Enhanced Bioavailability of Nimodipine from Bioadhesive Buccal Bilayered Patches in Human Volunteers.
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Date
2013-10
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Abstract
Aims: The objective of the present study was to develop a bioadhesive bilayered buccal
patch of Nimodipine (15 mg) using Eudragit Rs 100 as secondary layer and a primary
layer with Hydroxy propyl methyl cellulose and Hydroxy propyl cellulose JF.
Methodology: Bilayered buccal patches were prepared by solvent casting technique. The
absence of physiochemical interactions between NMDP and the polymer were
investigated by differential scanning calorimetry (DSC). Bilayered buccal patches of
NMDP were evaluated for in vitro drug permeation through porcine buccal membrane, in
vitro drug release, moisture absorption, surface pH, mechanical properties and in vitro
bioadhesion.
Results: The results indicated that suitable bioadhesive bilayered buccal patches with
desired permeability could be prepared. The bioavailability study was performed in
healthy humans in a crossover experimental design. Bioavailability studies revealed that
nimodipine possessed good buccal absorption. The relative bioavailability of the optimized
buccal patch was found to be 205% in comparison to 30 mg marketed oral tablet. The
formulation CC3 showed 68.84 ± 1.4% release and 46.85 ± 5.1% of drug permeated through porcine buccal membrane in 4 hr. A good correlation was seen between
percentage in vitro release the extent of bioavailability for nimodine buccal patch.
Conclusion: An improvement of bioavailability was obtained by buccal route to the extent
of 2.05 times higher than that of oral route for NMDP. Hence, the development of a
bioadhesive bilayered buccal patch for NMDP might be a promising one, as the necessary
dose of drug could be decreased, resulting less side effects. Good ex vivo - in vivo
correlation was obtained for NMDP.
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Keywords
Bilayered buccal patches, nimodipine, bioadhesion, mechanical properties, bioavailbility, In vitro- In vivo correlation
Citation
Vishnu Y Vamshi, Kishan V, Rao Y Madhusudan. Enhanced Bioavailability of Nimodipine from Bioadhesive Buccal Bilayered Patches in Human Volunteers. British Journal of Pharmaceutical Research. 2013 Oct; 3(4): 1015-1030.