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In vitro permeation through porcine buccal mucosa of caffeic acid phenetyl ester (CAPE) from a topical mucoadhesive gel containing propolis.

Abstract

Recent studies have shown that propolis has on the oral cavity appreciable antibacterial, antifungal and antiviral actions, as well as anti-inflammatory, anaesthetic and cytostatic properties. In light of these studies, an assessment of the diffusion and permeation of caffeic acid phenetyl ester (CAPE) through porcine buccal mucosa was considered useful as a possible application in the stomatological field. To do so, a mucoadhesive topical gel was prepared to apply to the buccal mucosa. The gel was formulated in such a way as to improve the solubility of the propolis, conducting to an increase of the flux. The mucosal permeation of CAPE from the formulation was evaluated using Franz cells, with porcine buccal mucosa as septum between the formulation (donor compartment) and the receptor phase chamber. The diffusion through the membrane was determined by evaluating the amount of CAPE present in the receiving solution, the flux and the permeation coefficient (at the steady state) in the different formulations at set intervals. Qualitative and quantitative determinations were done by HPLC analysis. From the results, CAPE allowed a high permeability coefficient in comparison to the coefficient of other molecules, as expected from its physical-chemical structure. Moreover, the developed gel improved the CAPE flux approximately 35 times more with respect to an ethanol solution formulated at the same gel concentration. The developed gel was also tested in order to evaluate the mucoadhesive behaviour and comfort in vivo on 10 volunteers in a period of 8 h. The in vivo evaluation of mucoadhesive gel revealed adequate comfort and non-irritancy during the period of study and it was well accepted by the volunteers.

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  • Authors

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    Source

    Fitoterapia 73 Suppl 1: 2002 Nov pg S44-52

    MeSH

    Adhesiveness
    Administration, Topical
    Animals
    Anti-Inflammatory Agents
    Caffeic Acids
    Chemistry, Pharmaceutical
    Chromatography, High Pressure Liquid
    Gels
    Humans
    Male
    Mouth Mucosa
    Permeability
    Phenylethyl Alcohol
    Phytotherapy
    Propolis
    Stomatitis
    Swine
    Time Factors

    Pub Type(s)

    Journal Article

    Language

    eng

    PubMed ID

    12495709

    Citation

    TY - JOUR T1 - In vitro permeation through porcine buccal mucosa of caffeic acid phenetyl ester (CAPE) from a topical mucoadhesive gel containing propolis. AU - Ceschel,G C, AU - Maffei,P, AU - Sforzini,A, AU - Lombardi Borgia,S, AU - Yasin,A, AU - Ronchi,C, PY - 2002/12/24/pubmed PY - 2003/1/22/medline PY - 2002/12/24/entrez SP - S44 EP - 52 JF - Fitoterapia JO - Fitoterapia VL - 73 Suppl 1 N2 - Recent studies have shown that propolis has on the oral cavity appreciable antibacterial, antifungal and antiviral actions, as well as anti-inflammatory, anaesthetic and cytostatic properties. In light of these studies, an assessment of the diffusion and permeation of caffeic acid phenetyl ester (CAPE) through porcine buccal mucosa was considered useful as a possible application in the stomatological field. To do so, a mucoadhesive topical gel was prepared to apply to the buccal mucosa. The gel was formulated in such a way as to improve the solubility of the propolis, conducting to an increase of the flux. The mucosal permeation of CAPE from the formulation was evaluated using Franz cells, with porcine buccal mucosa as septum between the formulation (donor compartment) and the receptor phase chamber. The diffusion through the membrane was determined by evaluating the amount of CAPE present in the receiving solution, the flux and the permeation coefficient (at the steady state) in the different formulations at set intervals. Qualitative and quantitative determinations were done by HPLC analysis. From the results, CAPE allowed a high permeability coefficient in comparison to the coefficient of other molecules, as expected from its physical-chemical structure. Moreover, the developed gel improved the CAPE flux approximately 35 times more with respect to an ethanol solution formulated at the same gel concentration. The developed gel was also tested in order to evaluate the mucoadhesive behaviour and comfort in vivo on 10 volunteers in a period of 8 h. The in vivo evaluation of mucoadhesive gel revealed adequate comfort and non-irritancy during the period of study and it was well accepted by the volunteers. SN - 0367-326X UR - https://www.unboundmedicine.com/medline/citation/12495709/In_vitro_permeation_through_porcine_buccal_mucosa_of_caffeic_acid_phenetyl_ester__CAPE__from_a_topical_mucoadhesive_gel_containing_propolis_ L2 - http://linkinghub.elsevier.com/retrieve/pii/S0367326X02001909 ER -