Rheological, Mechanical and Adhesive Properties of Surfactant-Containing Systems Designed as a Potential Platform for Topical Drug Delivery

Carvalho, Flávia Chiva; Silva, Hilris Rocha e; Luz, Gabriela Marielli da; Barbi, Mariana da Silva; Landgraf, Daniele Silveira; Chiavacci, Leila Aparecida; Sarmento, Víctor Hugo Vitorino; Gremião, Maria Palmira Daflon

doi:10.1166/jbn.2012.1373

Cited by 27 publications

(31 citation statements)

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“…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].…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Introductionmentioning

confidence: 99%

“…Therefore, surfactant systems have great potential as transdermal nanostructured drug delivery systems [6]. such as lamellar, hexagonal, and cubic phases, depending on the proportion of the components and the oily phases [6]. This capacity has been exploited as a technological platform to develop new drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Surfactant-based Transdermal System for Fluconazole Skin Delivery

Silva¹,

Luz²,

Satake³

et al. 2014

J Nanomed Nanotechnol

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“…43 However, pseudoplasticity can be due to the LC structure, which causes greater resistance to flow than the microemulsions, which are colloidal systems. 44 Such a property is desirable for formulations developed for oral administration, eg, during application at high shear rates, deinterlacing of the polymer chains, and subsequent thinning of the flow will occur, thereby facilitating administration of the formulation. However, upon withdrawal of this tension, the formulation will recover its initial viscosity, remaining longer in the oral environment.…”

Section: Discussionmentioning

confidence: 99%

“…The increase in viscosity and elastic characteristics contributes to the increase in the residence time of the formulation. 44 Furthermore, bioadhesion can be also attributed to presence of the negatively charged polymer C974. Although the literature reports that chitosan hydrogels are very bioadhesive due to the forces of molecular attraction by electrostatic interactions between positive groups of chitosan and negative groups of the biological surface, we were able to demonstrate that the F1C obtained values within the range of bioadhesion for chitosan-based LCS values.…”

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confidence: 99%

“…Most of the polyacrylic acid derivatives are not soluble in water, but form viscous gels when hydrated, increasing their ability to adhere to the tooth surface. 44 There is no standard formula available for bioadhesive drugdelivery systems for dental applications. However, the LCS formed by the C974 polymer as an aqueous phase was shown to be suitable, because upon hydration there was an increase in bioadhesion strength, pseudoplasticity, and elasticity, resulting in a promising platform for oral p1025 delivery.…”

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Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of <em>Streptococcus mutans </em>biofilms

Calixto¹,

Duque²,

Aida³

et al. 2017

IJN

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Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025–1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery. Potentiation of the action of LCS can be achieved with the use of bioadhesive polymers to prolong their residence on the teeth. In line with this, three formulations – polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, oleic acid, and Carbopol C974P in different combinations (F1C, F2C, and F3C) were developed to observe the influence of water in the LCS, with the aim of achieving in situ gelling in the oral environment. These formulations were assessed by polarized light microscopy, small-angle X-ray scattering, rheological analysis, and in vitro bioadhesion analysis. Then, p1025 and a control (chlorhexidine) were incorporated into the aqueous phase of the formulation (F + p1025 and F + chlorhexidine), to determine their antibiofilm effect and toxicity on epithelial cells. Polarized light microscopy and small-angle X-ray scattering showed that F1C and F2C were LCS, whereas F3C was a microemulsion. F1C and F2C showed pseudoplastic behavior and F3C Newtonian behavior. F1C showed the highest elastic and bioadhesive characteristics compared to other formulations. Antibiofilm effects were observed for F + p1025 when applied in the surface-bound salivary phase. The p1025-loaded nanostructured LCS presented limited cytotoxicity and effectively reduced S. mutans biofilm formation, and could be a promising p1025-delivery strategy to prevent the formation of S. mutans dental biofilm.

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