Effects of bile salts on transport rates and routes of FITC-labelled compounds across porcine buccal epithelium in vitro

Hoogstraate, Janet; Şenel, Sevda; Cullander, Christopher; Verhoef, J.; Junginger, Hans E.; Boddé, Harry E.

doi:10.1016/0168-3659(95)00187-5

Cited by 85 publications

(34 citation statements)

References 22 publications

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“…Some of the proposed modulation mechanisms of bile salts include solubilization and micellar entrapment of intercellular lipids, denaturation and extraction of proteins, enzyme inactivation, and tissue swelling. [23][24][25] A comparison of the enhancing effects of bile salts on the flux of decitabine across buccal mucosa is shown in Table 1. The permeation enhancement of dihydroxy bile salts (SDTC and SDGC) is better than that of trihydroxy bile salts (STC and SGC) for decitabine across porcine buccal mucosa.…”

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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“…The freshly excised buccal tissue obtained from the rabbit was used within 2 h of removal. Most of underline tissue was removed from the mucosa with surgical scissors making sure that the basal membrane was still present (24). Then mucosa was washed with physiological solution after drying mucosa were taken in cell and resveratrol NS complex 0.2 mM in 0.2% w/v hydroxyethyl cellulose in water was put on the mucosa for 24 h. Similarly plain resveratrol sample was prepared in mixture of ethanol and water (50:50 v/v).…”

Section: Accumulation Of Resveratrol In the Buccal Mucosa Ofmentioning

confidence: 99%

Cyclodextrin-Based Nanosponges for Delivery of Resveratrol: In Vitro Characterisation, Stability, Cytotoxicity and Permeation Study

et al. 2011

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Abstract. The aim of this work was to increase the solubility, stability and permeation of resveratrol by complexation with cyclodextrin-based nanosponges (NS). Nanosponges are recently developed hypercross-linked cyclodextrin polymers nanostructured to form three-dimensional networks; they are obtained by reacting cyclodextrin with a cross-linker such as carbonyldiimidazole. They have been used to increase the solubility and stability of poorly soluble actives. This study aimed at formulating complexes of resveratrol with β-cyclodextrin nanosponges in different weight ratios. DSC, FTIR and Xray powder diffraction (XRPD) studies confirmed the interaction of resveratrol with NS. XRPD showed that the crystallinity of resveratrol decrease after encapsulation. The particle sizes of resveratrol-loaded NS are in between 400 to 500 nm with low polydispersity indices. Zeta potential is sufficiently high to obtain a stable colloidal nanosuspension. TEM measurement also revealed a particle size around 400 nm for NS complexes. The in vitro release and stability of resveratrol complex were increased compared with plain drug. Cytotoxic studies on HCPC-I cell showed that resveratrol formulations were more cytotoxic than plain resveratrol. The permeation study indicates that the resveratrol NS formulation showed good permeation in pigskin. The accumulation study in rabbit mucosa showed better accumulation of resveratrol NS formulation than plain drug. These results signify that resveratrol NS formulation can be used for buccal delivery and topical application.

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“…It is widely recognized that temperature must be controlled during in vitro buccal permeation studies (11). However, individual laboratories have used different controlled temperatures, such as room temperature (25°C) (10,(12)(13)(14), 30°C (1), 34°C (15)(16)(17)(18)(19)(20), or physiological temperature (37°C) (21)(22)(23)(24)(25)(26)(27)(28)(29)(30). In the literature, the use of ambient or room temperature (25°C) for permeation studies has been justified by stating that diffusant permeation is not significantly different at body and ambient temperatures (14).…”

Section: Introductionmentioning

confidence: 99%

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

Kulkarni

Ravichandran

et al. 2011

AAPS PharmSciTech

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Abstract. The influence of experimental temperature on the permeability of model diffusants across porcine buccal mucosa was investigated in vitro. The permeability increased significantly as the experimental temperature was increased in increments of approximately 7°C. It was observed that the apparent permeability and temperature were related by an exponential relationship that conformed to the Arrhenius equation. Diffusants with higher lipophilicities-buspirone and bupivacaine-had lower activation energies for diffusion when compared to hydrophilic diffusants-antipyrine and caffeine. The activation energy for diffusion of the model diffusants decreased linearly with increasing distribution coefficients across porcine buccal mucosa. The results suggested that the buccal mucosa acts as a stronger barrier to the diffusion of hydrophilic diffusants than the lipophilic ones. The log-linear relationship between permeability and temperature indicates that temperature should be carefully controlled in diffusion experiments. These results also point to the possibility of developing heat-generating buccal delivery devices, especially for hydrophobic diffusants.

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Effects of bile salts on transport rates and routes of FITC-labelled compounds across porcine buccal epithelium in vitro

Cited by 85 publications

References 22 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

Cyclodextrin-Based Nanosponges for Delivery of Resveratrol: In Vitro Characterisation, Stability, Cytotoxicity and Permeation Study

Effect of Experimental Temperature on the Permeation of Model Diffusants Across Porcine Buccal Mucosa

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