Nanoparticles – An efficient carrier for drug delivery into the hair follicles

Lademann, Juergen; Richter, Heike; Teichmann, A.; Otberg, Nina; Blume-Peytavi, Ulrike; Luengo, Javiana; Weiß, Barbara; Schaefer, Ulrich F.; Lehr, Claus‐Michael; Wepf, Roger; Sterry, Wolfram

doi:10.1016/j.ejpb.2006.10.019

Cited by 494 publications

(346 citation statements)

References 20 publications

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“…To elucidate this topic further, a larger range in particle size should be investigated in the future. As for the controls, the amount detected in the hair follicle of free CP in an ethanolic solution and free CP in HG, with and without the application of massage, was below the lower limit of quantification (LLOQ) for both experimental setups and thus negligible [19,29,39]. This confirms that by means of encapsulation a more targeted delivery to the hair follicle was achieved.…”

Section: Follicular Uptake Of Clobetasol-loaded Nanocapsules and Contsupporting

confidence: 60%

“…This positive effect of the applied massage upon follicular penetration has already been explained in literature before, where the authors claim that the process of moving the hair by massaging the skin acts like a 'gear pump', transporting the particles into the hair follicle, i.e. into the hair shaft, by mimicking the natural movement of the hair together with the scaly structure of the hair cuticula [19]. Similar as in (a), NC provided a significantly higher follicular recovery as opposed to NS and LNC (two-way ANOVA, p<0.05) after application of the massage when formulated as both, an aqueous dispersion and HG.…”

Section: Follicular Uptake Of Drug-free Particlessupporting

confidence: 58%

“…Thus, a formulation with a sustained-release effect and/or targeted follicular delivery of glucocorticosteroids could be a new strategy to improve patient compliance and simultaneously minimize local adverse effects. In 2007, Lademann et al reported that poly(lactic-coglycolic acid) nanoparticles can accumulate in porcine hair follicles and be used to target drugs to this skin annex [19]. They demonstrated a depot effect of nanoparticles in the hair follicle for up to 10 days, while nanoparticles on the skin surface were only detectable for up to 24 h. Consequently, besides the already mentioned specific scalp diseases, typical high-prevalence, barrier-weakening inflammatory skin disorders, e.g.…”

Section: Introductionmentioning

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: Follicular Uptake Of Clobetasol-loaded Nanocapsules and Contsupporting

confidence: 60%

Section: Follicular Uptake Of Drug-free Particlessupporting

confidence: 58%

Section: Introductionmentioning

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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“…Porcine ear skin provides a structure similar to human skin [22,23] and is well suited for the investigation of the penetration of particles into the hair follicles, as previously shown [4,10,14]. Excised human skin is not applicable for follicular penetration studies, since human skin contracts directly after excision which leads to a permanent occlusion of the hair follicles by the contracted elastic fibers [24].…”

Section: Tissue Samplesmentioning

confidence: 99%

“…Additionally, dendritic cells [2] and stem cells [3], important for immunology and regenerative medicine, respectively, are closely associated with the hair follicles rendering them even more attractive for the development of selective drug delivery systems. Recently, it was demonstrated that particles in general [4][5][6][7][8][9] and especially at a size between 300 and 600 nm penetrate very efficiently and deeper into the hair follicles than non-particulate substances [4,10]. Likewise, the storage time was found to be increased by up to 10 days, in the case of the particulate substances, which is significantly longer than 4 days, as observed for the non-particulate substances [11,12].…”

Section: Introductionmentioning

confidence: 99%

Triggering of drug release of particles in hair follicles

Mak

Patzelt

Richter

et al. 2012

Journal of Controlled Release

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Particulate drug delivery via hair follicles represents a promising concept, although requirements are high. This process must be realized at the desired depth and at the appropriate time, due to the fact that the particles themselves are not able to overcome the follicular skin barrier.In the present study, a novel triggering concept for the release of a model drug from the delivering particles is presented basing on the application of two different particle types of the same size, where one particle type is the drug carrier, and the second one is loaded with a protease. The latter one is supposed to interact with the drugcarrying particles to trigger the drug release. A mixture of both particles was applied on porcine skin samples, followed by follicular analysis. As controls, the particles were applied unaided without protease, and one skin area remained untreated. The investigations revealed that the protease was able to release the model drug from the delivering particles in significant depths within the hair follicle (866 ± 62 nm).Additionally, an uptake of the model drug in the sebaceous gland was observed after release providing a promising novel approach for the development of treatment strategies of different skin diseases.

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