Skin permeation enhancement effects of linoleic acid and Azone on narcotic analgesics

Mahjour, Majid; Mauser, Bernadette E.; Fawzi, Mahdi B.

doi:10.1016/0378-5173(89)90054-9

Cited by 26 publications

(6 citation statements)

References 6 publications

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“…Transdermal application of LA was reported in terms of its cutaneous distribution, and it acted as a transdermal absorption-promoting agent. 17,18) In these studies on the topical application of LA, it was observed that the stratum corneum in the epidermis retained LA for 24 h after a single application, and its concentration in the dermis increased with time. However, the mechanism by which LA enhances the permeation of drugs through the skin is not clearly understood.…”

Section: Discussionmentioning

confidence: 99%

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Shigeta

Imanaka²,

Ando³

et al. 2004

Biological & Pharmaceutical Bulletin

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Hyperpigmentation on faces is a highly anxiety-producing symptom, especially for women from the aspect of beauty. We previously reported the skin whitening effect of linoleic acid (LA), 1,2) the mechanism of the whitening effect involving a decrease in tyrosinase level by LA, 3) and clinical trials of liposomal LA for skin hyperpigmentary disorders, such as melasma.4) Although these reports described the whitening effect of LA in transdermal application, and the stabilization of LA by liposomal formulation, it was not confirmed whether LA encapsulated in liposomes enhanced the skin whitening effect. There have been number of reports that describe transdermal application using liposomes on cutaneous absorption, 5-7) on the transdermal delivey of encapsulated drugs 8) and on effective interaction of dermal skin cells with liposomes containing drugs in liposomes.9-11) The synergistic effect of liposomes on active reagents for whitening via transdermal application was also reported.12) Compared to those reagents previously reported, LA is not only effective in whitening but also quite safe.13) Although there are many examples of the transdermal applications of liposomal formulations, little is known about the enhancement of drug efficacy by liposomalization. From this point of view, we were interested in the possible enhancement of LA's whitening activity by encapsulating it in liposomes. The present study clearly demonstrated that LA encapsulation in liposomes significantly enhanced it's whitening efficacy by transdermal application for UV-induced hyperpigmented dorsal skin of brownish guinea pigs. We also observed enhanced whitening efficacy by liposomalization of LA in UV-induced hyperpigmented human skin. MATERIALS AND METHODSWhitening Assay UVB-induced hyperpigmentation was elicited on the backs of brownish guinea pigs weighing about 600 g each (Saitama Experimental Animal Supply Co., Japan) using a modification of the method reported by Imokawa et al.14) Guinea pigs were gently tethered, and four separate areas (2.5 cmϫ2 cm) on the back of each animal were exposed to UVB radiation (ToRex FL20S-E-30/DMR, Toshiba, Japan) three times a week (every other day) for two consecutive weeks. The UVB intensity was 2 mW/cm 2 , and total energy dose was 1 J/cm 2 per exposure. Groups of six or more animals were used in each experiment. The animals were then left for an additional week to allow the UVBinduced hyperpigmentation to stabilize. Test samples were then topically applied daily to the hyperpigmented areas (0.01 ml/cm 2 ) five times per week for 3 successive weeks. The degree of pigmentation was assessed as the L-value measured with a chromameter (CR-200, Minolta, Japan) once every week from the beginning of sample application. The animals were cared for according to the guidelines for the Care and Use of Laboratory Animals of the University of Shizuoka.In the case of human skin assay, persons being tested were 6 healthy men in their 20 s or 30 s. After obtaining informed consents from the volunteers, UVB-induced hyp...

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Section: Discussionmentioning

confidence: 99%

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Shigeta

Imanaka²,

Ando³

et al. 2004

Biological & Pharmaceutical Bulletin

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“…l~~ agents. 95,166,167 588 SINGH AND SINGH tially enhanced the permeability coefficient of the pyridostigmine bromide through human cadaver skin.17' Okamoto et aL106 used four enhancers-1-farnesylazacycloheptan-2-one, 1,geranylazacycloheptan-2-one, l-geranylazacyclopentan-2-one, and 1-dodecylazacycloheptan-2-one-in combination with four vehicles to enhance the penetration of acyclovir through excised hairless mouse and rat skin. N-decylmethylsulfoxide was also used to enhance the permeation of a~i d o t h y m i d i n e l~~ and 5 -f l~o r o u r a c i l .~~~ Essential oils were evaluated as penetration enhancers towards 5-fluorouracil using excised human skin.…”

Section: Azonementioning

confidence: 99%

Transdermal drug delivery by passive diffusion and iontophoresis: A review

Singh

1993

Medicinal Research Reviews

121

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“…Recently, it has been shown that in atopic dermatitis and Netherton syndrome there is a significant increase in the level of MUFAs. , In Netherton syndrome patients, the level of MUFAs can approach around 80–90% of the total level of FFAs . In previous studies unsaturated fatty acids, such as oleic and linoleic acid, have been studied, as they were considered to be potent penetration enhancers. , …”

Section: Introductionmentioning

confidence: 99%

Monounsaturated Fatty Acids Reduce the Barrier of Stratum Corneum Lipid Membranes by Enhancing the Formation of a Hexagonal Lateral Packing

Mojumdar¹,

Helder²,

Gooris³

et al. 2014

Langmuir

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The effectiveness of the skin barrier underlies the outer layer of the skin: the stratum corneum (SC). However, in several skin diseases this barrier is impaired. In two inflammatory skin diseases, atopic eczema and Netherton syndrome, an increased level of monounsaturated fatty acids (MUFAs) has been observed as opposed to healthy skin. In the present study, we aimed to investigate the effect of MUFAs on the lipid organization and skin lipid barrier using an in vitro model membrane system, the stratum corneum substitute (SCS), mimicking the SC lipid composition and organization. To achieve our goal, the SCS has been prepared with increasing levels of MUFAs using various chain length. Permeation studies and trans-epidermal water loss measurements show that an increment of MUFAs reduces the lipid barrier in the SCS. The increased level of unsaturation exerts its effect by reducing the packing density in the lipid organization, while the lamellar phases are not affected. Our findings indicate that increased levels of MUFAs may contribute to the impaired skin barrier in diseased skin.

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Skin permeation enhancement effects of linoleic acid and Azone on narcotic analgesics

Cited by 26 publications

References 6 publications

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Transdermal drug delivery by passive diffusion and iontophoresis: A review

Monounsaturated Fatty Acids Reduce the Barrier of Stratum Corneum Lipid Membranes by Enhancing the Formation of a Hexagonal Lateral Packing

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