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. 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 cosolvent. Results: The screening of the best carrier for s-SEDDS manufacturing revealed that Gelucire®50/13 had greater performance. Then, surfactant-cosolvent systems were developed. Dissolution studies showed that all the formulations promoted the solubilization 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 minutes and micelles dimensions around 360 nm. Conclusions: spray congealing is a promising novel manufacturing technique of solid self-emulsifying systems.
Beatrice Albertini, Marcello Di Sabatino, Cecilia Melegari, Nadia Passerini (2015). Formulation of spray congealed microparticles with self-emulsifying ability for enhanced glibenclamide dissolution performance. JOURNAL OF MICROENCAPSULATION, 32(2), 181-192 [10.3109/02652048.2014.985341].
Formulation of spray congealed microparticles with self-emulsifying ability for enhanced glibenclamide dissolution performance
ALBERTINI, BEATRICE;MELEGARI, CECILIA;PASSERINI, NADIA
2015
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. 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 cosolvent. Results: The screening of the best carrier for s-SEDDS manufacturing revealed that Gelucire®50/13 had greater performance. Then, surfactant-cosolvent systems were developed. Dissolution studies showed that all the formulations promoted the solubilization 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 minutes and micelles dimensions around 360 nm. Conclusions: spray congealing is a promising novel manufacturing technique of solid self-emulsifying systems.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
