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Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica

Heck, Rouven; Lukić, Milica; Savić, Snežana; Daniels, Rolf; Lunter, Dominique

(Elsevier Science BV, Amsterdam, 2017)

TY  - JOUR
AU  - Heck, Rouven
AU  - Lukić, Milica
AU  - Savić, Snežana
AU  - Daniels, Rolf
AU  - Lunter, Dominique
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2806
AB  - Aim: The purpose of this study was to evaluate skin permeation and penetration of nonivamide which has been formulated in novel film-forming formulations (FFFs). These formulations aim to prolong the availability of capsaicinoids which are used in long-term treatment of chronic pruritus. Methods: An oily solution of nonivamide was loaded into porous silica particles which then were suspended in an aqueous dispersion of a sustained release polymer. Permeation and penetration experiments were performed ex vivo with postauricular porcine skin using modified Franz diffusion cells. The penetrated drug amount was assessed ex vivo by skin surface biopsy followed by cryo-sectioning. Furthermore, in vivo skin irritation experiments were performed to compare the potential skin irritation caused by the FFFs to conventionally used semi-solid formulations. Results: Permeation rates of nonivamide from FFF through the skin are comparable to that from clinically used immediate release formulations. This elucidates the therapeutic safety profile of the novel FFF. Penetration studies confirmed the prolonged drug availability at the site of action. FFFs were found not to irritate the skin of healthy volunteers. Conclusion: FFFs with sustained nonivamide penetration represent safe and easy-to-use formulations. They therefore may improve the treatment of chronic pruritus with capsaicinoids by enhancing patient compliance through a sustained release regime.
PB  - Elsevier Science BV, Amsterdam
T2  - European Journal of Pharmaceutical Sciences
T1  - Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica
VL  - 106
SP  - 34
EP  - 40
DO  - 10.1016/j.ejps.2017.05.045
ER  - 
@article{
author = "Heck, Rouven and Lukić, Milica and Savić, Snežana and Daniels, Rolf and Lunter, Dominique",
year = "2017",
abstract = "Aim: The purpose of this study was to evaluate skin permeation and penetration of nonivamide which has been formulated in novel film-forming formulations (FFFs). These formulations aim to prolong the availability of capsaicinoids which are used in long-term treatment of chronic pruritus. Methods: An oily solution of nonivamide was loaded into porous silica particles which then were suspended in an aqueous dispersion of a sustained release polymer. Permeation and penetration experiments were performed ex vivo with postauricular porcine skin using modified Franz diffusion cells. The penetrated drug amount was assessed ex vivo by skin surface biopsy followed by cryo-sectioning. Furthermore, in vivo skin irritation experiments were performed to compare the potential skin irritation caused by the FFFs to conventionally used semi-solid formulations. Results: Permeation rates of nonivamide from FFF through the skin are comparable to that from clinically used immediate release formulations. This elucidates the therapeutic safety profile of the novel FFF. Penetration studies confirmed the prolonged drug availability at the site of action. FFFs were found not to irritate the skin of healthy volunteers. Conclusion: FFFs with sustained nonivamide penetration represent safe and easy-to-use formulations. They therefore may improve the treatment of chronic pruritus with capsaicinoids by enhancing patient compliance through a sustained release regime.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "European Journal of Pharmaceutical Sciences",
title = "Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica",
volume = "106",
pages = "34-40",
doi = "10.1016/j.ejps.2017.05.045"
}
Heck, R., Lukić, M., Savić, S., Daniels, R.,& Lunter, D.. (2017). Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica. in European Journal of Pharmaceutical Sciences
Elsevier Science BV, Amsterdam., 106, 34-40.
https://doi.org/10.1016/j.ejps.2017.05.045
Heck R, Lukić M, Savić S, Daniels R, Lunter D. Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica. in European Journal of Pharmaceutical Sciences. 2017;106:34-40.
doi:10.1016/j.ejps.2017.05.045 .
Heck, Rouven, Lukić, Milica, Savić, Snežana, Daniels, Rolf, Lunter, Dominique, "Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica" in European Journal of Pharmaceutical Sciences, 106 (2017):34-40,
https://doi.org/10.1016/j.ejps.2017.05.045 . .
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