In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis
Psoriasis is chronic autoimmune disease that affects 2–5% of the global population. Fluocinolone acetonide (FLU) and acitretin (ACT) are widely used antipsoriatic drugs that belong to BCS classes II and IV, respectively. FLU exhibits side effects, such as skin irritation and a burning sensation. ACT...
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MDPI AG
2022-11-01
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| author | Hassan Raza Shefaat Ullah Shah Zakir Ali Atif Ullah Khan Irfa Basharat Rajput Arshad Farid Mohammed Al Mohaini Abdulkhaliq J. Alsalman Maitham A. Al Hawaj Saima Mahmood Abid Hussain Kifayat Ullah Shah |
| author_facet | Hassan Raza Shefaat Ullah Shah Zakir Ali Atif Ullah Khan Irfa Basharat Rajput Arshad Farid Mohammed Al Mohaini Abdulkhaliq J. Alsalman Maitham A. Al Hawaj Saima Mahmood Abid Hussain Kifayat Ullah Shah |
| author_sort | Hassan Raza |
| collection | DOAJ |
| description | Psoriasis is chronic autoimmune disease that affects 2–5% of the global population. Fluocinolone acetonide (FLU) and acitretin (ACT) are widely used antipsoriatic drugs that belong to BCS classes II and IV, respectively. FLU exhibits side effects, such as skin irritation and a burning sensation. ACT also shows adverse effects, such as gingivitis, teratogenic effects and xerophthalmia. In the present study, topical nanostructured lipid carriers (NLCs) were fabricated to reduce the side effects and enhance the therapeutic efficacy. FLU–ACT-coloaded NLCs were prepared by the modified microemulsion method and optimized by the Box–Behnken model of Design Expert<sup>®</sup> version 12. The optimization was based on the particle size (PS), zeta potential (ZP) and percentage of encapsulation efficiency (%EE). The physicochemical analyses were performed by TEM, FTIR, XRD and DSC to assess the morphology, chemical interactions between excipients, crystallinity and thermal behavior of the optimized FLU–ACT-coloaded NLCs. The FLU–ACT-coloaded NLCs were successfully loaded into gel and characterized appropriately. The dialysis bag method and Franz diffusion cells were used for the in vitro release and ex vivo permeation studies, respectively. The optimized FLU–ACT-coloaded NLCs had the desired particle size of 288.2 ± 2.3 nm, ZP of −34.2 ± 1.0 mV and %EE values of 81.6 ± 1.1% for ACT and 75 ± 1.3% for FLU. The TEM results confirmed the spherical morphology, while the FTIR results showed the absence of chemical interactions of any type among the ingredients of the FLU–ACT-coloaded NLCs. The XRD and DSC analyses confirmed the amorphous nature and thermal behavior. The in vitro study showed the sustained release of the FLU and ACT from the optimized FLU–ACT-coloaded NLCs and FLU–ACT-coloaded NLC gel compared with the FLU–ACT suspension and conventional gel. The ex vivo study confirmed the minimal permeation of both drugs from the FLU–ACT-coloaded NLC gel. |
| first_indexed | 2024-03-09T18:19:13Z |
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| language | English |
| last_indexed | 2024-03-09T18:19:13Z |
| publishDate | 2022-11-01 |
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| spelling | doaj.art-04f0258f5fb64cc692a8027d9e1c3cd12023-11-24T08:26:00ZengMDPI AGGels2310-28612022-11-0181174610.3390/gels8110746In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of PsoriasisHassan Raza0Shefaat Ullah Shah1Zakir Ali2Atif Ullah Khan3Irfa Basharat Rajput4Arshad Farid5Mohammed Al Mohaini6Abdulkhaliq J. Alsalman7Maitham A. Al Hawaj8Saima Mahmood9Abid Hussain10Kifayat Ullah Shah11Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Aam University, Islamabad 45230, PakistanFaculty of pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanDepartment of Pharmacy, Faculty of Biological Sciences, Quaid-i-Aam University, Islamabad 45230, PakistanDepartment of Pharmacy, Faculty of Biological Sciences, Quaid-i-Aam University, Islamabad 45230, PakistanDepartment of Pharmacy, Faculty of Biological Sciences, Quaid-i-Aam University, Islamabad 45230, PakistanGomal Center of Biochemistry