Size dependent skin penetration of nanoparticles in murine and porcine dermatitis models

Try, Céline; Moulari, Brice; Béduneau, Arnaud; Fantini, Oscar; Pin, Didier; Pellequer, Yann; Lamprecht, Alf

doi:10.1016/j.ejpb.2016.01.002

Cited by 51 publications

(43 citation statements)

References 43 publications

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“…Three structures with <75 nm in size (TH21, TH37, 6H714) showed considerable skin penetration, in which small tetrahedron TH37 (44 nm) and TH21 (17 nm) reached deeply to ~350–400 µm beneath skin surface in mice. This result aligns well with reported size-dependency on carrier skin penetrative ability 30 . However, the three distinct-shaped structures with similar size (~180 nm; TH337, R13730, and T14498) all showed minimal skin penetration (~50–75 µm from the skin surface).…”

Section: Discussionsupporting

confidence: 92%

Framework nucleic acids as programmable carrier for transdermal drug delivery

et al. 2019

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DNA nanostructures are promising drug carriers with their intrinsic biocompatibility, uniformity and versatility. However, rapid serum disintegration leads to low bioavailability at targeted sites following systemic administration, hindering their biomedical applications. Here we demonstrate transdermal delivery of framework nucleic acids (FNAs) through topical applications. By designing FNAs with distinct shapes and sizes, we interrogate their penetration on mice and human skin explant. Skin histology reveals size-dependent penetration, with FNAs ≤75 nm effectively reaching dermis layer. 17 nm-tetrahedral FNAs show greatest penetration to 350 µm from skin periphery. Importantly, structural integrity is maintained during the skin penetration. Employing a mouse melanoma model, topical application of doxorubicin-loaded FNAs accommodates ≥2-fold improvement in drug accumulation and tumor inhibition relative to topically-applied free doxorubicin, or doxorubicin loaded in liposomes and polymeric nanoparticles. Programmable penetration with minimal systemic biodistribution underlines FNA potential as localized transdermal drug delivery carriers.

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Section: Discussionsupporting

confidence: 92%

Framework nucleic acids as programmable carrier for transdermal drug delivery

et al. 2019

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“…Smaller sizes have been reported by introducing a sonication step during PEG conjugation reaction [ 25 ]. It is relevant to notice that nano-sized particles have been reported to result in improved skin permeation and skin retention, improving treatment outcomes of inflammatory skin diseases [ 35 , 36 ].…”

Section: Discussionmentioning

confidence: 99%

Near-Infrared Radiation-Based Mild Photohyperthermia Therapy of Non-Melanoma Skin Cancer with PEGylated Reduced Nanographene Oxide

et al. 2020

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Using a one-step thermal reduction and non-covalent chemical functionalization process, PEGylated reduced nanographene oxide (rGOn-PEG) was produced from nanographene oxide (GOn) and characterized in terms of particle size, dispersion stability, chemistry, and photothermal properties, in view of its use for photothermal therapy (PTT) of non-melanoma skin cancer. GOn infrared spectrum presented more intense bands assigned to oxygen containing functional groups than observed for rGOn-PEG. GOn C/O ratio decreased more than 50% comparing with rGOn-PEG and nitrogen was present in the latter (N at % = 20.6) due to introduction of PEG-NH2. Thermogravimetric analysis allowed estimating the amount of PEG in rGOn-PEG to be of about 56.1%. Simultaneous reduction and PEGylation increased the lateral dimensions from 287 ± 139 nm to 521 ± 397 nm, as observed by transmission electron microscopy and dynamic light scattering. rGOn-PEG exhibited ≈13-fold higher absorbance in the near-infrared radiation (NIR) region, as compared to unmodified GOn. Low power (150 mW cm−2) NIR irradiation using LEDs resulted in rGOn-PEG heating up to 47 °C, which is within the mild PTT temperature range. PEGylation strongly enhanced the dispersibility of rGOn in physiological media (phosphate buffered saline, fetal bovine serum, and cell culture medium) and also improved the biocompatibility of rGOn-PEG, in comparison to GOn (25–250 μg mL−1). After a single NIR LED irradiation treatment of 30 min, a decrease of ≈38% in A-431 cells viability was observed for rGOn-PEG (250 μg mL−1). Together, our results demonstrate the potential of irradiating rGOn-PEG using lower energy, cheaper, smaller, and safer LEDs, as alternative to high power lasers, for NIR mild hyperthermia therapy of cancer, namely non-melanoma skin cancer.

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“…In our study, AmB-CH-TPP nanoparticles (Size = 68 ± 7 nm, Zeta potential = 30 ± 2) presented greater permeation of AmB than AmB-CH-Dex nanoparticles (Size = 168 ± 7 nm, Zeta potential = −15.5 ± 2). Similarly, Try et al (2016) reported that smaller poly(L-lactide-co-glycolide) nanoparticles (70 nm) penetrated healthy male Swiss mice skin further than larger particles (300 nm) [ 70 ]. Another explanation of the greater penetration is that the positive surface charge of AmB-CH-TPP nanoparticles could interact with negative charges in the skin promoting close interaction and an occlusive barrier that could cause hydration, which would facilitate nanoparticle permeation through the skin [ 71 , 72 ].…”

Section: Discussionmentioning

confidence: 99%

Activity of Amphotericin B-Loaded Chitosan Nanoparticles against Experimental Cutaneous Leishmaniasis

et al. 2020

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Chitosan nanoparticles have gained attention as drug delivery systems (DDS) in the medical field as they are both biodegradable and biocompatible with reported antimicrobial and anti-leishmanial activities. We investigated the application of chitosan nanoparticles as a DDS for the treatment of cutaneous leishmaniasis (CL) by preparing two types of chitosan nanoparticles: positively charged with tripolyphosphate sodium (TPP) and negatively charged with dextran sulphate. Amphotericin B (AmB) was incorporated into these nanoparticles. Both types of AmB-loaded nanoparticles demonstrated in vitro activity against Leishmania major intracellular amastigotes, with similar activity to unencapsulated AmB, but with a significant lower toxicity to KB-cells and red blood cells. In murine models of CL caused by L. major, intravenous administration of AmB-loaded chitosan-TPP nanoparticles (Size = 69 ± 8 nm, Zeta potential = 25.5 ± 1 mV, 5 mg/kg/for 10 days on alternate days) showed a significantly higher efficacy than AmBisome® (10 mg/kg/for 10 days on alternate days) in terms of reduction of lesion size and parasite load (measured by both bioluminescence and qPCR). Poor drug permeation into and through mouse skin, using Franz diffusion cells, showed that AmB-loaded chitosan nanoparticles are not appropriate candidates for topical treatment of CL.

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Size dependent skin penetration of nanoparticles in murine and porcine dermatitis models

Cited by 51 publications

References 43 publications

Framework nucleic acids as programmable carrier for transdermal drug delivery

Framework nucleic acids as programmable carrier for transdermal drug delivery

Near-Infrared Radiation-Based Mild Photohyperthermia Therapy of Non-Melanoma Skin Cancer with PEGylated Reduced Nanographene Oxide

Activity of Amphotericin B-Loaded Chitosan Nanoparticles against Experimental Cutaneous Leishmaniasis

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