Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies
Hyperpigmentation is a crucial dermatological disorder. This study aims to formulate a nanoemulsion formulation containing chlorogenic acid (CA) for hyperpigmentation treatment, to carry out characterization studies, and to investigate its efficacy and safety in vitro and in silico analysis.In line...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-12-01
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| Series: | Arabian Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878535222006785 |
| _version_ | 1798015555718873088 |
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| author | Yasemin Budama-Kilinc Bahar Gok Serda Kecel-Gunduz Ebru Altuntas |
| author_facet | Yasemin Budama-Kilinc Bahar Gok Serda Kecel-Gunduz Ebru Altuntas |
| author_sort | Yasemin Budama-Kilinc |
| collection | DOAJ |
| description | Hyperpigmentation is a crucial dermatological disorder. This study aims to formulate a nanoemulsion formulation containing chlorogenic acid (CA) for hyperpigmentation treatment, to carry out characterization studies, and to investigate its efficacy and safety in vitro and in silico analysis.In line with this purpose, CA nanoemulsions (CA-NEs) were developed using the ultrasonic homogenization method. Accelerated stability tests were performed to examine the kinetic and thermodynamic stability of the CA-NEs to ascertain the presence of any stability issues. After the heating–cooling test, appropriate CA-NEs were stored for 60 days in three different stability environments to examine the physicochemical stability and determine the finalized formulation. The toxicity of the finalized CA-NE formulation was evaluated by genotoxicity/mutagenicity and cytotoxicity tests. The tyrosinase and melanogenesis activities of the finalized CA-NE formulation were determined on the Melanoma B16F0 cell line. Finally, the molecular docking method was used to reveal interactions of CA that play an essential role in tyrosinase inhibition. Additionally, the mushroom and human tyrosinase enzymes were used to determine the activity of CA. In addition, the comparison study with the molecular docking method was carried out using kojic acid as a reference molecule.In conclusion, the molecular docking study, pharmacokinetic analyses, and in vitro studies showed that F4P1 coded CA-NE formulation might hold promise as an innovative formulation in cosmetic applications such as skin-lightening effects with its high efficacy and safety profile. |
| first_indexed | 2024-04-11T15:36:30Z |
| format | Article |
| id | doaj.art-0c80ce377f474846888b67a3625bf8d2 |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-04-11T15:36:30Z |
| publishDate | 2022-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-0c80ce377f474846888b67a3625bf8d22022-12-22T04:15:56ZengElsevierArabian Journal of Chemistry1878-53522022-12-011512104362Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studiesYasemin Budama-Kilinc0Bahar Gok1Serda Kecel-Gunduz2Ebru Altuntas3Faculty of Chemical and Metallurgical Engineering, Department of Bioengineering, Yildiz Technical University, 34220 Istanbul, Turkey; Corresponding author.Graduate School of Natural and Applied Science, Yildiz Technical University, 34220 Istanbul, TurkeyFaculty of Science, Department of Physics, Istanbul University, 34134 Istanbul, TurkeyFaculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul University, 34116 Istanbul, TurkeyHyperpigmentation is a crucial dermatological disorder. This study aims to formulate a nanoemulsion formulation containing chlorogenic acid (CA) for hyperpigmentation treatment, to carry out characterization studies, and to investigate its efficacy and safety in vitro and in silico analysis.In line with this purpose, CA nanoemulsions (CA-NEs) were developed using the ultrasonic homogenization method. Accelerated stability tests were performed to examine the kinetic and thermodynamic stability of the CA-NEs to ascertain the presence of any stability issues. After the heating–cooling test, appropriate CA-NEs were stored for 60 days in three different stability environments to examine the physicochemical stability and determine the finalized formulation. The toxicity of the finalized CA-NE formulation was evaluated by genotoxicity/mutagenicity and cytotoxicity tests. The tyrosinase and melanogenesis activities of the finalized CA-NE formulation were determined on the Melanoma B16F0 cell line. Finally, the molecular docking method was used to reveal interactions of CA that play an essential role in tyrosinase inhibition. Additionally, the mushroom and human tyrosinase enzymes were used to determine the activity of CA. In addition, the comparison study with the molecular docking method was carried out using kojic acid as a reference molecule.In conclusion, the molecular docking study, pharmacokinetic analyses, and in vitro studies showed that F4P1 coded CA-NE formulation might hold promise as an innovative formulation in cosmetic applications such as skin-lightening effects with its high efficacy and safety profile.http://www.sciencedirect.com/science/article/pii/S1878535222006785Chlorogenic acidNanoemulsionTyrosinaseMelanogenesisHyperpigmentationMolecular docking |
| spellingShingle | Yasemin Budama-Kilinc Bahar Gok Serda Kecel-Gunduz Ebru Altuntas Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies Arabian Journal of Chemistry Chlorogenic acid Nanoemulsion Tyrosinase Melanogenesis Hyperpigmentation Molecular docking |
| title | Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies |
| title_full | Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies |
| title_fullStr | Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies |
| title_full_unstemmed | Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies |
| title_short | Development of nanoformulation for hyperpigmentation disorders: Experimental evaluations, in vitro efficacy and in silico molecular docking studies |
| title_sort | development of nanoformulation for hyperpigmentation disorders experimental evaluations in vitro efficacy and in silico molecular docking studies |
| topic | Chlorogenic acid Nanoemulsion Tyrosinase Melanogenesis Hyperpigmentation Molecular docking |
| url | http://www.sciencedirect.com/science/article/pii/S1878535222006785 |
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