Heparin penetration into and permeation through human skin from aqueous and liposomal formulations in vitro

Betz, Gabriele; Nowbakht, Pegah; Imboden, Roger; Imanidis, Georgios

doi:10.1016/s0378-5173(01)00832-8

Cited by 52 publications

(30 citation statements)

References 21 publications

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“…The considered LMWHs globally permeated the epidermis to a low extent after 24 h of application in agreement with the literature data (Betz et al, 2001;Gomaa et al, 2012;Lanke et al, 2009b;Mitragoti and Kost, 2001;Song et al, 2011;Song and Kim, 2006). The lack of diffusion of these compounds through the skin can be justified considering the large molecular size and hydrophilicity and the repulsive forces between the negatively charges of lipids of stratum corneum and LMWHs (Betz et al, 2001).…”

Section: Discussionsupporting

confidence: 87%

See 1 more Smart Citation

Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

Franzè

Gennari

Minghetti

et al. 2015

International Journal of Pharmaceutics

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Section: Discussionsupporting

confidence: 87%

“…The lack of diffusion of these compounds through the skin can be justified considering the large molecular size and hydrophilicity and the repulsive forces between the negatively charges of lipids of stratum corneum and LMWHs (Betz et al, 2001). However, some significant difference among the tested compounds was found.…”

Section: Discussionmentioning

confidence: 99%

Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

Franzè

Gennari

Minghetti

et al. 2015

International Journal of Pharmaceutics

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“…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.…”

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 tissue was then transferred to xylene and kept for 30 min. Then, wax scrapings were added to xylene up to the saturation level and were kept undisturbed for 24 h [6].…”

Section: Confocal Laser Scanning Microscopy Studymentioning

confidence: 99%

Treatment of cutaneous candidiasis through fluconazole encapsulated cubosomes

Prajapati

Jain

et al. 2014

Drug Deliv. and Transl. Res.

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Cubosomes encapsulating fluconazole were prepared by emulsification method and characterized for particle size, entrapment efficiency, SEM, in vitro release, skin irritation studies, and confocal laser scanning microscopy. The cubosomes prepared were 257.2 ± 2.94 nm in size and with drug entrapment efficiency of 66.2 ± 2.69 %. The prepared formulation was characterized for surface morphology by SEM analysis which revealed their smooth surface. The cumulative percentage of fluconazole from cubosomes permeated via dialysis membrane (molecular weight cutoff (MWCO) 12-14 kD) showed 76.86 % cumulative drug release, while fluconazole solution showed release up to 91.04 % in 24 h in phosphate-buffered saline (PBS) (pH 6.5), and sustained release is obtained after 24 h in case of cubosomes. The animal studies also revealed that the cubosomes are non-irritant and have sustained antifungal activity.

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Heparin penetration into and permeation through human skin from aqueous and liposomal formulations in vitro

Cited by 52 publications

References 21 publications

Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

Influence of chemical and structural features of low molecular weight heparins (LMWHs) on skin penetration

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

Treatment of cutaneous candidiasis through fluconazole encapsulated cubosomes

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