Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization

Hu, Fuqiang; Yuan, Hong; Zhang, H.H; Fang, Mengxiang

doi:10.1016/s0378-5173(02)00081-9

Cited by 230 publications

(106 citation statements)

References 11 publications

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“…In vitro drug release tests were performed using the dialysis bag method with water/polysorbate 80/PEG 400 (60:0.5:40 v/v) as the receptor medium [15,26,27]. According to previous studies, polysorbate 80 and PEG 400, at the concentrations described above, were added in order to maintain sink conditions during the experiments.…”

Section: Drug Release Studymentioning

confidence: 99%

Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects

Mathes

Melero

Conrad

et al. 2016

Journal of Controlled Release

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The treatment of various hair disorders has become a central focus of good dermatologic patient care as it affects men and women all over the world. For many inflammatory-based scalp diseases, glucocorticoids are an essential part of treatment, even though they are known to cause systemic as well as local adverse effects when applied topically. Therefore, efficient targeting and avoidance of these side effects are of utmost importance. Optimizing the balance between drug release, interfollicular permeation, and follicular uptake may allow minimizing these adverse events and simultaneously improve drug delivery, given that one succeeds in targeting a sustained release formulation to the hair follicle. To test this hypothesis, three types of polymeric nanocarriers (nanospheres, nanocapsules, lipid-core nanocapsules) for the potent glucocorticoid Clobetasol propionate (CP) were prepared. They all exhibited a sustained release of drug, as was desired. The particles were formulated as a dispersion and hydrogel and (partially) labeled with Rhodamin B for quantification purposes. Follicular uptake was investigated using the Differential Stripping method and was found highest for nanocapsules in dispersion after application of massage. Moreover, the active ingredient (CP) as well as the nanocarrier (Rhodamin B labeled polymer) recovered in the hair follicle were measured simultaneously, revealing an equivalent uptake of both. In contrast, only negligible amounts of CP could be detected in the hair follicle when applied as free drug in solution or hydrogel, regardless of any massage. Skin permeation experiments using heat-separated human epidermis mounted in Franz Diffusion cells revealed equivalent reduced transdermal permeability for all nanocarriers in comparison to application of the free drug. Combining these results, nanocapsules formulated as an aqueous dispersion and applied by massage appeared to be a good candidate to maximize follicular targeting and minimize drug penetration into the interfollicular epidermis. We conclude that such nanotechnology-based formulations provide a viable strategy for more efficient -2-drug delivery to the hair follicle. Moreover, they present a way to minimize adverse effects of potent glucocorticoids by releasing the drug in a controlled manner and simultaneously decreasing interfollicular permeation, offering an advantage over conventional formulations for inflammatorybased skin/scalp diseases. Graphical Abstract AbbreviationsAA: Alopecia areata ANOVA: Analysis of variance CCT: capric/caprylic triglyceride CP: Clobetasol propionate

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Section: Drug Release Studymentioning

confidence: 99%

Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects

Mathes

Melero

Conrad

et al. 2016

Journal of Controlled Release

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“…There are a variety of techniques used to manufacture these materials including high pressure homogenization and solvent diffusion. [5][6][7][8][9] The first method requires more mechanical energy input than the second method but does not depend on the use of an organic solvent which can be a limitation for certain products or markets. Solid lipid particles found initial applications for the delivery of therapeutic agents and represented an alternative to the use of liposomes for the encapsulation of bioactives.…”

Section: Introductionmentioning

confidence: 99%

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Holser

2011

Lipid�Insights

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Encapsulation of structurally sensitive compounds within a solid lipid matrix provides a barrier to prooxidant compounds and effectively limits the extent of oxidative degradation. This offers a simple approach to preserve the bioactivity of labile structures. The technology was developed for cosmetic and pharmaceutical products but may be applied to additives used in food and feed formulations. The encapsulation of docosahexaenoic acid (DHA) and α-linolenic acid (ALA) was examined as model compounds of current interest in functional foods and feeds. Solid lipid particles were prepared from triglycerides containing saturated and unsaturated fatty acids and evaluated by differential scanning calorimetry. The thermal characteristics of the lipids used to form the particle were related to molecular structure and could be adjusted by selection of the appropriate component fatty acids. Encapsulation by solid lipid particles provides a method to inhibit oxidation and improve shelf life of products formulated with DHA and ALA.

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“…These methods are high pressure homogenization [Liedtke, 2000;Jahnke, 1998;Wissing et al, 2004], microemulsion technique [Gasco, 1993;Gasco, 1997;Priano et al, 2007], emulsification-solvent evaporation [Sjöström & Bergenstahl, 1992], emulsificationsolvent diffusion method [Hu et al, 2002;Trotta et al, 2003], solvent injection (or solvent displacement) method [Schubert, & Müller-Goymann, 2003], phase inversion [Heurtault et al, 2002], multiple emulsion technique [Garcy´-Fuentes et al, 2002], ultrasonication [Pietkiewicz, & Sznitowska, 2004;Puglia et al, 2008] and membrane contractor technique [Charcosset et al, 2005]. However, high pressure homogenization technique has many advantages compared to the other methods, e.g.…”

Section: Preparation Methodsmentioning

confidence: 99%

Solid Lipid Nanoparticles: Technological Developments and in Vivo Techniques to Evaluate Their Interaction with the Skin

Bleve¹,

Pavanetto²,

Perugini³

2011

Progress in Molecular and Environmental Bioengineering - From Analysis and Modeling to Technology Applications

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Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization

Cited by 230 publications

References 11 publications

Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects

Nanocarriers for optimizing the balance between interfollicular permeation and follicular uptake of topically applied clobetasol to minimize adverse effects

Encapsulation of Polyunsaturated Fatty Acid Esters with Solid Lipid Particles

Solid Lipid Nanoparticles: Technological Developments and in Vivo Techniques to Evaluate Their Interaction with the Skin

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