Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain
Delivering highly water soluble drugs across blood–brain barrier (BBB) is a crucial challenge for the formulation scientists. A successful therapeutic intervention by developing a suitable drug delivery system may revolutionize treatment across BBB. Efforts were given here to unravel the capability...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2018-01-01
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| Series: | Drug Delivery |
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| Online Access: | http://dx.doi.org/10.1080/10717544.2018.1435749 |
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| author | Lopamudra Dutta Biswajit Mukherjee Tapash Chakraborty Malay Kumar Das Laboni Mondal Sanchari Bhattacharya Raghuvir H. Gaonkar Mita Chatterjee Debnath |
| author_facet | Lopamudra Dutta Biswajit Mukherjee Tapash Chakraborty Malay Kumar Das Laboni Mondal Sanchari Bhattacharya Raghuvir H. Gaonkar Mita Chatterjee Debnath |
| author_sort | Lopamudra Dutta |
| collection | DOAJ |
| description | Delivering highly water soluble drugs across blood–brain barrier (BBB) is a crucial challenge for the formulation scientists. A successful therapeutic intervention by developing a suitable drug delivery system may revolutionize treatment across BBB. Efforts were given here to unravel the capability of a newly developed fatty acid combination (stearic acid:oleic acid:palmitic acid = 8.08:4.13:1) (ML) as fundamental component of nanocarrier to deliver highly water soluble zidovudine (AZT) as a model drug into brain across BBB. A comparison was made with an experimentally developed standard phospholipid-based nanocarrier containing AZT. Both the formulations had nanosize spherical unilamellar vesicular structure with highly negative zeta potential along with sustained drug release profiles. Gamma scintigraphic images showed both the radiolabeled formulations successfully crossed BBB, but longer retention in brain was observed for ML-based formulation (MGF) as compared to soya lecithin (SL)-based drug carrier (SYF). Plasma and brain pharmacokinetic data showed less clearance, prolonged residence time, more bioavailability and sustained release of AZT from MGF in rats compared to those data of the rats treated with SYF/AZT suspension. Thus, ML may be utilized to successfully develop drug nanocarrier to deliver drug into brain across BBB, in a sustained manner for a prolong period of time and may provide an effective therapeutic strategy for many diseases of brain. Further, many anti-HIV drugs cannot cross BBB sufficiently. Hence, the developed formulation may be a suitable option to carry those drugs into brain for better therapeutic management of HIV. |
| first_indexed | 2024-12-21T01:57:33Z |
| format | Article |
| id | doaj.art-e1aea8c07401492c83233eac03bc0506 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-21T01:57:33Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-e1aea8c07401492c83233eac03bc05062022-12-21T19:19:44ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642018-01-0125150451610.1080/10717544.2018.14357491435749Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brainLopamudra Dutta0Biswajit Mukherjee1Tapash Chakraborty2Malay Kumar Das3Laboni Mondal4Sanchari Bhattacharya5Raghuvir H. Gaonkar6Mita Chatterjee Debnath7Jadavpur UniversityJadavpur UniversityDibrugarh UniversityDibrugarh UniversityJadavpur UniversityJadavpur UniversityCSIR-Indian Institute of Chemical BiologyCSIR-Indian Institute of Chemical BiologyDelivering highly water soluble drugs across blood–brain barrier (BBB) is a crucial challenge for the formulation scientists. A successful therapeutic intervention by developing a suitable drug delivery system may revolutionize treatment across BBB. Efforts were given here to unravel the capability of a newly developed fatty acid combination (stearic acid:oleic acid:palmitic acid = 8.08:4.13:1) (ML) as fundamental component of nanocarrier to deliver highly water soluble zidovudine (AZT) as a model drug into brain across BBB. A comparison was made with an experimentally developed standard phospholipid-based nanocarrier containing AZT. Both the formulations had nanosize spherical unilamellar vesicular structure with highly negative zeta potential along with sustained drug release profiles. Gamma scintigraphic images showed both the radiolabeled formulations successfully crossed BBB, but longer retention in brain was observed for ML-based formulation (MGF) as compared to soya lecithin (SL)-based drug carrier (SYF). Plasma and brain pharmacokinetic data showed less clearance, prolonged residence time, more bioavailability and sustained release of AZT from MGF in rats compared to those data of the rats treated with SYF/AZT suspension. Thus, ML may be utilized to successfully develop drug nanocarrier to deliver drug into brain across BBB, in a sustained manner for a prolong period of time and may provide an effective therapeutic strategy for many diseases of brain. Further, many anti-HIV drugs cannot cross BBB sufficiently. Hence, the developed formulation may be a suitable option to carry those drugs into brain for better therapeutic management of HIV.http://dx.doi.org/10.1080/10717544.2018.1435749nanosize lipid carrierblood–brain barriergamma scintigraphypharmacokineticsbiodistribution |
| spellingShingle | Lopamudra Dutta Biswajit Mukherjee Tapash Chakraborty Malay Kumar Das Laboni Mondal Sanchari Bhattacharya Raghuvir H. Gaonkar Mita Chatterjee Debnath Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain Drug Delivery nanosize lipid carrier blood–brain barrier gamma scintigraphy pharmacokinetics biodistribution |
| title | Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain |
| title_full | Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain |
| title_fullStr | Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain |
| title_full_unstemmed | Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain |
| title_short | Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood–brain barrier into brain |
| title_sort | lipid based nanocarrier efficiently delivers highly water soluble drug across the blood brain barrier into brain |
| topic | nanosize lipid carrier blood–brain barrier gamma scintigraphy pharmacokinetics biodistribution |
| url | http://dx.doi.org/10.1080/10717544.2018.1435749 |
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