We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Development of Buccal Patches for Delivery of Darifenacin from Beta-Cyclodextrin Complexes.
- Authors
Jagdale, Swati C.; Mohanty, Prachyasuman; Chabukswar, Aniruddha R.; Kuchekar, Bhanudas S.
- Abstract
Drug-cyclodextrin complexes improve aqueous solubility and dissolution rate of poorly water-soluble drugs. Solubilisation followed by buccal delivery of poorly water-soluble drugs can be advantageous for increasing drug absorption. Darifenacin is an antispasmodic used against urinary incontinence and specifically blocks M3 muscarinic acetylcholine receptors in smooth muscle. M3 receptors are mainly located in exocrine glands, smooth muscle and vascular endothelium. The oral absorption of darifenacin is poor owing to its low solubility. It also has poor bioavailability (15-19%) due to a high rate of first-pass metabolism. Complexation with beta-cyclodextrin was carried out to enhance solubility. The best results were obtained by co-grinding in a 1:1 molar ratio of drug: β-cyclodextrin. The solid inclusion complexes were characterized by DSC, X-ray diffractometry and FTIR. Inclusion complexes showed higher dissolution rates than the pure drug. Controlled-release mucoadhesive patches were prepared with two hydroxypropyl methylcellulose (HPMC) polymers, K100M CR and K15. The patches were assessed for surface pH, folding endurance, swelling, mucoadhesive properties, in-vitro residence time, vapor transmission test and in-vitro (cellophane, egg membrane) and ex-vivo (goat buccal mucosa) release. Formulations Ha2 (2%) HPMC K100M CR and Pa4 (4%) HPMC K15 showed good mucoadhesive strength, in-vitro and ex-vivo residence times, with controlled release for 10 hours.
- Subjects
BUCCAL administration; DRUG delivery systems; CYCLODEXTRINS in pharmaceutical technology; BENZOFURANS; DRUG solubility; DRUG bioavailability
- Publication
Revista de Ciências Farmacêuticas Básica e Aplicada, 2014, Vol 35, Issue 1, p29
- ISSN
1808-4532
- Publication type
Article