Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles
Laiba Arshad,1 Ibrahim Jantan,2 Syed Nasir Abbas Bukhari31Department of Pharmacy, Forman Christian College (A Chartered University), Lahore, Pakistan; 2School of Pharmacy, Faculty of Health and Medical Sciences, Taylor’s University, Subang Jaya, Selangor, Malaysia; 3Department of Pharmaceu...
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2019-04-01
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| Series: | Drug Design, Development and Therapy |
| Subjects: | |
| Online Access: | https://www.dovepress.com/enhanced-immunosuppressive-effects-of-35-bis4diethoxymethylbenzylidene-peer-reviewed-article-DDDT |
| _version_ | 1818082661180112896 |
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| author | Arshad L Jantan I Bukhari SNA |
| author_facet | Arshad L Jantan I Bukhari SNA |
| author_sort | Arshad L |
| collection | DOAJ |
| description | Laiba Arshad,1 Ibrahim Jantan,2 Syed Nasir Abbas Bukhari31Department of Pharmacy, Forman Christian College (A Chartered University), Lahore, Pakistan; 2School of Pharmacy, Faculty of Health and Medical Sciences, Taylor’s University, Subang Jaya, Selangor, Malaysia; 3Department of Pharmaceutical Chemistry, College of Pharmacy, Al Jouf University, Aljouf, Sakaka, Saudi ArabiaBackground: 3,5-Bis[4-(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one (BBP), a novel synthetic curcumin analogue has been revealed to possess strong in vitro and in vivo immunosuppressive effects.Purpose: The aim of present study was to prepare and characterize BBP-encapsulated polylactic-co-glycolic acid-block-polyethylene glycol (PLGA-b-PEG) nanoparticles and to evaluate its in vivo efficacy against innate and adaptive immune responses.Methods: Male BALB/c mice were orally administered with BBP alone and BBP- encapsulated nanoparticles equivalent to 5, 10 and 20 mg/kg of BBP in distilled water for a period of 14 days. The immunomodulatory potential was appraised by determining its effects on non-specific and specific immune parameters.Results: The results showed that BBP was successfully encapsulated in PLGA-b-PEG polymer with 154.3 nm size and high encapsulation efficiency (79%) while providing a sustained release for 48 hours. BBP nanoparticles showed significant enhanced dose-dependent reduction on the migration of neutrophils, Mac-1 expression, phagocytic activity, reactive oxygen species (ROS) production, serum levels of ceruloplasmin and lysozyme, immunoglobulins and myloperoxidase (MPO) plasma levels when compared to unencapsulated BBP. Enhanced dose-dependent inhibition was also observed on lymphocyte proliferation along with the downregulation of effector cells expression and release of cytokines, and reduction in rat paw oedema in BBP nanoparticles treated mice. At higher doses the suppressive effects of the BBP nanoparticles on various cellular and humoral parameters of immune responses were comparable to that of cyclosporine-A at 20 mg/kg.Conclusion: These findings suggest that the immunosuppressive effects of BBP were enhanced as PLGA-b-PEG nanoparticles.Keywords: αβ-unsaturated carbonyl-based compound, curcumin analogue, PLGA-b-PEG nanoparticles, immunosuppression, innate immune response, humoral immune response |
| first_indexed | 2024-12-10T19:25:39Z |
| format | Article |
| id | doaj.art-4621dc3d28454165b5703d559666fe7b |
| institution | Directory Open Access Journal |
| issn | 1177-8881 |
| language | English |
| last_indexed | 2024-12-10T19:25:39Z |
| publishDate | 2019-04-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | Drug Design, Development and Therapy |
| spelling | doaj.art-4621dc3d28454165b5703d559666fe7b2022-12-22T01:36:23ZengDove Medical PressDrug Design, Development and Therapy1177-88812019-04-01Volume 131421143645461Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticlesArshad LJantan IBukhari SNALaiba Arshad,1 Ibrahim Jantan,2 Syed Nasir Abbas Bukhari31Department of Pharmacy, Forman Christian College (A Chartered University), Lahore, Pakistan; 2School of Pharmacy, Faculty of Health and Medical Sciences, Taylor’s University, Subang Jaya, Selangor, Malaysia; 3Department of Pharmaceutical Chemistry, College of Pharmacy, Al Jouf University, Aljouf, Sakaka, Saudi ArabiaBackground: 3,5-Bis[4-(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one (BBP), a novel synthetic curcumin analogue has been revealed to possess strong in vitro and in vivo immunosuppressive effects.Purpose: The aim of present study was to prepare and characterize BBP-encapsulated polylactic-co-glycolic acid-block-polyethylene glycol (PLGA-b-PEG) nanoparticles and to evaluate its in vivo efficacy against innate and adaptive immune responses.Methods: Male BALB/c mice were orally administered with BBP alone and BBP- encapsulated nanoparticles equivalent to 5, 10 and 20 mg/kg of BBP in distilled water for a period of 14 days. The immunomodulatory potential was appraised by determining its effects on non-specific and specific immune parameters.Results: The results showed that BBP was successfully encapsulated in PLGA-b-PEG polymer with 154.3 nm size and high encapsulation efficiency (79%) while providing a sustained release for 48 hours. BBP nanoparticles showed significant enhanced dose-dependent reduction on the migration of neutrophils, Mac-1 expression, phagocytic activity, reactive oxygen species (ROS) production, serum levels of ceruloplasmin and lysozyme, immunoglobulins and myloperoxidase (MPO) plasma levels when compared to unencapsulated BBP. Enhanced dose-dependent inhibition was also observed on lymphocyte proliferation along with the downregulation of effector cells expression and release of cytokines, and reduction in rat paw oedema in BBP nanoparticles treated mice. At higher doses the suppressive effects of the BBP nanoparticles on various cellular and humoral parameters of immune responses were comparable to that of cyclosporine-A at 20 mg/kg.Conclusion: These findings suggest that the immunosuppressive effects of BBP were enhanced as PLGA-b-PEG nanoparticles.Keywords: αβ-unsaturated carbonyl-based compound, curcumin analogue, PLGA-b-PEG nanoparticles, immunosuppression, innate immune response, humoral immune responsehttps://www.dovepress.com/enhanced-immunosuppressive-effects-of-35-bis4diethoxymethylbenzylidene-peer-reviewed-article-DDDTαβ-Unsaturated carbonyl-based compoundcurcumin analoguePLGA-b-PEG nanoparticlesimmunosuppressioninnate immune responsehumoral immune response |
| spellingShingle | Arshad L Jantan I Bukhari SNA Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles Drug Design, Development and Therapy α β-Unsaturated carbonyl-based compound curcumin analogue PLGA-b-PEG nanoparticles immunosuppression innate immune response humoral immune response |
| title | Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles |
| title_full | Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles |
| title_fullStr | Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles |
| title_full_unstemmed | Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles |
| title_short | Enhanced immunosuppressive effects of 3,5-bis[4(diethoxymethyl)benzylidene]-1-methyl-piperidin-4-one, an α, β-unsaturated carbonyl-based compound as PLGA-b-PEG nanoparticles |
| title_sort | enhanced immunosuppressive effects of 3 5 bis 4 diethoxymethyl benzylidene 1 methyl piperidin 4 one an alpha beta unsaturated carbonyl based compound as plga b peg nanoparticles |
| topic | α β-Unsaturated carbonyl-based compound curcumin analogue PLGA-b-PEG nanoparticles immunosuppression innate immune response humoral immune response |
| url | https://www.dovepress.com/enhanced-immunosuppressive-effects-of-35-bis4diethoxymethylbenzylidene-peer-reviewed-article-DDDT |
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