FORMULATION AND EVALUATION OF CIMETIDINE LOADED BILOSOMES FOR ENHANCED DRUG DELIVERY

AbstractThe present study aimed to develop and evaluate cimetidine-loaded bilosomes as a lipidbased vesicular system for sustained oral drug delivery. Cimetidine-loaded bilosomes wereprepared using sodium deoxycholate (SDC), soy phosphatidylcholine (SPC), cholesterol, andSpan 60 as principal vesicle-forming components. Nine formulations (F1–F9) weredeveloped by varying the concentrations of the lipid and surfactant components whilemaintaining cimetidine at 200 mg. The aqueous solubility of cimetidine was found to be10.25 ± 0.08 mg/mL. UV-visible spectrophotometric analysis established a λmax of 229 nm,and the calibration curve showed excellent linearity over 2–20 µg/mL, with a regressionequation of y = 0.0442x + 0.0175 and R² = 0.9968. Entrapment efficiency varied from 67.60± 1.21% to 84.70 ± 0.72%, with F6 exhibiting the highest entrapment efficiency. Theoptimized F6 formulation contained0.3 g SDC, 0.3 g SPC, 0.8 g cholesterol, and 0.2 g Span 60. Particle-size analysisdemonstrated a nanosized vesicular population of approximately 150 nm with a PDI of 0.222± 0.004. The zeta potential of approximately -50 mV indicated favorable colloidal stability.SEM revealed predominantly spherical to near-spherical vesicles, while FTIR analysissupported compatibility between cimetidine and the formulation components. Allformulations exhibited prolonged drug release over 24 h. F6 demonstrated a controlledrelease profile, achieving 90.36± 1.39% cumulative drug release at 24 h. Overall, F6 showed promising entrapment,nanoscale characteristics, stability, and sustained drug release, supporting furtherinvestigation of cimetidine-loaded bilosomes as a potential oral lipid-based delivery system.