Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities

Tao Wan,* Wenhui Pan,* Yueming Long, Kaiyue Yu, Sibo Liu, Wenyi Ruan, Jingtong Pan, Mengyao Qin, Chuanbin Wu, Yuehong Xu Department of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China *These authors contributed equally to thi...

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Autores principales: Wan T, Pan W, Long Y, Yu K, Liu S, Ruan W, Pan J, Qin M, Wu C, Xu Y
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Publicado: Dove Medical Press 2017
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spelling oai:doaj.org-article:581f40e577f74a40920d9773dad3eef22021-12-02T02:10:35ZEffects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities1178-2013https://doaj.org/article/581f40e577f74a40920d9773dad3eef22017-02-01T00:00:00Zhttps://www.dovepress.com/effects-of-nanoparticles-with-hydrotropic-nicotinamide-on-tacrolimus-p-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Tao Wan,* Wenhui Pan,* Yueming Long, Kaiyue Yu, Sibo Liu, Wenyi Ruan, Jingtong Pan, Mengyao Qin, Chuanbin Wu, Yuehong Xu Department of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China *These authors contributed equally to this work Abstract: The hybrid system based on nanoparticles (NPs) self-assembled by the conjugations of hyaluronic acid with cholesterol (HA–Chol NPs) combined with nicotinamide (NIC) for tacrolimus (FK506), ie, FK506 NPs–NIC, has been confirmed to exhibit a significant synergistic effect on FK506 permeation through and into intact skin; thus, it may be a promising approach for FK506 to effectively treat skin diseases. The aim of this study was to evaluate its potential for the treatment of psoriasis. In vitro permeation through the psoriatic skin was carried out, and the results revealed that the combination of NPs with NIC exhibited a significant synergistic effect on FK506 deposition within the psoriatic skin (3.40±0.67 µg/cm2) and penetration through the psoriatic skin (30.86±9.66 µg/cm2). The antipsoriatic activity of FK506 NPs–NIC was evaluated through the treatment for imiquimod (IMQ)-induced psoriasis. The psoriasis area and severity index (PASI) score demonstrated that FK506 HA–Chol NPs–NIC exerted the effect on ameliorating the skin lesions comparable to clobetasol propionate (a positive drug for psoriasis) and superior to commercial FK506 ointment (Protopic®), and the histological study showed that it presented a synergistic effect on antipsoriasis after FK506 incorporation into NPs combined with NIC hydrotropic system, which might ultimately increase the therapeutic effect and minimize the systemic side effects by reducing the overall dose of FK506. RAW 264.7 cell uptake presented the enhancement of drugs delivered into cells by HA–Chol NPs–NIC. The antiproliferative activity on HaCaT cells identified that FK506 HA–Chol NPs–NIC exhibited significant inhibiting effects on HaCaT proliferation. The results support that the combination of HA–Chol NPs with NIC is a promising approach for FK506 for the treatment of psoriasis. Keywords: tacrolimus, nanoparticles, nicotinamide, percutaneous delivery, psoriasis, antiproliferationWan TPan WLong YYu KLiu SRuan WPan JQin MWu CXu YDove Medical Pressarticletacrolimusnanoparticlesnicotinamidepercutaneous deliverypsoriasisanti-proliferationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 1485-1497 (2017)
institution DOAJ
collection DOAJ
language EN
topic tacrolimus
nanoparticles
nicotinamide
percutaneous delivery
psoriasis
anti-proliferation
Medicine (General)
R5-920
spellingShingle tacrolimus
nanoparticles
nicotinamide
percutaneous delivery
psoriasis
anti-proliferation
Medicine (General)
R5-920
Wan T
Pan W
Long Y
Yu K
Liu S
Ruan W
Pan J
Qin M
Wu C
Xu Y
Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
description Tao Wan,* Wenhui Pan,* Yueming Long, Kaiyue Yu, Sibo Liu, Wenyi Ruan, Jingtong Pan, Mengyao Qin, Chuanbin Wu, Yuehong Xu Department of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China *These authors contributed equally to this work Abstract: The hybrid system based on nanoparticles (NPs) self-assembled by the conjugations of hyaluronic acid with cholesterol (HA–Chol NPs) combined with nicotinamide (NIC) for tacrolimus (FK506), ie, FK506 NPs–NIC, has been confirmed to exhibit a significant synergistic effect on FK506 permeation through and into intact skin; thus, it may be a promising approach for FK506 to effectively treat skin diseases. The aim of this study was to evaluate its potential for the treatment of psoriasis. In vitro permeation through the psoriatic skin was carried out, and the results revealed that the combination of NPs with NIC exhibited a significant synergistic effect on FK506 deposition within the psoriatic skin (3.40±0.67 µg/cm2) and penetration through the psoriatic skin (30.86±9.66 µg/cm2). The antipsoriatic activity of FK506 NPs–NIC was evaluated through the treatment for imiquimod (IMQ)-induced psoriasis. The psoriasis area and severity index (PASI) score demonstrated that FK506 HA–Chol NPs–NIC exerted the effect on ameliorating the skin lesions comparable to clobetasol propionate (a positive drug for psoriasis) and superior to commercial FK506 ointment (Protopic®), and the histological study showed that it presented a synergistic effect on antipsoriasis after FK506 incorporation into NPs combined with NIC hydrotropic system, which might ultimately increase the therapeutic effect and minimize the systemic side effects by reducing the overall dose of FK506. RAW 264.7 cell uptake presented the enhancement of drugs delivered into cells by HA–Chol NPs–NIC. The antiproliferative activity on HaCaT cells identified that FK506 HA–Chol NPs–NIC exhibited significant inhibiting effects on HaCaT proliferation. The results support that the combination of HA–Chol NPs with NIC is a promising approach for FK506 for the treatment of psoriasis. Keywords: tacrolimus, nanoparticles, nicotinamide, percutaneous delivery, psoriasis, antiproliferation
format article
author Wan T
Pan W
Long Y
Yu K
Liu S
Ruan W
Pan J
Qin M
Wu C
Xu Y
author_facet Wan T
Pan W
Long Y
Yu K
Liu S
Ruan W
Pan J
Qin M
Wu C
Xu Y
author_sort Wan T
title Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
title_short Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
title_full Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
title_fullStr Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
title_full_unstemmed Effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
title_sort effects of nanoparticles with hydrotropic nicotinamide on tacrolimus: permeability through psoriatic skin and antipsoriatic and antiproliferative activities
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/581f40e577f74a40920d9773dad3eef2
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