Design, development and characterization of buccal bioadhesive films of Doxepin for treatment of odontalgia

Abstract

Tricyclic antidepressants, as doxepin hydrochloride (DH), may have analgesic local effect due to its biochemical mechanism of action. Delivery of DH directly to the oral cavity could be an interesting alternative for toothache due to its analgesic local effect. One problem associated with the mucosal administration routes is the short residence time of the dosage form on the mucosal membranes. In this sense, we have developed new doxepin mucoadhesive films able of reducing pain and increasing the effectiveness of treatment. For this purpose, we tested three different polymers: chitosan, sodium hydroxypropylmethylcellulose (HPMC) and sodium carboxymethylcellulose (SCMC) in film elaboration. The results obtained show that all films are hydrophilic matrices that absorb water when placed in an aqueous media. All the films hydrated very quickly, reaching high percentage of swelling after just few minutes (5 min for SCMC, 2 min for HPMC and 30 min for chitosan). Moreover, the SCMC and HPMC films were dissolved whereas chitosan was not dissolved. Dissolution also leads to viscous liquids with a higher retention time over mucosal surfaces what may lead to adhesive interactions. In vitro permeation studies showed that for all the formulations studied, SCMC (19.91%), HPMC (69.5%) and chitosan (24.17%), the percentage of drug permeated increased compared to the drug solution (8.26%). Specifically the HPMC film presents greater amounts of doxepin permeated (49.27 ± 4.47 mg/cm 2 ).

Transbuccal Delivery of Spray Dried Lovastatin From Mucoadhesive Buccal Patches and in Vitro Characterization

“…The polymeric solution was stirred on magnetic stirrer for 2 h. The solid dispersion equivalent to 120 mg LVS was added followed by addition of plasticizer 0.7 % glycerol and 20 mg of menthol as permeation enhancer. The mixture was stirred for 30 min and then poured into Petri dish, which is stored at 4 °C to remove air bubbles entrapped and finally dried at 37 °C for 4 h. The dried films were cut into 1 cm 2 and packed in aluminum foil and stored [4,10].…”

“…The mixture was stirred for 30 min and then poured into petridish, which is stored at 4 °C to remove air bubbles entrapped. The patches were finally dried at 25 °C for 24 h. The dried films were cut into 1 cm 2 and packed in aluminium foil and stored [4]. F14 120 200 3 20 F15 120 300 3 20 F16 120 400 3 20 F17 120 500 3 20 F18 120 600 3 20…”

“…These polymers form viscous liquids when hydrated, increasing their retention time over mucosal surfaces which may lead to interaction between polymers chain and the oral mucosa. Thus, the adequate selection of the polymer is crucial for the correct delivery of drugs in mucoadhesive formulations [4].…”

Development and evaluation of buccal films impregnated with selegiline-loaded nanospheres

“…Mucoadhesive strength was measured using rabbit cheek pouch as biological substrate. A piece of film (size 1 cm 2 ) to be tested was cut and attached to the probe of the texture analyzer using cyanoacrylate adhesive (Castán et al, 2014). The rabbit epithelium mucosa was mounted on the stationary platform.…”

“…This alternative site offers rapid and direct delivery into the systemic circulation, easy accessibility, higher patient compliance, besides being capable of enhancing bioavailability (Palem et al, 2011). Among the various buccal dosage forms, buccal film is the most advanced and highly preferred drug delivery system on account of easy adherence to buccal mucosa, better adaptation to the mucosal surface and prolonged retention (Castán et al, 2014;Lv et al, 2014). It was also reported that the buccal delivery of selegiline is likely to enhance the absorption as well as reduce the formation of metabolites when compared to conventional therapy (Nyholm, 2006).…”