Percutaneous absorption of griseofulvin and proquazone in the rat and in isolated human skin

Franz, John M.; Gaillard, A.W.K.; Maibach, Howard I.; Schweitzer, A.

doi:10.1007/bf00409456

Cited by 11 publications

(7 citation statements)

References 4 publications

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“…Whereas erythromycin is only slightly soluble in water (0Á1%) it is freely soluble in organic solvents such as alcohol, chloroform, ether, acetone, acetonitrile and benzyl alcohol, which might enable its transfer to the lipoidal components of cells and matrices. The results from microautoradiography seem similar to those of Franz et al (1981) who observed progressive disappearance of radioactivity from the surface and a route of penetration which initially seemed to occur adjacent to the pilosebaceous glands and skin appendages, followed by diffusion of the labelled molecules through the epidermis before subsequent capillary transport. The erythromycin dissolved in the TPDS might penetrate the skin by various routes.…”

Section: Concentration Of N-methyl[ 14 C]erythromycin In the Skinðradsupporting

confidence: 82%

“…The dry slices were then stained with Paragon Blue. This is a variation of the methods of Franz et al (1981) and Sun et al (1994). Adjacent sections were also stained with haematoxylin±eosin.…”

Section: Animals and Proceduresmentioning

confidence: 99%

“…In general, the duct of the gland is ®lled with a soft, slowly extruded lipoidal medium, sebum, and drug dissolved in the lypophilic solvent mixture tends to accumulate in this area. This might be followed by diffusion through the sebum into the surrounding dermis, therefore, the pilosebaceous glands providing an accessory, although quantitatively less important, mechanism for penetration (Franz et al 1981). When the TPDS is used as carrier, diffusion might involve migration from sebum to epidermis and then steady entry into the systemic circulation.…”

Section: Concentration Of N-methyl[ 14 C]erythromycin In the Skinðradmentioning

confidence: 99%

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Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

Peng

Nimni

1999

Journal of Pharmacy and Pharmacology

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Topical administration of antibiotics is associated with reduced risk of systemic side-effects and alteration of gut microflora, and results in higher concentrations of antibiotics at the site of application (and so a lower dose of the drug is required). In conditions such as acne vulgaris, infiltration of the antibiotics into the infected subcutaneous layers is highly desirable. A trans-phase delivery system (TPDS), a mixture of benzyl alcohol, acetone and isopropanol, has been shown to enhance the effective transport of the antibiotic erythromycin across the epidermal barrier and enhance accumulation in the dermis. Two formulations containing N-methyl[14C]erythromycin were compared, a TPDS solution and a propylene glycol solution. They were applied to the dorsal areas of 4-6 week old Fischer rats and tissues were removed for analysis of radioactivity after 2, 4, 8, 12 or 24 h and skin was biopsied and sectioned for autoradiography. The erythromycin dissolved in the TPDS solvent mixture penetrated the stratum corneum and a relatively high concentration was maintained in adjacent tissues for up to 24 h. Penetration was very effective and the erythromycin was detected in significant amounts in the underlying muscle, various organs and later in the urine. In contrast the propylene glycol carrier, probably because of its primarily hydrophilic character, caused the erythromycin to traverse tissue barriers rapidly and appear in the urine. Microautoradiographs qualitatively revealed progressive disappearance of radioactivity from the surface; this correlated with results obtained by direct isotope counting. The route of penetration, in addition to following the interkeratinocyte spaces, seemed to include the perimeter of the pilosebaceous glands and their appendages before diffusion into the capillaries. The propylene glycol solution seemed to traverse the epidermis and the papillary and reticular dermis more rapidly, which might explain its rapid appearance in the urine. These data suggest that the different solutions penetrate the skin by different mechanisms.

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Section: Concentration Of N-methyl[ 14 C]erythromycin In the Skinðradsupporting

confidence: 82%

Section: Animals and Proceduresmentioning

confidence: 99%

Section: Concentration Of N-methyl[ 14 C]erythromycin In the Skinðradmentioning

confidence: 99%

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Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

Peng

Nimni

1999

Journal of Pharmacy and Pharmacology

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“…140,141 When creating novel formulations for griseofulvin, the urine excretion levels are also often investigated. 142,143 Recently, we have demonstrated a strong correlation between the in vivo degradation profile of vaterite carriers inside the hair follicles, intrafollicular storage of the loaded drug, and its excretion kinetics in urine. 46 Thus, here, the Gf excretion profiles were studied to assess the prolonged-release property of the designed carriers in vivo.…”

