Background: Mycobacterium tuberculosis (M. TB) remains the prime cause of bacterial
mortality and morbidity world-wide. Therefore, effective delivery and targeting of drug to the cellular
tropics is essentially required to generate significant results for tuberculosis treatment. The aim of the
present study was to develop and characterize ligand anchored pH sensitive liposomes (TPSL) as dry
powder inhaler for the targeted delivery of drugs in the target site i.e. lungs.
Method: Ligand anchored PSL (TPSL) was prepared by thin film hydration for the combined delivery of Isoniazid (INH)
and Ciprofloxacin HCl (CIP HCl) using 4-aminophenyl-α-D mannopyranoside (Man) as surface functionalized ligand and
characterized using different parameters.
Results: It was observed that size of the ligand anchored liposomes (TPSL) was slightly more than the non-ligand anchored
liposomes (PSL). Drug release was studied at different pH for 24 hrs and it was observed that liposomes exhibited
slow release at alkaline pH (58-64%) as compared to macrophage pH (81-87%) where it increased dramatically due to the
destabilization of pH sensitive liposome (PSL). In vitro cellular uptake study showed that much higher concentration was
achieved in the alveolar macrophage using ligand anchored liposomes as compared to its counterpart. In vivo study
showed that maximum drug accumulation was achieved in the lung by delivering drug using ligand anchored PSL as
compared to conventional PSL.
Conclusion: It was concluded that ligand anchored pH sensitive liposome is one of the promising systems for the targeted
drug therapy in pulmonary tuberculosis.