Lipid vesicles for skin delivery of drugs: Reviewing three decades of research

Elsayed, Mustafa M.A.; Abdallah, Ossama Y.; Naggar, Viviane F.; Khalafallah, Nawal

doi:10.1016/j.ijpharm.2006.12.005

Cited by 471 publications

(249 citation statements)

References 116 publications

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“…This observation supports the findings, of [18,19] which state that higher concentration of ethanol is responsible for decrease in the size of vesicle as it furnish a surface negative net charge to the vesicular systems by altering some surface characteristics.…”

Section: Resultssupporting

confidence: 91%

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Fatima

2017

AJP

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Aims: The aim of the present research work is to prepare ethosome of standardized Berberis aristata extract and to evaluate for vesicle shape, size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), and in vitro permeation studies. Materials and Methods: Ethosomes were prepared using soyaphosphatidylcholine (1-3%) and ethanol (10-40%) by modified cold method and were characterized. Results: The size of ethosomes were found to be in the range of 110.98-357.34 nm while PDI ranges from 0.114 to 1.56 and ZP was between −20.0 and −39.4 mV. Morphology studies showed unilamellar structure under transmission electron microscope and phase contrast microscope showed smooth surface. The EE of ethosomes was found to be in the range of 48.05% to 92.08%. Ethosomes were further added to carbopol 934P for gel formation, and subsequently, evaluated for their physicochemical properties. Discussion: In vitro diffusion study was conducted for ethosomal dispersion, hydroethanolic solution, ethosomes incorporated in viscous gel, and conventional gel using Franz diffusion cell for the biomarker compound berberine. Conclusions: It can be concluded that B. aristata loaded ethosomal delivery system is an encouraging approach for herbal drugs.

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Section: Resultssupporting

confidence: 91%

Untitled

Fatima

2017

AJP

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“…Chol can increase rigidity and packing density of PC molecules, thus to decrease elasticity of vesicle bilayers. 23,24) In contrast, the incorporation of edge activator e.g., CPC which have a high radius of curvature can increase deformability of the vesicle bilayers. MEN can decrease the orderly lipid microstructure by insertion and thus increase the fluidity or elasticity of vesicle bilayer.…”

Section: Resultsmentioning

confidence: 99%

Comparative Study of Novel Ultradeformable Liposomes: Menthosomes, Transfersomes and Liposomes for Enhancing Skin Permeation of Meloxicam

Duangjit

Obata

Sano

et al. 2014

Biological & Pharmaceutical Bulletin

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In the present study, novel ultradeformable liposomes (menthosomes; MTS), deformable liposomes (transfersomes; TFS) and conventional liposomes (CLP) were compared in their potential for transdermal delivery of meloxicam (MX). MTS, TFS and CLP were investigated for size, size distribution, zeta potential, elasticity, entrapment efficiency and stability. In vitro skin permeation using hairless mice skin was evaluated. Vesicular morphology was observed under freeze-fractured transmission electron microscopy (FF-TEM). Intrinsic thermal properties were performed using differential scanning calorimetry (DSC) and X-ray diffraction. The skin permeation mechanism was characterized using confocal laser scanning microscopy (CLSM). The results indicated that the difference in physicochemical characteristics of MTS, TFS and CLP affected the skin permeability. MTS and TFS showed higher flux of MX than CLP. CLSM image showed deformable vesicles mechanism for delivery of MX across the hairless mice skin. Our study suggested that ultradeformable and deformable liposomes (MTS and TFS) had a potential to use as transdermal drug delivery carriers for MX.Key words menthosome; transfersome; liposome; skin permeation; meloxicam; menthol Meloxicam (MX), a cyclooxygenase-2 inhibitor nonsteroidal anti-inflammatory drug (NSAID), is used to treat rheumatoid arthritis, osteoarthritis and other joint diseases. The injectable and oral administrations of NSAID drugs are not appropriate for needle-phobia and peptic ulcer patients. Moreover, the major limitation of MX is its low aqueous solubility (0.012 mg/mL in water and 0.086×10 −2 mg/mL in 0.1 M HCl) 1) with log P 1.91 and 0.07 at pH 5.0 and 7.4, respectively. MX delays its absorption from gastrointestinal tract (GI) and its prolonged use is associated with the incidence of GI side effects (bellyache, indigestion, ulceration and bleeding).2) If MX could be delivered without incidence of these limitations, MX administration would become safer and more acceptable. MX is suitable for development as a transdermal delivery candidate.Transdermal drug delivery or skin delivery has become a global priority because the conventional drug administration is associated with numerous limitations. Liposomes are one of potential strategies that utilize for skin delivery of hydrophilic drugs, 3) lipophilic drugs, 4) protein 5) and macromolecule.6) Although last decades, some design of conventional liposomes are of little or no value as carriers for transdermal drug delivery, but rather remain confined to the upper layer of the stratum corneum. However, recent approaches in vesicular modulating drug delivery through skin have resulted in many designs of novel vesicular carriers e.g., deformable liposomes (transfersomes), 7) niosomes, 8) ethosomes, 9) invasomes, 10) flexosomes 11) and menthosomes. 12) Transfersomes are the first generation of elastic vesicles introduced by Cevc and Blune 7) and consist mainly of phospholipids and an edge activator or a single-chain surfactant which having a high radius of curv...

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“…The vesicular carriers consist mainly of liposome, transfersome, noisome, and ethosome. Numerous studies have shown that conventional liposomes can enhance the accumulation of various molecules only in the upper skin strata, while ethosome and transfersome, novel liposomes, modified by appropriate composition could enhance and modulate the drug transport into or through the skin (Elsayed et al, 2007;Azeem et al, 2009).…”

Section: Discussionmentioning

confidence: 99%

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

et al. 2013

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The skin accumulation of therapeutic agents affects the efficiency of topical drug delivery. In this study, in vitro distribution of finasteride of ethosomes and liposomes in human cadaver skin after percutaneous delivery were investigated. Experiments were performed using modified Franz diffusion cells. Finasteride ethosomes, liposomes or hydroethanolic solutions were used as donor medium. Drug distribution at different skin layers and depths were studied by hotplate separation and frozen horizontal slicing technique. The result showed that the accumulation of finasteride in skin ranged from 9.7-24.3 mg/cm 2 at 12 or 24 hours. The ethosomes demonstrated better enhancing ability to deliver finasteride into the dermis layer than liposomes did. The finasteride concentration in the dermis layer from ethosomes was more than sevenfold higher than from liposomes. The finasteride accumulation in ethosomes group showed a distinctive reversed distribution profile. This distinctive reversed distribution profile is meaningful for exerting a favorable pharmacological effect for finasteride. The drug distribution profile in skin layers showed no significant difference between 12 and 24 hours application (p40.05). The study demonstrated that finasteride can be accumulated at target site more effectively and maintained at higher level through the application of novel ethosomal carriers.

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Lipid vesicles for skin delivery of drugs: Reviewing three decades of research

Cited by 471 publications

References 116 publications

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Untitled

Comparative Study of Novel Ultradeformable Liposomes: Menthosomes, Transfersomes and Liposomes for Enhancing Skin Permeation of Meloxicam

Penetration profile and human cadaver skin distribution of finasteride from vesicular nanocarriers

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