Liposomal Linoleic Acid Is Useful as a Skin Lightening Agent.

Imanaka, Hiromichi; Ando, Hironori; Ryu, Atsuko; Shigeta, Yasutami; Kishida, Satomi; Mori, Akira; Makino, Tomoki

doi:10.5107/sccj.33.3_277

Cited by 5 publications

(4 citation statements)

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“…1,21) In those studies, LA was applied as an ethanol solution, and its whitening effect was not compared with other formulations. On the other hand, liposomal LA has been used in clinical tests for melasma 4) : liposomes were used for the purpose of protecting unstable LA from oxidation. There seems to be no report so far for studying the enhancement effect of liposomalization on LA-induced skin whitening.…”

Section: Discussionmentioning

confidence: 99%

“…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][6][7] on the transdermal delivey of encapsulated drugs 8) and on effective interaction of dermal skin cells with liposomes containing drugs in liposomes.…”

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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%

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confidence: 98%

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Shigeta

Imanaka²,

Ando³

et al. 2004

Biological & Pharmaceutical Bulletin

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“…As the same with our results, 9,12-octadecadienoic acid (alpha-linoleic acid) had an inhibitory effect on melanin synthesis through tyrosinase inhibition. 64 , 65 Moreover, both alpha-linoleic acid and 9,12,15-octadecanoic acid (linoleic acid) inhibited melanin production through the activation of the desquamation of melanin pigment in the epidermis layer. 66 From all results, the diethyl ether, and butanol extracts had the potential compounds which showed inhibitory activity against tyrosinase and MITF as targets of hyperpigmentation treatment.…”

Section: Discussionmentioning

confidence: 99%

Melanogenesis Inhibitory Activity, Chemical Components and Molecular Docking Studies of Prunus cerasoides Buch.-Ham. D. Don. Flowers

Kooltheat

Tedasen

Yamasaki

et al. 2023

J Evid Based Complementary Altern Med

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Safe depigmenting agents are currently increasing in the cosmetic or pharmaceutical industry because various compounds have been found to have undesirable side effects. Therefore, the present study aimed to investigate the melanogenesis inhibitory effects of Prunus cerasoides Buch. -Ham. D. Don. flower extracts and their molecular mechanism in B16F10 mouse melanoma cells. Moreover, we also examined phenolic and flavonoid contents, antioxidant activity, chemical constituents of potential extracts, and molecular docking. The highest phenolic and flavonoid contents with the greatest scavenging activity were found in the butanol extract of the P. cerasoides flower compared to other extracts. From all extracts, only crude, diethyl ether, and butanol extracts showed an inhibition of mushroom tyrosinase activity, cellular tyrosinase activity, and melanin content as well as the downregulation of the gene expression of the microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein-1 (TRP-1), and tyrosinase-related protein-2 (TRP-2) in α-MSH-stimulated B16F10 cells. Based on the molecular docking study, n-hexadecanoic acid, heptadecanoic acid, octadecanoic acid, 9,12-octadecadienoic acid, 9,12,15-octadecanoic acid, and eicosanoic acid might show an inhibitory effect against tyrosinase and MITF. In conclusion, this finding demonstrates that both the diethyl ether and butanol extracts of the P. cerasoides flower can effectively reduce tyrosinase activity and melanin synthesis through the downregulation of the melanogenic gene expression in B16F10 cells and through the molecular docking study. Taken together, the diethyl ether and butanol extracts of the P. cerasoides flower could be an anti-melanogenic ingredient for hyperpigmentary or melasma treatment.

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“…[1][2][3] We previously observed that linoleic acid (LA) had a skin-whitening effect 4,5) and that the liposomal formulation of LA had hypopigmenting effects in clinical trials for skin hyperpigmentary disorders such as melasma. 6) Practical usage of whitening reagents has become increasingly important. Compared to previously reported reagents, LA is not only effective in whitening but also safe.…”

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confidence: 99%

Suppressed Permeation of Linoleic Acid in a Liposomal Formulation through Reconstructed Skin Tissue

Shigeta

Imanaka²,

Yonezawa

et al. 2004

Biological & Pharmaceutical Bulletin

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Since the liposomal formulation of linoleic acid (LA) exhibited an enhanced skin-whitening effect, the influence of liposomalization on the cutaneous absorption of LA was examined using a three-dimensional (3D) reconstructed skin model. Liposome entrapped [ 14 C]-LA was applied on the skin model, and the permeation of LA through the skin was monitored. The permeation rate of LA in the liposomal formulation was found to be lower than that in the conventional formulation without liposomes, suggesting the increased retention time of LA in the skin by the liposomal formulation. Next, to investigate the dependence of the LA permeation on melanocyte conditions and intactness of the reconstructed skin model, the effect of UV irradiation on LA permeation was examined. Low-dose UVB irradiation (0.03 J/cm 2 for 3 times), which activated melanocytes in the skin, did not influence the extent of LA permeation, while high-dose irradiation (0.30 J/cm 2 for 3 times) enhanced the permeation of LA in both the conventional and liposomal formulation. The present results suggest the importance of skin intactness for LA permeation and that the 3D reconstructed skin model would be useful for evaluating the characteristics of skin-oriented cosmetics and drugs.

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Liposomal Linoleic Acid Is Useful as a Skin Lightening Agent.

Cited by 5 publications

References 0 publications

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Skin Whitening Effect of Linoleic Acid Is Enhanced by Liposomal Formulations

Melanogenesis Inhibitory Activity, Chemical Components and Molecular Docking Studies of Prunus cerasoides Buch.-Ham. D. Don. Flowers

Suppressed Permeation of Linoleic Acid in a Liposomal Formulation through Reconstructed Skin Tissue

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