Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Gimeno, A.L.; Calpena, Ana Cristina; Sanz, Roser; Mallandrich, Mireia; Peraire, Concepción; Clares, Beatriz

doi:10.1016/j.ijpharm.2014.10.060

Cited by 11 publications

(3 citation statements)

References 27 publications

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“…The incubation time was 24 h for the skin and 6 h for the other tissues. These periods are common in the duration of the ex vivo permeation assays [29,30,32,36,37]. The C 0 solution was also incubated in the water bath in the same conditions as the tissues so as to evaluate any potential degradation of the drug in the experiment conditions.…”

Section: Drug Uptake and Drug Recovery From The Skin And Mucosaementioning

confidence: 99%

Assessing the Solubility of Baricitinib and Drug Uptake in Different Tissues Using Absorption and Fluorescence Spectroscopies

et al. 2022

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The low water solubility of baricitinib (BCT) limits the development of new formulations for the topical delivery of the drug. The aims of this study were to assess the solubility of BCT in different solvents, including Transcutol, a biocompatible permeation enhancer that is miscible in water, to evaluate the drug uptake in human skin and porcine tissues (sclera, cornea, oral, sublingual, and vaginal), and to subsequently extract the drug from the tissues so as to determine the drug recovery using in vitro techniques. Analytical methods were developed and validated for the quantification of BCT in Transcutol using absorption and fluorescence spectroscopies, which are complementary to each other and permit the detection of the drug across a broad range of concentrations. Results show that Transcutol permits an increased drug solubility, and that BCT is able to penetrate the tissues studied. The solutions of BCT in Transcutol were stable for at least one week. Hence, Transcutol may be a suitable solvent for further development of topical formulations.

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Section: Drug Uptake and Drug Recovery From The Skin And Mucosaementioning

confidence: 99%

Assessing the Solubility of Baricitinib and Drug Uptake in Different Tissues Using Absorption and Fluorescence Spectroscopies

et al. 2022

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“…In comparison to transdermal routes, the buccal mucosa demonstrates better permeability since human buccal mucosa is composed mostly of non-keratinized cells [17,18]. The ready permeability of NIC across the buccal mucosa has been attributed to its high solubility in both water and organic solvents (LogP of 1.17) and its low molecular weight (162.2 g/mol) [19,20].…”

Section: Introductionmentioning

confidence: 99%

“…The permeability of NIC species depends on pH; however, all species of NIC can readily permeate mucosal membranes with higher permeation for un-ionized species than ionized species [21]. Porcine buccal mucosa has similar morphology and permeation to the human buccal mucosa in terms of non-keratinized cells and enzymatic activities [17], as reported for drugs such as naratriptan [22], NIC [23], buspirone [24], omeprazole [25,26], and doxepin [18]. Other buccal mucosa models such as sheep buccal mucosa have been reported in permeation studies [27,28].…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Boateng

Okeke

2019

Pharmaceutics

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The functional physicochemical properties of nicotine (NIC)-loaded composite freeze-dried wafers and solvent-evaporated films comprising hydroxypropylmethylcellulose (HPMC) and sodium alginate (SA), stabilized with magnesium aluminium silicate (MAS), have been reported. The formulations were characterized for swelling capacity, mucoadhesion, in vitro drug dissolution properties in simulated saliva (SS) and PBS at pH 6.8, and ex vivo and in vitro permeation using pig buccal mucosa membrane and EpiOralTM buccal tissue culture, respectively; finally, the cell viability of the EpiOralTM tissues after contact with the NIC-loaded formulations was investigated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and the functional characteristics compared with those of commercially available NIC strips. Swelling and NIC release from the HPMC–SA wafers were more prolonged (30 min) compared to the commercially available NIC strips which disintegrated rapidly and released the drug within 5 min. Generally, swelling, mucoadhesion, and drug release was faster in PBS than in SS, and the presence of MAS was essential for maintaining a high dose recovery compared to non-MAS formulations and commercial NIC strips, which showed lower percentage of NIC content, possibly due to evaporation during analysis. Permeation studies showed that the NIC released was able to cross both porcine buccal membrane and the EpiOralTM buccal tissue, with the latter showing higher permeation flux for all the formulations tested. All the NIC-loaded, MAS-stabilized formulations showed high tissue viability, with values above 80%, showing their great potential for use as buccal delivery platforms for NIC replacement therapy to aid smoking cessation.

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Clotrimazole multiple W/O/W emulsion as anticandidal agent: Characterization and evaluation on skin and mucosae

Soriano-Ruiz

Suñer-Carbó

Calpena

et al. 2019

Colloids and Surfaces B: Biointerfaces

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Transbuccal delivery of doxepin: Studies on permeation and histological investigation

Cited by 11 publications

References 27 publications

Assessing the Solubility of Baricitinib and Drug Uptake in Different Tissues Using Absorption and Fluorescence Spectroscopies

Assessing the Solubility of Baricitinib and Drug Uptake in Different Tissues Using Absorption and Fluorescence Spectroscopies

Evaluation of Clay-Functionalized Wafers and Films for Nicotine Replacement Therapy via Buccal Mucosa

Clotrimazole multiple W/O/W emulsion as anticandidal agent: Characterization and evaluation on skin and mucosae

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