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Effect of a Hydrophobic Phospholipid Lining of the Gastric Mucosa in Bioadhesion

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Abstract

Purpose

The role of a model hydrophobic phospholipid simulating lining of the gastric mucosa, as to adhesion of polymers with different surface functional groups and surface hydrophobicities, was evaluated using an in vitro gastric mucus model.

Materials and Method

Front-faced fluorescence measurement was used to determine adhesion of fluorescent polystyrene microspheres with different surface functional groups. Contact angle measurements and sticking bubble technique were used to measure relative surface hydrophobicity of the polymers.

Results

Adhesion of fluorescent polystyrene microspheres using front-faced fluorescence measurement revealed the hydrophobic phospholipid lining of the in vitro gastric mucus model did not allow adhesion of microspheres with –COOH and –NH2 functional groups, whereas it did allow adhesion of microspheres with hydrophobic attributes. In addition, in vitro adhesive force studies using diblock copolymers of polystyrene and polyacrylate showed that the in vitro adhesive force between the hydrophobic phospholipid lining of the in vitro gastric mucus model and the polymer increased when the surface hydrophobicity of the polymer increased.

Conclusion

The hydrophobic phospholipid acts as an adhesion barrier to hydrophilic bioadhesive polymers and polymers with surface functional groups of carboxylic acid and amine. The hydrophobic phospholipid lining of the gastric mucosa should be taken into considerations for screening and designing of a new gastric bioadhesive polymer.

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Abbreviations

Amine-MS:

fluorescent amine-modified polystyrene microspheres

Carboxylate-MS:

fluorescent carboxylate-modified polystyrene microspheres

F.I.:

fluorescence intensity

IGM:

in vitro gastric mucus model without LPC

IGM-LPC:

in vitro gastric mucus model with LPC

LPC:

egg yolk L-α-phosphatidylcholine

MTS:

material testing workstations

Plain-MS:

fluorescent plain polystyrene microspheres

References

  1. H. S. Ch’ng, H. Park, P. Kelly, and J. R. Robinson. Bioadhesive polymers as platforms for oral controlled drug delivery. II. Synthesis and evaluation of some swelling water-insoluble polymers. J. Pharm. Sci. 74:399–405 (1985).

    Article  PubMed  CAS  Google Scholar 

  2. K. Park and J. R. Robinson. Bioadhesive polymers as platforms for oral controlled drug delivery: Method to study bioadhesion. Int. J. Pharm. 19:107–127 (1984).

    Article  CAS  Google Scholar 

  3. J. Woodley. Bioadhesion: New possibilities for drug administration? Clin. Pharmacokinet. 40:77–84 (2001).

    Article  PubMed  CAS  Google Scholar 

  4. R. Khosla and S. S. Davis. The effect of polycarbophil on the gastric emptying of pellets. J. Pharm. Pharmacol. 39:47–49 (1987).

    PubMed  CAS  Google Scholar 

  5. D. Harris, J. T. Fell, D. C. Taylor, J. Lynch, and H. L. Sharma. GI transit of potential bioadhesive systems in the rat. J. Control Release 12:55–65 (1990).

    Article  CAS  Google Scholar 

  6. J. Lee, J. Park, and J. R. Robinson. Bioadhesive-based on dosage forms: the next generation. J. Pharm. Sci. 89:850–866 (2000).

    Article  PubMed  CAS  Google Scholar 

  7. B. A. Slomiany, A. Piasek, J. Sarosiek, and A. Slomiany. The role of surface intracellular mucus in gastric mucosal protection against hydrogen. Scand. J. Gastroenterol. 20:1191–1196 (1985).

    Article  PubMed  CAS  Google Scholar 

  8. Y. J. Kao and L. M. Lichtenberger. Localization of phospholipid-rich zones in rat gastric mucosa: possible origin of a proactive hydrophobic luminal lining. J. Histochem. Cytochem. 35:1285–1298 (1987).

    PubMed  CAS  Google Scholar 

  9. Y. J. Kao and L. M. Lichtenberger. Ultrastructural evidence that the gastric surface mucous cell (SMC) secretes a surfactant-like phospholipid (SLPL). Gastroenterol. 92:1459 (1987).

    Google Scholar 

  10. B. A. Hills, B. D. Butler, and L. M. Lichtenberger. Gastric mucosal barrier: The hydrophobic lining to the lumen of the stomach. Am. J. Physiol. 244:G561–G568 (1983).

    PubMed  CAS  Google Scholar 

  11. B. A. Hills. A hydrophobic oligolamellar lining to surfaces in various tissues: A possible ubiquitous barrier. Med. Sci. Res. 20:543–550 (1992).

    Google Scholar 

  12. P. J. Goddard, B. A. Hills, and L. M. Lichtenberger. Does aspirin damage canine gastric mucosa by reducing its surface hydrophobicity? Am. J. Physiol. 252:G421–G430 (1987).

    PubMed  CAS  Google Scholar 

  13. P. J. Goddard, Y. J. Kao, and L. M. Lichtenberger. Luminal surface hydrophobicity of canine gastric mucosa is dependent on a surface mucous gel. Gastroenterol. 98:361–370 (1990).

