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Ternary nanocomposite carriers based on organic clay-lipid vesicles as an effective colon-targeted drug delivery system: preparation and in vitro/in vivo characterization

  • Kim, Hyeon Young1
  • Cheon, Jae Hee2
  • Lee, Sang Hoon1
  • Min, Jeong Youn1
  • Back, Seung-Yun1
  • Song, Jae Geun1
  • Kim, Da Hye2
  • Lim, Soo-Jeong3
  • Han, Hyo-Kyung1
  • 1 Dongguk University-Seoul, Dongguk-ro-32, Ilsan-Donggu, Goyang, Korea , Goyang (South Korea)
  • 2 Yonsei University College of Medicine, Seoul, Korea , Seoul (South Korea)
  • 3 Sejong University, 209 Neungdong-ro, Gwangjin-gu, Seoul, Korea , Seoul (South Korea)
Published Article
Journal of Nanobiotechnology
Springer (Biomed Central Ltd.)
Publication Date
Jan 21, 2020
DOI: 10.1186/s12951-020-0579-7
Springer Nature


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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