Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics

Siti Norhawani Harun,1 Syafinaz Amin Nordin,2 Siti Salwa Abd Gani,3,4 Ahmad Fuad Shamsuddin,5,6 Mahiran Basri,7 Hamidon Bin Basri1 1Department of Medicine, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia; 2Department of Medical Microbiology and Parasitology, Fa...

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Autores principales:	Harun SN, Amin Nordin S, Abd Gani SS, Shamsuddin AF, Basri M, Bin Basri H
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	parenteral nanoemulsion cefuroxime drug delivery pharmacokinetics blood brain barrier Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/baab6717353e4706a4847618e709e628
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spelling	oai:doaj.org-article:baab6717353e4706a4847618e709e6282021-12-02T06:08:02ZDevelopment of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics1178-2013https://doaj.org/article/baab6717353e4706a4847618e709e6282018-04-01T00:00:00Zhttps://www.dovepress.com/development-of-nanoemulsion-for-efficient-brain-parenteral-delivery-of-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Siti Norhawani Harun,1 Syafinaz Amin Nordin,2 Siti Salwa Abd Gani,3,4 Ahmad Fuad Shamsuddin,5,6 Mahiran Basri,7 Hamidon Bin Basri1 1Department of Medicine, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia; 2Department of Medical Microbiology and Parasitology, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia; 3Department of Agriculture Technology, Faculty of Agriculture, Universiti Putra Malaysia, Serdang, Malaysia; 4Halal Products Research Institute, Universiti Putra Malaysia, Serdang, Malaysia; 5Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia; 6Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur Royal College of Medicine Perak, Ipoh, Malaysia; 7Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, Serdang, Malaysia Background and aim: Drugs that are effective against diseases in the central nervous system and reach the brain via blood must pass through the blood–brain barrier (BBB), a unique interface that protects against potential harmful molecules. This presents a major challenge in neuro-drug delivery. This study attempts to fabricate the cefuroxime-loaded nanoemulsion (CLN) to increase drug penetration into the brain when parenterally administered. Methods: The nanoemulsions were formulated using a high-pressure homogenization technique and were characterized for their physicochemical properties. Results: The characterizations revealed a particle size of 100.32±0.75 nm, polydispersity index of 0.18±0.01, zeta potential of -46.9±1.39 mV, viscosity of 1.24±0.34 cps, and osmolality of 285.33±0.58 mOsm/kg, indicating that the nanoemulsion has compatibility for parenteral application. CLN was physicochemically stable within 6 months of storage at 4°C, and the transmission electron microscopy revealed that the CLN droplets were almost spherical in shape. The in vitro release of CLN profile followed a sustained release pattern. The pharmacokinetic profile of CLN showed a significantly higher Cmax, area under the curve (AUC)0–t, prolonged half-life, and lower total plasma clearance, indicating that the systemic concentration of cefuroxime was higher in CLN-treated rats as compared to cefuroxime-free treated rats. A similar profile was obtained for the biodistribution of cefuroxime in the brain, in which CLN showed a significantly higher Cmax, AUC0–t, prolonged half-life, and lower clearance as compared to free cefuroxime solution. Conclusion: Overall, CLN showed excellent physicochemical properties, fulfilled the requirements for parenteral administration, and presented improved in vivo pharmacokinetic profile, which reflected its practical approach to enhance cefuroxime delivery to the brain. Keywords: parenteral nanoemulsion, cefuroxime, drug delivery, pharmacokinetics, blood–brain barrierHarun SNAmin Nordin SAbd Gani SSShamsuddin AFBasri MBin Basri HDove Medical Pressarticleparenteral nanoemulsioncefuroximedrug deliverypharmacokineticsblood brain barrierMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 2571-2584 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	parenteral nanoemulsion cefuroxime drug delivery pharmacokinetics blood brain barrier Medicine (General) R5-920
spellingShingle	parenteral nanoemulsion cefuroxime drug delivery pharmacokinetics blood brain barrier Medicine (General) R5-920 Harun SN Amin Nordin S Abd Gani SS Shamsuddin AF Basri M Bin Basri H Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
description	Siti Norhawani Harun,1 Syafinaz Amin Nordin,2 Siti Salwa Abd Gani,3,4 Ahmad Fuad Shamsuddin,5,6 Mahiran Basri,7 Hamidon Bin Basri1 1Department of Medicine, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia; 2Department of Medical Microbiology and Parasitology, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia; 3Department of Agriculture Technology, Faculty of Agriculture, Universiti Putra Malaysia, Serdang, Malaysia; 4Halal Products Research Institute, Universiti Putra Malaysia, Serdang, Malaysia; 5Centre for Drug Delivery Research, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia; 6Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur Royal College of Medicine Perak, Ipoh, Malaysia; 7Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, Serdang, Malaysia Background and aim: Drugs that are effective against diseases in the central nervous system and reach the brain via blood must pass through the blood–brain barrier (BBB), a unique interface that protects against potential harmful molecules. This presents a major challenge in neuro-drug delivery. This study attempts to fabricate the cefuroxime-loaded nanoemulsion (CLN) to increase drug penetration into the brain when parenterally administered. Methods: The nanoemulsions were formulated using a high-pressure homogenization technique and were characterized for their physicochemical properties. Results: The characterizations revealed a particle size of 100.32±0.75 nm, polydispersity index of 0.18±0.01, zeta potential of -46.9±1.39 mV, viscosity of 1.24±0.34 cps, and osmolality of 285.33±0.58 mOsm/kg, indicating that the nanoemulsion has compatibility for parenteral application. CLN was physicochemically stable within 6 months of storage at 4°C, and the transmission electron microscopy revealed that the CLN droplets were almost spherical in shape. The in vitro release of CLN profile followed a sustained release pattern. The pharmacokinetic profile of CLN showed a significantly higher Cmax, area under the curve (AUC)0–t, prolonged half-life, and lower total plasma clearance, indicating that the systemic concentration of cefuroxime was higher in CLN-treated rats as compared to cefuroxime-free treated rats. A similar profile was obtained for the biodistribution of cefuroxime in the brain, in which CLN showed a significantly higher Cmax, AUC0–t, prolonged half-life, and lower clearance as compared to free cefuroxime solution. Conclusion: Overall, CLN showed excellent physicochemical properties, fulfilled the requirements for parenteral administration, and presented improved in vivo pharmacokinetic profile, which reflected its practical approach to enhance cefuroxime delivery to the brain. Keywords: parenteral nanoemulsion, cefuroxime, drug delivery, pharmacokinetics, blood–brain barrier
format	article
author	Harun SN Amin Nordin S Abd Gani SS Shamsuddin AF Basri M Bin Basri H
author_facet	Harun SN Amin Nordin S Abd Gani SS Shamsuddin AF Basri M Bin Basri H
author_sort	Harun SN
title	Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
title_short	Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
title_full	Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
title_fullStr	Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
title_full_unstemmed	Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
title_sort	development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/baab6717353e4706a4847618e709e628
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Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics

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