title: Preparation and in-vivo evaluation of dimenhydrinate buccal mucoadhesive films with enhanced bioavailability.
abstract: Dimenhydrinate (DMH)-loaded buccal bioadhesive films for the prevention and treatment of motion sickness were prepared and optimized. This study examines the rate of drug release from the films for prolonged periods of time to reduce or limit the frequency of DMH administration. Based on preliminary studies using various polymers and concentrations, hydroxyethylcellulose (2.5, 3.0, and 3.2%), and xanthan gum (2.8%) were chosen as matrix polymers. The films were analyzed with respect to their mechanical, physicochemical, bioadhesive, swelling, and in-vitro release properties. In in-vivo pharmacokinetic studies, xanthan gum-based DMH buccal film was associated with significantly increased DMH plasma levels between 1 h and 5 h after DMH dosing when compared with an oral drug solution. The area under the curve AUC0-7 h value of the mucoadhesive buccal film was two-fold higher than the oral DMH solution. Histological analysis revealed that DMH films cause mild morphological and inflammatory changes in rabbit buccal mucosa. The DMH buccal film is effective for approximately 7 h, thus representing an option for single-dose antiemetic therapy. This dosage regimen could be particularly beneficial for chain travelers who travel for long periods of time.
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey .
authors.forename: Ayca
authors.initials: A
authors.lastname: Yildiz Pekoz
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey .
authors.forename: Meryem
authors.initials: M
authors.lastname: Sedef Erdal
authors.affiliation: b Department of Pharmacology , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey .
authors.forename: Alper
authors.initials: A
authors.lastname: Okyar
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey .
authors.forename: Meltem
authors.initials: M
authors.lastname: Ocak
authors.affiliation: c Institute of Experimental Medicine (DETAE), Istanbul University , Capa , Istanbul , Turkey .
authors.forename: Fatma
authors.initials: F
authors.lastname: Tekeli
authors.affiliation: d Department of Biology , Faculty of Science, Istanbul University , Vezneciler-Istanbul , Turkey , and.
authors.forename: Engin
authors.initials: E
authors.lastname: Kaptan
authors.affiliation: e Department of Analytical Chemistry , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey.
authors.forename: Olcay
authors.initials: O
authors.lastname: Sagirli
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, Istanbul University , Beyazit-Istanbul , Turkey .
authors.forename: Ahmet
authors.initials: A
authors.lastname: Araman
mesh_terms: D000269:Adhesives / Q000008:administration & dosage* / Q000737:chemistry*; D000278:Administration, Buccal; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004111:Dimenhydrinate / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D009061:Mouth Mucosa / Q000378:metabolism*; D011135:Polysaccharides, Bacterial / Q000737:chemistry; D011817:Rabbits; D013499:Surface Properties
chemical_list: D000269:Adhesives; D011135:Polysaccharides, Bacterial; D002482:Cellulose; C002283:hydroxyethylcellulose; D004111:Dimenhydrinate; C002563:xanthan gum
keywords: Buccal drug delivery; dimenhydrinate; in-vivo evaluation in rabbits; motion sickness; mucoadhesive film; xanthan gum