Solidified reverse micellar solution-based chitosan-coated solid lipid nanoparticles as a new approach to enhance oral delivery of artemether in malaria treatment
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
Affiliations
Franklin Chimaobi Kenechukwu
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Kingsley Chinazam Ugwu
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Chibuzor Stanley Offorbuike
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Enyi Moses Ojukwu
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Thaddeus Harrison Gugu
Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, University of Nigeria
Reuben Ejike Eze
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Chinazom Precious Agbo
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Mumuni Audu Momoh
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Anthony Ikechukwu Onah
Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmaceutical Sciences, David Umahi Federal, University of Health Sciences
Chinekwu Sherridan Nwagwu
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Onyinyechi Lydia Ugorji
Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria
Emmanuel Chekwube Ossai
Department of Biochemistry, Faculty of Biological Sciences, University of Nigeria
Calister Elochukwu Ugwu
Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria
Paul Achile Akpa
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Adaeze Chidiebere Echezona
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Samuel WisdomofGod Uzondu
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
Chimaobi Odinaka Ugorji
Department of Science Laboratory Technology, Faculty of Physical Sciences, University of Nigeria
Wilfred Ikechukwu Ugwuoke
Department of Veterinary Anatomy and Microbiology, Faculty of Veterinary Medicine, University of Nigeria
Teerapol Srichana
Drug Delivery System Excellence Center (DDSEC), Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University
Anthony Amaechi Attama
Drug Delivery and Nanomedicines Research Laboratory, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria
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.
