Novel aqueous chitosan-based dispersions as efficient drug delivery systems for topical use. Rheological, textural and release studies

Lucero, M.J.; Ferris, Cristina; Sánchez‐Gutiérrez, Carla Andrea; Jiménez-Castellanos, M.R.; de-Paz, M.-Violante

doi:10.1016/j.carbpol.2016.06.006

Cited by 20 publications

(10 citation statements)

References 34 publications

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“…Thus, about four times greater force was needed to separate extract-loaded formulations from the probe. This can relate to the ability of the extract to modify the liquid crystalline arrangement forming more organized structures, which also led to increased viscosity as well as adhesiveness of all formulations [29].…”

Section: Resultsmentioning

confidence: 99%

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Structural Features and the Anti-Inflammatory Effect of Green Tea Extract-Loaded Liquid Crystalline Systems Intended for Skin Delivery

et al. 2017

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Abstract:Camellia sinensis, which is obtained from green tea extract (GTE), has been widely used in therapy owing to the antioxidant, chemoprotective, and anti-inflammatory activities of its chemical components. However, GTE is an unstable compound, and may undergo reactions that lead to a reduction or loss of its effectiveness and even its degradation. Hence, an attractive approach to overcome this problem to protect the GTE is its incorporation into liquid crystalline systems (LCS) that are drug delivery nanostructured systems with different rheological properties, since LCS have both fluid liquid and crystalline solid properties. Therefore, the aim of this study was to develop and characterize GTE-loaded LCS composed of polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, avocado oil, and water (F25E, F29E, and F32E) with different rheological properties and to determine their anti-inflammatory efficacy. Polarized light microscopy revealed that the formulations F25, F29, and F32 showed hexagonal, cubic, and lamellar liquid crystalline mesophases, respectively. Rheological studies showed that F32 is a viscous Newtonian liquid, while F25 and F29 are dilatant and pseudoplastic non-Newtonian fluids, respectively. All GTE-loaded LCS behaved as pseudoplastic with thixotropy; furthermore, the presence of GTE increased the S values and decreased the n values, especially in F29, indicating that this LCS has the most organized structure. Mechanical and bioadhesive properties of GTE-unloaded and -loaded LCS corroborated the rheological data, showing that F29 had the highest mechanical and bioadhesive values. Finally, in vivo inflammation assay revealed that the less elastic and consistent LCS, F25E and F32E presented statistically the same anti-inflammatory activity compared to the positive control, decreasing significantly the paw edema after 4 h; whereas, the most structured and elastic LCS, F29E, strongly limited the potential effects of GTE. Thereby, the development of drug delivery systems with suitable rheological properties may enhance GTE bioavailability, enabling its administration via the skin for the treatment of inflammation.

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Section: Resultsmentioning

confidence: 99%

“…Furthermore, the presence of the extract also increased the cohesiveness of all formulations, which indicates that intermolecular interactions occurred between the components of the formulation and the GTE, forming unbreakable structures with high recovery capacity after stress [29].…”

Section: Resultsmentioning

confidence: 99%

Structural Features and the Anti-Inflammatory Effect of Green Tea Extract-Loaded Liquid Crystalline Systems Intended for Skin Delivery

et al. 2017

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“…Rheological measurements of these materials should be made for a number of reasons including [30][31][32][33][34][35][36]:…”

Section: Rheological Properties Of the Drugs And Drug Carriersmentioning

confidence: 99%

Rheology of Drugs For Topical and Transdermal Delivery

Walicka

Falicki

Iwanowska-Chomiak

2019

International Journal of Applied Mechanics and Engineering

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Skin drug delivery systems are a constant source of interest because of the benefits that they offer to overcome many drawbacks associated with other modes of drug delivery (i.e. oral, intravenous, etc.). Because of the impermeable nature of the skin, designing a suitable drug delivery vehicle that penetrates the skin barrier is challenging. Skin drug delivery can be subdivided into topical and transdermal (Fig.1). In a topical administration the drug is intended to act at skin level, this is indicated for the treatment of skin diseases. The aim of transdermal administration is getting a systemic release and in this case the skin represents a barrier not a target. The availability of drugs or other active substances through the skin depends basically on two consecutive steps: the release of these drugs or substances from vehicle or carrier and their subsequent permeation through the skin. Hence, studies on the specific properties of vehicles or carriers, such as their rheological behaviours, are of great interest in the field of pharmaceutical products. The objective of the present study is to systematically characterize a nonlinear rheological behaviour and flow properties of drugs and drug carriers into topical and transdermal administration. To this aim, one- and threedimensional rheological models are presented, which may be used to describe drug release through the skin and through the extracellular and interstitial matrix structures. Finally, the rheological measurements of some commercial creams and ointments were made.

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“…CTS hydrogels can be prepared via physical association (ionic crosslinking) [5,6,7,8,9], coordination with metal ions [10], or irreversible/chemical cross-linking between chitosan and the crosslinker [11,12,13]. The chemical and/or physical linkages will prevent the networks from dissolving.…”

Section: Introductionmentioning

confidence: 99%

Reversible pH-Sensitive Chitosan-Based Hydrogels. Influence of Dispersion Composition on Rheological Properties and Sustained Drug Delivery

et al. 2018

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The present work deals with the synthesis of micro-structured biomaterials based on chitosan (CTS) for their applications as biocompatible carriers of drugs and bioactive compounds. Twelve dispersions were prepared by means of functional cross-linking with tricarballylic acid (TCA); they were characterized by Fourier transform infrared spectroscopy (FT-IR), modulated temperature differential scanning calorimetry (MTDSC) and scanning electron microscopy (SEM), and their rheological properties were studied. To the best of the authors’ knowledge, no study has been carried out on the influence of CTS concentration, degree of cross-linking and drug loading on chitosan hydrogels for drug delivery systems (DDS) and is investigated herein for the first time. The influence of dispersion composition (polymer concentration and degree of cross-linking) revealed to exert a marked impact on its rheological properties, going from liquid-like to viscoelastic gels. The release profiles of a model drug, diclofenac sodium (DCNa), as well as their relationships with polymer concentration, drug loading and degree of cross-linking were evaluated. Similar to the findings on rheological properties, a wide range of release profiles was encountered. These formulations were found to display a well-controlled drug release strongly dependent on the formulation composition. Cumulative drug release under physiological conditions for 96 h ranged from 8% to 67%. For comparative purpose, Voltaren emulgel® from Novartis Pharmaceuticals was also investigated and the latter was the formulation with the highest cumulative drug release (85%). Some formulations showed similar spreadability values to the commercial hydrogel. The comparative study of three batches confirmed the reproducibility of the method, leading to systems particularly suitable for their use as drug carriers.

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Novel aqueous chitosan-based dispersions as efficient drug delivery systems for topical use. Rheological, textural and release studies

Cited by 20 publications

References 34 publications

Structural Features and the Anti-Inflammatory Effect of Green Tea Extract-Loaded Liquid Crystalline Systems Intended for Skin Delivery

Structural Features and the Anti-Inflammatory Effect of Green Tea Extract-Loaded Liquid Crystalline Systems Intended for Skin Delivery

Rheology of Drugs For Topical and Transdermal Delivery

Reversible pH-Sensitive Chitosan-Based Hydrogels. Influence of Dispersion Composition on Rheological Properties and Sustained Drug Delivery

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