Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles

Wesley Nyaigoti Omwoyo,1,2 Bernhards Ogutu,3,4 Florence Oloo,3,5 Hulda Swai,6 Lonji Kalombo,6 Paula Melariri,6 Geoffrey Maroa Mahanga,2 Jeremiah Waweru Gathirwa3,4 1Department of Chemistry, Maasai Mara University, Narok, Kenya; 2Department of Chemistry, Jaramogi Oginga Odinga University of Science...

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Autores principales:	Omwoyo WN, Ogutu B, Oloo F, Swai H, Kalombo L, Melariri P, Mahanga GM, Gathirwa JW
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/0a90906324344812ba41dbdc98cd6f96
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spelling	oai:doaj.org-article:0a90906324344812ba41dbdc98cd6f962021-12-02T07:37:03ZPreparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles1178-2013https://doaj.org/article/0a90906324344812ba41dbdc98cd6f962014-08-01T00:00:00Zhttp://www.dovepress.com/preparation-characterization-and-optimization-of-primaquine-loaded-sol-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Wesley Nyaigoti Omwoyo,1,2 Bernhards Ogutu,3,4 Florence Oloo,3,5 Hulda Swai,6 Lonji Kalombo,6 Paula Melariri,6 Geoffrey Maroa Mahanga,2 Jeremiah Waweru Gathirwa3,4 1Department of Chemistry, Maasai Mara University, Narok, Kenya; 2Department of Chemistry, Jaramogi Oginga Odinga University of Science and Technology, Bondo, Kenya; 3Center for Research in Therapeutic Sciences, Strathmore University, Nairobi, Kenya; 4Kenya Medical Research Institute, Nairobi, Kenya; 5Department of Chemical Sciences and Technology, Technical University of Kenya, Nairobi, Kenya; 6Department of Polymers and Composites, Council for Scientific and Industrial Research, Pretoria, South Africa Abstract: Primaquine (PQ) is one of the most widely used antimalarial drugs and is the only available drug that combats the relapsing form of malaria. PQ use in higher doses is limited by severe tissue toxicity including hematological- and gastrointestinal-related side effects. Nanoformulation of drugs in an appropriate drug carrier system has been extensively studied and shown to have the potential to improve bioavailability, thereby enhancing activity, reducing dose frequency, and subsequently reducing toxicity. The aim of this work was to design, synthesize, and characterize PQ-loaded solid lipid nanoparticles (SLNs) (PQ-SLNs) as a potential drug-delivery system. SLNs were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNs were 236 nm, +23 mV, 14%, and 75%, respectively. The zeta potential of the SLNs changed dramatically, from -6.54 mV to +23.0 mV, by binding positively charged chitosan as surface modifier. A spherical morphology of PQ-SLNs was seen by scanning electron microscope. In vitro, release profile depicted a steady drug release over 72 hours. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. Negligible changes in characteristic peaks of drug in Fourier transform infrared spectra indicated absence of any interaction among the various components entrapped in the nanoparticle formulation. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei-infected Swiss albino mice. This study demonstrated an efficient method of forming a nanomedicine delivery system for antimalarial drugs. Keywords: double emulsion, nanomedicine drug-delivery system, antimalarial, nanotechnologyOmwoyo WNOgutu BOloo FSwai HKalombo LMelariri PMahanga GMGathirwa JWDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 3865-3874 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Omwoyo WN Ogutu B Oloo F Swai H Kalombo L Melariri P Mahanga GM Gathirwa JW Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
description	Wesley Nyaigoti Omwoyo,1,2 Bernhards Ogutu,3,4 Florence Oloo,3,5 Hulda Swai,6 Lonji Kalombo,6 Paula Melariri,6 Geoffrey Maroa Mahanga,2 Jeremiah Waweru Gathirwa3,4 1Department of Chemistry, Maasai Mara University, Narok, Kenya; 2Department of Chemistry, Jaramogi Oginga Odinga University of Science and Technology, Bondo, Kenya; 3Center for Research in Therapeutic Sciences, Strathmore University, Nairobi, Kenya; 4Kenya Medical Research Institute, Nairobi, Kenya; 5Department of Chemical Sciences and Technology, Technical University of Kenya, Nairobi, Kenya; 6Department of Polymers and Composites, Council for Scientific and Industrial Research, Pretoria, South Africa Abstract: Primaquine (PQ) is one of the most widely used antimalarial drugs and is the only available drug that combats the relapsing form of malaria. PQ use in higher doses is limited by severe tissue toxicity including hematological- and gastrointestinal-related side effects. Nanoformulation of drugs in an appropriate drug carrier system has been extensively studied and shown to have the potential to improve bioavailability, thereby enhancing activity, reducing dose frequency, and subsequently reducing toxicity. The aim of this work was to design, synthesize, and characterize PQ-loaded solid lipid nanoparticles (SLNs) (PQ-SLNs) as a potential drug-delivery system. SLNs were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNs were 236 nm, +23 mV, 14%, and 75%, respectively. The zeta potential of the SLNs changed dramatically, from -6.54 mV to +23.0 mV, by binding positively charged chitosan as surface modifier. A spherical morphology of PQ-SLNs was seen by scanning electron microscope. In vitro, release profile depicted a steady drug release over 72 hours. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. Negligible changes in characteristic peaks of drug in Fourier transform infrared spectra indicated absence of any interaction among the various components entrapped in the nanoparticle formulation. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei-infected Swiss albino mice. This study demonstrated an efficient method of forming a nanomedicine delivery system for antimalarial drugs. Keywords: double emulsion, nanomedicine drug-delivery system, antimalarial, nanotechnology
format	article
author	Omwoyo WN Ogutu B Oloo F Swai H Kalombo L Melariri P Mahanga GM Gathirwa JW
author_facet	Omwoyo WN Ogutu B Oloo F Swai H Kalombo L Melariri P Mahanga GM Gathirwa JW
author_sort	Omwoyo WN
title	Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
title_short	Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
title_full	Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
title_fullStr	Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
title_full_unstemmed	Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
title_sort	preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/0a90906324344812ba41dbdc98cd6f96
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Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles

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