Penetration and distribution of PLGA nanoparticles in the human skin treated with microneedles

Zhang, Wei; Gao, Jing; Zhu, Qian; Zhang, Min; Ding, Xueying; Wang, Xiaoyu; Hou, Xiaoning; Fan, Wei; Ding, Baoyue; Wu, Xin

doi:10.1016/j.ijpharm.2010.09.037

Cited by 95 publications

(81 citation statements)

References 21 publications

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“…These results were consistent with previous literature describing the usefulness of nanoparticles with MNs for increasing skin penetration of drug and its deposition in the upper layer of the skin. 15,16 The enhanced delivery efficiency of the NLC-MNs could be explained in two stages, as illustrated by step-wise controlled dermal delivery of NR (Figure 8). Firstly, MNs perforate the SC and liberate the NLCs as the polymeric matrix …”

Section: Discussionmentioning

confidence: 99%

“…Although MNs greatly enhance drug permeation rates, the permeated drugs are rapidly absorbed into the blood stream, leaving only a small quantity of drugs localized on the skin. 16 For controlled dermal delivery, incorporation of a particulate drug carrier within MNs has been investigated. 12,15,17 Recently, a particle-based MN system was introduced to develop a sustained skin immunization-based therapeutic strategy.…”

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confidence: 99%

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Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule

Lee¹,

Jeong²,

Lee³

et al. 2013

IJN

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Nanostructured lipid carriers (NLCs) were employed to formulate a lipophilic drug into hydrophilic polymeric microneedles (MNs). Hyaluronic acid (HA) was selected as a hydrophilic and bioerodible polymer to fabricate MNs, and nile red (NR) was used as a model lipophilic molecule. NR-loaded NLCs were consolidated into the HA-based MNs to prepare NLC-loaded MNs (NLC-MNs). A dispersion of NLCs was prepared by high-pressure homogenization after dissolving NR in Labrafil and mixing with melted Compritol, resulting in 268 nm NLCs with a polydispersity index of 0.273. The NLC dispersion showed a controlled release of NR over 24 hours, following Hixson–Crowell’s cube root law. After mixing the NLC dispersion with the HA solution, the drawing lithography method was used to fabricate NLC-MNs. The length, base diameter, and tip diameter of the NLC-MNs were approximately 350, 380, and 30 μm, respectively. Fluorescence microscopic imaging of the NLC-MNs helped confirm that the NR-loaded NLCs were distributed evenly throughout the MNs. In a skin permeation study performed using a Franz diffusion cell with minipig dorsal skin, approximately 70% of NR was localized in the skin after 24-hour application of NLC-MNs. Confocal laser scanning microscopy ( z -series) of the skin at different depths showed strong fluorescence intensity in the epidermal layer, which appeared to spread out radially with the passage of time. This study indicated that incorporation of drug-loaded NLCs into MNs could represent a promising strategy for controlled dermal delivery of lipophilic drugs.

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule

Lee¹,

Jeong²,

Lee³

et al. 2013

IJN

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“…Zhang et al reported that poly(D,L-lactic-coglycolic acid) (PLGA) nanosphere did not permeate the holesformed skin produced by micro-needles. 17) They concluded that these nanoparticles were distributed into the holes. Our results with their report suggest that insoluble nanoparticles may be permeated through big pores-existing skin membrane.…”

Section: Discussionmentioning

confidence: 99%

Measurement of Skin Permeation/Penetration of Nanoparticles for Their Safety Evaluation

Kimura

Kawano

Todo

et al. 2012

Biological & Pharmaceutical Bulletin

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The aim of the present study was to quantitatively evaluate the skin permeation/penetration of nanomaterials and to consider their penetration pathway through skin. Firstly, penetration/permeation of a model fluorescent nanoparticle, Fluoresbrite ® , was determined through intact rat skin and several damaged skins. Fluoresbrite ® permeated through only needle-punctured skin. The permeation profiles of soluble high molecular compounds, fluorescein isothiocyanate-dextrans (FITC-dextrans, FDs), with different molecular weights were also measured for comparison. The effects of molecular sizes and different skin pretreatments on the skin barrier were determined on the skin penetration/permeation of Fluoresbrite ® and FDs. Fluoresbrite ® was not permeated the intact skin, but FDs were permeated the skin. The skin distribution of titanium dioxide and zinc oxide nanoparticles was also observed after topical application of commercial cosmetics. Nanoparticles in sunscreen cosmetics were easily distributed into the groove and hair follicles after their topical application, but seldom migrated from the groove or follicles to viable epidermis and dermis. The obtained results suggested that nanoparticles did not permeate intact skin, but permeated pore-created skin. No or little permeation was observed for these nanomaterials through the stratum corneum.

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“…[11][12][13] Active strategies for enhancing drug permeation include iontophoresis, electroporation, ultrasound, and microneedle pretreatment. [14][15][16][17] To some extent, these enhancement approaches can promote percutaneous drug penetration. However, there are some problems, such as the skin inflammation induced by microneedles remaining in the skin, and the damage caused by the breakdown of skin structure during electroporating.…”

Section: Introductionmentioning

confidence: 99%

Study of magnetic silk fibroin nanoparticles for massage-like transdermal drug delivery

Chen¹,

Chen²,

Wang³

et al. 2015

IJN

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A synergistic approach by the combination of magnetic nanoparticles with an alternating magnetic field for transdermal drug delivery was investigated. Methotrexate-loaded silk fibroin magnetic nanoparticles were prepared using suspension-enhanced dispersion by supercritical CO 2 . The physiochemical properties of the magnetic nanoparticles were characterized. In vitro studies on drug permeation across skin were performed under different magnetic fields in comparison with passive diffusion. The permeation flux enhancement factor was found to increase under a stationary magnetic field, while an alternating magnetic field enhanced drug permeation more effectively; the combination of stationary and alternating magnetic fields, which has a massage-like effect on the skin, achieved the best result. The mechanistic studies using attenuated total reflection Fourier-transform infrared spectroscopy demonstrate that an alternating magnetic field can change the ordered structure of the stratum corneum lipid bilayers from the gel to the lipid-crystalline state, which can increase the fluidity of the stratum corneum lipids, thus enhancing skin penetration. Compared with the other groups, the fluorescence signal with a bigger area detected in deeper regions of the skin also reveals that the simulated massage could enhance the drug permeation across the skin by increasing the follicular transport. The combination of magnetic nanoparticles with stationary/alternating magnetic fields has potential for effective massage-like transdermal drug delivery.

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Penetration and distribution of PLGA nanoparticles in the human skin treated with microneedles

Cited by 95 publications

References 21 publications

Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule

Nanostructured lipid carrier-loaded hyaluronic acid microneedles for controlled dermal delivery of a lipophilic molecule

Measurement of Skin Permeation/Penetration of Nanoparticles for Their Safety Evaluation

Study of magnetic silk fibroin nanoparticles for massage-like transdermal drug delivery

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