Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema

Shanshan Gao, Baocheng Tian, Jingtian Han, Jing Zhang, Yanan Shi, Qingzhi Lv, Keke LiSchool of Pharmacy, Binzhou Medical University, Yantai, People’s Republic of chinaBackground: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The...

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Autores principales:	Gao S, Tian B, Han J, Zhang J, Shi Y, Lv Q, Li K
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	lornoxicam nanostructured lipid carriers cell penetrating peptides transdermal drug delivery anti-inflammatory effect Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/43f66d4ae47b4655b175258a649fae1d
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spelling	oai:doaj.org-article:43f66d4ae47b4655b175258a649fae1d2021-12-02T04:51:21ZEnhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema1178-2013https://doaj.org/article/43f66d4ae47b4655b175258a649fae1d2019-08-01T00:00:00Zhttps://www.dovepress.com/enhanced-transdermal-delivery-of-lornoxicam-by-nanostructured-lipid-ca-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Shanshan Gao, Baocheng Tian, Jingtian Han, Jing Zhang, Yanan Shi, Qingzhi Lv, Keke LiSchool of Pharmacy, Binzhou Medical University, Yantai, People’s Republic of chinaBackground: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs.Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect.Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs.Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs (P<0.05 or P<0.01). An in vitro skin permeation study showed better permeation-enhancing ability of R11 (0.02%, w/w) than that of other content (0.01% or 0.04%). In carrageenan-induced rat paw edema models, LN-NLC-R11 gels inhibited rat paw edema and the production of inflammatory cytokines compared with LN-NLC gels and LN gels (P<0.01).Conclusion: In our investigation, it was strongly demonstrated that the surface modification of NLC with R11 enhanced the translocation of LN across the skin, thereby alleviating inflammation.Keywords: lornoxicam, nanostructured lipid carriers, cell penetrating peptides, transdermal drug delivery, anti-inflammatory effectGao STian BHan JZhang JShi YLv QLi KDove Medical Pressarticlelornoxicamnanostructured lipid carrierscell penetrating peptidestransdermal drug deliveryanti-inflammatory effectMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 6135-6150 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	lornoxicam nanostructured lipid carriers cell penetrating peptides transdermal drug delivery anti-inflammatory effect Medicine (General) R5-920
spellingShingle	lornoxicam nanostructured lipid carriers cell penetrating peptides transdermal drug delivery anti-inflammatory effect Medicine (General) R5-920 Gao S Tian B Han J Zhang J Shi Y Lv Q Li K Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
description	Shanshan Gao, Baocheng Tian, Jingtian Han, Jing Zhang, Yanan Shi, Qingzhi Lv, Keke LiSchool of Pharmacy, Binzhou Medical University, Yantai, People’s Republic of chinaBackground: Nanostructured lipid carriers (NLCs) are emerging as attractive drug carriers in transdermal drug delivery. The surface modification of NLCs with cell-penetrating peptides (CPPs) can enhance the skin permeation of drugs.Purpose: The objective of the current study was to evaluate the ability of the cell-penetrating peptide (CPP) polyarginine to translocate NLCs loaded with lornoxicam (LN) into the skin layers and to evaluate its anti-inflammatory effect.Methods: The NLCs were prepared using an emulsion evaporation and low temperature solidification technique using glyceryl monostearates, triglycerides, DOGS-NTA-Ni lipids and surfactants, and then six histidine-tagged polyarginine containing 11 arginine (R11) peptides was modified on the surface of NLCs.Results: The developed NLCs formulated with LN and R11 (LN-NLC-R11) were incorporated into 2% HPMC gels. NLCs were prepared with a particle size of (121.81±3.61)–(145.72±4.78) nm, and the zeta potential decreased from (−30.30±2.07) to (−14.66±0.74) mV after the modification of R11 peptides. The encapsulation efficiency and drug loading were (74.61±1.13) % and (7.92±0.33) %, respectively, regardless of the surface modification. Cellular uptake assays using HaCaT cells suggested that the NLC modified with R11 (0.02%, w/w) significantly enhanced the cell internalization of nanoparticles relative to unmodified NLCs (P<0.05 or P<0.01). An in vitro skin permeation study showed better permeation-enhancing ability of R11 (0.02%, w/w) than that of other content (0.01% or 0.04%). In carrageenan-induced rat paw edema models, LN-NLC-R11 gels inhibited rat paw edema and the production of inflammatory cytokines compared with LN-NLC gels and LN gels (P<0.01).Conclusion: In our investigation, it was strongly demonstrated that the surface modification of NLC with R11 enhanced the translocation of LN across the skin, thereby alleviating inflammation.Keywords: lornoxicam, nanostructured lipid carriers, cell penetrating peptides, transdermal drug delivery, anti-inflammatory effect
format	article
author	Gao S Tian B Han J Zhang J Shi Y Lv Q Li K
author_facet	Gao S Tian B Han J Zhang J Shi Y Lv Q Li K
author_sort	Gao S
title	Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
title_short	Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
title_full	Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
title_fullStr	Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
title_full_unstemmed	Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
title_sort	enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/43f66d4ae47b4655b175258a649fae1d
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Enhanced transdermal delivery of lornoxicam by nanostructured lipid carrier gels modified with polyarginine peptide for treatment of carrageenan-induced rat paw edema

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