Formulation of spray congealed microparticles with self-emulsifying ability for enhanced glibenclamide dissolution performance

Abstract

Purpose: To develop a novel preparation approach of solid Self-Emulsifying Drug Delivery System (s-SEDDS) based on spray congealing as potential drug delivery technology for poorly water-soluble drug Glibenclamide (GBD). Methods: Several systems were formulated using suitable excipients, solid at room temperature, with different hydrophilic–lipophilic balance, such as Myverol, Myvatex, Gelucire®50/13 and Gelucire®44/14. Cremophor®EL and Poloxamer 188 were selected as surfactants and PEG 4000 as co-solvent. Results: The screening of the best carrier for s-SEDDS manufacturing revealed that Gelucire®50/13 had greater performance. Then, surfactant–co-solvent systems were developed. Dissolution studies showed that all the formulations promoted the solubilisation performance of the GBD with respect to pure drug; in particular the formulation containing Gelucire®50/13 and PEG 4000 increased the drug solubilisation of five times. These microparticles showed self-dispersibility within 60 min and micelles dimensions around 360 nm. Conclusions: Spray congealing is a promising novel manufacturing technique of solid self-emulsifying systems.

• Dissolution profiles
• poorly water-soluble drug
• solid SEDDS
• spray congealing
• surfactant–co-solvent systems

Declaration of interest

The authors report no declarations of interest.