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. 2013:2013:983702.
doi: 10.1155/2013/983702. Epub 2012 Oct 22.

Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes

Swati C Jagdale  1 , Prachyasuman Mohanty  1 , Aniruddha R Chabukswar  1 , Bhanudas S Kuchekar  1
Affiliations

Dissolution Rate Enhancement, Design and Development of Buccal Drug Delivery of Darifenacin Hydroxypropyl β-Cyclodextrin Inclusion Complexes

Swati C Jagdale et al. J Pharm (Cairo). 2013.

Abstract

Darifenacin is a urinary antispasmodic. The oral absorption of darifenacin is poor due to its low solubility and poor bioavailability (15-19%). Darifenacin was complexed with hydroxylropyl beta-cyclodextrin (Hpβ-CD). The best results were obtained with the coevaporation that interacts in a 1 : 1 drug : cyclodextrin molar ratio. The solid inclusion complexes were found to be amorphous in the characterization. The dissolution rate of darifenacin from the Hpβ-CD solid inclusion complex was increased compared to the powdered drug. The controlled release buccoadhesive patches for the delivery of darifenacin were prepared using HPMC K100M CR and HPMC K15. The coevaporation complex of the drug was used in the formulation due to its increased saturation solubility and increased ease of dissolution. The patches were evaluated for their surface pH, folding endurance, swelling, mucoadhesive properties, in vitro residence time, vapour transmission test, and in vitro and ex vivo release studies. Formulations Hb2 (2%) and Pb4 (4%) were found to be optimized. These two formulations can be used for buccal delivery of darifenacin which avoids first pass effect and leads to increased bioavailability of darifenacin.

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Figures

Figure 1
Figure 1
Phase solubility diagram of the darifenacin-Hpβ-CD system.
Figure 2
Figure 2
Differential scanning calorimetry (DSC) of darifenacin and HpβCD complex. (a) Darifenacin, (b) physical mixture, (c) coevaporation complex.
Figure 3
Figure 3
X-ray diffractometry of (a) darifenacin, (b) coevaporation complex and (c) physical mixture complex.
Figure 4
Figure 4
FTIR spectra of darifenacin and complexes. (a) Darifenacin, (b) physical mixture, (c) co-grounding complex, (d) coevaporation, (e) freeze dried, (f) spray dried, (g) melting method, (h) kneading method.
Figure 5
Figure 5
Dissolution profile of different complexes of darifenacin-Hpβ-CD in pH 6.8 buffer.
Figure 6
Figure 6
In vitro release profile of different formulations of HPMC K100 M CR containing Hpβ-CD-darifenacin complex. Hb1–Hb5 formulations of HPMC K100 M CR containaing 1%–5% of the polymer, D-formulation containing pure drug.
Figure 7
Figure 7
In vitro release profile of different formulations of HPMC K15 containing Hpβ-CD-darifenacin complex. Pa1–Pa5 formulations of HPMC K15 containaing 1%–5% of the polymer, D-formulation containing pure drug.
Figure 8
Figure 8
Drug diffusion study through goat buccal membrane and egg membrane (eg: egg membrane diffusion, buc: buccal membrane diffusion, ce: cellophane membrane).
Figure 9
Figure 9
FTIR spectra of darifenacin and formulations. (a) Darifenacin, (b) drug-Hpβ-CD complex with HPMC K15, (c) drug-Hpβ-CD complex with HPMC K100 M CR.
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