Abstract

Background: The choice of lipid excipients and their origin are crucial determinant factors in the design of self-nanoemulsifying drug delivery system (SNEDDS).Aim: To investigate the aspects of alternative excipients which can influence the development of efficient SNEDDS and determine the fate of fenofibrate in aqueous media.Methods: SNEDDS of two groups (a and b) were developed using Cremercoor MCT/Capmul MCM and Kollisolv MCT/Imwitor 742 blended oils and water soluble surfactants (to improve lipid polarity) for the model anti-cholesterol drug fenofibrate. Visual assessment was employed and droplet size measurement was taken into initial consideration for optimized SNEDDS. Further SNEDDS optimizations were done on the basis of maximum drug loading by equilibrium solubility studies and maximum solubilized drug upon aqueous dispersion by dynamic dispersion studies. In vitro lipolysis was examined under simulated Fed and Fasted conditions. Intestinal permeability study of the optimal SNEDDS formulation was compared with the raw fenofibrate dispersion using non- everted “intestinal sac technique.”Results: Initial characterization and solubility studies showed that mixed glycerides of Kollisolv MCT/Imwitor 742 (group b) containing formulations generated highly efficient SNEDDS as they are stable and produced lower nanodroplets with higher drug loading (group b) as compared to mixed glycerides of Cremercoor MCT/Capmul MCM (group a). In vitro dispersion and digestion studies confirmed that SNEDDS of group b (polar mixed glycerides) can retain high amount of drug (99% drug in solution for more than 24 h time) in dispersion media and have high recovery after digestion. The results from the permeability assessment confirmed that fenofibrate had 4.3-fold increase with F3b SNEDDS compared with the control.Conclusion: SNEDDS formulations containing alternative excipients (Kollisolv MCT/Imwitor 742 blend) could be a potential oral pharmaceutical product in taking anti-hyperlipidaemic agent fenofibrate to the systemic circulation as solubilized form.

Highlights

  • Hyperlipidaemia is defined as elevated lipid concentration in bloodstream

  • The most attractive Self-nanoemulsifying drug delivery systems (SNEDDS) formulations, which belong to LFCS Type III systems were investigated carefully using fenofibrate

  • Droplet Size Measurement, Polydispersity Index (PDI) and Zeta Potential The droplet size of the self-emulsifying formulations and the use of excipients in formulation is a crucial factor to its performance by which the rate and extent of drug release as well as absorption can be estimated (Gursoy and Benita, 2004)

Read more

Summary

Introduction

Hyperlipidaemia is defined as elevated lipid concentration in bloodstream. It is manifested clinically as hypercholesterolemia or hypertriglyceridemia. Plasma proteins with which lipids are associated and remain in the dissolved form in blood are called lipoproteins (Najib, 2002; Cho and Park, 2014). Hyperlipidaemia is the prime risk factor for atherosclerosis and cardiovascular disease which caused approximately 800,000 deaths in 2005 as first killer in United States (Farnier et al, 2007) with yet increasing number of incidents. 33.5% of adults in United States and 50% adults in Saudi Arabia have high cholesterol level (Najib, 2002), which possesses a significant threat and can cause considerable deaths in the regions. The choice of lipid excipients and their origin are crucial determinant factors in the design of self-nanoemulsifying drug delivery system (SNEDDS)

Objectives
Methods
Results
Conclusion
Full Text
Published version (Free)

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call