Nystatin–polyethylene oxide conjugates with enhanced solubility in water
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Due to its broad-action spectra nystatin has been used for years for mucocutaneous candidosis, still its clinical use has been limited due to the lack of absorption by the oral route, and systemic side-effects and toxicity. In order to overcome low water solubility and high toxicity new conjugates nystatin–polyethylene oxide were synthesized and characterized from physico-chemical, as also from the controlled release pattern and antifungal efficacy point of view. To the knowledge of the authors this structure has not been reported previously in the literature and indicate an interesting release pattern as well as increased biological activity.
KeywordsNystatin Sustained release PEO
This research was financially supported by European Social Fund –„Cristofor I. Simionescu” Postdoctoral Fellowship Programme (IDPOSDRU/89/1.5/S/55216), Human Resources Development 2007–2013. The authors will like to express their gratitude to Dr. Valeria Harabagiu, Dr. Xenia Patras and Dr. Aurica Farcas for their advice and guidance in understanding the complexity of the described phenomena.
- 1.Bolard, J.: How do the polyene macrolide antibiotics affect the cellular membrane properties? Biochim. Biophys. Acta. Rev. Biomembr. 864, 257–304 (1986)Google Scholar
- 2.Huber, W.G.: Antifungal and antiviral agents. In: Jones, L.M., Booth, N.H., McDonald, L.E. (eds.) Veterinary Pharmacology and Therapeutics, p. 977. Iowa State University Press, Ames (1977)Google Scholar
- 3.Wallace, T.L., Lopez-Berenstein, G.: Nystatin and liposomal nystatin. In: Yu, V.L., Merigan, T.C., Barriere, S., White, N.J. (eds.) Antimicrobial Therapy and Vaccines, pp. 1185–1191. Williams and Wilkins, Baltimore (1998)Google Scholar
- 4.Wallace, T.L., Paetznick, V., Cossum, P.A., Lopez-Berestein, G., Rex, J.H., Anaissie, E.: Activity of liposomal nystatin against disseminated Aspergillus fumigatus in neutropenic mice. Antimicrob. Agents Chemother. 41, 2238–2243 (1997)Google Scholar
- 5.Boutati, E., Maltezou, H.C., Lopez-Berenstein, G. V., Kinsky, S.C. Polyene antibiotics. In: Gottlieb, D., Shaw, P.D. (eds.) Antibiotics, vol. 1, pp. 122–141. Springer-Verlag, New York (1967)Google Scholar
- 8.Seymour, A.R., Meechan, J., Yates, M.S.: Pharmacology and Dental Therapeutics, 3rd edn, pp. 171–173. Oxford University Press, New York (2004)Google Scholar
- 10.Carillo-Munoz, A.J., Quindos, G., Tur, C., Ruesga, M.T., Miranda, Y., del Valle, O., Cossum, P.A., Wallace, T.L.: In vitro antifungal activity of liposomal nystatin in comparison with nystatin, amphotericin B cholesteryl sulphate, liposomal amphotericin B, amphotericin B lipid complex, amphotericin B desoxycholate, fluconazole and itraconazole. J. Antimicrob. Chemother. 44, 397–401 (1999)CrossRefGoogle Scholar
- 12.Storescu, V.: Bazele farmacologice ale practicii medicale. Ed. Medicala 1, 1240–1245 (1997)Google Scholar
- 16.Higuchi, T., Connors, K.A.: Phase-solubility techniques. Adv. Anal. Chem. Instrum. 4, 212–217 (1965)Google Scholar
- 17.Sletta, H., Borgos, S.E., Bruheim, P., Sekurova, O.N., Grasdalen, H., Aune, R., Ellingsen, T.E., Zotchev, S.B.: Nystatin biosynthesis and transport: nysH and Nys G genes encoding a putative ABC transporter system in Streptomyces noursei ATCC 1145 are required for efficient conversion of 10-deoxynystatin to nystatin. Antimicrob. Agents Chemother. 49, 4576–4583 (2005)CrossRefGoogle Scholar