Pharmaceutica Analytica Acta

Development and characterization of pH sensitive liposomes as dry powder inhaler using systematic design of experiment (DoE) approach for the treatment of Tuberculosis

5^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems

March 16-18, 2015 Crowne Plaza, Dubai, UAE

Abhinav Mehta, Ankur Bhardwaj and Anne Grobler

Posters & Accepted Abstracts: Pharm Anal Acta

Abstract:

The present study investigates the development and characterization of the surface functionalized pH sensitive liposomes as dry powder inhaler systems using systematic design of experiment approach (DOE) for the targeted delivery of the therapeutics to the lungs. Surface functionalized pH sensitive liposomes were prepared by thin film hydration method for the combined delivery of Isoniazid (INH) and Ciprofloxacin HCl (CIP HCl) using 4-aminophenyl-a-D-mannopyranoside (Man) as surface functionalized ligand. The developed systems were then characterized for their various physicochemical parameters such as aerodynamic diameter, morphology, drug entrapment, drug release, pH sensitivity and cell line study. It was observed that size of the ligand appended liposomes (TPSL) were slightly more than the non-ligand appended liposomes (PSL). It was found that percent drug entrapment (PDE) of TPSL was 70 ? 1.23% (INH), 67 ? 1.38 % (CIP HCl) while PDE of PSL was 66.3 ? 1.05 % (INH) and 65.0 ? 2.31 % (CIP HCl). Drug release was studied at different pH for 24 hrs it was observed that liposomes exhibited sustained release at pH 7.4 as compared to pH 5.5 and pH 5.0 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 appended liposomes as compared to its counterpart. Thus, it was concluded that ligand appended pH sensitive liposome is one of the promising system for the targeted therapy for pulmonary tuberculosis.