Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration

Maghraby, Gamal M. El; Williams, Adrian C.; Barry, Brian W.

doi:10.1016/s0378-5173(99)00441-x

Cited by 253 publications

(118 citation statements)

References 26 publications

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“…The grid was allowed to air dry thoroughly and samples were viewed on a TEM (Philips, TEM, New Brunswick, Canada). 17 A thin layer of PTG was spread on a slide and a drop of phosphate buffer was added through the side of the cover slip into the cavity slide and again observed. Photomicrographs were taken at 400× and 1000×, respectively, before and after addition of water for both plain and polarized light (Leica, DMLB, Bensheim, Germany).…”

Section: Visualization Of Vesiclesmentioning

confidence: 99%

Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

et al. 2005

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The present investigation aimed at formulation, performance evaluation, and stability studies of new vesicular drug carrier system protransfersomes for transdermal delivery of the contraceptive agent, levonorgestrel. Protransfersome gel (PTG) formulations of levonorgestrel were prepared and characterized for vesicle shape, size, entrapment efficiency, turbidity, and drug permeation across rat skin and were evaluated for their stability. The system was evaluated in vivo for biological assay of progestational activity including endometrial assay, inhibition of the formation of corpora lutea, and weight gain of uterus. The effects of different formulation variables (type of alcohol, type and concentration of surfactant) on transdermal permeability profile were assessed. The optimized PTG formulation showed enhanced in vitro skin permeation flux of 15.82 ± 0.37 μg/cm 2 /hr as compared to 0.032 ± 0.01 μg/cm 2 /hr for plain drug solution. PTG also showed good stability and after 2 months of storage there was no change in liquid crystalline nature, drug content, and other characteristic parameters. The peak plasma concentration of levonorgestrel (0.139 ± 0.05 μg/mL) was achieved within 4 hours and maintained until 48 hours by a single topical application of optimized PTG formulation. In vivo performance of the PTG formulation showed increase in the therapeutic efficacy of drug. Results indicated that the optimized protransfersomal formulation of levonorgestrel had better skin permeation potential, sustained release characteristic, and better stability than proliposomal formulation.

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Section: Visualization Of Vesiclesmentioning

confidence: 99%

Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

et al. 2005

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“…For vesicle size measurement, vesicular suspension was mixed with the appropriate medium (7.4 pH phosphate buffer) and the measurements were conducted in triplicate [7].…”

Section: Vesicle Size and Size Distributionmentioning

confidence: 99%

Nano-appended transdermal gel of Tenoxicam via ultradeformable drug carrier system

Negi

Chauhan

Garg

2013

Journal of Experimental Nanoscience

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Tenoxicam is one of the potent non-steroidal anti-inflammatory drugs (NSAIDs), which is used clinically in the treatment of rheumatoid arthritis. Like other NSAIDs, Tenoxicam also suffers from the drawback of being associated with gastrointestinal side effects. Further, transdermal penetration of this drug is very poor, which circumvents the use of transdermal route. The main objective of this study is to exploit the concept of ultradeformable vesicles to increase the transport of Tenoxicam through transdermal route, and also to present it as a possible replacement for the oral NSAID therapy for rheumatoid arthritis. Three concentrations (5%, 15% and 25%) of three different surfactants (Tween-80, Span-80 and sodium desoxycholate) were used along with soya lecithin to prepare the ultradeformable vesicles. Among nine different types of vesicles, T3 vesicles (with 25% Tween-80) were found to have shown the smallest size (82.80 AE 0.74 nm), highest release in 24 h (98.01 AE 0.33%) and highest deformability (31.27 AE 0.28) and hence chosen for formulating into the gel. Among three different Carbopol Õ 934 concentrations (1%, 1.5% and 2%), G-2 with 1.5% carbopol was chosen as the final formulation. The formulation has shown almost twice the transdermal flux as compared to the gel with free Tenoxicam. The in vivo performance was also found to be significantly better than the oral Tenoxicam and marketed aceclofenac gel (Hifenac Õ ). This study concluded that the gel containing Tenoxicam encapsulated in ultradeformable vesicles has a better prospective for the transdermal use to treat rheumatoid arthritis.

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“…Also, from the regression equation (7); the second effective factor was B in its high level (tween 80). This result was explained by the solubilizing effect and the HLB value of tween 80 [38][39][40]. Generally, the use of edge activators with lower HLB resulted in vesicles with the smaller size as in the case of tween 80 compared with SDC [22].…”

Section: Discussionmentioning

confidence: 94%

Betamethasone Dipropionate Gel for Treatment of Localized Plaque Psoriasis

Gizaway

Fadel

Mourad

et al. 2017

Int J Pharm Pharm Sci

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Objective: The main aim of this study was to design and characterise betamethasone di-propionate loaded transfersomes (BD-T); as a topical formulation for the treatment of localized plaque psoriasis. 3 ) was applied to study the effects of three independent variables: drug content, type of surfactants and surfactant contents on particle size (PS), entrapment efficiency (EE %), zeta potential (ZP), polydispersity index (PI) and drug release profiles. The optimized BD-T was formulated as a hydrogel using 5% sodium carboxymethyl cellulose. The gel was characterized for viscosity, drug content, in vitro drug release and stability. A comparative clinical study was performed on 20 patients with psoriasis to investigate the effect of BD-T gel and the marketed betamethasone dipropionate (BD) cream. Methods Results:The optimized BD-T formulation containing 50 mg betamethasone dipropionate (BD) and 5 mg tween 80 showed spherical unilamellar vesicles with an average particle size of 242.80, % EE of 90.19%, ZP of-15.00 mV, PI of 0.407 and K0 Keywords: Transfersomes, Betamethasone dipropionate (BD), Localized psoriasis of 4.290 mg/hr. The formulation showed good stability at 4 °C and 25 °C for 6 mo. The results revealed significant clinical improvement and a significant increase in safety and tolerability with BD-T gel compared with BD cream. Conclusion:As a conclusion, BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.

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Oestradiol skin delivery from ultradeformable liposomes: refinement of surfactant concentration

Cited by 253 publications

References 26 publications

Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

Nano-appended transdermal gel of Tenoxicam via ultradeformable drug carrier system

Betamethasone Dipropionate Gel for Treatment of Localized Plaque Psoriasis

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