Interaction of liposomes with human skin in vitro — The influence of lipid composition and structure

Kirjavainen, Merja; Urtti, Arto; Jääskeläinen, Ilpo; Suhonen, T. Marjukka; Paronen, Petteri; Valjakka-Koskela, Riitta; Kiesvaara, Juha; Mönkkönen, Jukka

doi:10.1016/s0005-2760(96)00126-9

Cited by 232 publications

(88 citation statements)

References 19 publications

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“…Kirjavainen et al reported in 1996 that the fluorescence from liposomal compositions con- taining DOPE (dioleylphosphatidyl ethanolamine) were able to penetrate deeper into the SC than that from liposomes without DOPE. A pretreatment of skin with unlabeled liposomes containing DOPE or lyso-phosphatidylcholine (lyso-PC) enhanced the subsequent penetration of the fluorescent markers, N-Rh-PE and sulforhodamine B into the skin, suggesting possible enhancer activity (Kirjavainen et al, 1996). In 1997, Boderke et al used CLSM to show that the amino peptidase activity was evenly distributed throughout the viable part of the epidermis, with enhanced fluorescence in the upper layers of the stratum granulosum, while dermis and SC showed considerably less amino peptidase activity (Boderke et al, 1997 demonstrate that vesicles made of native human SC lipids rapidly interact with phosphatidylserine liposomes, weakly with human stratum corneum lipid liposomes and have no effect on PC liposomes (Zellmer et al, 1998).…”

Section: Resultsmentioning

confidence: 99%

Particle size of liposomes influences dermal delivery of substances into skin

Verma

Blume

et al. 2003

International Journal of Pharmaceutics

567

257

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Section: Resultsmentioning

confidence: 99%

Particle size of liposomes influences dermal delivery of substances into skin

Verma

Blume

et al. 2003

International Journal of Pharmaceutics

567

257

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“…Confocal microscopic studies showed that intact fluorescent labeled liposomes were not able to penetrate into the granular layers of the epidermis. 1) Since the first paper to report the effectiveness of deformable liposomes which can be used for skin delivery of drug into deep skin region was published by Cevc and Blume, 2) new categories of vesicles with high elasticity or flexibility, such as transfersomes, 3) ethosomes, 4) flexosomes 5) and invasomes 6) have been introduced and developed. These vesicles mainly consist of phospholipids and an edge activator or penetration enhancer in which only a specially designed vesicle was shown to be able to allow transdermal drug delivery.…”

mentioning

confidence: 99%

Menthosomes, Novel Ultradeformable Vesicles for Transdermal Drug Delivery: Optimization and Characterization

Duangjit

Obata

Sano

et al. 2012

Biological & Pharmaceutical Bulletin

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Menthosomes, novel deformable carriers for the enhancement of transdermal delivery are introduced in this study. Meloxicam (MX)-loaded menthosomes were formulated, and their physicochemical characteristics and skin permeability were evaluated. A two-factor spherical and second-order composite experimental design was used to prepare the formulation of the menthosomes. Ten formulations of menthosomes composed of a phospholipid as the lipid bilayer carrier, cholesterol (Chol) as a stabilizer and cetylpyridinium chloride (CPC) and L-menthol as penetration enhancers were prepared. The amounts of Chol and CPC were selected as causal factors. Physicochemical characteristics (particle size, size distribution, zeta potential, elasticity and drug content) and an in vitro skin-permeation study of meloxicam-loaded menthosomes were evaluated. The concentrations of MX that permeated the skin at 2-12 h and the flux were selected as response variables. The optimal formulation was estimated using a nonlinear response-surface method incorporating thin-plate spline interpolation. The experimental values were very close to the values predicted by the computer programs in this study. A Bayesian network analysis was applied to gain a mechanistic understanding of the relationships between causal factors and response variables.Key words menthosome; liposome; optimization; skin permeation; meloxicam; menthol For the past few decades, the use of liposomal vesicles in drug-delivery systems for skin permeation has evoked considerable interest and attracted increasing attention. Many reports focus on the use of liposomes for enhancing skin permeation of hydrophilic and lipophilic compounds, proteins and macromolecules. However, recent studies indicate that in most cases, classic liposomes are of little or no value as transdermal drug-delivery carriers because they do not penetrate skin deeply, but rather remain confined to the upper layers of the stratum corneum. Confocal microscopic studies showed that intact fluorescent labeled liposomes were not able to penetrate into the granular layers of the epidermis. 1)Since the first paper to report the effectiveness of deformable liposomes which can be used for skin delivery of drug into deep skin region was published by Cevc and Blume, 2) new categories of vesicles with high elasticity or flexibility, such as transfersomes,3) ethosomes, 4) flexosomes 5) and invasomes 6) have been introduced and developed. These vesicles mainly consist of phospholipids and an edge activator or penetration enhancer in which only a specially designed vesicle was shown to be able to allow transdermal drug delivery. Menthosomes, novel deformable carriers consist of phospholipids, surfactant and menthol were also introduced in this study. Several intensive studies suggested that the permeability of drug in liposomes and their analogues depends on their physicochemical characteristics (e.g., particle size, size distribution, zeta potential, lamellarity, elasticity, drug content, etc.), and these characteristics were dir...

