Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment
Abstract Solidified reverse micellar technology and surface-modification are promising techniques for improving the biopharmaceutical properties of poorly water-soluble drugs such as artemether, a first-line antimalarial drug. Thus, the aim of this study was to develop and evaluate artemether-loaded...
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2025-03-01
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| Online Access: | https://doi.org/10.1186/s13065-025-01422-4 |
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| author | Franklin Chimaobi Kenechukwu Kingsley Chinazam Ugwu Chibuzor Stanley Offorbuike Enyi Moses Ojukwu Thaddeus Harrison Gugu Reuben Ejike Eze Chinazom Precious Agbo Mumuni Audu Momoh Anthony Ikechukwu Onah Chinekwu Sherridan Nwagwu Onyinyechi Lydia Ugorji Emmanuel Chekwube Ossai Calister Elochukwu Ugwu Paul Achile Akpa Adaeze Chidiebere Echezona Samuel WisdomofGod Uzondu Chimaobi Odinaka Ugorji Wilfred Ikechukwu Ugwuoke Teerapol Srichana Anthony Amaechi Attama |
| author_facet | Franklin Chimaobi Kenechukwu Kingsley Chinazam Ugwu Chibuzor Stanley Offorbuike Enyi Moses Ojukwu Thaddeus Harrison Gugu Reuben Ejike Eze Chinazom Precious Agbo Mumuni Audu Momoh Anthony Ikechukwu Onah Chinekwu Sherridan Nwagwu Onyinyechi Lydia Ugorji Emmanuel Chekwube Ossai Calister Elochukwu Ugwu Paul Achile Akpa Adaeze Chidiebere Echezona Samuel WisdomofGod Uzondu Chimaobi Odinaka Ugorji Wilfred Ikechukwu Ugwuoke Teerapol Srichana Anthony Amaechi Attama |
| author_sort | Franklin Chimaobi Kenechukwu |
| collection | DOAJ |
| description | Abstract Solidified reverse micellar technology and surface-modification are promising techniques for improving the biopharmaceutical properties of poorly water-soluble drugs such as artemether, a first-line antimalarial drug. Thus, the aim of this study was to develop and evaluate artemether-loaded chitosan-coated solid lipid nanoparticles (SLNs) based on solidified reverse micellar solution (SRMS) for improved oral malaria therapy. Artemether-loaded and unloaded SLNs were prepared from optimized SRMS (consisting of Phospholipon® 90G and Compritol® ATO 888 at 3:7 ratio) with or without chitosan by high-shear melt-homogenization, and thereafter characterized for physicochemical performance, stability, safety and antimalarial activity using Plasmodium berghei-infected mice. Results showed both smooth and irregular particles with a layer of polymer coating in chitosan-modified SLNs, increased drug amorphization as well as compatibility of the drug and excipients employed in the formulations. The optimized formulation was stable and nanomeric (size 292.90 ± 5.01 nm, polydispersity index 0.191 ± 0.09, and zeta-potential + 32.50 ± 1.58 mV) with good encapsulation efficiency (82.03%), demonstrated minimal toxicity on Caco-2 cells, exhibited controlled drug release compared with fast release of artemether suspension and gave significantly (p < 0.05) greater antimalarial activity than artemether suspension. Artemether-loaded chitosan-coated SRMS-based SLNs improved the antimalarial activity of the drug and can be pursued as a novel alternative for improved oral malaria treatment. |
| format | Article |
| id | doaj-art-2aec4bbfd65b4e48be2f466c7cde75f0 |
| institution | DOAJ |
| issn | 2661-801X |
| language | English |
| publishDate | 2025-03-01 |
| publisher | BMC |
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| series | BMC Chemistry |
