Skin Penetration of Nicotinic Acid, Methyl Nicotinate, and Butyl Nicotinate in the Guinea Pig

Osamura, Hiromi; Jimbo, Yuko; Ishihara, Masaru

doi:10.1111/j.1346-8138.1984.tb01510.x

Cited by 9 publications

(2 citation statements)

References 7 publications

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“…These data are typical of tape stripping experiments and are attributable to either reduced amounts of active being present at relatively deeper, more hydrophilic regions [12] or decreasing protein binding between the keratinocytes with increased depth [9] . Overall, the data illustrate clear trends between the gel 'snapshots', and also between the gel snapshots and the control solution.…”

Section: Effect Of Solvent Content On Skin Localisation Of Ketoprofenmentioning

confidence: 92%

Solvent Content and Macroviscosity Effects on the in vitro Transcutaneous Delivery and Skin Distribution of Ketoprofen from Simple Gel Formulations

Gallagher

Heard²

2005

Skin Pharmacol Physiol

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The effects of decreasing solvent content and macroviscosity of simple topical gel formulations on the transcutaneous delivery and distribution of ketoprofen through skin were studied. Simple topical gels, based on ketoprofen, PEG 400 and either Cabosil^® M-5 or hydroxypropylcellulose were formulated and applied to freshly excised pig ear skin in vitro. Receptor phase samples were taken to determine permeation and depth profiles of ketoprofen were constructed, following tape stripping and membrane separation. Reduction of solvent from the Cabosil-thickened gels resulted in a rank order reduction in the permeation and distribution of ketoprofen. Reduced amounts of ketoprofen were distributed through the skin, particularly the dermis, with decreasing solvent. Two gels sharing the same macroviscosity exhibited significantly different skin permeation and distribution characteristics. The rank order reduction in both permeation and distribution of ketoprofen was attributed to the physiochemical properties of the formulation and how they may change after application, in particular the increased adsorptivity of ketoprofen to the Cabosil relative to the amount of solvent present in the system. This effect appeared to be predominant over any interactions occurring between the formulation and the skin. The data provided further evidence that adsorption to the thickener, rather than changes in viscosity, were primarily responsible for reduced permeation and distribution in the system examined.

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Section: Effect Of Solvent Content On Skin Localisation Of Ketoprofenmentioning

confidence: 92%

Solvent Content and Macroviscosity Effects on the in vitro Transcutaneous Delivery and Skin Distribution of Ketoprofen from Simple Gel Formulations

Gallagher

Heard²

2005

Skin Pharmacol Physiol

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“…Dialysate and arterial blood were collected every 10 min for 4 h after application of ointment. A similar experiment was also performed on the skin surface without stratum corneum, the stratum corneum being removed by repeated stripping (20 times) with adhesive tape (Osamura et al 1984). Complete removal of the stratum corneum…”

Section: Animal Studiesmentioning

confidence: 99%

Effect of Ointment Bases on Topical and Transdermal Delivery of Salicylic Acid in Rats: Evaluation by Skin Microdialysis

Murakami

Yoshioka

Okamoto

et al. 1998

Journal of Pharmacy and Pharmacology

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Microdialysis has been used to determine the concentration of salicylic acid in skin tissue and plasma periodically for 4 h to evaluate the effect of ointment bases on topical and transdermal delivery of salicylic acid. The ointment bases examined were solbase (water-soluble), poloid and white petrolatum (oleaginous), hydrophilic poloid (water in oil (w/o) type emulsion lacking water) and absorptive ointment (w/o-type emulsion containing water). The ointments (0.1 g) containing 25 micromol salicylic acid were applied for 2 h to the surface of rat skin (1 cm2) with (intact) or without the stratum corneum. For intact skin, the extent of topical delivery from different ointments, evaluated by the area under the concentration-time curve (AUC) of salicylic acid in the skin tissue (AUCskin), increased in the order solbase << white petrolatum, poloid, hydrophilic poloid << absorptive ointment. The ratio of AUCskin (topical delivery) to the AUC of salicylic acid in plasma (AUCplasma, transdermal delivery) varied remarkably among the different bases, the greatest ratio being observed for absorptive ointment. When the ointments were applied to skin surface without stratum corneum, AUCskin for solbase was much higher (about 45 times that for intact skin), whereas only a small (two-fold) increase was observed for poloid and hydrophilic poloid and the increase was negligible for white petrolatum and absorptive ointment. For skin without the stratum corneum, the ratio AUCskin/AUCplasma for the different ointments was comparable, although the magnitudes of AUCskin and AUCplasma still varied substantially. The variance of AUC values arises as a result of the different rates of release of salicylic acid from the bases. These results indicate that: the topical and transdermal delivery of salicylic acid in intact skin varies substantially among different ointment bases, and the greatest topical delivery is observed for absorptive ointment; use of absorptive ointment increases the retention of salicylic acid in the stratum corneum; and the stratum corneum functions strongly as a penetration barrier for solbase, moderately for poloid and hydrophilic poloid, and less for absorptive ointment and white petrolatum.

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Percutaneous absorption in diseased skin: an overview

Chiang¹,

Tudela²,

Maibach³

2012

J of Applied Toxicology

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The stratum corneum's (SC) functions include protection from external hazardous environments, prevention of water loss and regulation of body temperature. While intact skin absorption studies are abundant, studies on compromised skin permeability are less common, although products are often used to treat affected skin. We reviewed literature on percutaneous absorption through abnormal skin models. Tape stripping is used to disrupt water barrier function. Studies demonstrated that physicochemical properties influence the stripping effect: water-soluble drugs are more affected. Abrasion did not affect absorption as much. Freezing is commonly used to preserve skin. It does not seem to modify water absorption, but still increases the penetration of compounds. Comparatively, heating the skin consistently increased percutaneous absorption. Removing SC lipids may increase percutaneous absorption of drugs. Many organic solvents are employed to delipidize. Delipidization with chloroform-methanol increased hydrophilic compound permeability, but not lipophilic. Acetone pre-treatment enhanced hydrophilic compound penetration. More data is needed to determine influence on highly lipophilic compound penetration. Sodium lauryl sulfate (SLS) induces irritant dermatitis and is frequently used as a model. Studies revealed that SLS increases hydrophilic compound absorption, but not lipophilic. However, skin irritation with other chemicals increases lipophilic penetration as much as hydrophilic. Animal studies show that UV exposure increases percutaneous absorption whereas human studies do not. Human studies show increased penetration in psoriatic and atopic dermatitis skin. The data summarized here begin to characterize flux alteration associated with damaged skin. Understanding the degree of alteration requires interpretation of involved conditions and the enlarging of our database to a more complete physicochemical spectrum.

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Skin Penetration of Nicotinic Acid, Methyl Nicotinate, and Butyl Nicotinate in the Guinea Pig

Cited by 9 publications

References 7 publications

Solvent Content and Macroviscosity Effects on the in vitro Transcutaneous Delivery and Skin Distribution of Ketoprofen from Simple Gel Formulations

Solvent Content and Macroviscosity Effects on the in vitro Transcutaneous Delivery and Skin Distribution of Ketoprofen from Simple Gel Formulations

Effect of Ointment Bases on Topical and Transdermal Delivery of Salicylic Acid in Rats: Evaluation by Skin Microdialysis

Percutaneous absorption in diseased skin: an overview

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