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 in questo prodotto:
File Dimensione Formato  
Investigating the prilling-vibration technique to produce gastric-directed drug delivery systems for misoprostol.pdf

accesso aperto

Licenza: Creative commons
Dimensione 4.33 MB
Formato Adobe PDF
4.33 MB Adobe PDF Visualizza/Apri

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11586/470601
Citazioni
  • ???jsp.display-item.citation.pmc??? 0
  • Scopus 4
  • ???jsp.display-item.citation.isi??? 4
social impact