Buccal delivery of fluorescein isothiocyanate-dextran 4400 and the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs

Hoogstraate, Janet; Verhoef, J.; Tuk, B.; Pijpers, A.; Leengoed, L.A.M.G. van; Verheijden, J.H.M.; Junginger, Hans E.; Boddé, Harry E.

doi:10.1016/0168-3659(96)01358-2

Cited by 24 publications

(16 citation statements)

References 19 publications

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“…Five-to seven-fold enhancement in absolute bioavailability of buserelin and fluorescein isothiocyanate dextran was observed when 10 mM of SDGC was used. [29][30][31] Although dihydroxy bile salts showed a higher permeation-enhancing effect for decitabine than trihydroxy bile salts did, the dihydroxy bile salts' safety for buccal mucosa at these concentrations may be a factor in their selection. An earlier report published by Senel et al showed that the morphological changes caused by 10 mM of SDGC were comparable to those caused by 100 mM SGC.…”

Section: Effect Of Bile Salts On Permeationmentioning

confidence: 99%

Transbuccal delivery of 5-Aza-2′-deoxycytidine: Effects of drug concentration, buffer solution, and bile salts on permeation

et al. 2007

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Delivery of 5-aza-2´-deoxycytidine (decitabine) across porcine buccal mucosa was evaluated as an alternative to the complex intravenous infusion regimen currently used to administer the drug. A reproducible high-performance liquid chromatography method was developed and optimized for the quantitative determination of this drug. Decitabine showed a concentration-dependent passive diffusion process across porcine buccal mucosa. An increase in the ionic strength of the phosphate buffer from 100 to 400 mM decreased the flux from 3.57 ± 0.65 to 1.89 ± 0.61 μg/h/cm 2 . Trihydroxy bile salts significantly enhanced the flux of decitabine at a 100 mM concentration (P 9 .05). The steady-state flux of decitabine in the presence of 100 mM of sodium taurocholate and sodium glycocholate was 52.65 ± 9.48 and 85.22 ± 7.61 μg/cm 2 /h, respectively. Two dihydroxy bile salts, sodium deoxytaurocholate and sodium deoxyglycocholate, showed better enhancement effect than did trihydroxy bile salts. A 38-fold enhancement in flux was achieved with 10 mM of sodium deoxyglycocholate.

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Section: Effect Of Bile Salts On Permeationmentioning

confidence: 99%

Transbuccal delivery of 5-Aza-2′-deoxycytidine: Effects of drug concentration, buffer solution, and bile salts on permeation

et al. 2007

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“…14 The area under the plasma sCT concentration versus time curve was calculated using the trapezoidal rule within the time periods of 0-2 h following buccal administration although the experiments were carried out beyond 2 h. In an attempt to estimate the apparent bioavailability, the data was truncated at 2 h following buccal administration because the total duration of the intravenous experiments was 2 h. Equations 1 and 2 were used to estimate the apparent bioavailability and clearance of sCT following buccal administration. 15,16 The Cmax, Cmin, and tmax were estimated directly from the plasma sCT versus time profiles following buccal administration. In eqs 1 and 2, F denotes the apparent bioavailability, D is the dose of sCT contained in the buccal tablets, and AUC 0-tbuccal represents the area under the plasma sCT concentration vs time curve following buccal administration from 0 to 2 h. A dose of 40 µg of sCT was used to calculate the apparent bioavailability as the amount of sCT remaining in the tablet after buccal administration was not estimated.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of a novel, natural oligosaccharide gum as a sustained-release and mucoadhesive component of calcitonin buccal tablets

Alur

Beal

Pather³

et al. 1999

Journal of Pharmaceutical Sciences

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The objective of this study was to evaluate the gum from Hakea gibbosa (hakea) as a sustained-release and mucoadhesive component in buccal tablets for a model peptide, namely, salmon calcitonin. Flat-faced core tablets containing either 12 or 32 mg of hakea and 40 microg (200 IU) of salmon calcitonin (sCT) per tablet were formulated using a direct compression technique and were coated with Cutina on all but one face. The in vitro release profiles were sigmoidal in nature and according to a mathematical model indicated super Case II transport as the primary mechanism of release. The resulting plasma sCT and calcium concentrations were determined following both intravenous administration and buccal application of mucoadhesive tablets in rabbits. Following intravenous administration, the mean values determined for t(1/2) (alpha), t(1/2) (beta), V(d), and CL for sCT were 0.76 +/- 0.06 min, 67 +/- 18 min, 1484 +/- 454 mL/kg, and 19 +/- 2 mL/min.kg, respectively. Following the application of the mucoadhesive buccal tablets which contained 40 microg of sCT and either 12 or 32 mg of hakea, the calculated apparent bioavailability (F) and clearance (CL) were 37 +/- 6% and 19 +/- 3.3 mL/min.kg and 16 +/- 8% and 18 +/- 0.4 mL/min. kg, respectively. Serum calcium concentrations indicated that biologically active sCT was delivered across the rabbit buccal mucosa. The strength of mucoadhesion of the tablets was also quantitated in terms of the force of detachment as a function of time. The force of detachment for the mucoadhesive buccal tablets containing either 12 or 32 mg of hakea and 40 microg of sCT increased from 4.47 +/- 0.68 to 8.41 +/- 1.0 N and 8.23 +/- 1.62 to 14.98 +/- 1.63 N, respectively, from 5 to 90 min following application to excised rabbit intestinal mucosa. These results demonstrate that the novel, natural gum from Hakea gibbosa may be used to sustain the release of sCT from a unidirectional-release buccal tablet. The mechanism of in vitro release is likely to involve peptide diffusion/polymer dissolution. The mucoadhesive strength, as measured by the force of detachment, can be modulated by altering the amount of hakea in the tablet. The mucoadhesive buccal tablets described in this paper represent an improved transbuccal delivery system for therapeutic polypeptides.

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“…500-1000 Da, above which protein/peptide permeation is hindered must be considered, requiring an optimization of oral film formulation to overcome buccal permeability issues [7]. Buccal* [21] *Formulation must contain permeability enhancers. **May require permeability enhancers in the formulation.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Oral films as breakthrough tools for oral delivery of proteins/peptides

Castro

Fonte

Sousa

et al. 2015

Journal of Controlled Release

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Buccal delivery of fluorescein isothiocyanate-dextran 4400 and the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs

Cited by 24 publications

References 19 publications

Transbuccal delivery of 5-Aza-2′-deoxycytidine: Effects of drug concentration, buffer solution, and bile salts on permeation

Transbuccal delivery of 5-Aza-2′-deoxycytidine: Effects of drug concentration, buffer solution, and bile salts on permeation

Evaluation of a novel, natural oligosaccharide gum as a sustained-release and mucoadhesive component of calcitonin buccal tablets

Oral films as breakthrough tools for oral delivery of proteins/peptides

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