Formulation development and characterization of nanocochleates for the improvement of permeability of drug

Abstract

Rifampicin is the first choice drug for treatment of tuberculosis (TB), but it shows variable absorption in presence of other anti-TB drugs, so high dose is required. To overcome this problem nanocochleates of rifampicin were prepared through the interaction of calcium ions with the negatively charged phospholipids. It was done by two step process; first the liposomes of the drug were prepared by film hydration method using rotary evaporator, then dropwise calcium ions were added to the liposomes under constant stirring to form nanocochleates. Liposomes were evaluated for parameters of vesicle size and percentage entrapment, and the best formulations were selected for preparing nanocochleates. Cochleates thus prepared were subjected under particle size analysis, size distribution and SEM, which shows the elongated rod shaped sub micron size particles. Permeability studies were performed using the ex-vivo model, everted rat intestine was used to determine apparent permeability of rifampicin and comparing it to the apparent permeability shown by the rifampicin loaded nanocochleates. A significant increase in the apparent permeability of rifampicin (3.56 × 10-6cm/sec) was shown when given as nanocochleates of rifampicin (7.78 × 10-6cm/sec), thus this strategy can be used to improve the absorption of rifampicin through small intestine.