongkot et al, 2012). The use of nanopharmaceuticals enables the alteration of the pharmacokinetic properties of a given drug and increases its bioavailability.…”

Effect of liposomal fluidity on skin permeation of sodium fluorescein entrapped in liposomes

“…[13][14][15] Terpenes, a class of penetration enhancers obtained from natural sources, have successfully been used as skin penetration enhancers for percutaneous absorption enhancement in various types of liposomes, specifically invasomes, 16,17 and ULs. 18,19 Electron spin resonance (ESR), also known as electron paramagnetic resonance, is a spectroscopy technique used to study molecular mobility by characterizing the unpaired electron of free radicals, also called spin probes, in an extreme applied magnetic field. This technique has been used to study membrane fluidity, 20,21 the skin penetration enhancement mechanism of penetration enhancers and nanocarriers, According to our previous study, 18 ULs consisting of terpenes as a skin penetration enhancer and Tween 20 as a terpene solubilizer significantly enhanced the skin penetration of sodium fluorescein (NaFl).…”

“…18,19 Electron spin resonance (ESR), also known as electron paramagnetic resonance, is a spectroscopy technique used to study molecular mobility by characterizing the unpaired electron of free radicals, also called spin probes, in an extreme applied magnetic field. This technique has been used to study membrane fluidity, 20,21 the skin penetration enhancement mechanism of penetration enhancers and nanocarriers, According to our previous study, 18 ULs consisting of terpenes as a skin penetration enhancer and Tween 20 as a terpene solubilizer significantly enhanced the skin penetration of sodium fluorescein (NaFl). Since ULs with terpenes penetrated via transfollicular pathway as major skin penetration pathway, 19 we suggested that ULs with terpenes increased NaFl penetration by penetrating through hair follicles to bypass stratum corneum.…”