Design and Characterization of Agarose/HPMC Buccal Films Bearing Ondansetron HCl In Vitro and In Vivo: Enhancement Using Iontophoretic and Chemical Approaches

Abstract

The study was aimed at designing and characterizing the ondansetron hydrochloride (OND) bearing agarose (AG), and hydroxypropyl methyl cellulose (HPMC) mucoadhesive buccal films employing glycerol as a plasticizer. The buccal delivery of ondansetron hydrochloride was remarkably boosted by employing physical (iontophoresis) and chemical enhancement approaches (chemical penetration enhancers). To explore the influence of different formulation components, i.e., agarose, hydroxypropyl methyl cellulose (HPMC), and glycerol on various evaluating parameters, i.e., tensile strength, swelling index, ex vivo mucoadhesion time, and subsequently on in vitro drug release, a D-optimal design was opted. A buccal film bearing OND was mounted on bovine buccal mucosa for ex vivo permeation studies and impact of chemical and physical enhancement techniques on the permeation profile was also analysed. A linear release profile was revealed in in vitro drug release of OND over 60 minutes and outcomes ascertained the direct relationship between HPMC content and in vitro drug release and inverse relationship was depicted by AG content. The FTIR and DSC thermal analysis was executed to determine the physicochemical interactions and results exposed no chemical interactions between drug and polymers. The drug (OND) appeared as tiny crystals on smooth film surface during scanning electron microscopy (SEM) analysis. A notable enhancement in permeation flux, i.e., 761.02 μg/min of OND during ex vivo permeation studies was witnessed after the application of current (0.5-1 mA) without any time lag and with enhancement ratio of 3.107. A time lag of 15 minutes, 19 minutes, and 26 minutes with permeation flux of 475.34 μg/min, 399.35 μg/min, and 244.81 μg/min was observed after chemical enhancer pretreatment with propylene glycol, Tween 80, and passive, respectively. Rabbit was employed as the experimental animal for pharmacokinetic studies (in vivo) and cats for pharmacological activity (in vivo), and the results illustrated the enhanced bioavailablity (2.88 times) in the iontophoresis animal group when compared with the rabbits of control group. Likewise, a remarkable reduction in emesis events was recorded in cats of iontophoresis group. Conclusively, the histopathological examinations on excised buccal mucosa unveiled no severe necrotic or cytopathetic outcomes of current.

Evaluation of Usnea barbata (L.) Weber ex F.H. Wigg Extract in Canola Oil Loaded in Bioadhesive Oral Films for Potential Applications in Oral Cavity Infections and Malignancy

“…The X-ray diffractograms of R and F-UBO exhibited two peaks at 2θ = 8° and 2θ = 20°. They represent the prominent HPMC XRD peaks, portraying their semicrystalline structure [ 62 , 63 ]. The peak at 2θ = 22° is attributed to P407 [ 64 ].…”

Design, Characterization, and Anticancer and Antimicrobial Activities of Mucoadhesive Oral Patches Loaded with Usnea barbata (L.) F. H. Wigg Ethanol Extract F-UBE-HPMC

“…The X-ray diffractograms of R and F-UBE-HPMC are presented in Figure 2 c. The X-ray diffraction patterns of the Reference and F-UBE-HPMC ( Figure 2 c) show that both mucoadhesive oral patches exhibited the characteristic diffraction peaks of HPMC at 2θ = 8° and 2θ = 20° [ 67 ]. A careful analysis of their XRD patterns indicates that the amorphous region peak (2θ = 8°) and crystalline region (2θ = 20°) decrease in their intensities due to the UBE blending in the polymer matrix in the case of F-UBE-HPMC ( Figure 2 c).…”

Three-Dimensional Printing Technologies in Oral Films Manufacturing—A Minireview

“…They release the drug when placed in the oral cavity by dissolving or adhering to the buccal mucosa [5]. Their action can be topical [6][7][8] or systemic [9][10][11]. The variety of active ingredients contained in OF is wide: plant extracts [12][13][14][15], herbal compounds [16][17][18], nutraceuticals [19], conventional drugs [20][21][22][23][24][25][26], antibiotics [27], antivirals [28,29], vaccines [30], insulin [31], and other proteins [32].…”