Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies
Levocetirizine hydrochloride (LVC) is an antihistaminic drug that is repurposed for the treatment of alopecia. This investigation is targeted for formulating LVC into cationic ceramide/phospholipid composite (CCPCs) for the management of alopecia. CCPCs were fabricated by ethanol-injection approach,...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Drug Delivery |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2022.2108939 |
| _version_ | 1811337600540082176 |
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| author | Rofida Albash Rania Moataz El-Dahmy Mohammed I. A. Hamed Khaled M. Darwish Abdulrahman M. Alahdal Amira B. Kassem Abdurrahman M. Fahmy |
| author_facet | Rofida Albash Rania Moataz El-Dahmy Mohammed I. A. Hamed Khaled M. Darwish Abdulrahman M. Alahdal Amira B. Kassem Abdurrahman M. Fahmy |
| author_sort | Rofida Albash |
| collection | DOAJ |
| description | Levocetirizine hydrochloride (LVC) is an antihistaminic drug that is repurposed for the treatment of alopecia. This investigation is targeted for formulating LVC into cationic ceramide/phospholipid composite (CCPCs) for the management of alopecia. CCPCs were fabricated by ethanol-injection approach, through a central composite experiment. CCPCs were evaluated by inspecting their entrapment efficiency (EE%), polydispersity index (PDI), particle size (PS), and zeta potential (ZP). The optimum CCPCs were additionally studied by in-vitro, ex-vivo, in-silico, and in-vivo studies. The fabricated CCPCs had acceptable EE%, PS, PDI, and ZP values. The statistical optimization elected optimum CCPCs composed of 5 mg hyaluronic acid, 10 mg ceramide III, and 5 mg dimethyldidodecylammonium bromide employing phytantriol as a permeation enhancer. The optimum CCPCs had EE%, PS, PDI, and ZP of 88.36 ± 0.34%, 479.00 ± 50.34 nm, 0.377 ± 0.0035, and 20.20 ± 1.13 mV, respectively. The optimum CCPC maintained its stability for up to 90 days. It also viewed vesicles of tube shape via transmission electron microscope. The in-silico assessment resulted in better interaction and stability between LVC and vesicle components in water. The ex-vivo and in-vivo assessments showed satisfactory skin retention of LVC from optimum CCPCs. The histopathological assessment verified the safety of optimum CCPCs to be topically applied. Overall, the optimum CCPCs could be utilized as a potential system for the topical management of alopecia, with a prolonged period of activity, coupled with reduced LVC shortcomings. |
| first_indexed | 2024-04-13T17:57:23Z |
| format | Article |
| id | doaj.art-c7975c27b1a646248532a2f1ebcb5bc2 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-13T17:57:23Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-c7975c27b1a646248532a2f1ebcb5bc22022-12-22T02:36:25ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642022-12-012912784279510.1080/10717544.2022.2108939Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studiesRofida Albash0Rania Moataz El-Dahmy1Mohammed I. A. Hamed2Khaled M. Darwish3Abdulrahman M. Alahdal4Amira B. Kassem5Abdurrahman M. Fahmy6Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, 6th of October City, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Cairo, EgyptDepartment of Organic and Medicinal Chemistry, Faculty of Pharmacy, Fayoum University, Faiyum, EgyptDepartment of Medicinal Chemistry, Faculty of Pharmacy, Suez Canal University, Ismailia, EgyptDepartment of Pharmacy Practice, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi ArabiaDepartment of Clinical Pharmacy and Pharmacy Practice Faculty of Pharmacy, Damanhour University, Damanhour, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Giza, EgyptLevocetirizine hydrochloride (LVC) is an antihistaminic drug that is repurposed for the treatment of alopecia. This investigation is targeted for formulating LVC into cationic ceramide/phospholipid composite (CCPCs) for the management of alopecia. CCPCs were fabricated by ethanol-injection approach, through a central composite experiment. CCPCs were evaluated by inspecting their entrapment efficiency (EE%), polydispersity index (PDI), particle size (PS), and zeta potential (ZP). The optimum CCPCs were additionally studied by in-vitro, ex-vivo, in-silico, and in-vivo studies. The fabricated CCPCs had acceptable EE%, PS, PDI, and ZP values. The statistical optimization elected optimum CCPCs composed of 5 mg hyaluronic acid, 10 mg ceramide III, and 5 mg dimethyldidodecylammonium bromide employing phytantriol as a permeation enhancer. The optimum CCPCs had EE%, PS, PDI, and ZP of 88.36 ± 0.34%, 479.00 ± 50.34 nm, 0.377 ± 0.0035, and 20.20 ± 1.13 mV, respectively. The optimum CCPC maintained its stability for up to 90 days. It also viewed vesicles of tube shape via transmission electron microscope. The in-silico assessment resulted in better interaction and stability between LVC and vesicle components in water. The ex-vivo and in-vivo assessments showed satisfactory skin retention of LVC from optimum CCPCs. The histopathological assessment verified the safety of optimum CCPCs to be topically applied. Overall, the optimum CCPCs could be utilized as a potential system for the topical management of alopecia, with a prolonged period of activity, coupled with reduced LVC shortcomings.https://www.tandfonline.com/doi/10.1080/10717544.2022.2108939Alopecialevocetirizine hydrochloridein-silico studyceramidedrug discoveryindustrial development |
| spellingShingle | Rofida Albash Rania Moataz El-Dahmy Mohammed I. A. Hamed Khaled M. Darwish Abdulrahman M. Alahdal Amira B. Kassem Abdurrahman M. Fahmy Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies Drug Delivery Alopecia levocetirizine hydrochloride in-silico study ceramide drug discovery industrial development |
| title | Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies |
| title_full | Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies |
| title_fullStr | Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies |
| title_full_unstemmed | Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies |
| title_short | Repurposing levocetirizine hydrochloride loaded into cationic ceramide/phospholipid composite (CCPCs) for management of alopecia: central composite design optimization, in- silico and in-vivo studies |
| title_sort | repurposing levocetirizine hydrochloride loaded into cationic ceramide phospholipid composite ccpcs for management of alopecia central composite design optimization in silico and in vivo studies |
| topic | Alopecia levocetirizine hydrochloride in-silico study ceramide drug discovery industrial development |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2022.2108939 |
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