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“…It is not clear why the drug loaded into cationic liposomes resulted in greater penetration over anionic liposomes. But it appears that cationic charge on the surface of liposome played a role because epidermis layer contains negatively charged lipids (Burnette and Ongpipattanakul, 1987;Kirjavainen et al, 1996). This speculation is further supported by the fact that the higher percentage of DOTAP shows the greater penetration.…”

Section: Resultsmentioning

confidence: 94%

Effect of Charge Carrier Lipid on Skin Penetration, Retention, and Hair Growth of Topically Applied Finasteride-Containing Liposomes

Lee¹,

Kumar²,

Sriraman³

et al. 2011

Biomolecules and Therapeutics

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The aim of this study was to investigate the effect of charge carrier lipid on the skin penetration, retention, and hair growth of topically applied fi nasteride-containing liposomes. Finasteride-containing liposomes were prepared by traditional thin fi lm hydration method using Phospholipon ® 85 G and cholesterol with or without charge carrier lipid (1,2 dimyristoyl-sn-glycero-3-phosphate or 1,2-dioleoyl-trimethylammonium-propane for anionic and cationic charge, respectively). Freshly prepared fi nasteride-containing liposome suspension was applied on the hairless mouse skin, and skin penetration and retention were measured using KesharyChien diffusion cell. Non-liposomal formulation (ethanol 10% solution containing 0.5 mg/ml of FNS) was also used as a control. The amount of fi nasteride in the diffusion cell and mouse skin was measured by HPLC. The hair growth was evaluated using depilated male C57BL/6N mice. Mean particle size of all fi nasteride-containing liposomes was less than a micron, and polydispersity index revealed size homogeneity. Skin penetration and retention studies showed that signifi cantly less amount of fi nasteride was penetrated when applied as anionic liposome while more amount of the drug was retained. Specifi cally, in liposome prepared with 10% anionic charge carrier lipid, penetration was 12.99 μg/cm 2 while retention was 79.23 μg/cm 2 after 24 h of application. In hair growth study, fi nasteride-containing anionic liposomes showed moderate effi cacy, but the effi cacy was not found when applied as cationic liposomes. In conclusion, topical application of fi nasteride using anionic liposome formulation appears to be useful option for the treatment of androgenetic alopecia to avoid systemic side effects of the drug. Abstract cifi c inhibitor towards type II 5α-reductase, an intracellular enzyme that converts testosterone into 5α-dihydrotestosterone which is believed to cause androgenetic alopecia. There are two distinct isozymes of the enzyme, i.e., type I and type II. In humans, type I 5α-reductase is predominantly expressed in the sebaceous glands of most regions of skin. In contrast, type II 5α-reductase is predominantly found in hair follicles where hair growth begins as well as prostate, seminal vesicles, and epididymis. Therefore, FNS is widely used for the treatment of androgenetic alopecia and benign prostate hyperplasia.Although FNS is effective in the treatment of androgenetic alopecia, oral use of this drug is largely limited due to various side effects such as erectile dysfunction and impotence. Another serious adverse effect includes gynecomastia, develop-

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Interaction of liposomes with human skin in vitro — The influence of lipid composition and structure

Cited by 232 publications

References 19 publications

Particle size of liposomes influences dermal delivery of substances into skin

Particle size of liposomes influences dermal delivery of substances into skin

Menthosomes, Novel Ultradeformable Vesicles for Transdermal Drug Delivery: Optimization and Characterization

Effect of Charge Carrier Lipid on Skin Penetration, Retention, and Hair Growth of Topically Applied Finasteride-Containing Liposomes

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