Prilling/vibration technique to produce oral microcapsules was explored to achieve local delivery of misoprostol (MIS), a prostaglandin E1 analogue indicated for the treatment of gastric-duodenal ulcers, at the gastric mucosa. To improve MIS chemical stability and reduce its associated systemic side effects, drug delivery systems were designed and developed as microcapsules consisting of a core of sunflower oil and MIS (F-s6 and F-s14) or a MIS complex with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) (F-s18), confirmed by specific studies, and a polymeric shell. The produced microcapsules showed high encapsulation efficiencies for those with MIS solubilized in sunflower oil (>59.86 %) and for the microcapsules with MIS/HP-beta-CD (97.61 %). To demonstrate the ability of these systems to deliver MIS into the stomach, swelling and drug release experiments were also conducted in simulated gastric fluid. Among the three formulations, F-S18 showed gastric release within 30 min and was the most advantageous formulation because the presence of the MIS/HP-beta-CD inclusion complex ensured a greater ability to stabilise MIS in the simulated gastric environment. In addition, these new systems have a small size (<540 m), and good flow properties and the dose of the drug could be easily adapted using different amounts of microcapsules (flexibility), making them a passepartout for different age population groups.
Investigating the prilling/vibration technique to produce gastric-directed drug delivery systems for misoprostol
D'Amico V.Writing – Original Draft Preparation
;Denora N.Conceptualization
;Ivone M.;Iacobazzi R. M.;Laquintana V.;Cutrignelli A.;Franco M.;Barone M.;Lopalco A.
Conceptualization
;Lopedota A. A.Conceptualization
2024-01-01
Abstract
Prilling/vibration technique to produce oral microcapsules was explored to achieve local delivery of misoprostol (MIS), a prostaglandin E1 analogue indicated for the treatment of gastric-duodenal ulcers, at the gastric mucosa. To improve MIS chemical stability and reduce its associated systemic side effects, drug delivery systems were designed and developed as microcapsules consisting of a core of sunflower oil and MIS (F-s6 and F-s14) or a MIS complex with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) (F-s18), confirmed by specific studies, and a polymeric shell. The produced microcapsules showed high encapsulation efficiencies for those with MIS solubilized in sunflower oil (>59.86 %) and for the microcapsules with MIS/HP-beta-CD (97.61 %). To demonstrate the ability of these systems to deliver MIS into the stomach, swelling and drug release experiments were also conducted in simulated gastric fluid. Among the three formulations, F-S18 showed gastric release within 30 min and was the most advantageous formulation because the presence of the MIS/HP-beta-CD inclusion complex ensured a greater ability to stabilise MIS in the simulated gastric environment. In addition, these new systems have a small size (<540 m), and good flow properties and the dose of the drug could be easily adapted using different amounts of microcapsules (flexibility), making them a passepartout for different age population groups.File | Dimensione | Formato | |
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Investigating the prilling-vibration technique to produce gastric-directed drug delivery systems for misoprostol.pdf
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