Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery : QbD-driven design, optimization, and in vitro and ex vivo evaluations
© 2021. Controlled Release Society..
The present study is concerned with the QbD-based design and development of luliconazole-loaded nanostructured lipid carriers (NLCs) hydrogel for enhanced skin retention and permeation. The NLCs formulation was optimized employing a 3-factor, 3-level Box-Behnken design. The effect of formulation variable lipid content, surfactant concentration, and sonication time was studied on particle size and % EE. The optimized formulation exhibited particle size of 86.480 ± 0.799 nm; 0.213 ± 0.004 PDI, ≥ - 10 mV zeta potential and 85.770 ± 0.503% EE. The in vitro release studies revealed sustained release of NLCs up to 42 h. The designed formulation showed desirable occlusivity, spreadability (0.748 ± 0.160), extrudability (3.130 ± 1.570), and the assay was found to be 99.520 ± 0.890%. The dermatokinetics assessment revealed the Cmax Skin to be ~ 2-fold higher and AUC0-24 to be ~ 3-fold higher in the epidermis and dermis of NLCs loaded gel in contrast with the marketed cream. The Tmax of both the formulations was found to be 6 h in the epidermis and dermis. The obtained results suggested that luliconazole NLCs can serve as a promising formulation to enhance luliconazole's antifungal activity and also in increasing patient compliance by reducing the frequency of application.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:12 |
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| Enthalten in: |
Drug delivery and translational research - 12(2022), 5 vom: 24. Mai, Seite 1118-1135 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Mahmood, Arisha [VerfasserIn] |
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| Links: |
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| Themen: |
Dermatokinetic |
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| Anmerkungen: |
Date Completed 08.04.2022 Date Revised 08.04.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1007/s13346-021-00986-7 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM324494971 |
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| 100 | 1 | |a Mahmood, Arisha |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery |b QbD-driven design, optimization, and in vitro and ex vivo evaluations |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2021. Controlled Release Society. | ||
| 520 | |a The present study is concerned with the QbD-based design and development of luliconazole-loaded nanostructured lipid carriers (NLCs) hydrogel for enhanced skin retention and permeation. The NLCs formulation was optimized employing a 3-factor, 3-level Box-Behnken design. The effect of formulation variable lipid content, surfactant concentration, and sonication time was studied on particle size and % EE. The optimized formulation exhibited particle size of 86.480 ± 0.799 nm; 0.213 ± 0.004 PDI, ≥ - 10 mV zeta potential and 85.770 ± 0.503% EE. The in vitro release studies revealed sustained release of NLCs up to 42 h. The designed formulation showed desirable occlusivity, spreadability (0.748 ± 0.160), extrudability (3.130 ± 1.570), and the assay was found to be 99.520 ± 0.890%. The dermatokinetics assessment revealed the Cmax Skin to be ~ 2-fold higher and AUC0-24 to be ~ 3-fold higher in the epidermis and dermis of NLCs loaded gel in contrast with the marketed cream. The Tmax of both the formulations was found to be 6 h in the epidermis and dermis. The obtained results suggested that luliconazole NLCs can serve as a promising formulation to enhance luliconazole's antifungal activity and also in increasing patient compliance by reducing the frequency of application | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Dermatokinetic | |
| 650 | 4 | |a Luliconazole | |
| 650 | 4 | |a Nanostructured lipid carriers | |
| 650 | 4 | |a Quality by design | |
| 650 | 4 | |a Skin retention | |
| 650 | 4 | |a Spreadability | |
| 650 | 7 | |a Drug Carriers |2 NLM | |
| 650 | 7 | |a Imidazoles |2 NLM | |
| 650 | 7 | |a Lipids |2 NLM | |
| 650 | 7 | |a luliconazole |2 NLM | |
| 650 | 7 | |a RE91AN4S8G |2 NLM | |
| 700 | 1 | |a Rapalli, Vamshi Krishna |e verfasserin |4 aut | |
| 700 | 1 | |a Gorantla, Srividya |e verfasserin |4 aut | |
| 700 | 1 | |a Waghule, Tejashree |e verfasserin |4 aut | |
| 700 | 1 | |a Singhvi, Gautam |e verfasserin |4 aut | |
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