Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity
Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. Howev...
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| Format: | Article |
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MDPI AG
2023-10-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/20/7115 |
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| author | Burcu Uner Ahmet Dogan Ergin Irfan Aamer Ansari Melahat Sedanur Macit-Celebi Siddique Akber Ansari Hamad M. Al Kahtani |
| author_facet | Burcu Uner Ahmet Dogan Ergin Irfan Aamer Ansari Melahat Sedanur Macit-Celebi Siddique Akber Ansari Hamad M. Al Kahtani |
| author_sort | Burcu Uner |
| collection | DOAJ |
| description | Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC’s high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer<sup>®</sup> 407 (surfactant), Compritol<sup>®</sup> 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations’ effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (<i>p</i> < 0.05). |
| first_indexed | 2024-03-10T21:00:39Z |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T21:00:39Z |
| publishDate | 2023-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-671468794e5a4e4a859a7dd1b4ca161f2023-11-19T17:32:58ZengMDPI AGMolecules1420-30492023-10-012820711510.3390/molecules28207115Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating ObesityBurcu Uner0Ahmet Dogan Ergin1Irfan Aamer Ansari2Melahat Sedanur Macit-Celebi3Siddique Akber Ansari4Hamad M. Al Kahtani5Department of Administrative and Pharmaceutical Sciences, University of Health Science and Pharmacy in St. Louis, St. Louis, MO 63110, USADepartment of Pharmaceutical Technology, Faculty of Pharmacy, Trakya University, 22030 Edirne, TurkeyDepartment of Drug Science and Technology, University of Turin, 10124 Turin, ItalyDepartment of Nutrition and Dietetics, Faculty of Health Sciences, Ondokuz Mayıs University, 55270 Samsun, TurkeyDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaAddressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC’s high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer<sup>®</sup> 407 (surfactant), Compritol<sup>®</sup> 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations’ effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (<i>p</i> < 0.05).https://www.mdpi.com/1420-3049/28/20/7115NLCcarnitineobesitycell cultureopen-field test |
| spellingShingle | Burcu Uner Ahmet Dogan Ergin Irfan Aamer Ansari Melahat Sedanur Macit-Celebi Siddique Akber Ansari Hamad M. Al Kahtani Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity Molecules NLC carnitine obesity cell culture open-field test |
| title | Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity |
| title_full | Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity |
| title_fullStr | Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity |
| title_full_unstemmed | Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity |
| title_short | Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity |
| title_sort | assessing the in vitro and in vivo performance of l carnitine loaded nanoparticles in combating obesity |
| topic | NLC carnitine obesity cell culture open-field test |
| url | https://www.mdpi.com/1420-3049/28/20/7115 |
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