Background: Buccal delivery of drugs can be used as an alternative administration route to conventional oral route avoiding the liver first-pass effect and improving patient compliance. Objective: The goal of this work was to develop dry emulsions for buccal delivery of ketoprofen, used as a lipophilic model drug. The influence of two vegetable oils, olive oil or wheat germ oil, in the pres-ence of α-cyclodextrin and different drying techniques on the dry emulsion properties was evaluated. Methods: Emulsions were prepared by adding olive oil or wheat germ oil to an aqueous solution of α-cyclodextrin and subsequently dried through an oven, freeze-dryer or spray-dryer. Dry emulsions were characterized in terms of yield, encapsulation efficiency, morphology and drug solid-state. In vitro drug release and permeation studies were carried out to evaluate dry emulsion ability to release the drug and to allow its permeation through the esophageal porcine epithelium. Results: The formation of stable and milky emulsion was assured by cyclodextrin ability to interact with oil components obtaining an inclusion complex with amphiphilic property able to act as a surface-active agent. The drying process influenced the yield and the encapsulation efficiency, while no signifi-cant differences were observed between olive oil and wheat germ oil. Freeze-dried emulsions, selected as the best formulations, resulted in fast release of drug thereby ensuring its permeation across the epi-thelium. Conclusion: Dry emulsions prepared with a simple and easy method, using natural ingredients and avoiding synthetic surfactants and organic solvents, could be used for buccal delivery of lipophilic drugs.

Dry emulsions based on alpha cyclodextrin and vegetable oils for buccal delivery of lipophilic drugs

Dalena F.;Nicoletta F. P.;
2020

Abstract

Background: Buccal delivery of drugs can be used as an alternative administration route to conventional oral route avoiding the liver first-pass effect and improving patient compliance. Objective: The goal of this work was to develop dry emulsions for buccal delivery of ketoprofen, used as a lipophilic model drug. The influence of two vegetable oils, olive oil or wheat germ oil, in the pres-ence of α-cyclodextrin and different drying techniques on the dry emulsion properties was evaluated. Methods: Emulsions were prepared by adding olive oil or wheat germ oil to an aqueous solution of α-cyclodextrin and subsequently dried through an oven, freeze-dryer or spray-dryer. Dry emulsions were characterized in terms of yield, encapsulation efficiency, morphology and drug solid-state. In vitro drug release and permeation studies were carried out to evaluate dry emulsion ability to release the drug and to allow its permeation through the esophageal porcine epithelium. Results: The formation of stable and milky emulsion was assured by cyclodextrin ability to interact with oil components obtaining an inclusion complex with amphiphilic property able to act as a surface-active agent. The drying process influenced the yield and the encapsulation efficiency, while no signifi-cant differences were observed between olive oil and wheat germ oil. Freeze-dried emulsions, selected as the best formulations, resulted in fast release of drug thereby ensuring its permeation across the epi-thelium. Conclusion: Dry emulsions prepared with a simple and easy method, using natural ingredients and avoiding synthetic surfactants and organic solvents, could be used for buccal delivery of lipophilic drugs.
Dry emulsions
Freeze-drying
Ketoprofen
Olive oil
Spray-drying
Wheat germ oil
α-cyclodextrin
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/309428
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