Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies

Artusi, Mariella; Santi, Patrizia; Colombo, Paolo; Junginger, Hans E.

doi:10.1016/s0378-5173(02)00545-8

Cited by 71 publications

(32 citation statements)

References 17 publications

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“…Heat-separated epithelia were also included as one study reported the thickness of the heat-separated tissue to be 410 μ (43). The permeabilities for the following compounds were obtained from literature: sotalol, flecainide, morphine, zalcitabine, fentanyl, thiocolchicoside, nicotine, estradiol, triamcinololne acetonide, testosterone, labetalol, acebutolol, timolol, oxprenolol, alprenolol, and tertatolol (43)(44)(45)(46)(47)(48)(49)(50)(51). Sotalol was excluded as it has a logD 6.8 of −2.59, which is lower than that of atenolol, the most hydrophilic compound (logD 6.8 =−1.3) in the training group used in developing the model (16).…”

Section: Validation Using An External Data Setmentioning

confidence: 99%

In Silico Prediction of Drug Permeability Across Buccal Mucosa

Kokate

Williams

et al. 2009

Pharm Res

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Section: Validation Using An External Data Setmentioning

confidence: 99%

In Silico Prediction of Drug Permeability Across Buccal Mucosa

Kokate

Williams

et al. 2009

Pharm Res

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“…Various in vivo and ex vivo models for investigating drug permeation through the buccal mucosa have been reported for different animals such as hamster (Eggerth et al, 1987), rabbit (Nair & Chien, 1993;Dowty et al, 1992), dog (Galey et al, 1976), pig (Chen et al, 1999;Artusia et al, 2003;Sandri et al, 2004) and sheep (Giovino et al, 2013, 95 Boateng & Ayensu., 2014. However, the buccal epithelium of rodents such as hamsters is thick and keratinised and the surface area is small (Shojaei 1998), which limits the extent of drug permeation.…”

Section: Introductionmentioning

confidence: 99%

Functional physico-chemical, ex vivo permeation and cell viability characterization of omeprazole loaded buccal films for paediatric drug delivery

Khan

Trivedi

Boateng

2016

International Journal of Pharmaceutics

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25Buccal films were prepared from aqueous and ethanolic Metolose gels using the solvent casting approach (40°C). The hydration (PBS and simulated saliva), mucoadhesion, physical stability (20°C, 40°C), in vitro drug (omeprazole) dissolution (PBS and simulated saliva), ex vivo permeation (pig buccal mucosa) in presence of simulated saliva, ex vivo bioadhesion and cell viability using MTT of drug loaded (DL) films were investigated. Hydration and mucoadhesion 30 results showed that swelling capacity and adhesion was higher in the presence of PBS than simulated saliva (SS) due to differences in ionic strength. Omeprazole was more stable at 20°C than 40°C whilst omeprazole release reached a plateau within 1 hour and faster in PBS than in SS. Fitting release data to kinetic models showed that Korsmeyer-Peppas equation best fit the dissolution data. Drug release in PBS was best described by zero order via non-Fickian 35 diffusion but followed super case II transport in SS attributed to drug diffusion and polymer erosion. The amount of omeprazole permeating over 2 hours was 275ug/cm 2 whilst the formulations and starting materials showed cell viability values greater than 95%, confirming their safety for potential use in paediatric buccal delivery.

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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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Buccal delivery of thiocolchicoside: in vitro and in vivo permeation studies

Cited by 71 publications

References 17 publications

In Silico Prediction of Drug Permeability Across Buccal Mucosa

In Silico Prediction of Drug Permeability Across Buccal Mucosa

Functional physico-chemical, ex vivo permeation and cell viability characterization of omeprazole loaded buccal films for paediatric drug delivery

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

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