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Permeability of Mycobacterium leprae to dapsone: alteration by purification procedures

K Prabhakaran, E B Harris, W F Kirchheimer

    Leprosy in India
    |April 1, 1981
    PubMed

    Insights

    Dapsone (DDS) permeability into Mycobacterium leprae was assessed by its enzyme inhibition. Pre-treatment of M. leprae enhanced DDS penetration, enabling effective inhibition of o-diphenoloxidase.

    Area of Science:

    • Microbiology
    • Pharmacology
    • Biochemistry

    Background:

    • Leprosy is caused by Mycobacterium leprae.
    • Dapsone (DDS) is a key drug for leprosy treatment.
    • Understanding drug permeability is crucial for treatment efficacy.

    Purpose of the Study:

    • To determine the in vitro permeability of Mycobacterium leprae to dapsone.
    • To assess the effect of dapsone on Mycobacterium leprae o-diphenoloxidase activity.
    • To evaluate methods for enhancing dapsone penetration into M. leprae.

    Main Methods:

    • Assessing dapsone's inhibition of M. leprae o-diphenoloxidase.
    • Treating M. leprae with trypsin, NaOH, acetone, and ether to alter permeability.
    • Measuring changes in enzyme inhibition after pre-treatment.

    Main Results:

    • Intact M. leprae showed low dapsone permeability and enzyme inhibition.
    • Pre-treatment of M. leprae with trypsin, NaOH, or organic solvents significantly increased dapsone penetration.
    • Enhanced penetration led to effective inhibition of o-diphenoloxidase.

    Conclusions:

    • Mycobacterium leprae exhibits limited dapsone permeability in its native state.
    • Pre-treatment methods can overcome M. leprae's permeability barrier to dapsone.
    • This approach may aid in studying M. leprae metabolism and drug interactions.

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