Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery

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

doi:10.1016/j.ijpharm.2006.05.027

Cited by 352 publications

(226 citation statements)

References 54 publications

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“…Transfersomes containing EGCG alone (EGCG-TF) showed a significantly higher (p50.05) EGCG deposition in skin (28.49 ± 1.74 mg/cm 2 ) than that observed with plain EGCG solution. Similar observation has been reported in previous literature where transfersomes increased the skin deposition of drugs like cyclosporin A, estradiol, dipotassium glycyrrhizinate, dexamethasone and ketotifen along with enhancement in permeation rate in their transfersomal forms due to transcutaneous hydration gradient (Maghraby et al, 1999;Guo et al, 2000;Trotta et al, 2002;Jain et al, 2003;Elsayed et al, 2007). Further enhancement in skin deposition of EGCG (38.90 ± 1.16 mg/cm 2 ) was observed with the transfersomal formulation containing both EGCG as well as HA (ETF20).…”

Section: In Vitro Skin Permeation and Deposition Studysupporting

confidence: 89%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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(2017) Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage, Drug Delivery, 24:1, 61-74, DOI: 10.1080/10717544.2016 AbstractThe present work attempts to develop and statistically optimize transfersomes containing EGCG and hyaluronic acid to synergize the UV radiation-protective ability of both compounds, along with imparting antioxidant and anti-aging effects. Transfersomes were prepared by thin film hydration technique, using soy phosphatidylcholine and sodium cholate, combined with high-pressure homogenization. They were characterized with respect to size, polydispersity index, zeta potential, morphology, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), in vitro antioxidant activity and ex vivo skin permeation studies. Cell viability, lipid peroxidation, intracellular ROS levels and expression of MMPs (2 and 9) were determined in human keratinocyte cell lines (HaCaT). The composition of the transfersomes was statistically optimized by Design of Experiments using Box-Behnken design with four factors at three levels. The optimized transfersome formulation showed vesicle size, polydispersity index and zeta potential of 101.2 ± 6.0 nm, 0.245 ± 0.069 and À44.8 ± 5.24 mV, respectively. FTIR and DSC showed no interaction between EGCG and the selected excipients. XRD results revealed no form conversion of EGCG in its transfersomal form. The optimized transfersomes were found to increase the cell viability and reduce the lipid peroxidation, intracellular ROS and expression of MMPs in HaCaT cells. The optimized transfersomal formulation of EGCG and HA exhibited considerably higher skin permeation and deposition of EGCG than that observed with plain EGCG. The results underline the potential application of the developed transfersomes in sunscreen cream/lotions for improvement of UV radiation-protection along with deriving antioxidant and anti-aging effects.

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Section: In Vitro Skin Permeation and Deposition Studysupporting

confidence: 89%

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

et al. 2017

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“…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 curvature that increases deformability of the bilayers. 13) Niosomes are the second generation of elastic vesicles introduced by van den Bergh et al 8) and compose of the optimal ration of non-ionic surfactant and cholesterol. Ethosomes are another novel vesicular carriers, developed and introduced by Touitou et al 9) and incorporate ethanol into vesicle bilayer.…”

Section: Hcl)mentioning

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 results of an in vivo anti-inflammatory activity study showed that GA elastic vesicles had a significant reduction in ear thickness and mass (25.52 and 49.23%) ( p < 0.05) as compared with a positive control group (triamcinolone acetonide and econazole nitrate cream in the market)[77]CatechinAntioxidentVeregen®In this study were compared catechin-loaded conventional liposomal, deformable conventional liposomal, and deformable liposomes prepared by the reverse-phase evaporation (REV) methodL-α-phosphatidylcholine, cholesterol, sodiumdeoxycholateResults suggested that all liposomal formulations exhibited a prolonged catechin release. Compared with deformable liposomes, the REV deformable liposomes showed a greater deposition of (+)-catechin while catechin solution did not permeate into the porcine ear skin[78]DipotassiumglycyrrhizinateAnti-inflammatoryagent–Studied the possibility of elastic liposomes for skin release of dipotassium glycyrrhizinate (KG) for treatment of acute and chronic dermatitisSoya lecithin (PC) or hydrogenated soya lecithinDipotassium glycyrrhizinate interacted with liposomes disrupting and fluidizing the lipid bilayer, skin deposition increased 4.5-fold compared with aqueous solution while KG was formulated in liposomes[79]KetotifenAntihistaminicZaditor ketotifenIn this study were investigated possible mechanisms of deformable liposomes and ethosomes for improving skin delivery of ketotifen under non-occlusive conditionsPhosphatidylcholine,Tween-80Results suggested that both the penetration-enhancing effect and the intact vesicle permeation into the stratum corneum might play a role in improving skin delivery of drugs by deformable liposomes, under non-occlusive conditions, and that the penetration-enhancing effect was of greater importance in the case of ketotifen[80]Quercetin andresveratrolTo reduce subcutaneousfat–In this study, proposed quercetin and resveratrol-containing SDC-elastic liposomes as a new approach for dissolving the subcutaneous fatSoya phosphatidylcholine cholesterol, stearylamine, sodium deoxycholateResults showed optimized elastic quercetin and resveratrol-loaded liposomes with suitable physicochemical properties and kinetic drug profiles for subcutaneous injection[81]TetanusVaccineAdacel (Tdap)In the present study, elastic vesicle transfersomes, non-ionic surfactant vesicles (niosomes) and liposomes were used to stu...…”

Section: Methods Of Preparationmentioning

confidence: 99%

Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: the state of the art

Rai¹,

Pandey²,

Rai³

2017

Nano Reviews & Experiments

206

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Introduction: The skin acts as a barrier and prevents transcutaneous delivery of therapeutic agents. Transfersomes are novel vesicular systems that are several times more elastic than other vesicular systems. These are composed of edge activator, phospholipids, ethanol, and sodium cholate and are applied in a non-occlusive manner. Areas covered: This article covers information such as merits/demerits of transfersomes, regulatory aspects of materials used in preparation, different methods of preparation, mechanism of action, review of clinical investigations performed, marketed preparations available, research reports, and patent reports related to transfersomes. Expert opinion: Research over the past few years has provided a better understanding of transfersomal permeation of therapeutic agents across stratum corneum barrier. Transfersomes provides an essential feature of their application to variety of compositions in order to optimize the permeability of a range of therapeutic molecules. This is evidenced by the fact that there are several Transfersome products being processed in advanced clinical trials. It is noteworthy that a number of Transfersome products for dermal and transdermal delivery will gain a global market success in near future.

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Deformable liposomes and ethosomes: Mechanism of enhanced skin delivery

Cited by 352 publications

References 54 publications

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

Skin delivery of epigallocatechin-3-gallate (EGCG) and hyaluronic acid loaded nano-transfersomes for antioxidant and anti-aging effects in UV radiation induced skin damage

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

Transfersomes as versatile and flexible nano-vesicular carriers in skin cancer therapy: the state of the art

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