Title:Dry Emulsions based on Alpha Cyclodextrin and Vegetable Oils for Buccal Delivery of Lipophilic Drugs
VOLUME: 10 ISSUE: 3
Author(s):Angela Abruzzo, Bruno Saladini, Francesco Dalena, Fiore P. Nicoletta, Barbara Luppi, Federica Bigucci and Teresa Cerchiara*
Affiliation:Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127, Bologna, PolyCrystalLine SpA, Via F.S. Fabri 127/1, 40059, Medicina, Bologna, Department of Chemistry and Chemical Technology, University of Calabria, Via P. Bucci, Cubo 15D, 87036, Arcavacata di Rende, Cosenza, Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Edificio Polifunzionale, 87036, Arcavacata di Rende, Cosenza, Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127, Bologna, Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127, Bologna, Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, Via San Donato 19/2, 40127, Bologna
Keywords:Ketoprofen, α-cyclodextrin, olive oil, wheat germ oil, dry emulsions, freeze-drying, spray-drying.
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 presence
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 surfaceactive
agent. The drying process influenced the yield and the encapsulation efficiency, while no significant
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 epithelium.
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.
