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Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal
Flurbiprofen (FLUR) is a potent non-steroidal anti-inflammatory drug used for the management of arthritis. Unfortunately, its therapeutic effect is limited by its rapid clearance from the joints following intra-articular injection. To improve its therapeutic efficacy, hyaluronic acid-coated bovine s...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778214/ https://www.ncbi.nlm.nih.gov/pubmed/35057036 http://dx.doi.org/10.3390/pharmaceutics14010140 |
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author | Mohamed, Hagar I. El-Kamel, Amal H. Hammad, Ghada O. Heikal, Lamia A. |
author_facet | Mohamed, Hagar I. El-Kamel, Amal H. Hammad, Ghada O. Heikal, Lamia A. |
author_sort | Mohamed, Hagar I. |
collection | PubMed |
description | Flurbiprofen (FLUR) is a potent non-steroidal anti-inflammatory drug used for the management of arthritis. Unfortunately, its therapeutic effect is limited by its rapid clearance from the joints following intra-articular injection. To improve its therapeutic efficacy, hyaluronic acid-coated bovine serum albumin nanoparticles (HA-BSA NPs) were formulated and loaded with FLUR to achieve active drug targeting. NPs were prepared by a modified nano-emulsification technique and their HA coating was proven via turbidimetric assay. Physicochemical characterization of the selected HA-BSA NPs revealed entrapment efficiency of 90.12 ± 1.06%, particle size of 257.12 ± 2.54 nm, PDI of 0.25 ± 0.01, and zeta potential of −48 ± 3 mv. The selected formulation showed in-vitro extended-release profile up to 6 days. In-vivo studies on adjuvant-induced arthritis rat model exhibited a significant reduction in joint swelling after intra-articular administration of FLUR-loaded HA-BSA NPs. Additionally, there was a significant reduction in CRP level in blood as well as TNF-α, and IL-6 levels in serum and joint tissues. Immunohistochemical study indicated a significant decrease in iNOS level in joint tissues. Histopathological analysis confirmed the safety of FLUR-loaded HA-BSA NPs. Thus, our results reveal that FLUR loaded HA-BSA NPs have a promising therapeutic effect in the management of arthritis. |
format | Online Article Text |
id | pubmed-8778214 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87782142022-01-22 Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal Mohamed, Hagar I. El-Kamel, Amal H. Hammad, Ghada O. Heikal, Lamia A. Pharmaceutics Article Flurbiprofen (FLUR) is a potent non-steroidal anti-inflammatory drug used for the management of arthritis. Unfortunately, its therapeutic effect is limited by its rapid clearance from the joints following intra-articular injection. To improve its therapeutic efficacy, hyaluronic acid-coated bovine serum albumin nanoparticles (HA-BSA NPs) were formulated and loaded with FLUR to achieve active drug targeting. NPs were prepared by a modified nano-emulsification technique and their HA coating was proven via turbidimetric assay. Physicochemical characterization of the selected HA-BSA NPs revealed entrapment efficiency of 90.12 ± 1.06%, particle size of 257.12 ± 2.54 nm, PDI of 0.25 ± 0.01, and zeta potential of −48 ± 3 mv. The selected formulation showed in-vitro extended-release profile up to 6 days. In-vivo studies on adjuvant-induced arthritis rat model exhibited a significant reduction in joint swelling after intra-articular administration of FLUR-loaded HA-BSA NPs. Additionally, there was a significant reduction in CRP level in blood as well as TNF-α, and IL-6 levels in serum and joint tissues. Immunohistochemical study indicated a significant decrease in iNOS level in joint tissues. Histopathological analysis confirmed the safety of FLUR-loaded HA-BSA NPs. Thus, our results reveal that FLUR loaded HA-BSA NPs have a promising therapeutic effect in the management of arthritis. MDPI 2022-01-07 /pmc/articles/PMC8778214/ /pubmed/35057036 http://dx.doi.org/10.3390/pharmaceutics14010140 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Mohamed, Hagar I. El-Kamel, Amal H. Hammad, Ghada O. Heikal, Lamia A. Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title | Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title_full | Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title_fullStr | Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title_full_unstemmed | Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title_short | Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal |
title_sort | design of targeted flurbiprofen biomimetic nanoparticles for management of arthritis: in vitro and in vivo appraisal |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778214/ https://www.ncbi.nlm.nih.gov/pubmed/35057036 http://dx.doi.org/10.3390/pharmaceutics14010140 |
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