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.
Highlights
Inflammatory bowel diseases (IBD) are chronic relapsing disorders of the gastrointestinal tract and are caused by complex interactions of environmental and genetic factors along with subsequent changes in immune dysregulation [1, 2]
The addition of anionic Eudragit® S100 as a pH-sensitive layer resulted in the alteration of the surface charge to negative and increased the particle size (321 nm) when compared to AC-budesonide [uncoated liposome (Bud-Lip)
Given that cationic nanoparticles adhere to the mucosal surface via the interaction between the positively charged nanoparticle and the negatively charged intestinal mucosa, the mucoadhesion properties of cationic nanoparticles can promote better contact with the Conclusion In the present study, three different liposomal formulations were prepared with narrow size distribution and high encapsulation efficiency
Summary
Inflammatory bowel diseases (IBD) are chronic relapsing disorders of the gastrointestinal tract and are caused by complex interactions of environmental and genetic factors along with subsequent changes in immune dysregulation [1, 2]. Nano-sized carriers have gained a great attention as a potential colon-specific drug delivery system due to their preferential uptake into inflamed colonic mucosa [5, 6]. Nanoparticulate drug carriers have been extensively studied for targeting the inflamed intestinal mucosa. To enhance colonic drug delivery, the liposomal surface can be coated with mucoadhesive or pH-sensitive polymers to release the drug preferably at the distal part of the intestine and lengthen the retention time in the colon [12,13,14]. Given that an ideal colon-specific delivery system should prevent premature drug release before reaching the colon, the properties of surface coating materials have a great impact on the effectiveness of liposomal drug carriers for colon targeting
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