Cubic Microcontainers Improve In Situ Colonic Mucoadhesion and Absorption of Amoxicillin in Rats

Abstract

An increased interest in colonic drug delivery has led to a higher focus on the design of delivery devices targeting this part of the gastrointestinal tract. Microcontainers have previously facilitated an increase in oral bioavailability of drugs. The surface texture and shape of microcontainers have proven to influence the mucoadhesion ex vivo. In the present work, these findings were further investigated using an in situ closed-loop perfusion technique in the rat colon, which allowed for simultaneous evaluation of mucoadhesion of the microcontainers as well as drug absorption. Cylindrical, triangular and cubic microcontainers, with the same exterior surface area, were evaluated based on in vitro release, in situ mucoadhesion and in situ absorption of amoxicillin. Additionally, the mucoadhesion of empty cylindrical microcontainers with and without pillars on the top surface was investigated. From the microscopy analysis of the colon sections after the in situ study, it was evident that a significantly higher percentage of cubic microcontainers than cylindrical microcontainers adhered to the intestinal mucus. Furthermore, the absorption rate constants and blood samples indicated that amoxicillin in cubic microcontainers was absorbed more readily than when cylindrical or triangular microcontainers were dosed. This could be due to a higher degree of mucoadhesion for these particular microcontainers.

Colon-Specific Delivery of Bioactive Agents Using Genipin-Cross-Linked Chitosan Coated Microcontainers

“…polymeric devices for oral drug delivery, are designed and fabricated as a reservoir with an opening on one side, to hold and carry a compound to the target site of release 15,16 . Previous studies have shown that microcontainers can facilitate protection of loaded contents through the various local environments of the GI tract 17,18 , controlled release of pharmaceuticals 19,20 and their tunable properties can increase the intestinal retention of a drug formulation 21,22 . After fabrication, the microcontainers are loaded with a compound followed by sealing with a polymeric lid 23 .…”

Open-source force analyzer with broad sensing range based on an optical pickup unit

“…They have a cavity for drug loading on the top side, and since only one side is open, they can provide unidirectional drug release through the GI tract to increase drug absorption efficiency. The transit mechanism has been investigated using an ex vivo intestinal perfusion model and animal studies [7] , [21] . However, the mucoadhesion force of a single MC has not been thoroughly studied because of the limited resolution of the conventional texture analyzer.…”

Micromechanical Punching: A Versatile Method for Non-Spherical Microparticle Fabrication

“…The conventional punching or blanking process includes three basic steps illustrated in Figure 1A: (1) A metal sheet is positioned on an inflexible die. (2) The punch and the metal sheet are brought into contact by the application of a high force. The penetration of the punch into the voids of the die results in build-up of stresses in the metal sheet with the maximum stress located at the edges of the punch.…”

“…In order to influence the biodistribution of drug-loaded micro- and nanoparticles in pharmaceutics and the targeting, release profile, and bioavailability of the drug, the ability to precisely manipulate size, shape, and surface properties of the particles is important [ 1 , 2 ]. Similarly, the composition, size and shape of a metallic nanoparticle dictate the resonant frequency of the electron oscillation in localized surface plasmonics.…”