Section: Biomaterials Sciencementioning

confidence: 99%

CaCO₃-based carriers with prolonged release properties for antifungal drug delivery to hair follicles

et al. 2022

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“…Some GEFA derivatives were reported as enhancers of the percutaneous absorption of drugs. 26,27) Figure 1 shows the effect of the substitution degree of the caprylic chain in GEFA-C 8 on the skin permeation of PTZ. GEFA-DiC 8 and GEFATriC 8 did not have an enhancing effect on the skin permeation of PTZ.…”

Section: Screening Test For Effective Enhancersmentioning

confidence: 99%

Effect of Permeation Enhancers on the in Vitro Percutaneous Absorption of Pentazocine1)

Furuishi

Oda

Saito

et al. 2007

Biological & Pharmaceutical Bulletin

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The transdermal drug delivery system (TDDS) has some advantages as an alternative dosage form (i) avoiding firstpass metabolism, (ii) easy discontinuation of administration, and (iii) reduced side effects; however, the stratum corneum, which is the outermost layer of skin, provides a primary barrier to transdermal drug delivery.Pentazocine (PTZ), a relatively short-acting narcotic-antagonist analgesic, is used clinically for the relief of cancerrelated or postoperative pain, and PTZ shows an analgesic effect, a third as strong as morphine. As PTZ has a short halflife of 2 to 3 h 2) and undergoes extensive first-pass metabolism in the liver, conventional therapy with tablets or injection may result in unstable plasma concentration of the drug, which results in the induction of unexpected side effects. Long-term delivery of PTZ is thus needed at a controlled rate in the body for chronic pain management.3) Mandal et al. have reported the percutaneous absorption of PTZ together with isopropyl myristate (IPM) as an enhancer, 4,5) however, the enhanced skin permeation of PTZ is considered limited when IPM is used alone, and increased concentration of the enhancer would cause skin irritation.6) It is well known that the combination of various enhancers improved the percutaneous absorption of drugs much greater than either enhancer alone. 7,8) Regarding opioid analgesics, Morimoto et al. have reported that the percutaneous absorption of morphine hydrochloride was improved with a combination of l-menthol and ethanol. The cumulative amount of morphine permeated through hairless rat skin over 10 h was 5-fold times higher than the sum of those with 40% ethanol alone and l-menthol alone. 9)In the present study, therefore, we tried to improve the percutaneous absorption of PTZ using a combination of various enhancers. The skin permeation of PTZ through hairless mouse skin as a model membrane was determined using Franz diffusion cells and to select an appropriate enhancer for developing a new transdermal system. The flux, lag time and cumulative amount of permeated PTZ were measured as indicators of skin permeation improvement. Moreover, the effects of the structure of enhancers and hydrophiliclipophilic balance (HLB) on permeation rates of PTZ were discussed. MATERIALS AND METHODSMaterials PTZ was purchased from Kobayashi Kako Co., Ltd. (Fukui, Japan). IPM, citric acid, urea, and 1-octadecanol were purchased from Wako Pure Chemical Industries, Ltd. (Osaka, Japan). N-Methyl-2-pyrrolidone (Pharmasolve ® , Japanese Pharmaceutical Excipient grade) was a gift from ISP Japan (Tokyo, Japan). Glyceryl monocaprylate (GEFA-C 8 , Sunsoft ® 700P-2), glyceryl monocaprate (GEFA-C 10 , Sunsoft ® 760), glyceryl monolaurate (GEFA-C 12 , Sunsoft ® 750), gylceryl monostearete (GEFA-C 18 , Sunsoft ® 8000V) and glyceryl dicaprylate (GEFA-DiC 8 , Sunsoft ® GDC-S) were a gift from Taiyo Kagaku Co., Ltd. (Mie, Japan). Glyceryl tricaprylate (GEFA-TriC8, Panacate ® 800) and polyoxyethylene laurylether (NONION K-204) were a gift from NOF Corporation (T...

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Percutaneous absorption of griseofulvin and proquazone in the rat and in isolated human skin

Cited by 11 publications

References 4 publications

Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

CaCO₃-based carriers with prolonged release properties for antifungal drug delivery to hair follicles

Effect of Permeation Enhancers on the in Vitro Percutaneous Absorption of Pentazocine1)

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Percutaneous absorption of griseofulvin and proquazone in the rat and in isolated human skin

Cited by 11 publications

References 4 publications

Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

Delivery of Erythromycin to Subcutaneous Tissues in Rats by Means of a Trans-phase Delivery System

CaCO3-based carriers with prolonged release properties for antifungal drug delivery to hair follicles

Effect of Permeation Enhancers on the in Vitro Percutaneous Absorption of Pentazocine1)

Contact Info

Product

Resources

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CaCO₃-based carriers with prolonged release properties for antifungal drug delivery to hair follicles