The aim of this study was to analyze characteristics of the barrier function of excised porcine buccal mucosa to the test compounds, estradiol, propranolol HCI, melatonin, and mannitol with a wide range of partition coefficient values. The permeability of melatonin was measured through frozen, store...
The aim of this study was to analyze characteristics of the barrier function of excised porcine buccal mucosa to the test compounds, estradiol, propranolol HCI, melatonin, and mannitol with a wide range of partition coefficient values. The permeability of melatonin was measured through frozen, stored, and fresh porcine buccal mucosa to examine the impact of storage conditions on the permeability of porcine buccal mucosa. The results demonstrated that the ex vivo permeability of the porcine buccal mucosa was greater for more lipophilic solutes, which was consistent with a series of molecules transported by passive transepithelial diffusion. The melatonin permeation profiles through frozen, stored, and fresh mucosa illustrated that damage was incurred by the freezing process of the mucosal tissue, leading to loss of the barrier function and thereby an increased permeation coefficient. It can be observed that the influence of compound lipophilicity on the association of the compounds with buccal mucosa was clear. The relationship between permeation coefficient and Log P values for the four compounds investigated demonstrated a proportional relationship, further confirming the importance of the lipophilicity of a compound to permeate the buccal mucosa. These results showed that the ex vivo porcine buccal mucosa model is a suitable tool to screen oral mucosal permeability.
The aim of this study was to analyze characteristics of the barrier function of excised porcine buccal mucosa to the test compounds, estradiol, propranolol HCI, melatonin, and mannitol with a wide range of partition coefficient values. The permeability of melatonin was measured through frozen, stored, and fresh porcine buccal mucosa to examine the impact of storage conditions on the permeability of porcine buccal mucosa. The results demonstrated that the ex vivo permeability of the porcine buccal mucosa was greater for more lipophilic solutes, which was consistent with a series of molecules transported by passive transepithelial diffusion. The melatonin permeation profiles through frozen, stored, and fresh mucosa illustrated that damage was incurred by the freezing process of the mucosal tissue, leading to loss of the barrier function and thereby an increased permeation coefficient. It can be observed that the influence of compound lipophilicity on the association of the compounds with buccal mucosa was clear. The relationship between permeation coefficient and Log P values for the four compounds investigated demonstrated a proportional relationship, further confirming the importance of the lipophilicity of a compound to permeate the buccal mucosa. These results showed that the ex vivo porcine buccal mucosa model is a suitable tool to screen oral mucosal permeability.
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대상 데이터
Louis, MO, USA). NCS-II Tissue Solubilizer and HiSafe 3 liquid scintillation cocktail were obtained from Amershmn Corporation (Arlington Heights, IL, USA) and Fisher Chemicals (Loughborough, UK), respectively. Fresh distilled water was used throughout.
이론/모형
mucosa. The shake-flask method was used. PBS and n-octanol were shaken to co-saturate in a 50 ml screw capped test tube for 24 hr at 37℃.
성능/효과
46 x 10 6 cm s- , respectively, which were not significantly different at the confidence limits tested (95%). However, frozen buccal tissue resulted in a considerably increased Pc value of 5.49 ± 1.10 x IO-6 cm s-1, which was significantly different at the confidence limits tested (95%). This illustrates that damage was incurred by the freezing process.
The ex vivo buccal permeation results were statistically analyzed using ANOVA and P values of 0.05 or less were considered statistically significant.
후속연구
The objective of the present study was to develop and characterize an ex vivo model to allow the investigation of solute permeability across buccal mucosal tissue, which could be related to the human situation." Porcine buccal mucosa was selected as the chosen model, as it has non-keratinized epithelium and has been shown to have structural similarities with human buccal mucosa.
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