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

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. Thi...

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Main Authors: Harun, Siti Norhawani, Amin Nordin, Syafinaz, Abd Gani, Siti Salwa, Shamsuddin, Ahmad Fuad, Basri, Mahiran, Basri, Hamidon
Format: Article
Language:English
Published: Dove Medical Press 2018
Online Access:http://psasir.upm.edu.my/id/eprint/72266/1/development-of-nanosystem-efficient-utilizing-emulsion-for-b_042618.pdf
http://psasir.upm.edu.my/id/eprint/72266/
https://www.dovepress.com/development-of-nanoemulsion-for-efficient-brain-parenteral-delivery-of-peer-reviewed-article-IJN
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spelling my.upm.eprints.722662020-04-27T06:23:55Z http://psasir.upm.edu.my/id/eprint/72266/ Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics Harun, Siti Norhawani Amin Nordin, Syafinaz Abd Gani, Siti Salwa Shamsuddin, Ahmad Fuad Basri, Mahiran Basri, Hamidon 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. Dove Medical Press 2018 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/72266/1/development-of-nanosystem-efficient-utilizing-emulsion-for-b_042618.pdf Harun, Siti Norhawani and Amin Nordin, Syafinaz and Abd Gani, Siti Salwa and Shamsuddin, Ahmad Fuad and Basri, Mahiran and Basri, Hamidon (2018) Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics. International Journal of Nanomedicine, 2018 (13). 2571 - 2584. ISSN 1176-9114; ESSN: 1178-2013 https://www.dovepress.com/development-of-nanoemulsion-for-efficient-brain-parenteral-delivery-of-peer-reviewed-article-IJN 10.2147/IJN.S151788
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description 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.
format Article
author Harun, Siti Norhawani
Amin Nordin, Syafinaz
Abd Gani, Siti Salwa
Shamsuddin, Ahmad Fuad
Basri, Mahiran
Basri, Hamidon
spellingShingle Harun, Siti Norhawani
Amin Nordin, Syafinaz
Abd Gani, Siti Salwa
Shamsuddin, Ahmad Fuad
Basri, Mahiran
Basri, Hamidon
Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
author_facet Harun, Siti Norhawani
Amin Nordin, Syafinaz
Abd Gani, Siti Salwa
Shamsuddin, Ahmad Fuad
Basri, Mahiran
Basri, Hamidon
author_sort Harun, Siti Norhawani
title Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
title_short Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
title_full Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
title_fullStr Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
title_full_unstemmed Development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
title_sort development of nanoemulsion for efficient brain parental delivery of cefuroxime: designs,characterizations,and pharmacokinetics
publisher Dove Medical Press
publishDate 2018
url http://psasir.upm.edu.my/id/eprint/72266/1/development-of-nanosystem-efficient-utilizing-emulsion-for-b_042618.pdf
http://psasir.upm.edu.my/id/eprint/72266/
https://www.dovepress.com/development-of-nanoemulsion-for-efficient-brain-parenteral-delivery-of-peer-reviewed-article-IJN
_version_ 1665895995086471168
score 13.211869

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