Evaluation of different pig oral mucosa sites as permeability barrier models for drug permeation studies

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• 作者：Michelle Franz-Montan^a ; ^{michelle@fop.unicamp.br" class="auth_mail" title="E-mail the corresponding author} ; Luciano Serpe^a ; Claudia Cristina Maia Martinelli^a ; Camila Batista da Silva^a ; Cleiton Pita dos Santos^a ; Pedro Duarte Novaes^b ; Maria Cristina Volpato^a ; Eneida de Paula^c ; Renata Fonseca Vianna Lopez^d ; Francisco Carlos Groppo^a
• 关键词：Oral mucosa drug delivery ; Permeability ; In vitro model ; Diffusion
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2016
• 出版时间：1 January 2016
• 年：2016
• 卷：81
• 期：Complete
• 页码：52-59
• 全文大小：1162 K

文摘

The objective of the present study was to investigate the influence of preparation and storage conditions on the histology and permeability of different parts of porcine oral mucosa used for in vitro studies of transbuccal formulations. Fresh and frozen (− 20 °C and − 80 °C, with or without cryoprotectant) epithelia of porcine palatal, gingival, dorsum of the tongue, and buccal mucosa were submitted for histological analyses to determine the effects of storage conditions on barrier integrity. Permeation of lidocaine hydrochloride (used as a hydrophilic model drug) across fresh and previously frozen oral epithelium was measured in order to evaluate the barrier function. Histological evaluation demonstrated that the oral epithelium was successfully separated from the connective tissue, except for gingival mucosa. After storage under different conditions, all tissues presented desquamation of superficial layers and spherical spaces induced by the freezing process. The permeability of lidocaine hydrochloride varied among the fresh oral mucosa and generally increased after freezing. In conclusion, fresh epithelium from the buccal and dorsum of the tongue mucosa should be used for in vitro studies investigating hydrophilic drug transport when these are the desired clinical application sites. However, when the palate is the target site, both fresh and frozen (for up to 4 weeks, without addition of cryoprotectant) samples could be used. The addition of glycerol as a cryoprotectant should be avoided due to increased lidocaine hydrochloride permeability.