and Biotechnology, Gomal University, Dera Ismail Khan 29050, PakistanBasic Sciences Department, College of Applied Medical Sciences, King Saud bin Abdulaziz University for Health Sciences, Alahsa 31982, Saudi ArabiaDepartment of Clinical Pharmacy, Faculty of Pharmacy, Northern Border University, Rafha 91911, Saudi ArabiaDepartment of Pharmacy Practice, College of Clinical Pharmacy, King Faisal University, Ahsa 31982, Saudi ArabiaFaculty of pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanDepartment of Pharmacy, Faculty of Medical and Health Sciences, University of Poonch Rawalakot, Rawalakot 12350, PakistanDepartment of Pharmacy, Faculty of Biological Sciences, Quaid-i-Aam University, Islamabad 45230, PakistanPsoriasis is chronic autoimmune disease that affects 2–5% of the global population. Fluocinolone acetonide (FLU) and acitretin (ACT) are widely used antipsoriatic drugs that belong to BCS classes II and IV, respectively. FLU exhibits side effects, such as skin irritation and a burning sensation. ACT also shows adverse effects, such as gingivitis, teratogenic effects and xerophthalmia. In the present study, topical nanostructured lipid carriers (NLCs) were fabricated to reduce the side effects and enhance the therapeutic efficacy. FLU–ACT-coloaded NLCs were prepared by the modified microemulsion method and optimized by the Box–Behnken model of Design Expert<sup>®</sup> version 12. The optimization was based on the particle size (PS), zeta potential (ZP) and percentage of encapsulation efficiency (%EE). The physicochemical analyses were performed by TEM, FTIR, XRD and DSC to assess the morphology, chemical interactions between excipients, crystallinity and thermal behavior of the optimized FLU–ACT-coloaded NLCs. The FLU–ACT-coloaded NLCs were successfully loaded into gel and characterized appropriately. The dialysis bag method and Franz diffusion cells were used for the in vitro release and ex vivo permeation studies, respectively. The optimized FLU–ACT-coloaded NLCs had the desired particle size of 288.2 ± 2.3 nm, ZP of −34.2 ± 1.0 mV and %EE values of 81.6 ± 1.1% for ACT and 75 ± 1.3% for FLU. The TEM results confirmed the spherical morphology, while the FTIR results showed the absence of chemical interactions of any type among the ingredients of the FLU–ACT-coloaded NLCs. The XRD and DSC analyses confirmed the amorphous nature and thermal behavior. The in vitro study showed the sustained release of the FLU and ACT from the optimized FLU–ACT-coloaded NLCs and FLU–ACT-coloaded NLC gel compared with the FLU–ACT suspension and conventional gel. The ex vivo study confirmed the minimal permeation of both drugs from the FLU–ACT-coloaded NLC gel.https://www.mdpi.com/2310-2861/8/11/746fluocinolone acetonideacitretinnanostructured lipid carrierbioavailabilityocclusive effectentrapment efficiency |
| spellingShingle | Hassan Raza Shefaat Ullah Shah Zakir Ali Atif Ullah Khan Irfa Basharat Rajput Arshad Farid Mohammed Al Mohaini Abdulkhaliq J. Alsalman Maitham A. Al Hawaj Saima Mahmood Abid Hussain Kifayat Ullah Shah In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis Gels fluocinolone acetonide acitretin nanostructured lipid carrier bioavailability occlusive effect entrapment efficiency |
| title | In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis |
| title_full | In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis |
| title_fullStr | In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis |
| title_full_unstemmed | In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis |
| title_short | In Vitro and Ex Vivo Evaluation of Fluocinolone Acetonide–Acitretin-Coloaded Nanostructured Lipid Carriers for Topical Treatment of Psoriasis |
| title_sort | in vitro and ex vivo evaluation of fluocinolone acetonide acitretin coloaded nanostructured lipid carriers for topical treatment of psoriasis |
| topic | fluocinolone acetonide acitretin nanostructured lipid carrier bioavailability occlusive effect entrapment efficiency |
| url | https://www.mdpi.com/2310-2861/8/11/746 |
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