The Studies of Phase Equilibria and Efficiency Assessment for Self-Emulsifying Lipid-Based Formulations

Abstract

The study was designed to build up a database for the evaluation of the self-emulsifying lipid formulations performance. A standard assessment method was constructed to evaluate the self-emulsifying efficiency of the formulations based on five parameters including excipients miscibility, spontaneity, dispersibility, homogeneity, and physical appearance. Equilibrium phase studies were conducted to investigate the phase changes of the anhydrous formulation in response to aqueous dilution. Droplet size studies were carried out to assess the influence of lipid and surfactant portions on the resulted droplet size upon aqueous dilution. Formulations containing mixed glycerides showed enhanced self-emulsification with both lipophilic and hydrophilic surfactants. Increasing the polarity of the lipid portion in the formulation leaded to progressive water solubilization capacity. In addition, formulations containing medium chain mixed glycerides and hydrophilic surfactants showed lower droplet size compared with their long chain and lipophilic counterparts. The inclusion of mixed glycerides in the lipid formulations enormously enhances the formulation efficiency.

Novel Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Oral Delivery of Cinnarizine: Design, Optimization, and In-Vitro Assessment

“…The formulations were diluted (in a ratio of 1:1,000v/v) and mixed for 1 min before testing (4,18). A full droplet size study was carried out for a wide range of formulations in the authors' recent study (19). The droplet size of selected formulations was presented and correlated with the findings of the current study.…”

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

“…A previously reported (Kommuru et al, 2001;Shahba, Mohsin, Alanazi, 2012b) visual test, used to assess self-emulsification efficiency, was modified and adopted for the current study. In accordance with routine practice, formulation dispersion in water was utilized as a fast and general tool to assess formulation self-emulsification efficiency.…”

“…Primarily, formulations were subjected to 1:400 aqueous dilution in a 50.0 mL glass beaker, and the contents were gently mixed (~500 rpm) using a magnetic stirrer (Nekkanti et al, 2010;Shahba, Mohsin, Alanazi, 2012b). Alternatively, formulations (20-30 mg) were diluted with 50.0 mL of 0.1 N HCl (pH 1.2) in order to mimic gastric pH.…”

“…The formulations were evaluated on the basis of performance indicator tools, such as excipient miscibility, spontaneity, and homogeneity/dispersibility (Shahba, Mohsin, Alanazi, 2012b).…”

“…Prior to OD measurement, drug free and/or drug equilibrated formulations were subjected to 1:400 aqueous dilutions in a 50.0 mL glass beaker, and the contents were gently mixed using a magnetic stirrer (~500 rpm) (Nekkanti et al, 2010;Shahba, Mohsin, Alanazi, 2012b). Formulation clarity was categorized according to the following OD 600 ranges: transparent: OD 600 = 0.00-0.05, bluish: OD 600 = 0.05-0.1, turbid: OD 600 = 0.1-0.3, and milky: OD 600 > 0.3 (Shahba, Mohsin, Alanazi, 2012b).…”