    CAS  Google Scholar 

  14. X. Yang. Gastric retentive systems. Master thesis, University of Wisconsin-Madison (1998).

  15. M. D. Lelah, T. G. Grasel, J. A. Pietce, and S. L. Cooper. The measurement of contact angles on circular tubing surfaces using the captive bubble technique. J. Biomed. Mat. Res. 19:1011–1015 (1985).

    Article  CAS  Google Scholar 

  16. R. Dierichs and M. Inczedy-Marcsek. Iodoplatinate as a marker of quaternary ammonium compounds in electron microscopy. J. Histochem. Cytochem. 24:962–964 (1976).

    PubMed  CAS  Google Scholar 

  17. G. R. Barlett. Phosphorous assay in column chromatography. J. Biol. Chem. 234:466–468 (1959).

    Google Scholar 

  18. J. T. F. Keurentjes, J. G. Harbrecht, D. Brinkman, J. H. Hanemaaijer, M. A. Cohen Stuart, and K. van’t Riet. Hydrophobicity measurements of microfiltration and ultrafiltration membranes. J. Membr. Sci. 47:333–344 (1989).

    Article  CAS  Google Scholar 

  19. T. T. Kararli. Comparision of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm. Drug Dispos. 16:351–380 (1995).

    Article  PubMed  CAS  Google Scholar 

  20. Y. J. Kao, P. J. Goddard, and L. M. Lichtenberger. Morphological effects of aspirin and prostaglandin on the canine gastric mucosal surface. Gastroenterol. 98:592–606 (1990).

    CAS  Google Scholar 

  21. M. G. J. Schmitz and W. Renooij. Phospholipids from rat, human, and canine gastric mucosa. Gastroenterol. 99:1292–1296 (1990).

    CAS  Google Scholar 

  22. W. Bernhard, A. O. Postle, M. Linck, and K. F. Sewing. Composition of phospholipid classes and phosphatidylcholine molecular species of gastric mucosa and mucus. Biochim. Biophys. Acta 1255:99–104 (1995).

    PubMed  Google Scholar 

  23. D. A. Norris and P. J. Sinko. Effect of size, surface charge, and hydrophobicity on the translocation of polystyrene microspheres through gastrointestinal mucin. J. Appl. Polym. Sci. 63:1481–1492 (1997).

    Article  CAS  Google Scholar 

  24. J. Sarosiek, A. Slomiany, and B. A. Slomiany. Retardation of hydrogen ion diffusion by gastric mucus constituents: Effect of proteolysis. Biochem. Biophys. Res. Commun. 115:1053–1060 (1983).

    Article  PubMed  CAS  Google Scholar 

  25. J. Sarosiek and A. Slomiany. Hydrogen ion diffusion in dog gastric mucus glycoprotein: effect of associated lipids and covalently bound fatty acids. Biochem. Biophys. Res. Commun. 118:523–531 (1984).

    Article  PubMed  CAS  Google Scholar 

  26. S. E. Williams and L. A. Turnberg. Retardation of acid diffusion by pig gastric mucus: A potential role in mucosal protection. Gastroenterol. 79:299–304 (1980).

    CAS  Google Scholar 

  27. P. M. Goggin, T. C. Northfield, and R. T. Spychal. Factors affecting gastric mucosal hydrophobicity in man. Scand. J. Gastroenterol. 26:65–73 (1991).

    Article  Google Scholar 

  28. R. T. Spychal, J. M. Marrero, S. H. Saverymuttu, and T. C. Northfield. Measurement of the surface Hydrophobicity of human gastrointestinal mucosa. Gastroenterol. 97:104–111 (1989).

    CAS  Google Scholar 

  29. B. A. Slomiany, J. Sarosiek, Y. H. Liau, W. Laszewicz, and A. Slomiany. Lysolecithin affects the viscosity, permeability, and peptic susceptibility of gastric mucin. Scand. J. Gastroenterol. 21:1073–1079 (1986).

    Article  PubMed  CAS  Google Scholar 

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Acknowledgments

The authors would like to thank Jason Sims and Jennifer Loeb, School of Pharmacy, University of Wisconsin-Madison, USA, for kindly providing the pig stomachs, and Randall Massey for his help on the morphological study of the pig gastric mucosal surface.

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Authors and Affiliations

  1. Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin-Madison, Madison, Wisconsin, 53705-2222, USA

    Jae Han Park & Joseph R. Robinson

  2. Mallinckrodt Pharmaceuticals, Covidien Healthcare, 385 Marshall Ave, Webster Groves, Missouri, 63119, USA

    Jae Han Park

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  1. Jae Han Park
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  2. Joseph R. Robinson
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Correspondence to Jae Han Park.

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Park, J.H., Robinson, J.R. Effect of a Hydrophobic Phospholipid Lining of the Gastric Mucosa in Bioadhesion. Pharm Res 25, 16–24 (2008). https://doi.org/10.1007/s11095-007-9353-x

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  • DOI: https://doi.org/10.1007/s11095-007-9353-x

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