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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Main Authors: 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
Format: Article
Language:English
Published: BMC 2020-01-01
Series:Journal of Nanobiotechnology
Subjects:
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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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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