Impact of various solid carriers and spray drying on pre/post compression properties of solid SNEDDS loaded with glimepiride: in vitro-ex vivo evaluation and cytotoxicity assessment

Abstract

Development of self-nanoemulsifying drug delivery systems (SNEDDS) of glimepiride is reported with the aim to achieve its oral delivery. Lauroglycol FCC, Tween-80, and ethanol were used as oil, surfactant, and co-surfactant, respectively as independent variables. The optimized composition of SNEDDS formulation (F1) was 10% v/v Lauroglycol FCC, 45% v/v Tween 80, 45% v/v ethanol, and 0.005% w/v glimepiride. Further, the optimized liquid SNEDDS were solidified through spray drying using various hydrophilic and hydrophobic carriers. Among the various carriers, Aerosil 200 was found to provide desirable flow, compression, dissolution, and diffusion. Both, liquid and solid-SNEDDS have shown release of more than 90% within 10 min. Results of permeation studies performed on Caco-2 cell showed that optimized SNEDDS exhibited 1.54 times higher drug permeation amount and 0.57 times lower drug excretion amount than that of market tablets at 4 hours (p < .01). Further, the cytotoxicity study performed on Caco-2 cell revealed that the cell viability was lower in SNEDDS (92.22% ± 4.18%) compared with the market tablets (95.54% ± 3.22%; p > .05, i.e. 0.74). The formulation was found stable with temperature variation and freeze thaw cycles in terms of droplet size, zeta potential, drug precipitation and phase separation. Crystalline glimepiride was observed in amorphous state in solid SNEDDS when characterized through DSC, PXRD, and FT-IR studies. The study revealed successful formulation of SNEDDS for glimepiride.

Coadministration of Polypeptide-k and Curcumin Through Solid Self-Nanoemulsifying Drug Delivery System for Better Therapeutic Effect Against Diabetes Mellitus: Formulation, Optimization, Biopharmaceutical Characterization, and Pharmacodynamic Assessment

“…To each formulation, 30 mg PPK and 2.75 mg CRM were added. 5,21 The obtained results were correlated with the theoretical values of responses that were obtained through BBD.…”

“…12,18 This indicated that the emulsions were found stable. 5,21 Moreover, cloud point temperature of emulsions was within the range of 85.34°C-96.32°C ( Table 3). The stability of emulsions above 37°C indicate that they will be stable in gastrointestinal tract (GIT) upon oral administration.…”

“…The study was carried out in hexaplicate and mean data -SD (standard deviation) was recorded. 5,21,24,25 Ex vivo diffusion studies. Intestine of 24-h fasting goat was collected from a local slaughterhouse and used for permeation study.…”

“…The study was performed three times and mean data with SD were recorded. 5,21 Stability studies of S-SNEDDS. The stability studies were carried out for optimized batch of S-SNEDDS powder and tablets at 5°C -3°C, 25°C -2°°/65% R.H. -5% R.H., and 40°C -2°C/75% R.H. -5% R.H., in the stability chamber (Remi Electrotechnik, Mumbai, India) for 180 days, respectively.…”

“…The results of their freshly prepared formulations were used as standard to compare the results of samples kept for stability studies. 5,21 In Vivo Studies The result of dissolution and ex vivo diffusion studies showed absence in drug release and diffusion profiles of liquid formulation, powder formulation their tablets. Hence, the powder formulation was used for animal studies due to ease of administration.…”