Bioadhesive Drug Delivery System for Enhancing the Permeability of a BCS Class III Drug via Hot-Melt Extrusion Technology View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2017-10

AUTHORS

Nicole S. Mendonsa, Priyanka Thipsay, Dong Wuk Kim, Scott T. Martin, Michael A. Repka

ABSTRACT

As the buccal route of administration has the ability to avoid the GI tract and first-pass effect by directing the absorption toward the cheek area, the bioavailability of BCS class III drugs can be increased through this route. Only a handful of studies have been conducted using oleic acid as a permeation enhancer in any transbuccal drug delivery system. Therefore, the objectives of this novel study were to develop a buccal tablet using two concentrations of oleic acid for a model BCS class III drug via hot-melt extrusion technology and to investigate the effects of oleic acid on the physicochemical properties of the tablet. The model drug selected was ondansetron hydrochloride. Formulations consisting of polymers (hydroxypropyl methylcellulose and polyethylene oxide) and two concentrations of oleic acid were prepared by hot-melt extrusion techniques. A melting point depression of the drug was obtained in the extruded granules as seen by the DSC thermograms. The ex vivo permeation studies showed a greater permeation of the drug in the formulation containing 10% oleic acid (F2) as compared to the formulation containing 20% oleic acid (F1), although not statistically significant. The in vitro bioadhesion studies, swelling studies, and surface pH measurements of the tablets were also conducted. In conclusion, permeation studies exhibited the potential of oleic acid as a buccal permeation enhancer as a significant permeation of the drug was obtained in the formulations. Hot-melt extrusion technology was successfully employed to formulate buccal tablets of ondansetron hydrochloride. More... »

PAGES

2639-2647

Identifiers

URI

http://scigraph.springernature.com/pub.10.1208/s12249-017-0728-y

DOI

http://dx.doi.org/10.1208/s12249-017-0728-y

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1084255437

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/28247291


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53 schema:description As the buccal route of administration has the ability to avoid the GI tract and first-pass effect by directing the absorption toward the cheek area, the bioavailability of BCS class III drugs can be increased through this route. Only a handful of studies have been conducted using oleic acid as a permeation enhancer in any transbuccal drug delivery system. Therefore, the objectives of this novel study were to develop a buccal tablet using two concentrations of oleic acid for a model BCS class III drug via hot-melt extrusion technology and to investigate the effects of oleic acid on the physicochemical properties of the tablet. The model drug selected was ondansetron hydrochloride. Formulations consisting of polymers (hydroxypropyl methylcellulose and polyethylene oxide) and two concentrations of oleic acid were prepared by hot-melt extrusion techniques. A melting point depression of the drug was obtained in the extruded granules as seen by the DSC thermograms. The ex vivo permeation studies showed a greater permeation of the drug in the formulation containing 10% oleic acid (F2) as compared to the formulation containing 20% oleic acid (F1), although not statistically significant. The in vitro bioadhesion studies, swelling studies, and surface pH measurements of the tablets were also conducted. In conclusion, permeation studies exhibited the potential of oleic acid as a buccal permeation enhancer as a significant permeation of the drug was obtained in the formulations. Hot-melt extrusion technology was successfully employed to formulate buccal tablets of ondansetron hydrochloride.
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