<p>Hexyl alginate derivative, an amphiphilic innovative buccal film-forming material of promising mechanical and release characteristics for the improvement of repaglinide bioavailability</p>

Abstract

BackgroundAssociation of long hydrocarbon chain with alginate molecule imparts surface active properties and increases chain flexibility.PurposeThis work studied the efficacy of synthesized hexyl alginate derivative as a film-forming material with unique amphiphilic and mechanical properties for the preparation of rapidly disintegrating repaglinide oral films with higher drug release rate and improved bioavailability.MethodsAlginate hexyl amide derivative was prepared and used in the formulation of oral films by solvent casting technique. Using Box–Behnken experimental design, formulations were optimized at different polymer, plasticizer, and disintegrant levels as independent variables for maximum drug release rate, higher tensile strength, and shortest disintegration time as responses. Optimized film formulae were fully evaluated and subjected to further in vivo bioavailability studies in rabbits.ResultsHigher dependency of response results on the selected variables was observed. Optimized formula showed satisfactory tensile strength (145.862 g/cm2), rapid disintegration (22.2 seconds), and higher drug release rate (97.799% within 30 minutes). The drug bioavailability was significantly improved in comparison with plain drug and conventional alginate oral films, where the AUC and Cmax values reached 296.072 μg.h/mL and 116.932 μg/mL in comparison with 164.917 μg.h/mL and 56.568 μg/mL for alginate film and 95.368 μg.h/mL and 31.925 μg/mL for plain drug, respectively. Tmax also showed significant reduction to be only 30 minutes in comparison with 60 minutes for other forms.ConclusionThis led to the final conclusion that the synthesized alginate derivative is an innovative promising film-forming material with unique mechanical and drug release properties for application in buccal drug delivery especially of Biopharmaceutics Classification System (BCS) class II drugs to increase solubility and improve bioavailability.

Sesame Oil-Based Nanostructured Lipid Carriers of Nicergoline, Intranasal Delivery System for Brain Targeting of Synergistic Cerebrovascular Protection

“…In polynomial model equation, A, B, and C represent the independent variables, while (AB, AC, and BC) and (A 2 , B 2 , and C 2 ) signify the interaction and quadratic terms, respectively [ 75 ]. Reproducibility of experimental results is affected with applied controllable factors, while variability results from uncontrollable factors, which is described as noise and measured in terms of adequate precision.…”

“…Significant changes in response values when the factor and/or its level changed indicates the suitability of the independent factors selection due to the high dependency of formulation characteristics (responses) on their values and levels. In polynomial model equation, A, B, and C represent the independent variables, while (AB, AC, and BC) and (A 2 , B 2 , and C 2 ) signify the interaction and quadratic terms, respectively [75]. Reproducibility of experimental results is affected with applied controllable factors, while variability results from uncontrollable factors, which is described as noise and measured in terms of adequate precision.…”

Development and Characterization of Ulvan Polysaccharides-Based Hydrogel Films for Potential Wound Dressing Applications

“…Plasticizers are the most important additive and almost always present in film formulations, especially films made from natural materials to improve the flexibility, elasticity, processability, and mechanical properties of polymers. 36,37 Glycerol is a polyol compound containing three hydroxyl groups in its molecule, when interspaced in the polysaccharide network, the distance between the polysaccharide chains increases, and direct interactions are reduced resulting in an increase in the elongation, 38,39 thickness, moisture content, solubility, and smooth surface structure. 40,41 In this work, we report the preparation and characterization of hydrogel films of Ulvan to be used as a dressing for wound healing applications.…”

Orodispersible Films: Current Innovations and Emerging Trends

“…Alginate is additionally employed in the preparation of ODFs as a film-forming agent, either independently or in conjunction with other polymers [ 39 ]. A film-forming alginate hexyl amide derivative was prepared and used to enhance the bioavailability of repaglinide [ 46 ]. Sodium alginate was used as a film-forming polymer by utilizing many drugs, namely nebivolol [ 47 ], cetirizine [ 48 ], and piroxicam [ 49 ].…”