Preparation and characterization of isoniazid-loaded crude soybean lecithin liposomes

Int J Pharm. 2017 Jun 30;526(1-2):466-473. doi: 10.1016/j.ijpharm.2017.04.074. Epub 2017 Apr 29.

Abstract

Tuberculosis (TB) is a poverty related infectious disease that is rapidly giving rise to public health concerns. Lengthy drug administration and frequent adverse side-effects associated with TB treatment make anti-tubercular drugs (ATDs) good candidates for drug delivery studies. This work aimed to formulate and prepare liposomes as a cost-effective option for ATD delivery. Liposomes were prepared by film hydration using crude soybean lecithin (CL) and not pure phospholipids as in the normal practice. Cholesterol was also used (up to 25% mass ratio), and isoniazid (INH) was encapsulated as model drug using a freeze-thaw loading technique. Purified soybean lecithin (PL) was also used for comparative purposes, under the same conditions. INH-loaded liposomes were characterized for particle size, Zeta Potential (ZP), encapsulation efficiency (EE) and drug release. Physicochemical properties were investigated using thermogravimetric analysis, differential scanning calorimetry, X-ray diffraction and Fourier transform infrared. INH-loaded CL-based liposomes showed high EE (79±2.45%). The average particle size (813.00±9.21nm) and ZP (-42.80±4.31mV) of this formulation are promising for the treatment of TB by pulmonary delivery. These findings suggest the possibility of encapsulating ATDs in liposomes made of crude soybean lecithin that is cheap and readily available.

Keywords: Acetone (PubChem CID: 180); Acetonitrile (PubChem CID: 6342); Anti-tubercular drugs; Chloroform (PubChem CID: 6212); Cholesterol (PubChem CID: 5997); Dibasic sodium phosphate (PubChem CID: 24203); Ethyl acetate (PubChem CID: 8857); Isoniazid; Isoniazid (PubChem CID: 3767); Liposomes; Methanol (PubChem CID: 887); Monobasic sodium phosphate (PubChem CID: 23672064); Soybean lecithin; Tuberculosis.

MeSH terms

  • Chemistry, Pharmaceutical
  • Drug Liberation
  • Glycine max / chemistry*
  • Isoniazid / chemistry*
  • Lecithins / chemistry*
  • Liposomes / chemistry*

Substances

  • Lecithins
  • Liposomes
  • Isoniazid