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The mucosal toxicity of different benzalkonium chloride analogues evaluated with an alternative test using slugs

(2001) PHARMACEUTICAL RESEARCH. 18(7). p.937-942
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Organization
Abstract
Purpose. The objective of this study was to evaluate the mucosal toxicity of different benzalkonium chloride (BAC) analogues using slugs as the alternative test organism. Methods. The effect of different BAC analogues on the mucosal tissue of slugs was determined from the protein, lactate dehydrogenase, and alkaline phosphatase released from the foot mucosa after treatment. Additionally, mucus production and reduction in body weight of the slugs were measured. The eye irritation potency of the molecules was evaluated with the Bovine Corneal Opacity and Permeability (BCOP) assay. The antimicrobial activity of the different BAC analogues was also assessed. Results. All BAC analogues induced severe damage to the mucosal epithelium of the slugs, and the irritation increased with decreasing alkyl chain length: BAC-C16 < BAC-C14 < BAC-C12 similar to BAG-mix. A similar ranking was obtained with the BCOP assay for eye irritation. The relative order of activities among the three BAC analogues was the same, i.e., BAC-C14 greater than or equal to BAC-C16 > BAC-C12. The BAC-C14 exhibited higher activity than the BAG-mix. Conclusions. The toxicity and activity of BAG analogues depend on the alkyl chain length. The use of BAC-C14 as a conservative agent in pharmaceutical preparations instead of the BAG-mix should be considered.
Keywords
BCOP assay, mucosal toxicity, BAC analogues, antimicrobial activity, HUMAN RESPIRATORY MUCOSA, slug, BOVINE CORNEAL OPACITY, TOPICAL NASAL STEROIDS, IN-VITRO, ABSORPTION ENHANCERS, ASSAY, DRUGS, VIVO

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MLA
Adriaens, Els, et al. “The Mucosal Toxicity of Different Benzalkonium Chloride Analogues Evaluated with an Alternative Test Using Slugs.” PHARMACEUTICAL RESEARCH, vol. 18, no. 7, 2001, pp. 937–42, doi:10.1023/A:1010928025753.
APA
Adriaens, E., Dierckens, K., Bauters, T., Nelis, H., Van Goethem, F., Vanparys, P., & Remon, J. P. (2001). The mucosal toxicity of different benzalkonium chloride analogues evaluated with an alternative test using slugs. PHARMACEUTICAL RESEARCH, 18(7), 937–942. https://doi.org/10.1023/A:1010928025753
Chicago author-date
Adriaens, Els, Kristof Dierckens, Tieneke Bauters, Hans Nelis, Freddy Van Goethem, Philipe Vanparys, and Jean Paul Remon. 2001. “The Mucosal Toxicity of Different Benzalkonium Chloride Analogues Evaluated with an Alternative Test Using Slugs.” PHARMACEUTICAL RESEARCH 18 (7): 937–42. https://doi.org/10.1023/A:1010928025753.
Chicago author-date (all authors)
Adriaens, Els, Kristof Dierckens, Tieneke Bauters, Hans Nelis, Freddy Van Goethem, Philipe Vanparys, and Jean Paul Remon. 2001. “The Mucosal Toxicity of Different Benzalkonium Chloride Analogues Evaluated with an Alternative Test Using Slugs.” PHARMACEUTICAL RESEARCH 18 (7): 937–942. doi:10.1023/A:1010928025753.
Vancouver
1.
Adriaens E, Dierckens K, Bauters T, Nelis H, Van Goethem F, Vanparys P, et al. The mucosal toxicity of different benzalkonium chloride analogues evaluated with an alternative test using slugs. PHARMACEUTICAL RESEARCH. 2001;18(7):937–42.
IEEE
[1]
E. Adriaens et al., “The mucosal toxicity of different benzalkonium chloride analogues evaluated with an alternative test using slugs,” PHARMACEUTICAL RESEARCH, vol. 18, no. 7, pp. 937–942, 2001.
@article{412495,
  abstract     = {{Purpose. The objective of this study was to evaluate the mucosal toxicity of different benzalkonium chloride (BAC) analogues using slugs as the alternative test organism.
Methods. The effect of different BAC analogues on the mucosal tissue of slugs was determined from the protein, lactate dehydrogenase, and alkaline phosphatase released from the foot mucosa after treatment. Additionally, mucus production and reduction in body weight of the slugs were measured. The eye irritation potency of the molecules was evaluated with the Bovine Corneal Opacity and Permeability (BCOP) assay. The antimicrobial activity of the different BAC analogues was also assessed.
Results. All BAC analogues induced severe damage to the mucosal epithelium of the slugs, and the irritation increased with decreasing alkyl chain length: BAC-C16 < BAC-C14 < BAC-C12 similar to BAG-mix. A similar ranking was obtained with the BCOP assay for eye irritation. The relative order of activities among the three BAC analogues was the same, i.e., BAC-C14 greater than or equal to BAC-C16 > BAC-C12. The BAC-C14 exhibited higher activity than the BAG-mix.
Conclusions. The toxicity and activity of BAG analogues depend on the alkyl chain length. The use of BAC-C14 as a conservative agent in pharmaceutical preparations instead of the BAG-mix should be considered.}},
  author       = {{Adriaens, Els and Dierckens, Kristof and Bauters, Tieneke and Nelis, Hans and Van Goethem, Freddy and Vanparys, Philipe and Remon, Jean Paul}},
  issn         = {{0724-8741}},
  journal      = {{PHARMACEUTICAL RESEARCH}},
  keywords     = {{BCOP assay,mucosal toxicity,BAC analogues,antimicrobial activity,HUMAN RESPIRATORY MUCOSA,slug,BOVINE CORNEAL OPACITY,TOPICAL NASAL STEROIDS,IN-VITRO,ABSORPTION ENHANCERS,ASSAY,DRUGS,VIVO}},
  language     = {{eng}},
  number       = {{7}},
  pages        = {{937--942}},
  title        = {{The mucosal toxicity of different benzalkonium chloride analogues evaluated with an alternative test using slugs}},
  url          = {{http://doi.org/10.1023/A:1010928025753}},
  volume       = {{18}},
  year         = {{2001}},
}

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