Buccal penetration enhancers—How do they really work?

Nicolazzo, Joseph A.; Reed, Barry L.; Finnin, Barrie C.

doi:10.1016/j.jconrel.2005.01.024

Cited by 172 publications

(122 citation statements)

References 100 publications

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“…(e.g. In earlier reports, sodium glycocholate was shown to enhance the buccal transport of flecainide acetate and not the more lipophilic flecainide base, which was attributed to the different pathways for each permeant and the ability of the bile salt to affect only the paracellular route) (22,35). Figure 6 shows a photo micrograph of buccal mucosa depicting the outermost layer of stratified squamous epithelium, below which can be seen the basement membrane, lamina propria, and submucosa.…”

Section: Effect Of Permeation Enhancers On Buccal Permeation Of Fumentioning

confidence: 89%

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

Dhiman

Dhiman²,

Sawant

2009

AAPS PharmSciTech

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Abstract. The purpose of this study was to determine the effect of permeation enhancers on the transbuccal delivery of 5-fluorouracil (FU). The effect of permeation enhancers on in vitro buccal permeability was assessed using sodium deoxycholate (SDC), sodium dodecyl sulphate (SDS), sodium tauroglycocholate (STGC), and oleic acid and their concentrations for absorption enhancement were optimized. STGC appeared to be most effective for enhancing the buccal permeation of FU than the other enhancers. These enhancements by STGC were statistically significant (p<0.05) compared to control. The order of permeation enhancement was STGC > SDS > SDC > oleic acid. Histological investigations were performed on buccal mucosa and indicated no major morphological changes. The enhancing effect of STGC on the buccal absorption of FU was evaluated from the mucoadhesive gels in rabbits. The absolute bioavailability of FU from mucoadhesive gels containing STGC increased 1.6-fold as compared to the gels containing no permeation enhancer. The mean residence time and mean absorption time considerably increased following administration of gel containing penetration enhancer compared with the gel without penetration enhancer.

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Section: Effect Of Permeation Enhancers On Buccal Permeation Of Fumentioning

confidence: 89%

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

Dhiman

Dhiman²,

Sawant

2009

AAPS PharmSciTech

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“…Oleic acid may reduce the lipid packing order in epithelial cell membranes. This effect could increase the fluidity of the lipid layer and decrease the diffusion resistance, thus assisting the permeation of compounds through the skin [31]. Therefore, AO4F may be explored for a systemic effect because it promoted drug transportation across the skin.…”

Section: Proof Of Concept Of the Formulationsmentioning

confidence: 99%

Surfactant-based Transdermal System for Fluconazole Skin Delivery

Silva¹,

Luz²,

Satake³

et al. 2014

J Nanomed Nanotechnol

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The development of a controlled-release dosage form of antifungals is of crucial importance in view of the side-effects of conventional oral and intravenous treatments of Sporotrichosis. In this study, systems composed of polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (PPG-5-CETETH-20) as a surfactant, oleic acid as an oil phase, and water were developed as a possible fluconazole transdermal drug delivery system. The systems were characterised by polarised light microscopy (PLM), SAXS, and rheological analysis, followed by cellular and histological analyses, in vitro release assays, and ex vivo skin permeation and retention studies using porcine ear tissue and a Franz diffusion cell. PLM and SAXS results indicated that the mixtures of surfactant, oil and water formed micellar and lamellar phases. The incorporation of fluconazole in these systems was greater than in water and conventional dosage forms. Micellar systems behave as Newtonian fluids, being more viscous than elastic in rheological analysis, and lamellar phases behave as pseudoplastic fluids with high elastic moduli. In vitro and in vivo biological assays showed that the formulations did not affect normal cell macrophages and did not promote skin irritation. The release profile indicated that fluconazole could be released in a controlled manner. It was found that the systems enhanced drug permeation and skin retention by changing only the composition of the components in the formulations. Therefore, PPG-5-CETETH-20-based systems have great potential as transdermal systems with different structural and rheological characteristics for Sporotrichosis treatment using antifungal drugs.vehicles. Surfactants are able to stabilise mixtures of components with different polarities, thus creating additional regions for hydrophilic and lipophilic solubilisation of drugs. The drug can be protected against the dissolution medium due to the interfacial membrane, which is composed of the surfactant layer that the drug must pass through to be released. In this manner, surfactant systems also confer reservoir properties. The phase behaviour of surfactants enable the formation of microemulsions and liquid crystals, which is extremely attractive for nanotechnology because these structures are organised on the nanometric scale. In addition to the advantage of increased stability, their production can be scaled up easily. Varying the composition and proportions of surfactant, oil, and aqueous phase, it is possible to control the viscosity and texture of the systems above, which could lead to the immobilisation or localisation of the formulation at specific sites in the body and routes of administration. Therefore, surfactant systems have great potential as transdermal nanostructured drug delivery systems [6].Recently, our research group has demonstrated that the surfactant polyoxypropylene (5)

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“…While the mucosae of the oral cavity are generally considered more permeable than the skin (19), the buccal mucosa still acts as a barrier and may limit the penetration of a drug administered. Moreover, Cx is highly lipophilic (log P value of 4.21) and could show low retention in this tissue.…”

Section: Celecoxib (Cx) or 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-mentioning

confidence: 99%

In Vitro Characterization of Chitosan Gels for Buccal Delivery of Celecoxib: Influence of a Penetration Enhancer

et al. 2011

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Abstract. Celecoxib (Cx) shows high efficacy in the treatment of osteoarthritis and rheumatoid arthritis as a result of its high specificity for COX-2, without gastrolesivity or interference with platelet function at therapeutic concentrations. Besides of anti-inflammatory effects, Cx also has a potential role for oral cancer chemoprevention. For these conditions, oral administration in long-term treatment is a concern due to its systemic side effects. However, local application at the site of injury (e.g., buccal inflammation conditions or chemoprevention of oral cancer) is a promising way to reduce its toxicity. In this study, the in vitro characterization of mucoadhesive chitosan (CHT) gels associated to Azone® was assessed to explore the potential buccal mucosal administration of Cx in this tissue. Rheological properties of gels were analyzed by a rheometer with cone-plate geometry. In vitro Cx release and permeability studies used artificial membranes and pig cheek mucosa, respectively. Mucoadhesion were measured with a universal test machine. CHT gels (3.0%) containing 2.0% or 3.0% Az showed more appropriate characteristics compared to the others: pH values, rheology, higher amount of Cx retained in the mucosa, and minimal permeation through mucosa, besides the highest mucoadhesion values, ideal for buccal application. Moreover, the flux (J) and amounts of drug released decreased with increased CHT and Az concentrations. CHT gels (3.0%) associated with 2.0% or 3.0% Az may be considered potential delivery systems for buccal administration of Cx.

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Buccal penetration enhancers—How do they really work?

Cited by 172 publications

References 100 publications

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

Transbuccal Delivery of 5-Fluorouracil: Permeation Enhancement and Pharmacokinetic Study

Surfactant-based Transdermal System for Fluconazole Skin Delivery

In Vitro Characterization of Chitosan Gels for Buccal Delivery of Celecoxib: Influence of a Penetration Enhancer

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