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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| Format: | Article |
| Language: | English |
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Dove Medical Press
2018
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| Online Access: | http://psasir.upm.edu.my/id/eprint/72266/1/development-of-nanosystem-efficient-utilizing-emulsion-for-b_042618.pdf |
| _version_ | 1825950056209973248 |
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| author | Harun, Siti Norhawani Amin Nordin, Syafinaz Abd Gani, Siti Salwa Shamsuddin, Ahmad Fuad Basri, Mahiran Basri, Hamidon |
| author_facet | Harun, Siti Norhawani Amin Nordin, Syafinaz Abd Gani, Siti Salwa Shamsuddin, Ahmad Fuad Basri, Mahiran Basri, Hamidon |
| author_sort | Harun, Siti Norhawani |
| collection | UPM |
| 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. |
| first_indexed | 2024-03-06T10:08:46Z |
| format | Article |
| id | upm.eprints-72266 |
| institution | Universiti Putra Malaysia |
| language | English |
| last_indexed | 2024-03-06T10:08:46Z |
| publishDate | 2018 |
| publisher | Dove Medical Press |
| record_format | dspace |
| spelling | 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 |
| 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 |
| title | 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_short | 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 |
| url | http://psasir.upm.edu.my/id/eprint/72266/1/development-of-nanosystem-efficient-utilizing-emulsion-for-b_042618.pdf |
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