Preparation, Optimization and Characterization of Chitosan-coated Liposomes for Solubility Enhancement of Furosemide: A Model BCS IV Drug.

Abstract

Most of drugs are administered orally and they must be absorbed from gastrointestinal tract for systemic effect. Generally drug molecules be dissolved in GI fluids before absorption. Solubility and permeability of drugs are considered as two parameters in biopharmaceutical classification system (BCS). Many researches performed to change permeability and solubility of drugs to improve abruption and bioavailability of them. Lipidic nanocarriers such as nanoliposomes are one approach to dissolve poorly water soluble drugs. Furosemide (FMD) as a typical molecule in BCS IV has low solubility and permeability. Thermodynamically, molecules of FMD could stay in the space of liposomal membrane. In this study effective parameters to preparation of nanoliposomes coated by chitosan (CCLs) were screened optimized by experimental design. Particle size, polydispersity index and surface potential of optimized CCLs have 155.8 ±3.5 nm, 0.229±0.022 and 25.2±3.5 mV, respectively. FMD was loaded in optimized CCLs 98.94±0.7%. Size of CCLs have verified by atomic force electron microscope. CCLs loaded by FMD were dried and in vitro study was performed to test release of FMD from powder. Results showed that solubility and dissolution of FMD increased by loading in CCLs in comparison to crystalline FMD and physical mixture of FMD and materials of CCLs.