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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.

Piperine has various pharmacological effects and can modulate the functional activity of metabolic enzymes and drug transporters. Consequently, there is a great interest in the application of piperine as an alternative medicine or bioavailability enhancer. Areas covered: This review deals with the effects of piperine on metabolizing enzymes and drug transporters. It provides the readers with an update on transporter-mediated and also metabolic enzyme-mediated piperine-drug interactions, with emphasis on its in vivo implications. This article also encompasses recent advances in the formulation approaches and technologies for optimizing the delivery of piperine. Expert opinion: Piperine can influence the pharmacokinetics of coadministered drugs, which may result in a therapeutically beneficial or adverse effect. Given that piperine inhibits or stimulates the activity of metabolic enzymes and transporters depending on the treatment conditions, the clinical significance of piperine-drug interactions should be assessed by varying the dose, dosing frequency, and the duration of treatment. In particular, better understanding the clinical relevance of piperine-drug interactions based on long-term assessments will provide a strong basis for the feasibility and applicability of piperine as a bioenhancer or a health-promoting agent. The development of effective formulations is also critical to facilitate the therapeutic applications of piperine.

Backgrounds/AimsCholedochal cyst of the bile duct is characterized by cystic dilatation of the intra- or extrahepatic bile ducts. It is a relatively uncommon disease and there is still much controversy regarding its etiology as being congenital or acquired.MethodsThe medical records of 60 patients who underwent surgical treatments for choledochal cyst between April 1995 and April 2009 at the Gachon University Gil Hospital were reviewed retrospectively. To compare the clinical characteristics, patients under 19 years of age were grouped into children and the others were grouped into adults.ResultsOf the overall 60 patients, 24 were grouped into children and 36 were grouped into adults. Female predominance was common in both groups (M : F=1 : 6.5). The most common clinical symptom was abdominal pain (73.3%) in both groups. Children had remarkable jaundice (33.3% vs. 0%) and gastrointestinal symptoms including nausea and vomiting. Fever and chills were more common in children because of the associated complications of cholangitis. According to the Todani classification, type I was the most common form of choledochal cyst in both groups, and type IVa was significantly more common in children than adults (45.3% vs. 16.7%). Thirty patients (50%) had anomalous pancreaticobiliary ductal union which was confirmed by preoperative imaging studies or intraoperative cholangiography. All patients except for one child underwent cyst excision with hepaticojejunostomy.ConclusionThere was no significant difference in the clinical characteristics of choledochal cysts between children and adults. However, combined diseases especially bile duct malignancy were common in aged patients, early detection and more aggressive surgery is necessary for patients with choledochal cysts.