Diverse deformation properties of polymeric nanocapsules and lipid-core nanocapsules

Fiel, Luana Almeida; Rebêlo, L. M.; Santiago, Thiago de Melo; Adorne, Márcia Duarte; Guterres, Sílvia Stanisçuaski; Sousa, J. S. de; Pohlmann, Adriana Raffin

doi:10.1039/c1sm05508a

Cited by 59 publications

(37 citation statements)

References 46 publications

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“…-10.0 mV to -14.5 mV). The slight negative ζ-potential can be explained by the end-terminal carboxylic acid groups present in PCL coated by polysorbate 80 micelles as has previously been reported [34,35]. The actual stability, which prevents coalescence, is obtained due to steric effects of the surfactant between the two phases [36].…”

Section: Size Distribution ζ-Potential and Phmentioning

confidence: 51%

“…Due to the core and shell structure of NC one can assume that they are more flexible than a rigid matrix system like the NS. Moreover, a previous study on NC and LNC revealed that LNC exhibit a stiffness almost twice as high as NC based on the calculated Young's modulus (MPa) from atomic force microscopy force-displacement curves [34]. Therefore it might be speculated that an enhanced uptake into the hair follicle may be a results of using more flexible particles.…”

Section: Follicular Uptake Of Drug-free Particlesmentioning

confidence: 99%

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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: Size Distribution ζ-Potential and Phmentioning

confidence: 51%

Section: Follicular Uptake Of Drug-free Particlesmentioning

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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show abstract

“…43,44 Moreover, controlled release systems can prolong the release and increase the contact time between the drug and the skin. 21 In addition, LNC-Hst increased the retention of the drug in the stratum corneum, possibly due to its rigid structure, 45 which maintains controlled release of the drug in the skin. LNCs lose their shape a few hours after cutaneous application due to the interaction between the lipids in the nanoparticles and the stratum corneum.…”

mentioning

confidence: 99%

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Menezes

Frank

Lima

et al. 2017

IJN

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Chronic venous insufficiency is characterized by chronic reflux disorder of blood from the peripheral to the central vein, with subsequent venous hypertension and resulting changes in the skin. Traditionally, nonsurgical treatments relied on the use of compression therapy, and more recently a variety of flavonoids have been shown to have positive effects. There have also been developments of more effective drug delivery systems using various textiles and nanotechnology to provide new therapeutic options. Our objective was to use nanotechnology to develop a new formulation containing hesperetin (Hst), a substance not previously used in the treatment of chronic venous insufficiency, impregnated into textile fibers as a possible alternative treatment of venous diseases. We prepared the nanocapsules using the interfacial deposition of preformed polymer method with an Hst concentration of 0.5 mg/mL and then characterized the size and distribution of particles. To quantify the Hst in the samples, we developed an analytical method using high-performance liquid chromatography. Studies of encapsulation efficiency (98.81%±0.28%), microscopy, drug release (free-Hst: 104.96%±12.83%; lipid-core nanocapsule-Hst: 69.90%±1.33%), penetration/permeation, drug content (0.46±0.01 mg/mL) and the effect of washing the textile after drug impregnation were performed as part of the study. The results showed that nanoparticles of a suitable size and distribution with controlled release of the drug and penetration/permeation into the skin layers were achieved. Furthermore, it was established that polyamide was able to hold more of the drug, with a 2.54 times higher content than the cotton fiber; after one wash and after five washes, this relation was 2.80 times higher. In conclusion, this is a promising therapeutic alternative to be further studied in clinical trials.

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“…Three distinct formulations of ZnPc-loaded nanocapsules (Nano A, Nano B and Nano C), with conventional and lipid-core (Pohlmann et al, 2013;Fiel et al, 2011), were made in triplicate through the interfacial deposition of preformed polymer method (Fessi et al, 1989). The ZnPc final concentration inside the nanoparticles was 3.75 μM for photophysical (aggregation) and photochemical (DPBF photodegradation and ZnPc photobleaching) evaluation, and 50 μM for determination of the encapsulation efficiency (EE) and drug release.…”

Section: Preparation Of Znpc-loaded Nanoparticlesmentioning

confidence: 99%

Evaluation of photodynamic activity, photostability and in vitro drug release of zinc phthalocyanine-loaded nanocapsules

Souza

Ziembowicz

Müller

et al. 2016

European Journal of Pharmaceutical Sciences

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Diverse deformation properties of polymeric nanocapsules and lipid-core nanocapsules

Cited by 59 publications

References 46 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

Hesperetin-loaded lipid-core nanocapsules in polyamide: a new textile formulation for topical drug delivery

Evaluation of photodynamic activity, photostability and in vitro drug release of zinc phthalocyanine-loaded nanocapsules

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