Design and Characterization of Silicone and Surfactant Based Systems for Topical Drug Delivery

Satake

Calixto

et al. 2017

IJN

Self Cite

Resveratrol (Res) is a common phytoalexin present in a few edible materials, such as grape skin, peanuts, and red wine. Evidence has shown the beneficial effects of Res on human health, which may be attributed to its anti-inflammatory activity. However, the poor aqueous solubility of Res limits its therapeutic effectiveness. Therefore, the use of nanostructured delivery systems for Res, such as liquid-crystalline systems, could be beneficial. In this study, we aimed to develop, characterize, and determine the in vivo effectiveness of Res-loaded liquid-crystalline systems. Systems containing copaiba balsam oil, polyethylene glycol-40 hydrogenated castor oil, and water were designed. Results of polarized light microscopy, small-angle X-ray scattering, texture-profile analysis, and flow-rheology analysis showed that the Res-loaded liquid-crystalline system had a lamellar structure, textural and mechanical (hardness, compressibility, and adhesiveness) properties, and behaved as a non-Newtonian fluid, showing pseudoplastic behavior upon skin application. Furthermore, all liquid-crystalline systems presented bioadhesive properties that may have assisted in maintaining the anti-inflammatory activity of Res, since the topical application of the Res-loaded lamellar mesophase liquid crystals resulted in edema inhibition in a carrageenan-induced paw-inflammation mouse model. Therefore, Res-loaded lamellar mesophases represent a promising new therapeutic approach for inhibition of skin inflammation.

mentioning

confidence: 99%

Trans-resveratrol-loaded nonionic lamellar liquid-crystalline systems: structural, rheological, mechanical, textural, and bioadhesive characterization and evaluation of in vivo anti-inflammatory activity

Satake

Calixto

et al. 2017

IJN

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“…Furthermore, the results were consistent with the previous findings that hexagonal phases have high hardness and compressibility parameters. 13,65 Compressibility reflects the ease of taking the prepared formulation from the container and the ease of spreading on the application site, 66 and adhesiveness is the work required to overcome the attractive forces between the surface of the sample and the surface of the probe. 64 Formulations for cutaneous application should have both good hardness and adhesiveness.…”

mentioning

confidence: 99%

Design, characterization, and biological evaluation of curcumin-loaded surfactant-based systems for topical drug delivery

Santos

Rodero

et al. 2016

IJN

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From previous studies, it has been found that curcumin exhibits an anti-inflammatory activity and is being used for the treatment of skin disorders; however, it is hydrophobic and has weak penetrating ability, resulting in poor drug transport through the stratum corneum. The aim of this study was to develop liquid crystalline systems for topical administration of curcumin for the treatment of inflammation. These liquid crystalline systems were developed from oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, and water as the surfactant, oil phase, and aqueous phase, respectively. These systems were characterized, and polarized light microscopy showed anisotropy with lamellar mesophases (Formulation 1) and hexagonal mesophases (Formulations 2 and 3), which were confirmed by the peak ratio measured using small-angle X-ray scattering. In addition, rheological tests revealed that the formulations exhibited gel-like behavior (G′>G″), as evidenced by the increased G′ values that indicate structured systems. Texture profile analysis showed that hexagonal mesophases have high values of hardness, adhesiveness, and compressibility, which indicate structured systems. In vitro studies on bioadhesion revealed that the hexagonal mesophases increased the bioadhesiveness of the systems to the skin of the pig ear. An in vivo inflammation experiment showed that the curcumin-loaded hexagonal mesophase exhibited an anti-inflammatory activity as compared to the positive control (dexamethasone). The results suggest that this system has a potential to be used as a bioadhesive vehicle for the topical administration of curcumin. Therefore, it is possible to conclude that these systems can be used for the optimization of drug delivery systems to the skin.

“…The same study was performed by others authors using J-774 mouse macrophages as the cellular model. The results of cellular viability for formulations of liquid crystals and nanostructured lipid carriers were greater than 92% (Gonçalez, Correa, Chorilli, 2013;Oliveira et al, 2014;Kolenyak-Santos et al, 2015;Oyafuso et al, 2015).…”

Section: In Vitro Safety Profilementioning

confidence: 92%

Organic cocoa extract -loaded surfactant-based systems intended to skin bioadhesion

Funagoshi

Oliveira

et al. 2017

Braz. J. Pharm. Sci.

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This study was to develop, characterize, and evaluate the physical-chemical stability, in vitro antioxidant activity and in vitro safety profile of liquid crystalline systems (LCS) and microemulsions (MEs) with and without organic cocoa (OC) extract. LCS stabilized by surfactant polyoxyethylene 20 cetyl ether, containing water and oleic acid were studied. LCS and MEs were characterized using polarized light microscopy, small angle X-ray scattering, rheology and in vitro bioadhesion, and were evaluated for a period of 30 days by visual aspects, centrifuge test, pH value and relative density. PLM and SAXS assays showed the presence of domains of MEs, cubic and hexagonal mesophasephases, varying the proportions of the components of the formulations; where in the addition of the extract did not change rheological behavior of the formulations. All of the formulations were stable in the period analyzed and presented higher bioadhesive strength. In vitro antioxidant activity suggests that LCS and MEs presented a high capacity to maintain the antioxidant activity of OC extract. The results showed that the incorporation of OC in LCS improved the safety profile, according to cytotoxicity assays of systems may be a promising platform to OC extract for topical application for the potential treatment of skin disorders. Keywords:Liquid crystals/evaluation/physical-chemical stability. Microemulsions/evaluation. Surfactant-based system. Organic cocoa extract. Skin bioadhesion. INTRODUCTIONSkin is routinely exposed to stressful environmental factors such as pollutants and UV radiation. These factors produce a large number of aggressive oxidants that damage all of the biological skin cell membranes (Silva et al., 2010;Binic et al., 2013;Datta et al., 2011;Dupont, Gomez, Bilodeau, 2013). Accordingly, the use of skin care products and cosmetics has been utilized to mitigate the cutaneous photoaging process (Visscher, Pan, Kitzmiller, 2013) and these products are commonly composed of plant extracts (Binic et al., 2013).A great number of plants and plant extracts are studied for their antioxidative action arising from their phenolic substructures. Phenolic compounds are composed of an aromatic ring that is linked to a hydroxyl group, which donates electrons and hydrogen atoms. As a result, these compounds are exceptional antioxidants (Silva et al., 2010;Binic et al., 2013;Reuter, Merfort, Schempp, 2010).Cocoa, the dried and fermented seeds derived from Theobroma cacao, has been consumed since 1100 B.C. by ancient civilizations such as the Mayans and Aztecs (Hurst et al., 2002). Cocoa contains high amounts of the flavonoids (−)-epicatechin (EC) and (+)-catechin, and procyanidins B2 and B1. Additionally, other polyphenols such as quercetin, isoquercitrin (quercetin 3-O-glucoside), quercetin 3-O-arabinose, hyperoside (quercetin 3-O-galactoside), naringenin, luteolin, and apigenin have also been found in cocoa in minor quantities (Sánchez-Rabaneda et al., 2003). While the natural amount B. Fonseca-Santos, E. E. Funagoshi, J. R. S. Olivei...