Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization
Abstract This study aimed to develop a new colon-targeted drug delivery system via the preparation of ternary nanocomposite carriers based on organic polymer, aminoclay and lipid vesicles. Budesonide (Bud), an anti-inflammatory drug was chosen as a model drug and encapsulated into three different fo...
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BMC
2020-01-01
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Series: | Journal of Nanobiotechnology |
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Online Access: | https://doi.org/10.1186/s12951-020-0579-7 |
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author | Hyeon Young Kim Jae Hee Cheon Sang Hoon Lee Jeong Youn Min Seung-Yun Back Jae Geun Song Da Hye Kim Soo-Jeong Lim Hyo-Kyung Han |
author_facet | Hyeon Young Kim Jae Hee Cheon Sang Hoon Lee Jeong Youn Min Seung-Yun Back Jae Geun Song Da Hye Kim Soo-Jeong Lim Hyo-Kyung Han |
author_sort | Hyeon Young Kim |
collection | DOAJ |
description | Abstract This study aimed to develop a new colon-targeted drug delivery system via the preparation of ternary nanocomposite carriers based on organic polymer, aminoclay and lipid vesicles. Budesonide (Bud), an anti-inflammatory drug was chosen as a model drug and encapsulated into three different formulations: liposome (Bud-Lip), aminoclay-coated liposome (AC-Bud-Lip), and Eudragit® S100-aminoclay double coated liposome (EAC-Bud-Lip). The formation of the aminoclay-lipid vesicle nanocomposite was confirmed by energy dispersive X-ray spectrum, transmission electron microscopy, and Fourier-transform infrared spectroscopy. All formulations were produced with a high encapsulation efficiency in a narrow size distribution. Drug release from EAC-Bud-Lip was approximately 10% for 2-h incubation at pH 1.2, implying the minimal drug release in acidic gastric condition. At pH 7.4, EAC-Bud-Lip underwent significant size reduction and exhibited drug release profiles similar to that from AC-Bud-Lip, implying the pH-dependent removal of the outer coating layer. Compared to free Bud solution, EAC-Bud-Lip achieved a higher drug uptake in Caco-2 cells and exhibited a stronger inhibition of TNF-α and IL-6 secretion in LPS-stimulated Raw264.7 cells. Furthermore, a bio-distribution study in mice demonstrated that Eudragit® S100-aminoclay dual coating led to a higher colonic distribution with a longer residence time, which correlated well with the delayed systemic drug exposure in rats. Taken together, the present study suggests that the ternary nanocomposite carrier consisting of Eudragit® S100, aminoclay, and lipid vesicle might be useful as an effective colon-targeted drug delivery system. |
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language | English |
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publishDate | 2020-01-01 |
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series | Journal of Nanobiotechnology |
spelling | doaj.art-a5c796e266e340e29d572efc54ffe4b52022-12-22T04:09:19ZengBMCJournal of Nanobiotechnology1477-31552020-01-0118111510.1186/s12951-020-0579-7Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterizationHyeon Young Kim0Jae Hee Cheon1Sang Hoon Lee2Jeong Youn Min3Seung-Yun Back4Jae Geun Song5Da Hye Kim6Soo-Jeong Lim7Hyo-Kyung Han8College of Pharmacy, Dongguk University-SeoulDepartment of Internal Medicine and Institute of Gastroenterology, Yonsei University College of MedicineCollege of Pharmacy, Dongguk University-SeoulCollege of Pharmacy, Dongguk University-SeoulCollege of Pharmacy, Dongguk University-SeoulCollege of Pharmacy, Dongguk University-SeoulDepartment of Internal Medicine and Institute of Gastroenterology, Yonsei University College of MedicineDepartment of Integrated Bioscience and Biotechnology, Sejong UniversityCollege of Pharmacy, Dongguk University-SeoulAbstract This study aimed to develop a new colon-targeted drug delivery system via the preparation of ternary nanocomposite carriers based on organic polymer, aminoclay and lipid vesicles. Budesonide (Bud), an anti-inflammatory drug was chosen as a model drug and encapsulated into three different formulations: liposome (Bud-Lip), aminoclay-coated liposome (AC-Bud-Lip), and Eudragit® S100-aminoclay double coated liposome (EAC-Bud-Lip). The formation of the aminoclay-lipid vesicle nanocomposite was confirmed by energy dispersive X-ray spectrum, transmission electron microscopy, and Fourier-transform infrared spectroscopy. All formulations were produced with a high encapsulation efficiency in a narrow size distribution. Drug release from EAC-Bud-Lip was approximately 10% for 2-h incubation at pH 1.2, implying the minimal drug release in acidic gastric condition. At pH 7.4, EAC-Bud-Lip underwent significant size reduction and exhibited drug release profiles similar to that from AC-Bud-Lip, implying the pH-dependent removal of the outer coating layer. Compared to free Bud solution, EAC-Bud-Lip achieved a higher drug uptake in Caco-2 cells and exhibited a stronger inhibition of TNF-α and IL-6 secretion in LPS-stimulated Raw264.7 cells. Furthermore, a bio-distribution study in mice demonstrated that Eudragit® S100-aminoclay dual coating led to a higher colonic distribution with a longer residence time, which correlated well with the delayed systemic drug exposure in rats. Taken together, the present study suggests that the ternary nanocomposite carrier consisting of Eudragit® S100, aminoclay, and lipid vesicle might be useful as an effective colon-targeted drug delivery system.https://doi.org/10.1186/s12951-020-0579-7Colon-targetedInflammatory diseaseAminoclayLiposomeNanocompositepH-dependent |
spellingShingle | Hyeon Young Kim Jae Hee Cheon Sang Hoon Lee Jeong Youn Min Seung-Yun Back Jae Geun Song Da Hye Kim Soo-Jeong Lim Hyo-Kyung Han Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization Journal of Nanobiotechnology Colon-targeted Inflammatory disease Aminoclay Liposome Nanocomposite pH-dependent |
title | Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization |
title_full | Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization |
title_fullStr | Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization |
title_full_unstemmed | Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization |
title_short | Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization |
title_sort | ternary nanocomposite carriers based on organic clay lipid vesicles as an effective colon targeted drug delivery system preparation and in vitro in vivo characterization |
topic | Colon-targeted Inflammatory disease Aminoclay Liposome Nanocomposite pH-dependent |
url | https://doi.org/10.1186/s12951-020-0579-7 |
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