Preclinical Study on the Luteolin-Self-Nanoemulsifying Drug Delivery System: Pharmacokinetics, Toxicity, and Antiulcer Activity Evaluation
Rashmi Pathak, Phool ChandraIntroduction:
Utilising self-nanoemulsifying drug delivery systems (SNEDDS), several drugs have had their bioavailability increased. Despite having several pharmacological properties, luteolin's limited solubility limits both its bioavailability and its utilisation. Self-nanoemulsifying drug delivery systems (SNEDDS) were created to solve this issue. This study thus involved the formulation and evaluation of luteolin-loaded self-nanoemulsifying drug delivery systems in terms of pharmacokinetics, toxicity, and in vivo antiulcer activity.
Methods:
Luteolin-SNEDDS were formulated by conducting solubility testing of luteolin in various excipients, constructing a pseudo-ternary phase diagram, and characterizing the systems using emulsification time, percentage transmittance, thermodynamic stability, droplet size, polydispersity index, and morphological analysis (TEM). Additionally, the luteolin-SNEDDS formulations were evaluated for acute oral toxicity, pharmacokinetic parameters, in vivo antiulcer efficacy, and antioxidant activity in stomach tissue.
results:
The luteolin-SNEDDS was prepared using Tween 80, propylene glycol, and olive oil as a surfactant, co-surfactant, and oil phase, respectively. The emulsification ability and droplet size were then optimised. The resulting Luteolin-SNEDDS had an emulsification time of 10 s and a droplet size of less than 100 nm. The pharmacokinetic investigation demonstrated enhanced systemic drug absorption, which raises oral bioavailability, and additional assessments revealed that these luteolin-SNEDDS are totally safe. On stomach tissue, luteolin-SNEDDS demonstrated strong anti-ulcer and in vivo antioxidant properties.
Results:
The luteolin-SNEDDS was prepared using Tween 80, propylene glycol, and olive oil as surfactant, co-surfactant, and oil phase, respectively. The emulsification ability and droplet size were then optimised. The resulting luteolin-SNEDDS formulations had an emulsification time of 10 seconds and a droplet size of less than 100 nm. The pharmacokinetic investigation demonstrated enhanced systemic drug absorption, raising oral bioavailability, and additional assessments revealed these luteolin-SNEDDS as safe. On stomach tissue, luteolin-SNEDDS demonstrated strong anti-ulcer and in vivo antioxidant properties.
Discussion:
The luteolin-loaded SNEDDS significantly improved luteolin’s solubility and oral bioavailability, as evidenced by rapid emulsification and nanoscale droplet formation. Pharmacokinetic results confirmed higher systemic exposure compared to pure luteolin. The formulation exhibited notable anti-ulcer and antioxidant effects in vivo, demonstrating therapeutic potential. Overall, luteolin-SNEDDS appeared to be a safe and effective strategy to enhance luteolin’s pharmacological applications.
Conclusion:
Luteolin's gastroprotective properties and anti-oxidative efficacy can be improved by SNEDDS, according to research, and it has a good probability of becoming a bioactive substance used as an anti-ulcer agent.