Cited by 507Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryInhalation and Respiratory Drug Delivery

Size-Dependent Bioadhesion of Micro- and Nanoparticulate Carriers to the Inflamed Colonic Mucosa

Lamprecht, Alf, Schäfer, Ulrich, Lehr, Claus-Michael·2001·Pharmaceutical Research

Abstract

Purpose The size-dependent deposition of microparticles and nanoparticles after oral administration to rats using an experimental model colitis was examined. Local delivery of an entrapped drug could reduce side effects and would be a distinct improvement compared with existing colon delivery devices.Methods Ulcerative colitis was induced in Lewis rats with trinitrobenzenesulfonic acid. Fluorescent polystyrene particles with a size of 0.1, 1, or 10 microm were administered for 3 days. The animals then were sacrificed and their guts resected. Particle distribution in the colon was imaged by confocal laser scanning microscopy and quantified by fluorescence spectrophotometry.Results In the inflamed tissue, an increased adherence of particles was observed at the thicker mucus layer and in the ulcerated regions. A size dependency of the deposition was found, and an increased number of attached particles to the colon was determined compared with the control group. For 10-micorm particles, only fair deposition was observed (control group: 1.4 +/- 0.6%; colitis: 5.2 +/- 3.8% of administered particle mass). One-micrometer particles showed higher binding (control group: 2.0 +/- 0.8%; colitis: 9.1 +/- 4.2%). Highest binding was found for 0.1-microm particles (control group: 2.2 +/- 1.6%; colitis: 14.5 +/- 6.3%). The ratio of colitis/control deposition increased with smaller particle sizes.Conclusions The use of submicron-sized carriers holds promise for the targeted delivery of drugs to the inflamed colonic mucosal areas in inflammatory bowel disease.

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Crossref · 10.1023/a:1011032328064

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  • Particle size is pivotal for stability, distribution, release of encapsulated antigens, and induction of immune responses.

    “The particles’ size is pivotal for stability, distribution, release of the encapsulated antigens and induction of immune responses [36,37].”

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Authors
Lamprecht, A., Schäfer, U., & Lehr, C.-M.
Affiliations
Saarland University (DE)
Corresponding author
Lamprecht, Alf
Venue
Pharmaceutical Research
Published
2001-06
Volume
18
Issue
6
Pages
788-793
ISSN
  • 0724-8741 (ISSN-L)
  • 1573-904X
OpenAlex
W1823279151
Cited by
507
References
30
Citations by year
2026: 11 · 2025: 28 · 2024: 23 · 2023: 18 · 2022: 33 · 2021: 21 · 2020: 33 · 2019: 30 · 2018: 24 · 2017: 38 · 2016: 23 · 2015: 20 · 2014: 29 · 2013: 22 · 2012: 30
FWCI
5.09
Type
journal article
Language
en
Open access
closed
Locations
  • Pharmaceutical Research (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
Keywords
bioadhesion, nanocarriers, microparticles, particle size, colon-targeted drug delivery, ulcerative colitis, colonic mucosa, mucus layer, inflammatory bowel disease, targeted drug delivery
MeSH terms
Adhesives, Animals, Capsules, Colitis, Drug Carriers, Female, Intestinal Mucosa, Particle Size, Rats, Inbred Lew, Drug Delivery Systems, Rats

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