An estimate of turnover time of intestinal mucus gel layer in the rat in situ loop

Lehr, Claus‐Michael; Poelma, F. G. J.; Junginger, Hans E.; Tukker, Josef J.

doi:10.1016/0378-5173(91)90287-x

Cited by 185 publications

(69 citation statements)

References 12 publications

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“…35 In many routes of administration, surface mucus is encountered by the bioadhesive before it reaches the tissue. The extent of interaction between the polymer and the mucus depends on mucus viscosity, degree of entanglement, and water content.…”

Section: Environment-related Factorsmentioning

confidence: 99%

Bioadhesive‐Based Dosage Forms: The Next Generation

Lee

Park

Robinson

2000

Journal of Pharmaceutical Sciences

464

152

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Section: Environment-related Factorsmentioning

confidence: 99%

Bioadhesive‐Based Dosage Forms: The Next Generation

Lee

Park

Robinson

2000

Journal of Pharmaceutical Sciences

464

152

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“…To protect the mucosal epithelium the constant fast turnover of the mucus layer serves to remove potentially damaging compounds introduced to the GI tract, and therefore the microcontainers provide a transient mucoadhesion and thereby prolong the contact time for epithelial uptake of furosemide. However, furosemide was released within minutes from the microcontainers ( Figure 5) (Ensign et al, 2012;C. M. Lehr et al, 1991), and this is probably why there was an increased absorption of furosemide through the intestinal wall.…”

Section: In Situ Closed-loop Rat Intestinal Perfusionmentioning

confidence: 99%

“…The main role of the mucus layer is to protect and lubricate the epithelial lining, and for drugs, the mucus layer may be a physical barrier to absorption. The mucus has variable turnover time in the GI tract, and the turnover time in the intestine is reported not to be longer than 2 h (Crater and Carrier, 2010;Ensign et al, 2012;C.-M. Lehr et al, 1991;Lehr, 2000). For being able to study the interaction of the drug delivery system with the intestinal membrane and also the mucus layer, in situ intestinal perfusion studies are ideal (Lennernas, 1998;Lennernäs, 2014;Lozoya-Agullo et al, 2015;Song et al, 2013).…”

mentioning

confidence: 99%

Polymeric microcontainers improve oral bioavailability of furosemide

Nielsen

Melero

Keller

et al. 2016

International Journal of Pharmaceutics

117

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Microcontainers with an inner diameter of 223 µm are fabricated using the polymer SU-8, and evaluated in vitro, in situ and in vivo for their application as an advanced oral drug delivery system for the poorly water soluble drug furosemide. An amorphous sodium salt of furosemide (ASSF) is filled into the microcontainers followed by applying a lid using Eudragit L100. It is possible to control the drug release in vitro, and in vitro absorption studies show that the microcontainers are not a hindrance for absorption of ASSF. In situ perfusion studies in rats are performed with ASSF-filled microcontainers coated with Eudragit and compared to a furosemide solution. The absorption rate constant of ASSF confined in microcontainers is found to be significantly different from the solution, and by light microscopy, it is observed that the microcontainers are engulfed by the intestinal mucus. An oral bioavailability study in rats is performed with ASSF confined in microcontainers coated with Eudragit and a control group with ASSF in Eudragit-coated capsules. A relative bioavailability of 220% for the ASSF in microcontainers compared to ASSF in capsules is found. These studies indicate that the microcontainers could serve as a promising oral drug delivery system.

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“…However, residence times of bioadhesives that are thought to attach to mucin are typically longer than the reported mucin turnover, suggesting that the presence of bioadhesive polymer on mucin may alter the turnover of this biopolymer. The residence time of dosage forms is limited by the mucin turnover time, which has been calculated to range between 47 and 270 min in rats and 12 -24 h in humans [45].…”

Section: Mucin Turnover Ratementioning

confidence: 99%