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EnglishIrinotecan (CPT-11) is used to treat advanced colorectal cancer as an intravenous therapy. Depending on pH, CPT-11 exists in either a lactone (active) or carboxylate (inactive) form, or both. In this investigation, the feasibility for systemic delivery of CPT-11 through the buccal route was evaluated. Permeation of CPT-11 across porcine buccal mucosa was studied in vitro using side-by-side flow through diffusion cells at 37°C. Experiments were performed over a pH range from 4 to 9, and the permeability of both the lactone and carboxylate forms of CPT-11 was measured. CPT-11 steady state flux was determined over a range of donor concentrations at pH 4 (0.5, 1, 5, 10, 15, 20 mg/ml) and pH 6.8 (0.5, 5, 10 mg/ml). Steady state flux increased linearly with increasing donor concentration of CPT-11 at pH 4 (r2 = 0.9935) and at pH 6.8 (r2 = 0.9886). CPT-11 permeability was independent of pH, although the distribution coefficient increased with increasing pH. Estimates of permeability for the lactone and carboxylate forms were 4.16 × 10−5 cm/s and 2.6 × 10−5 cm/s, respectively. These calculated permeability values were in agreement with the in vitro experimental data. Overall, CPT-11 was found to permeate through porcine buccal mucosa via passive diffusion. CPT-11 permeability was independent of pH, suggesting that the compound was transported mainly via a paracellular route. Overall, the results of this research suggest that the buccal route is a potential extravascular mode of delivery for CPT-11.
Shah, V., Bellantone, R. D. A., Taft, D. R., Evaluating the Potential for Delivery of Irinotecan via the Buccal Route: Physicochemical Characterization and In Vitro Permeation Assessment Across Porcine Buccal Mucosa, <<AAPS PHARMSCITECH>>, 2016; (Giugno): 1-8. [doi:10.1208/s12249-016-0578-z] [http://hdl.handle.net/10807/91619]
| Autori: | |
| Titolo: | Evaluating the Potential for Delivery of Irinotecan via the Buccal Route: Physicochemical Characterization and In Vitro Permeation Assessment Across Porcine Buccal Mucosa |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1208/s12249-016-0578-z |
| URL: | http://www.springerlink.com/content/1530-9932/ |
| Data di pubblicazione: | 2016 |
| Abstract: | Irinotecan (CPT-11) is used to treat advanced colorectal cancer as an intravenous therapy. Depending on pH, CPT-11 exists in either a lactone (active) or carboxylate (inactive) form, or both. In this investigation, the feasibility for systemic delivery of CPT-11 through the buccal route was evaluated. Permeation of CPT-11 across porcine buccal mucosa was studied in vitro using side-by-side flow through diffusion cells at 37°C. Experiments were performed over a pH range from 4 to 9, and the permeability of both the lactone and carboxylate forms of CPT-11 was measured. CPT-11 steady state flux was determined over a range of donor concentrations at pH 4 (0.5, 1, 5, 10, 15, 20 mg/ml) and pH 6.8 (0.5, 5, 10 mg/ml). Steady state flux increased linearly with increasing donor concentration of CPT-11 at pH 4 (r2 = 0.9935) and at pH 6.8 (r2 = 0.9886). CPT-11 permeability was independent of pH, although the distribution coefficient increased with increasing pH. Estimates of permeability for the lactone and carboxylate forms were 4.16 × 10−5 cm/s and 2.6 × 10−5 cm/s, respectively. These calculated permeability values were in agreement with the in vitro experimental data. Overall, CPT-11 was found to permeate through porcine buccal mucosa via passive diffusion. CPT-11 permeability was independent of pH, suggesting that the compound was transported mainly via a paracellular route. Overall, the results of this research suggest that the buccal route is a potential extravascular mode of delivery for CPT-11. |
| Lingua: | Inglese |
| Rivista: | |
| Citazione: | Shah, V., Bellantone, R. D. A., Taft, D. R., Evaluating the Potential for Delivery of Irinotecan via the Buccal Route: Physicochemical Characterization and In Vitro Permeation Assessment Across Porcine Buccal Mucosa, <<AAPS PHARMSCITECH>>, 2016; (Giugno): 1-8. [doi:10.1208/s12249-016-0578-z] [http://hdl.handle.net/10807/91619] |
| Appare nelle tipologie: | Articolo in rivista, Nota a sentenza |
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