Selective follicular targeting by modification of the particle sizes

Patzelt, Alexa; Richter, Heike; Knorr, Fanny; Schäfer, U.; Lehr, Claus‐Michael; Dähne, Lars; Sterry, Wolfram; Lademann, Juergen

doi:10.1016/j.jconrel.2010.11.015

Cited by 284 publications

(174 citation statements)

References 23 publications

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“…This result contradicts the report of Patzelt et al, which showed that reductions in particle size (643 nm, 470 nm, 300 nm, 122 nm) led to a significant reduction in particle penetration depth. 30 In support of the current findings, Abddel Mottaleb et al reported results indicating that the follicular penetration of nanoparticles increases following a decrease in size. 31 …”

Section: 25supporting

confidence: 89%

The Effect of Particle Size on the Deposition of Solid Lipid Nanoparticles in Different Skin Layers: A Histological Study

Adib¹,

Ghanbarzadeh²,

Kouhsoltani³

et al. 2016

Adv Pharm Bull

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Section: 25supporting

confidence: 89%

The Effect of Particle Size on the Deposition of Solid Lipid Nanoparticles in Different Skin Layers: A Histological Study

Adib¹,

Ghanbarzadeh²,

Kouhsoltani³

et al. 2016

Adv Pharm Bull

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“…For these particles quantitative data on follicular uptake of both, the active ingredient (CP) and the nanocarrier itself (100% labeled PCL), was measured for the same sample set and revealed no significant difference after applying the two quantification methods (p>0.05; see Table 4: CP-loaded NC, 100% labeled). Of note, the small range in particle size investigated in this study may be responsible that no size-dependent effect could be observed in comparison to the data presented previously by Lademann et al [38]. To elucidate this topic further, a larger range in particle size should be investigated in the future.…”

Section: Follicular Uptake Of Clobetasol-loaded Nanocapsules and Contmentioning

confidence: 45%

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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“…As it was described before, the follicles are deep invaginations inside skin where the SC is thinner, the vascularisation is denser, and there are several targets of interest along a follicle structure from both cosmetic and pharmaceutical viewpoints [172]. Here, minoxidil which is an antihypertensive has been introduced in a block of copolymer poly (-caprolactone)-block-poly(ethyleneglycol) to treat the alopecia areata disorder , by widening blood vessels and opening potassium channels, it allows more oxygen, blood, and nutrients to the follicle.…”

Section: Applications Of Nanocarrier Systems In Topical/transdermal Dmentioning

confidence: 94%

Nanocarrier Systems for Transdermal Drug Delivery

Escobar-Chávez¹,

Rodríguez-Cruz²,

Domínguez-Delgado³

et al. 2012

Recent Advances in Novel Drug Carrier Systems

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is an open discussion, in one hand, the nanotechnologist continue making new and more sophisticated nanocarriers and in the other hand, toxicologist continue evaluating possible damaging effects.Whatever it happens, nanotechnology is the new era and nanomedicine cannot be taking off. New nanocarriers will be created and the entire scientist working in nanomedicine bet for it to be the cure of diseases that in this moment are difficult to deal with [3] The application of preparations to the skin for medical purposes is as old as the history of medicine itself, with references to the use of ointments and salves found in the records of Babylonian and Egyptian medicine. The historical development of permeation research is well described by Hadgraft & Lane [4]. Over time, the skin has become an important route for drug delivery in which topical, regional or systemic effects are desired. Nevertheless, skin constitutes an excellent barrier and presents difficulties for the transdermal delivery of therapeutic agents, since few drugs possess the characteristics required to permeate across the stratum corneum in sufficient quantities to reach a therapeutic concentration in the blood. In order to enhance drug transdermal absorption different methodologies have been investigated developed and patented [5,6]. Improvement in physical permeationenhancement technologies has led to renewed interest in transdermal drug delivery. Some of these novel advanced transdermal permeation enhancement technologies include: iontophoresis, electroporation, ultrasound, microneedles to open up the skin and more recently the use of transdermal nanocarriers [3,[7][8][9][10].A number of excellent reviews that have been published contain detailed discussions concerning many aspects of transdermal nanocarriers [11][12][13][14][15][16][17]. The present chapter shows an updated overview of the use of submicron particles and other nanostructures in the pharmaceutical field, specifically in the area of topical and transdermal drugs. This focus is justified due to the magnitude of the experimental data available with the use of these nanocarriers. The development of submicron particles and other nanostructures in the pharmaceutical and cosmetic fields has been emerged in the last decades for designing best formulations for application through the skin [18][19][20][21]. The skinThe skin is the largest organ of the body [22][23][24], accounting for more than 10% of body mass, and the one that enables the body to interact more intimately with its environment. Essentially, the skin consists of four layers: The SC, that is the outer layer of the skin (nonviable epidermis), and forms the rate-controlling barrier for diffusion for almost all compounds. It is composed of dead flattened, keratin-rich cells, the corneocytes. These dense cells are surrounded by a complex mixture of intercellular lipids, namely, ceramides, free fatty acids, cholesterol, and cholesterol sulphate. Their most important feature is that they are structured as ordered bilayer arrays [25]...

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Selective follicular targeting by modification of the particle sizes

Cited by 284 publications

References 23 publications

The Effect of Particle Size on the Deposition of Solid Lipid Nanoparticles in Different Skin Layers: A Histological Study

The Effect of Particle Size on the Deposition of Solid Lipid Nanoparticles in Different Skin Layers: A Histological Study

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

Nanocarrier Systems for Transdermal Drug Delivery

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