A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects

Qi Li,1 Fen Chen,2 Yun Liu,1 Shihui Yu,1 Xiumei Gai,1 Mingzhu Ye,1 Xinggang Yang,1 Weisan Pan1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People’s Republic of China; 2Key Laboratory of Ministry of Education for TCM Viscera-State...

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Autores principales:	Li Q, Chen F, Liu Y, Yu S, Gai X, Ye M, Yang X, Pan W
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	Nanosuspensions inflammation targeting BSA meloxicam acid–base neutralization Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/85da7a09af36400bb8adc34b6a5a628f
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spelling	oai:doaj.org-article:85da7a09af36400bb8adc34b6a5a628f2021-12-02T05:58:09ZA novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects1178-2013https://doaj.org/article/85da7a09af36400bb8adc34b6a5a628f2018-08-01T00:00:00Zhttps://www.dovepress.com/a-novel-albumin-wrapped-nanosuspension-of-meloxicam-to-improve-inflamm-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Qi Li,1 Fen Chen,2 Yun Liu,1 Shihui Yu,1 Xiumei Gai,1 Mingzhu Ye,1 Xinggang Yang,1 Weisan Pan1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People’s Republic of China; 2Key Laboratory of Ministry of Education for TCM Viscera-State Theory and Applications, Liaoning University of Traditional Chinese Medicine, Shenyang 110016, People’s Republic of China Background: The objective of this study was to develop a more bio-available and safe nanosuspension of meloxicam (MX), which could dramatically improve inflammation targeting. Methods and results: MX-loaded bovine serum albumin (BSA) nanosuspensions were prepared using acid–base neutralization in aqueous solution and the prepared nanosuspensions were characterized. The results obtained showed that the prepared nanosuspensions had a narrow size distribution with a mean particle size of 78.67±0.22 nm, a polydispersity index of 0.133±0.01, and a zeta potential of -11.87±0.91 mV. The prepared MX nanosuspensions were spherically wrapped by BSA with a smooth surface as shown by transmission electron microscopy. Stability studies showed that the nanosuspensions were physically stable at 4°C with a shelf life of at least 6 months. In the in vitro dissolution test, the MX-loaded BSA nanosuspension (MX-BSA-NS) exhibited sustained release. In addition, an in vivo pharmacokinetic study in rats following intravenous injection showed that the half-life (t1/2), mean residence time (MRT), and area under the concentration–time curve (AUC0–∞) of MX-BSA-NS was increased by 169.83%, 150.13%, and 148.80%, respectively, in comparison with MX conventional solution (MX solution). Furthermore, results from inflammation targeting studies showed that the concentration of MX increased significantly in inflamed tissues but was reduced in normal tissues compared with the MX solution group after injection of MX-BSA-NS. Conclusion: The prepared MX-BSA-NS significantly increased the inflammation-targeting properties and bioavailability of MX, suggesting its potential as a promising formulation for the targeted drug delivery of MX in future clinical applications. Keywords: nanosuspensions, inflammation targeting, BSA, meloxicam, acid–base neutralizationLi QChen FLiu YYu SGai XYe MYang XPan WDove Medical PressarticleNanosuspensionsinflammation targetingBSAmeloxicamacid–base neutralizationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 4711-4725 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	Nanosuspensions inflammation targeting BSA meloxicam acid–base neutralization Medicine (General) R5-920
spellingShingle	Nanosuspensions inflammation targeting BSA meloxicam acid–base neutralization Medicine (General) R5-920 Li Q Chen F Liu Y Yu S Gai X Ye M Yang X Pan W A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
description	Qi Li,1 Fen Chen,2 Yun Liu,1 Shihui Yu,1 Xiumei Gai,1 Mingzhu Ye,1 Xinggang Yang,1 Weisan Pan1 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People’s Republic of China; 2Key Laboratory of Ministry of Education for TCM Viscera-State Theory and Applications, Liaoning University of Traditional Chinese Medicine, Shenyang 110016, People’s Republic of China Background: The objective of this study was to develop a more bio-available and safe nanosuspension of meloxicam (MX), which could dramatically improve inflammation targeting. Methods and results: MX-loaded bovine serum albumin (BSA) nanosuspensions were prepared using acid–base neutralization in aqueous solution and the prepared nanosuspensions were characterized. The results obtained showed that the prepared nanosuspensions had a narrow size distribution with a mean particle size of 78.67±0.22 nm, a polydispersity index of 0.133±0.01, and a zeta potential of -11.87±0.91 mV. The prepared MX nanosuspensions were spherically wrapped by BSA with a smooth surface as shown by transmission electron microscopy. Stability studies showed that the nanosuspensions were physically stable at 4°C with a shelf life of at least 6 months. In the in vitro dissolution test, the MX-loaded BSA nanosuspension (MX-BSA-NS) exhibited sustained release. In addition, an in vivo pharmacokinetic study in rats following intravenous injection showed that the half-life (t1/2), mean residence time (MRT), and area under the concentration–time curve (AUC0–∞) of MX-BSA-NS was increased by 169.83%, 150.13%, and 148.80%, respectively, in comparison with MX conventional solution (MX solution). Furthermore, results from inflammation targeting studies showed that the concentration of MX increased significantly in inflamed tissues but was reduced in normal tissues compared with the MX solution group after injection of MX-BSA-NS. Conclusion: The prepared MX-BSA-NS significantly increased the inflammation-targeting properties and bioavailability of MX, suggesting its potential as a promising formulation for the targeted drug delivery of MX in future clinical applications. Keywords: nanosuspensions, inflammation targeting, BSA, meloxicam, acid–base neutralization
format	article
author	Li Q Chen F Liu Y Yu S Gai X Ye M Yang X Pan W
author_facet	Li Q Chen F Liu Y Yu S Gai X Ye M Yang X Pan W
author_sort	Li Q
title	A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
title_short	A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
title_full	A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
title_fullStr	A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
title_full_unstemmed	A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
title_sort	novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/85da7a09af36400bb8adc34b6a5a628f
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A novel albumin wrapped nanosuspension of meloxicam to improve inflammation-targeting effects

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