1Department
of Pharmaceutics, Faculty of Pharmacy, Babu Banarasi Das
National Institute of Technology & Management, 2Faculty
of Pharmacy, Northern India Engineering College, Lucknow
(Uttar Pradesh), India
*
Purpose:
To develop a
niosomal formulation for the delivery of isoniazid to
achieve effective treatment of tuberculosis.
Methods:
Niosomes were prepared by
reverse phase evaporation method and given a charge with
a charge-inducing agent, dicetyl phosphate. Drug
entrapment efficiency in the niosomes was determined
spectrophotometrically. The niosomes were further
characterized for their particle size, polydispersity
index (PI) and zeta potential as well as by scanning
electron microscopy and stability studies. Furthermore,
in vitro drug release and cellular uptake studies on the
niosomes by macrophage J744 A were undertaken.
Results:
Suitable isoniazid niosomes
were obtained. The niosomes demonstrated a potential to
remain in the treated site for prolonged periods and
were also capable of maintaining steady drug
concentrations for up to 30 h. Cellular uptake of the
drug-loaded niosomes by macrophage cells was as high as
61.8 %, a
level that is capable of achieving effective treatment
of tuberculosis.
Conclusion:
The isoniazid niosomes
developed are capable of reducing drug dose and toxicity
as well as dosing frequency which should bring about
improved patient compliance. More importantly,
macrophage targeting should be feasible at sites where
tuberculosis bacteria are harbored.
Keywords:
Niosome, Macrophage
targeting, Isoniazid, Tuberculosis, Drug release,
Cellular uptake.
