In Vitro Evaluation of Various Buccal Permeation Enhancing Systems for PACAP (Pituitary Adenylate Cyclase-Activating Polypeptide)

Langoth, Nina; Bernkop‐Schnürch, Andreas; P, Kurka

doi:10.1007/s11095-005-7894-4

Cited by 34 publications

(16 citation statements)

References 26 publications

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“…Porcine buccal mucosa was used because it better resembles human buccal mucosa with regard to permeability, lipid barrier composition, thickness and histology (Langoth et al, 2005). Porcine buccal tissue from domestic pigs was obtained from a local slaughter house and used within 2 h of slaughter.…”

Section: Tissue Preparation (Isolation)mentioning

confidence: 99%

Transmucosal delivery of domperidone from bilayered buccal patches: In Vitro, Ex Vivo and In Vivo characterization

et al. 2011

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Bilayered mucoadhesive buccal patches for systemic administration of domperidone (DOM), a dopamine-receptor (D(2)) antagonist, were developed using hydroxy propyl methyl cellulose and PVPK30 as a primary layer and Eudragit RLPO and PEO as a secondary layer. Ex vivo drug permeation through porcine buccal membrane was performed. Bilayered buccal patches were developed by solvent casting technique and evaluated for in vitro drug release, moisture absorption, mechanical properties, surface pH, in vitro bioadhesion, in vivo residence time and ex vivo permeation of DOM through porcine buccal membrane from a bilayered buccal patch. Formulation DB4 was associated with 99.5% drug release with a higuchi model release profile and 53.9% of the drug had permeated in 6 h, with a flux of 0.492 mg/h/cm(2) through porcine buccal membrane. DB4 showed 5.58 N and 3.28 mJ peak detachment force and work of adhesion, respectively. The physicochemical interactions between DOM and the polymer were investigated by differential scanning calorimetry (DSC) and fourier transform infrared (FTIR) Spectroscopy. DSC and FTIR studies revealed no interaction between drug and polymer. Stability studies for optimized patch DB4 was carried out at 40°C/75% relative humidity. The formulations were found to be stable over a period of 3 months with respect to drug content, in vitro release and ex vivo permeation through porcine buccal membrane. The results indicate that suitable bilayered mucoadhesive buccal patches with desired permeability could be prepared.

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Section: Tissue Preparation (Isolation)mentioning

confidence: 99%

Transmucosal delivery of domperidone from bilayered buccal patches: In Vitro, Ex Vivo and In Vivo characterization

et al. 2011

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“…Porcine buccal mucosa was used as it resembles the human buccal mucosa regarding permeability, barrier lipid composition, thickness, and histology (Wertz & Squier., 1991;Langoth et al, 2005). Buccal tissue from pigs was obtained from a local slaughterhouse and used within 2 h of slaughter.…”

Section: Ex Vivo Drug Permeation Studies Through Porcine Buccal Membranementioning

confidence: 99%

Development of bioadhesive buccal tablets for felodipine and pioglitazone in combined dosage form: In vitro, ex vivo, and in vivo characterization

et al. 2011

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“…In these studies, porcine buccal mucosa was used due to its high similarity to the human buccal mucosa in certain important characteristics such as permeability, barrier lipid composition, histology, and ultrastructural organization (40). Buccal mucosa from pigs weighing 70-100 Kg was obtained freshly from a local slaughterhouse and used not later than 2 h after slaughtering.…”

Section: In Vitro Permeation Studiesmentioning

confidence: 99%

A Comprehensive Development Strategy in Buccal Drug Delivery

2010

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Abstract. This work combines several methods in an integrated strategy to develop a matrix for buccal administration. For this purpose, tablets containing selected mucoadhesive polymers loaded with a model drug (omeprazole), free or in a complexed form with cyclodextrins, and in the absence and presence of alkali agents were subjected to a battery of tests. Mucoadhesion studies, including simple factorial analysis, in vitro release studies with both model-dependent and model-independent analysis, and permeation studies were performed. Mucoadhesive profiles indicated that the presence of the drug decreases the mucoadhesion profile, probably due its hydrophobic character. In tablets loaded with the drug complexed with β-cyclodextrin or methyl-β-cyclodextrin, better results were obtained with the methylated derivative. This effect was attributed to the fact that in the case of β-cyclodextrin, more hydroxyl groups are available to interact with the mucoadhesive polymers, thus decreasing the mucoadhesion performance. The same result was observed in presence of the alkali agent (L-arginine), in this case due to the excessive hydrophilic character of L-arginine. Drug release from tablets was also evaluated, and results suggested that the dissolution profile with best characteristics was observed in the matrix loaded with omeprazole complexed with methyl-β-cyclodextrin in the presence of L-arginine. Several mathematical models were applied to the dissolution curves, indicating that the release of the drug, in free or in complexed state, from the mucoadhesive matrices followed a super case II transport, as established on the basis of the Korsmeyer-Peppas function. The feasibility of drug buccal administration was assessed by permeation experiments on porcine buccal mucosa. The amount of drug permeated from mucoadhesive tablets presented a maximum value for the system containing drug complexed with the methylated cyclodextrin derivative in presence of L-arginine. According to these results, the system containing the selected polymer mixture and the drug complexed with methyl-β-cyclodextrin in presence of L-arginine showed a great potential as a buccal drug delivery formulation, in which a good compromise among mucoadhesion, dissolution, and permeation properties was achieved.

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In Vitro Evaluation of Various Buccal Permeation Enhancing Systems for PACAP (Pituitary Adenylate Cyclase-Activating Polypeptide)

Abstract: Based on their permeation-enhancing properties, chitosan-TBA conjugates represent a promising tool for the buccal administration of peptide drugs, e.g., PACAP.

Cited by 34 publications

References 26 publications

Transmucosal delivery of domperidone from bilayered buccal patches: In Vitro, Ex Vivo and In Vivo characterization

Transmucosal delivery of domperidone from bilayered buccal patches: In Vitro, Ex Vivo and In Vivo characterization

Development of bioadhesive buccal tablets for felodipine and pioglitazone in combined dosage form: In vitro, ex vivo, and in vivo characterization

A Comprehensive Development Strategy in Buccal Drug Delivery

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