The skin: a pathway for systemic treatment with patches and lipid-based agent carriers

Cevc, Gregor; Blume, G.; Schätzlein, Andreas; Gebauer, D; Paul, Amla

doi:10.1016/0169-409x(95)00091-k

Cited by 210 publications

(120 citation statements)

References 67 publications

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“…6 Biocompatible surfactant, also called edge activator, destabilizes the lipid bilayer and causes an increase in its fluidity and elasticity, allowing dramatically improved delivery of the encapsulated agents to and through the skin. 7,8 Surfactant is solely responsible for the flexibility of the transfersomes and imparts better hydration properties and extraordinary skin penetration ability. Cevc and Blume reported the permeation mechanism of transfersomes as hydrotaxis (xerophobia) which is moisture-seeking tendency of transfersomes towards the deeper part of skin instead of outer dry surroundings caused by evaporation of moisture from the transfersomes formulation when it is applied to the skin.…”

Section: Introductionmentioning

confidence: 99%

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Mahmood¹,

Taher²,

Mandal³

2014

IJN

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Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon ® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 μg/cm 2 /hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 μM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug.

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Section: Introductionmentioning

confidence: 99%

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Mahmood¹,

Taher²,

Mandal³

2014

IJN

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“…Stearylamine and sodium cholate are used as edge activators. This approach has also been successfully demonstrated with other polypeptides such as interferons a, b, and g, calcitonin, and superoxide dismutase in preclinical experiments [57][58][59].…”

Section: Formulation Approachesmentioning

confidence: 90%

Non Invasive Delivery of Protein and Peptide Drugs: A Review

Lakshmi

Prasanthi

Veeresh

2017

Asian J Pharm Clin Res

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The most common and improved bioavailable route for protein and peptide drugs is injectable route. These drugs are generally preferred to give in invasive route to get high bioavailability though possessing disadvantages and the major one is patient non-compliance. Hence, various non-invasive route of administration has been under research for these drugs to fetch more advantages. Although bioavailability is a major problem with non-invasive route such as oral, nasal, ocular, transdermal, rectal, colon, and vaginal route, these routes have been preferred compared to existing invasive one. Many researches have been conducted in this area, but achieving success is significantly challenging. The nasal delivery has been successfully exploited for vaccines compare to all other non-invasive drug delivery system. Currently, only molecule to reach market is oral cyclosporine. The present review aims to discuss the potential non-invasive routes of protein and peptide drug delivery. The factors which will affect drug permeation, and the bioavailability of proteins administered through these routes is also emphasized.

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“…The osmotic gradient is caused by the difference in water concentration between the skin surface and skin interiors. Transfersomes are highly deformable, and this property assists in their quick penetration through the intercellular lipid pathway of the subcutaneous tissue. Some of the exploratory findings reported on the existence of misdeeds inside the intercellular lipid packing of murine subcutaneous tissue, which acts as the virtual channel through which transfersomes can penetrate [6,10]. Transfersomes have been defined as specially designed vesicular particles consisting of at least one inner aqueous compartment enclosed by lipid vesicles; liposomes in morphology, but, functionally, transfersomes are suitably deformable to go through pores much smaller than their own size.…”

Section: Introductionmentioning

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

192

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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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The skin: a pathway for systemic treatment with patches and lipid-based agent carriers

Cited by 210 publications

References 67 publications

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Non Invasive Delivery of Protein and Peptide Drugs: A Review

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

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