Conversion of sustained release omeprazole loaded buccal films into fast dissolving strips using supercritical carbon dioxide (scCO2) processing, for potential paediatric drug delivery

Abstract

This study involves the development of thin oral solvent cast films for the potential delivery of the proton pump inhibitor, omeprazole (OME) via the buccal mucosa for paediatric patients. OME containing films were prepared from ethanolic gels (1% w/w) of metolose (MET) with polyethylene glycol (PEG 400) (0.5% w/w) as plasticiser, and L-arg (0.2% w/w) as a stabilizer and dried in an oven at 40°C. The blank and drug loaded films were divided into two groups, one group was subjected to supercritical carbon dioxide (scCO2) treatment and the other group untreated. The untreated and scCO2 treated films were then characterised using differential scanning calorimetry, thermogravimetric analysis, scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, hydration (swelling), mucoadhesion and in vitro drug dissolution studies. Treatment of the solvent cast films with scCO2 caused significant changes to the functional and physical properties of the MET films. The original drug loaded MET films showed a sustained release of OME (1 hour), whereas scCO2 treatment of the formulations resulted in fast dissolving films with more than 90% drug release within 15 minutes.

Effects of Cyclodextrins (β and γ) and l-Arginine on Stability and Functional Properties of Mucoadhesive Buccal Films Loaded with Omeprazole for Pediatric Patients

“…Solvent cast films were formulated from ethanolic gels of the mucoadhesive polymer (MET) and loaded with drug (OME) as previously reported [17]. Briefly, the OME was dissolved in 20% v / v EtOH together with βCD or γCD at different ratios to form an OME solution as summarized in Table 1a.…”

“…To avoid such stomach acid breakdown, OME is formulated as enteric-coated granules in the form of capsules [2]. As a result, alternative formulations for administration via non-enteric routes such as buccal mucosa have been proposed [16,17]. These notwithstanding, the physical instability of OME remains an issue during formulation and storage and therefore requires stabilizing agents such as l -arginine and cyclodextrins.…”