Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management
Nanostructured lipid carriers (NLC) have been widely studied as delivery systems for a variety of routes, including the skin. Their composition results in an imperfect lipid matrix, allowing increased drug encapsulation. Allopurinol (AP), a xanthine oxidase inhibitor, is characterized by low water s...
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| Format: | Article |
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MDPI AG
2021-11-01
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| Series: | Bioengineering |
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| Online Access: | https://www.mdpi.com/2306-5354/8/12/192 |
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| author | Carla Varrica Manuela Carvalheiro Catarina Faria-Silva Carla Eleutério Giuseppina Sandri Sandra Simões |
| author_facet | Carla Varrica Manuela Carvalheiro Catarina Faria-Silva Carla Eleutério Giuseppina Sandri Sandra Simões |
| author_sort | Carla Varrica |
| collection | DOAJ |
| description | Nanostructured lipid carriers (NLC) have been widely studied as delivery systems for a variety of routes, including the skin. Their composition results in an imperfect lipid matrix, allowing increased drug encapsulation. Allopurinol (AP), a xanthine oxidase inhibitor, is characterized by low water solubility and high melting point, which has hampered its use through the topical route. In this work, AP was incorporated in a NLC formulation to enhance drug-carrier association and skin delivery as a topical approach to treat wounds. AP-NLC system was characterized in terms of size, charge, rheological behavior, and in vitro skin permeation. The in vitro cytotoxicity was evaluated using HaCaT cells. The wound healing efficacy of the AP-NLC formulation on animal skin lesions was evaluated in male Wistar rats. The AP-NLC presented a mean size of 193 ± 15 nm with a PdI of 0.240 ± 0.02, zeta potential values around −49.6 mV, and an encapsulation efficiency of 52.2%. The AP-NLC formulation presented an adequate profile to be used topically, since epidermal and dermal drug retention were achieved. No reduction in HaCaT cells viability was observed at the tested concentrations (AP < 10 μg/mL). The in vivo application of the AP-NLC formulation resulted in the regeneration of skin lesions when compared with non-treated controls. |
| first_indexed | 2024-03-10T04:35:12Z |
| format | Article |
| id | doaj.art-e764a8c0b76347d1af96d190f45b14e5 |
| institution | Directory Open Access Journal |
| issn | 2306-5354 |
| language | English |
| last_indexed | 2024-03-10T04:35:12Z |
| publishDate | 2021-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Bioengineering |
| spelling | doaj.art-e764a8c0b76347d1af96d190f45b14e52023-11-23T03:52:06ZengMDPI AGBioengineering2306-53542021-11-0181219210.3390/bioengineering8120192Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing ManagementCarla Varrica0Manuela Carvalheiro1Catarina Faria-Silva2Carla Eleutério3Giuseppina Sandri4Sandra Simões5Department of Drug Sciences, University of Pavia, 27100 Pavia, ItalyFaculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, PortugalFaculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, PortugalFaculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, PortugalDepartment of Drug Sciences, University of Pavia, 27100 Pavia, ItalyFaculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, PortugalNanostructured lipid carriers (NLC) have been widely studied as delivery systems for a variety of routes, including the skin. Their composition results in an imperfect lipid matrix, allowing increased drug encapsulation. Allopurinol (AP), a xanthine oxidase inhibitor, is characterized by low water solubility and high melting point, which has hampered its use through the topical route. In this work, AP was incorporated in a NLC formulation to enhance drug-carrier association and skin delivery as a topical approach to treat wounds. AP-NLC system was characterized in terms of size, charge, rheological behavior, and in vitro skin permeation. The in vitro cytotoxicity was evaluated using HaCaT cells. The wound healing efficacy of the AP-NLC formulation on animal skin lesions was evaluated in male Wistar rats. The AP-NLC presented a mean size of 193 ± 15 nm with a PdI of 0.240 ± 0.02, zeta potential values around −49.6 mV, and an encapsulation efficiency of 52.2%. The AP-NLC formulation presented an adequate profile to be used topically, since epidermal and dermal drug retention were achieved. No reduction in HaCaT cells viability was observed at the tested concentrations (AP < 10 μg/mL). The in vivo application of the AP-NLC formulation resulted in the regeneration of skin lesions when compared with non-treated controls.https://www.mdpi.com/2306-5354/8/12/192wound healingallopurinoltopical formulationsnanocarrier systemsnanostructured lipid carriers |
| spellingShingle | Carla Varrica Manuela Carvalheiro Catarina Faria-Silva Carla Eleutério Giuseppina Sandri Sandra Simões Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management Bioengineering wound healing allopurinol topical formulations nanocarrier systems nanostructured lipid carriers |
| title | Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management |
| title_full | Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management |
| title_fullStr | Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management |
| title_full_unstemmed | Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management |
| title_short | Topical Allopurinol-Loaded Nanostructured Lipid Carriers: A Novel Approach for Wound Healing Management |
| title_sort | topical allopurinol loaded nanostructured lipid carriers a novel approach for wound healing management |
| topic | wound healing allopurinol topical formulations nanocarrier systems nanostructured lipid carriers |
| url | https://www.mdpi.com/2306-5354/8/12/192 |
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