The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were p...

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Published in:	Nanomaterials (Basel, Switzerland) Vol. 7; no. 9; p. 241
Main Authors:	Kim, Bo-Sik, Choi, Jae-Hwan, Kim, Inhye, Lee, Eunji, Kim, Sung-Yeon, Lee, Jae-Young, Cho, Cheong-Weon
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 28.08.2017 MDPI
Subjects:	Bearing strength Biocompatibility cellular tyrosinase inhibition assay Controlled release Glycerol Lipids Melanoma Nanostructure nanostructured lipid carriers Oils & fats Olive oil phenylethyl resorcinol Polydispersity Resorcinol Skin Solubility Stability Sustained release topical drug delivery Tyrosinase Ultrasonic testing topical drug delivery cellular tyrosinase inhibition assay nanostructured lipid carriers phenylethyl resorcinol stability
ISSN:	2079-4991, 2079-4991
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Abstract	Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.
AbstractList	Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents. Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.
Author	Kim, Bo-Sik Kim, Inhye Lee, Eunji Lee, Jae-Young Kim, Sung-Yeon Choi, Jae-Hwan Cho, Cheong-Weon
AuthorAffiliation	4 Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 54538, South Korea; sungykim@wku.ac.kr 2 IN2BIO Research and Development center, Suwon 16681, South Korea; shevlove@hanmail.net 1 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, South Korea; kimbosik1098@naver.com (B.-S.K.); youngguk@cnu.ac.kr (Y.-G.N.); jaeyoung@cnu.ac.kr (J.-Y.L.) 3 Graduate School of Analytical Science and Technology, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, South Korea; inhyekim@cnu.ac.kr (I.K.); eunjilee@cnu.ac.kr (E.L.)
AuthorAffiliation_xml	– name: 2 IN2BIO Research and Development center, Suwon 16681, South Korea; shevlove@hanmail.net – name: 3 Graduate School of Analytical Science and Technology, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, South Korea; inhyekim@cnu.ac.kr (I.K.); eunjilee@cnu.ac.kr (E.L.) – name: 4 Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 54538, South Korea; sungykim@wku.ac.kr – name: 1 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, South Korea; kimbosik1098@naver.com (B.-S.K.); youngguk@cnu.ac.kr (Y.-G.N.); jaeyoung@cnu.ac.kr (J.-Y.L.)
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Keywords	topical drug delivery cellular tyrosinase inhibition assay nanostructured lipid carriers phenylethyl resorcinol stability
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Snippet	Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity....
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SubjectTerms	Bearing strength Biocompatibility cellular tyrosinase inhibition assay Controlled release Glycerol Lipids Melanoma Nanostructure nanostructured lipid carriers Oils & fats Olive oil phenylethyl resorcinol Polydispersity Resorcinol Skin Solubility Stability Sustained release topical drug delivery Tyrosinase Ultrasonic testing
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Title	The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers
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