Dry Gel Containing Optimized Felodipine-Loaded Transferosomes: a Promising Transdermal Delivery System to Enhance Drug Bioavailability

Citation:
Kassem, M. A., M. H. Aboul-Einien, and M. M. E. Taweel, "Dry Gel Containing Optimized Felodipine-Loaded Transferosomes: a Promising Transdermal Delivery System to Enhance Drug Bioavailability", AAPS PharmSciTech, vol. Vol. 19, issue No. 5,, pp. 2155-2173, 2018.

Abstract:

Abstract. Felodipine has a very low bioavailability due to first-pass metabolism. The aim
of this study was to enhance its bioavailability by transdermal application. Felodipine-loaded
transferosomes were prepared by thin-film hydration using different formulation variables.
An optimized formula was designed using statistical experimental design. The independent
variables were the used edge activator, its molar ratio to phosphatidylcholine, and presence
or absence of cholesterol. The responses were entrapment efficiency of transferosomes, their
size, polydispersity index, zeta potential, and percent drug released after 8 h. The optimized
formula was subjected to differential scanning calorimetry studies and its stability on storage
at 4┬░C for 6 months was estimated. This formula was improved by incorporation of different
permeation enhancers where ex vivo drug flux through mice skin was estimated and the best
improved formula was formulated in a gel and lyophilized. The prepared gel was subjected to
in vivo study using Plendil® tablets as a reference. According to the calculated desirability,
the optimized transferosome formula was that containing sodium deoxycholate as edge
activator at 5:1 M ratio to phosphatidylcholine and no cholesterol. The thermograms of this
formula indicated the incorporation of felodipine inside the prepared vesicles. None of the
tested parameters differed significantly on storage. The lyophilized gel of labrasol-containing
formula was chosen for in vivo study. The relative bioavailability of felodipine from the
designed gel was 1.7. In conclusion, topically applied lyophilized gel containing felodipineloaded
transferosomes is a promising transdermal delivery system to enhance its
bioavailability.

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