ABSTRACT
This research aims to identify regional differences in vildagliptin absorption across the intestinal membrane. Furthermore, it was to investigate the effect of verapamil or metformin on vildagliptin absorptive clearance. The study utilized an in situ rabbit intestinal perfusion technique to determine vildagliptin oral absorption from duodenum, jejunum, ileum, and ascending colon. This was conducted both with and without perfusion of metformin or verapamil. The findings revealed that the vildagliptin absorptive clearance per unit length varied by site and was in the order as follows: ileum < jejunum < duodenum < ascending colon, implying that P-gp is significant in the reduction of vildagliptin absorption. Also, the arrangement cannot reverse intestinal P-gp, but the observations suggest that P-gp is significant in reducing vildagliptin absorption. Verapamil co-perfusion significantly increased the vildagliptin absorptive clearance by 2.4 and 3.2 fold through the jejunum and ileum, respectively. Metformin co-administration showed a non-significant decrease in vildagliptin absorptive clearance through all tested segments. Vildagliptin absorption was site-dependent and may be related to the intestinal P-glycoprotein content. This may aid in understanding the important elements that influence vildagliptin absorption, besides drug-drug interactions that can occur in type 2 diabetic patients taking vildagliptin in conjunction with other drugs that can modify the P-glycoprotein level.
Subject(s)
Metformin , Animals , Humans , Rabbits , Vildagliptin/pharmacology , Metformin/pharmacology , Verapamil/pharmacology , Intestinal Absorption , Intestines , ATP Binding Cassette Transporter, Subfamily BABSTRACT
The utilization of novel drug delivery systems loaded with essential oils has gained significant attention as a promising approach for biomedical applications in recent years. Plants possess essential oils that exhibit various medicinal properties, i.e., anti-oxidant, anti-microbial, anti- inflammatory, anti-cancer, immunomodulatory, etc., due to the presence of various phytoconstituents, including terpenes, phenols, aldehydes, ketones, alcohols, and esters. An understanding of conventional and advanced extraction techniques of Essential Oils (EOs) from several plant sources is further required before considering or loading EOs into drug delivery systems. Therefore, this article summarizes the various extraction techniques of EOs and their existing limitations. The in-built biological applications of EOs are of prerequisite importance for treating several diseases. Thus, the mechanisms of action of EOs for anti-inflammatory, anti-oxidant, anti-bacterial activities, etc., have been further explored in this article. The encapsulation of essential oils in micro or nanometric systems is an intriguing technique to render adequate stability to the thermosensitive compounds and shield them against environmental factors that might cause chemical degradation. Thus, the article further summarizes the advanced drug delivery approaches loaded with EOs and current challenges in the future outlook of EOs for biomedical applications.