Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line
Aceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citrone...
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MDPI AG
2023-09-01
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| author | Mona K. Younis Islam A. Khalil Nancy S. Younis Rasha R. Fakhr Eldeen Rana M. Abdelnaby Reem A. Aldeeb Amal A. Taha Doaa H. Hassan |
| author_facet | Mona K. Younis Islam A. Khalil Nancy S. Younis Rasha R. Fakhr Eldeen Rana M. Abdelnaby Reem A. Aldeeb Amal A. Taha Doaa H. Hassan |
| author_sort | Mona K. Younis |
| collection | DOAJ |
| description | Aceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citronellol, a monoterpenoid alcohol found in essential oils, exhibits antioxidant properties and activities such as inhibiting cell growth and acetylcholinesterase inhibition. In this study, the objective was to formulate and evaluate an aceclofenac/citronellol oil nanoemulsion for its antiproliferative effects on melanoma. The optimal concentrations of citronellol oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were characterized for droplet size, zeta potential, thermophysical stability, and in vitro release. The selected formula (F1) consisted of citronellol oil (1 gm%), Tween 80 (4 gm%), and Transcutol HP (1 gm%). F1 exhibited a spherical appearance with high drug content, small droplet size, and acceptable negative zeta potential. The amorphous state of the drug in the nanoemulsion was confirmed by Differential Scanning Calorimetry, while FTIR analysis indicated its homogenous solubility. The nanoemulsion showed significant antiproliferative activity, with a lower IC50 value compared to aceclofenac or citronellol alone. Flow cytometric analysis revealed cell cycle arrest and increased apoptosis induced by the nanoemulsion. In silico studies provided insights into the molecular mechanism underlying the observed antitumor activity. In conclusion, the developed aceclofenac/citronellol oil nanoemulsion exhibited potent cytotoxicity and pro-apoptotic effects, suggesting its potential as a repurposed antiproliferative agent for melanoma treatment. In a future plan, further animal model research for validation is suggested. |
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| language | English |
| last_indexed | 2024-03-10T23:00:52Z |
| publishDate | 2023-09-01 |
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| series | Biomedicines |
| spelling | doaj.art-ebd4f042ca7e4bd594a485d277d42c622023-11-19T09:42:38ZengMDPI AGBiomedicines2227-90592023-09-01119253110.3390/biomedicines11092531Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell LineMona K. Younis0Islam A. Khalil1Nancy S. Younis2Rasha R. Fakhr Eldeen3Rana M. Abdelnaby4Reem A. Aldeeb5Amal A. Taha6Doaa H. Hassan7Department of Pharmaceutics, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptDepartment of Pharmaceutics, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Biochemistry, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptDepartment Pharmaceutical Chemistry, Faculty of Pharmacy, Heliopolis University, Cairo 11785, EgyptDepartment of Pharmaceutics, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptDepartment of Pharmaceutics, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptDepartment of Pharmaceutics, College of Pharmaceutical Science and Drug Manufacturing, Misr University for Science and Technology, 6th of October City 12566, EgyptAceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citronellol, a monoterpenoid alcohol found in essential oils, exhibits antioxidant properties and activities such as inhibiting cell growth and acetylcholinesterase inhibition. In this study, the objective was to formulate and evaluate an aceclofenac/citronellol oil nanoemulsion for its antiproliferative effects on melanoma. The optimal concentrations of citronellol oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were characterized for droplet size, zeta potential, thermophysical stability, and in vitro release. The selected formula (F1) consisted of citronellol oil (1 gm%), Tween 80 (4 gm%), and Transcutol HP (1 gm%). F1 exhibited a spherical appearance with high drug content, small droplet size, and acceptable negative zeta potential. The amorphous state of the drug in the nanoemulsion was confirmed by Differential Scanning Calorimetry, while FTIR analysis indicated its homogenous solubility. The nanoemulsion showed significant antiproliferative activity, with a lower IC50 value compared to aceclofenac or citronellol alone. Flow cytometric analysis revealed cell cycle arrest and increased apoptosis induced by the nanoemulsion. In silico studies provided insights into the molecular mechanism underlying the observed antitumor activity. In conclusion, the developed aceclofenac/citronellol oil nanoemulsion exhibited potent cytotoxicity and pro-apoptotic effects, suggesting its potential as a repurposed antiproliferative agent for melanoma treatment. In a future plan, further animal model research for validation is suggested.https://www.mdpi.com/2227-9059/11/9/2531aceclofenaccitronellolnanoemulsionmelanomaantiproliferativeapoptosis |
| spellingShingle | Mona K. Younis Islam A. Khalil Nancy S. Younis Rasha R. Fakhr Eldeen Rana M. Abdelnaby Reem A. Aldeeb Amal A. Taha Doaa H. Hassan Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line Biomedicines aceclofenac citronellol nanoemulsion melanoma antiproliferative apoptosis |
| title | Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line |
| title_full | Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line |
| title_fullStr | Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line |
| title_full_unstemmed | Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line |
| title_short | Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line |
| title_sort | aceclofenac citronellol oil nanoemulsion repurposing study formulation in vitro characterization and in silico evaluation of their antiproliferative and pro apoptotic activity against melanoma cell line |
| topic | aceclofenac citronellol nanoemulsion melanoma antiproliferative apoptosis |
| url | https://www.mdpi.com/2227-9059/11/9/2531 |
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