Oxide Terpenes as Human Skin Penetration Enhancers of Haloperidol from Ethanol and Propylene Glycol and Their Modes of Action on Stratum Corneum.

Vaddi, H.K; Ho, Paul C.; Chan, Yew Weng; Chan, Sui Yung

doi:10.1248/bpb.26.220

Cited by 24 publications

(26 citation statements)

References 24 publications

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“…3. The usual mechanism reported for EtOH enhancement of SC transport is through skin lipid and protein extraction and membrane disruption (42)(43)(44). This work suggests that an ethanol induced reduction in diffusion rate constant may be synergistic with these mechanisms.…”

Section: % Etoh/water Vehiclementioning

confidence: 70%

An Integrated Pharmacokinetic and Imaging Evaluation of Vehicle Effects on Solute Human Epidermal Flux and, Retention Characteristics

et al. 2007

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Section: % Etoh/water Vehiclementioning

confidence: 70%

An Integrated Pharmacokinetic and Imaging Evaluation of Vehicle Effects on Solute Human Epidermal Flux and, Retention Characteristics

et al. 2007

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“…The skin sample, with the SC facing up, was incubated in a petri dish over a Whatman ® filter paper saturated with 0.1% (weight to volume) trypsin in 0.5% (weight to volume) sodium bicarbonate solution at 37°C±1°C for 3 hours. 25 The SC was detached from the rest of the skin, thoroughly washed, and kept for drying in a vacuum dessicator. Around 20 mg of dried SC sample was taken and allowed to hydrate in saturated sodium sulphate solution for 5 days.…”

Section: Drug Entrapment Efficiencymentioning

confidence: 99%

“…The changes in structure of the SC were assessed from the obtained thermograms. 25 Weight of hydrated SC Weight of dry SC Hydration % 100. Weight of dry SC…”

Section: Drug Entrapment Efficiencymentioning

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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“…Limonene oxide and pinene oxide were used to study the penetration of haloperidol from ethanol and propylene glycol and to carry out haloperidol-stratum corneum binding studies. It was shown that the mode of interactions of terpenes with the stratum corneum is different in two different solvent systems [70] . Essential oils from Ocimum basilicum containing terpenes with various carbon numbers effectively accelerated indomethacin permeation across the skin and caused no or negligible irritation [71] .…”

Section: Terpenes and Terpenoidsmentioning

confidence: 99%

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

Trommer

Neubert

2006

Skin Pharmacol Physiol

459

279

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It is preferred that topically administered drugs act either dermally or transdermally. For that reason they have to penetrate into the deeper skin layers or permeate the skin. The outermost layer of the human skin, the stratum corneum, is responsible for its barrier function. Most topically administered drugs do not have the ability to penetrate the stratum corneum. In these cases modulations of the skin penetration profiles of these drugs and skin barrier manipulations are necessary. A skin penetration enhancement can be achieved either chemically, physically or by use of appropriate formulations. Numerous chemical compounds have been evaluated for penetration-enhancing activity, and different modes of action have been identified for skin penetration enhancement. In addition to chemical methods, skin penetration of drugs can be improved by physical options such as iontophoresis and phonophoresis, as well as by combinations of both chemical and physical methods or by combinations of several physical methods. There are cases where skin penetration of the drug used in the formulation is not the aim of the topical administration. Penetration reducers can be used to prevent chemicals entering the systemic circulation. This article concentrates on the progress made mainly over the last decade by use of chemical penetration enhancers. The different action modes of these substances are explained, including the basic principles of the physical skin penetration enhancement techniques and examples for their application.

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Oxide Terpenes as Human Skin Penetration Enhancers of Haloperidol from Ethanol and Propylene Glycol and Their Modes of Action on Stratum Corneum.

Cited by 24 publications

References 24 publications

An Integrated Pharmacokinetic and Imaging Evaluation of Vehicle Effects on Solute Human Epidermal Flux and, Retention Characteristics

An Integrated Pharmacokinetic and Imaging Evaluation of Vehicle Effects on Solute Human Epidermal Flux and, Retention Characteristics

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

Overcoming the Stratum Corneum: The Modulation of Skin Penetration

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