Amphotericin B-loaded deformable lipid vesicles for topical treatment of cutaneous leishmaniasis skin lesions
Cutaneous leishmaniasis (CL), the most common clinical form of human leishmaniasis, is a non-fatal chronic and disabling disease characterized by erythema and nodular or ulcerative skin lesions that may cause permanent scars and disfigurement. Topical drug delivery represents a simple and efficacious approach to treat CL skin lesions. The association of drugs with nanocarrier systems enhances their permeation properties and increases the drug amount available in the dermis. Here, a deformable lipid vesicle (DLV) was optimized for the topical administration of Amphotericin B (AmB), with the aim of studying and understanding the advantages of this type of delivery system in the transport of a drug through the skin layers. AmB-DVL were characterized in terms of incorporation parameters, stability, and elasticity, and evaluated in vitro for their permeation properties, cytotoxicity, and anti-leishmanial activity. The AmB-DVL exhibited a translucent fluid gel-like aspect and a yellow color, a mean size of 132 nm (PdI ≤ 0.1), zeta potential values around zero (mV), and an AmB incorporation efficiency of 95%. Permeation and penetration assays suggest that AmB-DLV are suitable for topical administration since AmB was detected in the epidermal and dermal skin layers. AmB-DVL was able to reduce promastigote viability in a dose-dependent manner, as well as the number of intracellular amastigotes in THP-1 macrophages. Selectivity index (SI) value for AmB-DLV was considerably higher than that observed for free AmB. Results suggest that DLV may represent an attractive vehicle for dermal delivery of AmB and a new low-cost and safe therapeutic option in CL treatment.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Drug delivery and translational research - 11(2021), 2 vom: 03. Apr., Seite 717-728 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Carvalheiro, Manuela [VerfasserIn] |
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| Links: |
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| Themen: |
7XU7A7DROE |
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| Anmerkungen: |
Date Completed 03.12.2021 Date Revised 14.12.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1007/s13346-021-00910-z |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM320949400 |
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| 245 | 1 | 0 | |a Amphotericin B-loaded deformable lipid vesicles for topical treatment of cutaneous leishmaniasis skin lesions |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Cutaneous leishmaniasis (CL), the most common clinical form of human leishmaniasis, is a non-fatal chronic and disabling disease characterized by erythema and nodular or ulcerative skin lesions that may cause permanent scars and disfigurement. Topical drug delivery represents a simple and efficacious approach to treat CL skin lesions. The association of drugs with nanocarrier systems enhances their permeation properties and increases the drug amount available in the dermis. Here, a deformable lipid vesicle (DLV) was optimized for the topical administration of Amphotericin B (AmB), with the aim of studying and understanding the advantages of this type of delivery system in the transport of a drug through the skin layers. AmB-DVL were characterized in terms of incorporation parameters, stability, and elasticity, and evaluated in vitro for their permeation properties, cytotoxicity, and anti-leishmanial activity. The AmB-DVL exhibited a translucent fluid gel-like aspect and a yellow color, a mean size of 132 nm (PdI ≤ 0.1), zeta potential values around zero (mV), and an AmB incorporation efficiency of 95%. Permeation and penetration assays suggest that AmB-DLV are suitable for topical administration since AmB was detected in the epidermal and dermal skin layers. AmB-DVL was able to reduce promastigote viability in a dose-dependent manner, as well as the number of intracellular amastigotes in THP-1 macrophages. Selectivity index (SI) value for AmB-DLV was considerably higher than that observed for free AmB. Results suggest that DLV may represent an attractive vehicle for dermal delivery of AmB and a new low-cost and safe therapeutic option in CL treatment | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Amphotericin B | |
| 650 | 4 | |a Cutaneous leishmaniasis | |
| 650 | 4 | |a Deformable lipid vesicles | |
| 650 | 4 | |a Drug delivery | |
| 650 | 4 | |a Topical formulations | |
| 650 | 7 | |a Antiprotozoal Agents |2 NLM | |
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| 700 | 1 | |a Faria-Silva, Catarina |e verfasserin |4 aut | |
| 700 | 1 | |a Marto, Joana |e verfasserin |4 aut | |
| 700 | 1 | |a Simões, Sandra |e verfasserin |4 aut | |
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