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Biotechnology and Applied Biochemistry (2001) 33, (123–125) (Printed in Great Britain)

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Activation of diacetyldapsone and a preliminary evaluation of a cyclodextrin–diacetyldapsone complex in cultured lung cells

Dipali Nimbalkar*, Raj Birudaraj†, Patrick R. Jones‡ and Timothy J. Smith*¹

*Department of Physiology and Pharmacology, University of the Pacific, Stockton, CA 95211, U.S.A., †Department of Pharmaceutics and Medicinal Chemistry, University of the Pacific, Stockton, CA 95211, U.S.A., and ‡Department of Chemistry, University of the Pacific, Stockton, CA 95211, U.S.A.

Abbreviations used: CD, 2-hydroxypropyl-b-cyclodextrin; DADDS, diacetyldapsone.

¹ To whom correspondence should be addressed (e-mail tsmith@uop.edu).

A diacetyldapsone–2-hydroxypropyl-b-cyclodextrin complex (DADDS–CD) was evaluated with regard to the ability of cultured lung cells to activate DADDS to the active metabolite dapsone. The same system was used to assess the effect of the complex on cell growth. The complex was incubated with cells for periods of 24 to 72 h, followed by extraction of metabolites from the incubation medium and analysis by HPLC. In addition, the Trypan Blue exclusion technique was used to assess cell viability during this time period. Results indicated that lung cells could activate DADDS to dapsone and that, while the complex appeared to delay cell growth in the first 24 h period, no significant difference was seen between cells incubated in the presence and absence of the complex at 72 h. These results indicate that DADDS–CD has significant potential as a drug-delivery system for DADDS in the lung based upon the ability of the cells to activate DADDS. The mixed effects of the complex on cell growth may have important implications when considering the frequency of administration of the complex to the lung.

Received 24 November 2000; accepted 17 December 2000

Portland Press Ltd © 2001