Formulation Design and Characterization of Rifapentine Nano Liposome by Lipid Film Hydration Method Using a Constitutive Lipids (Sunflower Lecithin: Cholesterol) For the Improvement of Drug Permeability

Abstract

Rifapentine is considered a first-line drug for treating tuberculosis (TB), but its absorption can be inconsistent when  administered alongside other anti-TB medications, often necessitating higher doses. To address this issue, Nano liposomal formulations of Rifapentine were developed by introducing calcium ions to interact with the negatively  charged phospholipids. The preparation involved a two-step method: initially, liposomes of the drug were formed using  a film hydration technique with a rotary evaporator. Following this, calcium ions were added drop wise to the liposomal suspension under continuous stirring, resulting in the formation of Nano-liposomes.

The liposomes were then assessed for various characteristics such as vesicle size and drug entrapment efficiency. The  most promising formulations were selected for further processing. The resulting Cochleates were subjected to particle  size analysis, size distribution studies, and scanning electron microscopy (SEM), which revealed that the particles had an elongated, rod-like shape at sub-micron dimensions.

To evaluate the potential of the Nano-liposomal Rifapentine for enhanced absorption, permeability studies were  conducted using an ex-vivo rat intestine model. The apparent permeability of Rifapentine from the standard formulation  was compared to that of Rifapentine-loaded Nano-liposomes. The results showed a notable increase in the apparent  permeability of Rifapentine when delivered in the Nano-liposomal form (7.78 × 10.6 cm/sec) compared to the  conventional drug (3.56 × 10.6 cm/sec). This enhancement suggests that Nano-liposomal Rifapentine can significantly  improve drug absorption across the small intestine, offering a potential strategy for optimizing Rifapentine therapeutic efficacy. Keywords: Rifapentine, Nano liposomes, Cochleates, apparent permeability, liposomes.