Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers
The oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit®L100-55 (Eu-NLCs)...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Drug Delivery |
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| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1785050 |
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| author | Pataranapa Nimtrakul Pakawadee Sermsappasuk Waree Tiyaboonchai |
| author_facet | Pataranapa Nimtrakul Pakawadee Sermsappasuk Waree Tiyaboonchai |
| author_sort | Pataranapa Nimtrakul |
| collection | DOAJ |
| description | The oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit®L100-55 (Eu-NLCs) for the oral delivery of AmB. This study aimed to compare their ability in protecting the drug from degradation in gastrointestinal fluids and permeation enhancement in Caco-2 cells. Uncoated NLCs and Eu-NLCs possessed a mean particle size of ∼180 and ∼550 nm, with a zeta potential of ∼−30 and ∼−50 mV, respectively. Both NLCs demonstrated an AmB entrapment efficiency up to ∼75%. They possessed significantly greater AmB water solubility than the free drug by up to 10-fold. In fasted state simulated gastric fluid, Eu-NLCs provided significantly greater AmB protection from acidic degradation than uncoated NLCs. In fasted state simulated intestinal fluid, both uncoated and Eu-NLCs showed a fast release characteristic. Caco-2 cells permeation studies revealed that uncoated NLCs provided significantly higher apparent permeation coefficient (Papp) value than Eu-NLCs. Moreover, after 6 months of storage at 4 °C in the absence of light, the physicochemical stabilities of the lyophilized uncoated and Eu-NLCs could be maintained. In conclusion, the developed NLCs and Eu-NLCs could be a potential drug delivery system in improving the oral bioavailability of AmB. |
| first_indexed | 2024-12-14T17:44:58Z |
| format | Article |
| id | doaj.art-64efaf4d5e524e93b437b763a07e6def |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-14T17:44:58Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-64efaf4d5e524e93b437b763a07e6def2022-12-21T22:52:45ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642020-01-012711054106210.1080/10717544.2020.17850501785050Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriersPataranapa Nimtrakul0Pakawadee Sermsappasuk1Waree Tiyaboonchai2Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan UniversityDepartment of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Naresuan UniversityDepartment of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan UniversityThe oral delivery of amphotericin B (AmB) has remained a challenge due to its low solubility, permeability, and instability in gastric acidic pH. To solve these issues, herein, we reported a novel approach of using nanostructured lipid carriers (NLCs) and NLCs coating with Eudragit®L100-55 (Eu-NLCs) for the oral delivery of AmB. This study aimed to compare their ability in protecting the drug from degradation in gastrointestinal fluids and permeation enhancement in Caco-2 cells. Uncoated NLCs and Eu-NLCs possessed a mean particle size of ∼180 and ∼550 nm, with a zeta potential of ∼−30 and ∼−50 mV, respectively. Both NLCs demonstrated an AmB entrapment efficiency up to ∼75%. They possessed significantly greater AmB water solubility than the free drug by up to 10-fold. In fasted state simulated gastric fluid, Eu-NLCs provided significantly greater AmB protection from acidic degradation than uncoated NLCs. In fasted state simulated intestinal fluid, both uncoated and Eu-NLCs showed a fast release characteristic. Caco-2 cells permeation studies revealed that uncoated NLCs provided significantly higher apparent permeation coefficient (Papp) value than Eu-NLCs. Moreover, after 6 months of storage at 4 °C in the absence of light, the physicochemical stabilities of the lyophilized uncoated and Eu-NLCs could be maintained. In conclusion, the developed NLCs and Eu-NLCs could be a potential drug delivery system in improving the oral bioavailability of AmB.http://dx.doi.org/10.1080/10717544.2020.1785050amphotericin bnanostructured lipid carrierseudragit®l100-55caco-2 cellspermeationoral administration |
| spellingShingle | Pataranapa Nimtrakul Pakawadee Sermsappasuk Waree Tiyaboonchai Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers Drug Delivery amphotericin b nanostructured lipid carriers eudragit®l100-55 caco-2 cells permeation oral administration |
| title | Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
| title_full | Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
| title_fullStr | Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
| title_full_unstemmed | Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
| title_short | Strategies to enhance oral delivery of amphotericin B: a comparison of uncoated and enteric-coated nanostructured lipid carriers |
| title_sort | strategies to enhance oral delivery of amphotericin b a comparison of uncoated and enteric coated nanostructured lipid carriers |
| topic | amphotericin b nanostructured lipid carriers eudragit®l100-55 caco-2 cells permeation oral administration |
| url | http://dx.doi.org/10.1080/10717544.2020.1785050 |
| work_keys_str_mv | AT pataranapanimtrakul strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers AT pakawadeesermsappasuk strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers AT wareetiyaboonchai strategiestoenhanceoraldeliveryofamphotericinbacomparisonofuncoatedandentericcoatednanostructuredlipidcarriers |