| spelling | doaj-art-2aec4bbfd65b4e48be2f466c7cde75f02025-08-20T03:05:50ZengBMCBMC Chemistry2661-801X2025-03-0119112510.1186/s13065-025-01422-4Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatmentFranklin Chimaobi Kenechukwu0Kingsley Chinazam Ugwu1Chibuzor Stanley Offorbuike2Enyi Moses Ojukwu3Thaddeus Harrison Gugu4Reuben Ejike Eze5Chinazom Precious Agbo6Mumuni Audu Momoh7Anthony Ikechukwu Onah8Chinekwu Sherridan Nwagwu9Onyinyechi Lydia Ugorji10Emmanuel Chekwube Ossai11Calister Elochukwu Ugwu12Paul Achile Akpa13Adaeze Chidiebere Echezona14Samuel WisdomofGod Uzondu15Chimaobi Odinaka Ugorji16Wilfred Ikechukwu Ugwuoke17Teerapol Srichana18Anthony Amaechi Attama19Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDepartment of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDepartment of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, David Umahi Federal, University of Health SciencesDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDepartment of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of NigeriaDepartment of Biochemistry, Faculty of Biological Sciences, University of NigeriaDepartment of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaDepartment of Science Laboratory Technology, Faculty of Physical Sciences, University of NigeriaDepartment of Veterinary Anatomy and Microbiology, Faculty of Veterinary Medicine, University of NigeriaDrug Delivery System Excellence Center (DDSEC), Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla UniversityDrug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of NigeriaAbstract Solidified reverse micellar technology and surface-modification are promising techniques for improving the biopharmaceutical properties of poorly water-soluble drugs such as artemether, a first-line antimalarial drug. Thus, the aim of this study was to develop and evaluate artemether-loaded chitosan-coated solid lipid nanoparticles (SLNs) based on solidified reverse micellar solution (SRMS) for improved oral malaria therapy. Artemether-loaded and unloaded SLNs were prepared from optimized SRMS (consisting of Phospholipon® 90G and Compritol® ATO 888 at 3:7 ratio) with or without chitosan by high-shear melt-homogenization, and thereafter characterized for physicochemical performance, stability, safety and antimalarial activity using Plasmodium berghei-infected mice. Results showed both smooth and irregular particles with a layer of polymer coating in chitosan-modified SLNs, increased drug amorphization as well as compatibility of the drug and excipients employed in the formulations. The optimized formulation was stable and nanomeric (size 292.90 ± 5.01 nm, polydispersity index 0.191 ± 0.09, and zeta-potential + 32.50 ± 1.58 mV) with good encapsulation efficiency (82.03%), demonstrated minimal toxicity on Caco-2 cells, exhibited controlled drug release compared with fast release of artemether suspension and gave significantly (p < 0.05) greater antimalarial activity than artemether suspension. Artemether-loaded chitosan-coated SRMS-based SLNs improved the antimalarial activity of the drug and can be pursued as a novel alternative for improved oral malaria treatment.https://doi.org/10.1186/s13065-025-01422-4Solidified reverse micellar solutionAntimalarial activityChitosanSolid lipid nanoparticlesArtemetherPlasmodium berghei |
| spellingShingle | Franklin Chimaobi Kenechukwu Kingsley Chinazam Ugwu Chibuzor Stanley Offorbuike Enyi Moses Ojukwu Thaddeus Harrison Gugu Reuben Ejike Eze Chinazom Precious Agbo Mumuni Audu Momoh Anthony Ikechukwu Onah Chinekwu Sherridan Nwagwu Onyinyechi Lydia Ugorji Emmanuel Chekwube Ossai Calister Elochukwu Ugwu Paul Achile Akpa Adaeze Chidiebere Echezona Samuel WisdomofGod Uzondu Chimaobi Odinaka Ugorji Wilfred Ikechukwu Ugwuoke Teerapol Srichana Anthony Amaechi Attama Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment BMC Chemistry Solidified reverse micellar solution Antimalarial activity Chitosan Solid lipid nanoparticles Artemether Plasmodium berghei |
| title | Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| title_full | Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| title_fullStr | Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| title_full_unstemmed | Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| title_short | Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| title_sort | solidified reverse micellar solution based chitosan coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment |
| topic | Solidified reverse micellar solution Antimalarial activity Chitosan Solid lipid nanoparticles Artemether Plasmodium berghei |
| url | https://doi.org/10.1186/s13065-025-01422-4 |
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