DEVELOPMENT, OPTIMISATION, AND CHARACTERISATION OF SNEDDS OF ANTI-LIPASE INHIBITOR

Background: Self-Nanoemulsifying Drug Delivery System (SNEDDS) has been employed extensively by the formulation of scientists to tackle the low solubility issues of various drugs and lift the bioavailability profile. But the potential of SNEDDS is not limited to augment the dissolution profile only. Objective: The objective of the study was to develop, optimization, and characterization of SNEDDS of anti-lipase inhibitors. Method: Orlistat was added in an accurately weighed amount of oil into a screw-capped glass vial and heated in a water bath at 40 ºC. The surfactant and co-surfactant were added to the oily mixture using positive displacement pipette and stirred with a magnetic bar. The formulation was further sonicated for 15 min and stored at room temperature until its use in subsequent studies. A 2³ full factorial design was selected because an experiment may be designed to focus attention on a single independent variable or factor. Results: The drug loading efficiency for all Orlistat SNEDDS formulae was found in the range of 92.37% ± 0.75% (PF1) to 99.09% ± 0.56% (PF4), indicating uniform drug dispersion in formulae. To optimize and select a self-emulsifying region with minimum globule size (<300 nm), the concentration of the oil, surfactant, and co-surfactant in the isotropic mixture was determined by constructing a ternary phase diagram. Fourier-transform infrared spectroscopy was optimized Orlistat, indicating no existence of the interaction between the Orlistat and polymer. The Differential Scanning Calorimetry study also confirmed for orlistat (45.77 ºC and formulation F1 to F4 (45.21 ºC, 45.61 ºC, 45.41 ºC, and 45.61 ºC) respectively. In the present study observation of acute toxicity study carried out, and none of the rats showed observable signs of toxicity upon single administration of test drug. The HFD treated rats showed a significant increase (p<0.05) in HDL-c compared to control group, while significant (p<0.05) increase were observed in standard (orlistat 12 mg/kg), and formulation treated groups (30 and 60 mg kg) when compared to HFD treated rats. Conclusion: This technique can minimize cost and cut short the number of formulations needed to identify the optimum composition. The Orlistat SNEDDS formulation was successfully developed, optimized, and characterized.