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

Abstract

Omeprazole (OME) is employed for treating ulcer in children, but is unstable and exhibits first pass metabolism via the oral route. This study aimed to stabilize OME within mucoadhesive metolose (MET) films by combining cyclodextrins (CD) and L-arginine (L-arg) as stabilizing excipients and functionally characterizing for potential delivery via the buccal mucosa of paediatric patients. Polymeric solutions at a concentration of 1% w/w were obtained by dispersing the required weight of metolose in 20% v/v ethanol as solvent at a temperature of 40 • C using polyethylene glycol (PEG 400) (0.5% w/w) as plasticizer. The films were obtained by drying the resulting polymer solutions at in an oven at 40 • C. Textural (tensile and mucoadhesion) properties, physical form (differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy), residual moisture content (thermogravimetric analysis (TGA)) and surface morphology (scanning electron microscopy (SEM)) were investigated. Optimized formulations containing OME, CDs (β or γ) and L-arg (1:1:1) were selected to investigate the stabilization of the drug. The DSC, XRD, and FTIR showed possible molecular dispersion of OME in metolose film matrix. Plasticized MET films containing OME:βCD:L-arg 1:1:1 were optimum in terms of transparency and ease of handling and therefore further functionally characterized (hydration, mucoadhesion, in vitro drug dissolution and long term stability studies). The optimized formulation showed sustained drug release that was modelled by Korsmeyer-Peppas equation, while the OME showed stability under ambient temperature conditions for 28 days. The optimized OME loaded MET films stabilized with βCD and L-arg have potential for use as paediatric mucoadhesive buccal delivery system, which avoids degradation in the stomach acid as well as first pass metabolism in the liver.

Beneficial Effect of β‐Cyclodextrin Assisted Synthesis of CuO/Hydroxyapatite Catalyst in Toluene Oxidation

“…[36] The mean crystallite size of copper hydroxynitrate, based on the Scherrer equation from the peak located at 2θ = 12.8°, is of the same order of magnitude for the 10 Cu/Hap D and 10 Cu-CD/Hap D samples with values of 84 nm and 96 nm, respectively. The presence of multiple peaks in the 10-25°2θ range characteristic of the XRD pattern of pure β-CD (Figure 1-b) in accordance with literature reports [37][38] are not observed for 10 Cu-CD/Hap D sample, suggesting a homogeneous distribution of β-CD in the material.…”

Effects of Sucrose Palmitate on the Physico-Chemical and Mucoadhesive Properties of Buccal Films

“…The buccal administration of active ingredients by mucoadhesive films is one of the most innovative ways that can be used to achieve systemic drug delivery. Because of their ease of use, they have good patient compliance and can be used in elderly people, children [6], or patients with difficulty in swallowing. The great advantage of this administration route is that the active ingredient is introduced into the bloodstream without degradation and avoids the first-pass effect.…”

Development and Characterization of Inkjet Printed Edible Films for Buccal Delivery of B-Complex Vitamins

“…Buccal formulations are recommended for pediatric dosage forms as they are patient-friendly and adjustable to the different physiological and pharmacokinetic profiles of infants, children and adolescents [21]. Clobetasol, omeprazole, and hydrocortisone are representative model drugs which have been formulated for buccal delivery [22][23][24]. The applicability of various printing technologies for patient-centric buccal formulations has been demonstrated by previous reports, in terms of (i) incorporating personalized doses or thermolabile drugs, and (ii) fabricating multi-layered buccal films [4,8,9,25].…”