Dermal Delivery of Niacinamide—In Vivo Studies
In vivo human studies are considered to be the “gold standard” when investigating (trans)dermal delivery of actives. Previously, we reported the effects of a range of vehicles on the delivery of niacinamide (NIA) using conventional Franz cell studies. In the present work, dermal delivery of NIA was...
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doaj-343038c89e20443cbd67af949b1bd3872021-06-01T00:05:59ZengMDPI AGPharmaceutics1999-49232021-05-011372672610.3390/pharmaceutics13050726Dermal Delivery of Niacinamide—In Vivo StudiesYanling Zhang0Chin-Ping Kung1Fotis Iliopoulos2Bruno C. Sil3Jonathan Hadgraft4Majella E. Lane5Department of Pharmaceutics, University College London School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UKDepartment of Pharmaceutics, University College London School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UKDepartment of Pharmaceutics, University College London School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UKSchool of Human Sciences, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, UKDepartment of Pharmaceutics, University College London School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UKDepartment of Pharmaceutics, University College London School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, UKIn vivo human studies are considered to be the “gold standard” when investigating (trans)dermal delivery of actives. Previously, we reported the effects of a range of vehicles on the delivery of niacinamide (NIA) using conventional Franz cell studies. In the present work, dermal delivery of NIA was investigated in vivo in human subjects using confocal Raman spectroscopy (CRS) and tape stripping (TS). The vehicles investigated included propylene glycol (PG), Transcutol<sup>®</sup> P (TC), binary combinations of PG with oleic acid (OA) or linolenic acid (LA) and a ternary system comprising of TC, caprylic/capric triglyceride (CCT) and dimethyl isosorbide (DMI). For the CRS studies, higher area under curve (AUC) values for NIA were observed for the PG:LA binary system compared with PG, TC and TC:CCT:DMI (<i>p</i> < 0.05). A very good correlation was found between the in vitro cumulative permeation of NIA and the AUC values from Raman intensity depth profiles, with a Pearson correlation coefficient (R<sup>2</sup>) of 0.84. In addition, an excellent correlation (R<sup>2</sup> = 0.97) was evident for the signal of the solvent PG and the active. CRS was also shown to discriminate between NIA in solution versus crystalline NIA. The findings confirm that CRS is emerging as a powerful approach for dermatopharmacokinetic studies of both actives and excipients in human.https://www.mdpi.com/1999-4923/13/5/726niacinamideskin permeationin vivoconfocal Raman spectroscopytape strippingin vitro-in vivo correlation |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Yanling Zhang Chin-Ping Kung Fotis Iliopoulos Bruno C. Sil Jonathan Hadgraft Majella E. Lane |
spellingShingle |
Yanling Zhang Chin-Ping Kung Fotis Iliopoulos Bruno C. Sil Jonathan Hadgraft Majella E. Lane Dermal Delivery of Niacinamide—In Vivo Studies Pharmaceutics niacinamide skin permeation in vivo confocal Raman spectroscopy tape stripping in vitro-in vivo correlation |
author_facet |
Yanling Zhang Chin-Ping Kung Fotis Iliopoulos Bruno C. Sil Jonathan Hadgraft Majella E. Lane |
author_sort |
Yanling Zhang |
title |
Dermal Delivery of Niacinamide—In Vivo Studies |
title_short |
Dermal Delivery of Niacinamide—In Vivo Studies |
title_full |
Dermal Delivery of Niacinamide—In Vivo Studies |
title_fullStr |
Dermal Delivery of Niacinamide—In Vivo Studies |
title_full_unstemmed |
Dermal Delivery of Niacinamide—In Vivo Studies |
title_sort |
dermal delivery of niacinamide—in vivo studies |
publisher |
MDPI AG |
series |
Pharmaceutics |
issn |
1999-4923 |
publishDate |
2021-05-01 |
description |
In vivo human studies are considered to be the “gold standard” when investigating (trans)dermal delivery of actives. Previously, we reported the effects of a range of vehicles on the delivery of niacinamide (NIA) using conventional Franz cell studies. In the present work, dermal delivery of NIA was investigated in vivo in human subjects using confocal Raman spectroscopy (CRS) and tape stripping (TS). The vehicles investigated included propylene glycol (PG), Transcutol<sup>®</sup> P (TC), binary combinations of PG with oleic acid (OA) or linolenic acid (LA) and a ternary system comprising of TC, caprylic/capric triglyceride (CCT) and dimethyl isosorbide (DMI). For the CRS studies, higher area under curve (AUC) values for NIA were observed for the PG:LA binary system compared with PG, TC and TC:CCT:DMI (<i>p</i> < 0.05). A very good correlation was found between the in vitro cumulative permeation of NIA and the AUC values from Raman intensity depth profiles, with a Pearson correlation coefficient (R<sup>2</sup>) of 0.84. In addition, an excellent correlation (R<sup>2</sup> = 0.97) was evident for the signal of the solvent PG and the active. CRS was also shown to discriminate between NIA in solution versus crystalline NIA. The findings confirm that CRS is emerging as a powerful approach for dermatopharmacokinetic studies of both actives and excipients in human. |
topic |
niacinamide skin permeation in vivo confocal Raman spectroscopy tape stripping in vitro-in vivo correlation |
url |
https://www.mdpi.com/1999-4923/13/5/726 |
work_keys_str_mv |
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1721415759193702400 |