Ultra-small NLC for improved dermal delivery of coenyzme Q10

Schwarz, Julia C.; Baisaeng, Nuttakorn; Hoppel, Magdalena; Löw, Monika; Keck, Cornelia M.; Valenta, Claudia

doi:10.1016/j.ijpharm.2013.02.037

Cited by 76 publications

(25 citation statements)

References 19 publications

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“…Due to the more pronounced release of the active a better in vivo performance can be expected. This was confirmed by AOC measurements and by ex vivo penetration studies on pig ears (Schwarz et al, 2013). Based on this, the flip-flop core-shell usNLC, which were developed in this study, were shown to possess superior properties, when compared to classical carriers.…”

Section: Discussionsupporting

confidence: 71%

Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): A novel delivery system based on flip–flop structure

Keck

Baisaeng

Durand

et al. 2014

International Journal of Pharmaceutics

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Section: Discussionsupporting

confidence: 71%

Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): A novel delivery system based on flip–flop structure

Keck

Baisaeng

Durand

et al. 2014

International Journal of Pharmaceutics

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“…41 Greater amounts of the drug are entrapped in the core lipid matrix and lower amounts of the drug are deposited at the shell and/or the surface of the lipid nanoparticles. 42 Therefore, the formulation contains less amount of drug on the surface and the outer shell of the NLC contributes to the initial slow release; moreover, the drug present in the core of the lipid matrix contributes to the second fast release phase.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Rajinikanth¹,

Chellian²

2016

IJN

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The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol ® ATO 5 (glyceryl palmitostearate) and Labrasol ® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol ® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol ® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, −21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 μg/cm 2 /h) as compared with plain 5-FU gel (2.85±1.12 μg/cm 2 /h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 μg/cm 2 ) as compared with that from the 5-FU plain gel (12.23±3.86 μg/cm 2 ) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations.

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“…Notably, SLNs typically possess a particle size > 150 nm; the lipidic nature makes the particles prone to immediate recrystallization into larger size SLNs. Therefore, the production of ultra-small SLNs (< 100 nm) remains challenging and was rarely reported [25]. Us-SLNs are expected to improve drug loading, mucus penetration as well as internalization by bacterial targets [26].…”

Section: Accepted Manuscript Introductionmentioning

confidence: 99%

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

Nafee

Husari

Maurer

et al. 2014

Journal of Controlled Release

176

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Cystic fibrosis (CF) is a genetic disease mainly manifested in the respiratory tract. Pseudomonas aeruginosa (P. aeruginosa) is the most common pathogen identified in cultures of the CF airways, however, its eradication with antibiotics remains challenging as it grows in biofilms that counterwork human immune response and dramatically decrease susceptibility to antibiotics. P. aeruginosa regulates pathogenicity via a cell-to-cell communication system known as quorum sensing (QS) involving the virulence factor (pyocyanin), thus representing an attractive target for coping with bacterial pathogenicity. The first in vivo potent QS inhibitor (QSI) was recently developed. Nevertheless, its lipophilic nature might hamper its penetration of non-cellular barriers such as mucus and bacterial biofilms, which limits its biomedical application. Successful anti-infective inhalation therapy necessitates proper design of a biodegradable nanocarrier allowing: 1) high loading and prolonged release, 2) mucus penetration, 3) effective pulmonary delivery, and 4) maintenance of the anti-virulence activity of the QSI. In this context, various pharmaceutical lipids were used to prepare ultra-small solid lipid nanoparticles (us-SLNs) by hot melt homogenization. Plain and QSI-loaded SLNs were characterized in terms of colloidal properties, drug loading, in vitro release and acute toxicity on Calu-3 cells. Mucus penetration was studied using a newly-developed confocal microscopy technique based on 3D-time-lapse imaging. For pulmonary application, nebulization efficiency of SLNs and lung deposition using next generation impactor (NGI) were performed. The anti-virulence efficacy was investigated by pyocyanin formation in P. aeruginosa cultures. Ultra-small SLNs (<100nm diameter) provided high encapsulation efficiency (68-95%) according to SLN composition, high burst in phosphate buffer saline compared to prolonged release of the payload over >8h in simulated lung fluid with minor burst. All types and concentrations of plain and QSI-loaded SLNs maintained the viability of Calu-3 cells. 3D time-lapse confocal imaging proved the ability of SLNs to penetrate into artificial sputum model. SLNs were efficiently nebulized; NGI experiments revealed their deposition in the bronchial region. Overall, nanoencapsulated QSI showed up to sevenfold superior anti-virulence activity to the free compound. Most interestingly, the plain SLNs exhibited anti-virulence properties themselves, which was shown to be related to anti-virulence effects of the emulsifiers used. These startling findings represent a new perspective of ultimate significance in the area of nano-based delivery of novel anti-infectives.

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Ultra-small NLC for improved dermal delivery of coenyzme Q10

Cited by 76 publications

References 19 publications

Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): A novel delivery system based on flip–flop structure

Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): A novel delivery system based on flip–flop structure

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

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