Roxithromycin-loaded lipid nanoparticles for follicular targeting

Wosicka-Frąckowiak, Hanna; Cal, Krzysztof; Stefanowska, Justyna; Główka, Eliza; Nowacka, Magdalena; Struck-Lewicka, Wiktoria; Govedarica, Biljana; Pasikowska, Monika; Dębowska, Renata; Jesionowski, Teofil; Srčič, Stanko; Markuszewski, Michał J.

doi:10.1016/j.ijpharm.2015.09.068

Cited by 36 publications

(10 citation statements)

References 25 publications

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“…For freeze-dried PR-NLCs, the particle size doubled and PDI displayed a slight increase up to 0.3 compared to non-freeze-dried PR-NLCs. However, the particle size and PDI of freeze-dried PR-NLCs was still in the acceptable range [ 26 ]. When PR-NLCs were stored in the solution state, they were precipitated.…”

Section: Resultsmentioning

confidence: 99%

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Kim

Choi

et al. 2017

Nanomaterials

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Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.

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Section: Resultsmentioning

confidence: 99%

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Kim

Choi

et al. 2017

Nanomaterials

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“…In addition, Roxithromycin has been shown to effectively promote hair re-growth [25-27], possibly by stimulating the production of normal hair follicle stem cells. Mechanistically, this hair re-growth phenomenon could be due to the highly efficient removal of neighboring senescent skin fibroblasts.…”

Section: Discussionmentioning

confidence: 99%

Azithromycin and Roxithromycin define a new family of “senolytic” drugs that target senescent human fibroblasts

Ózsvári

Nuttall

Sotgia

et al. 2018

Aging

101

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Here, we employed a “senolytic” assay system as a screening tool, with the goal of identifying and repurposing FDA-approved antibiotics, for the targeting of the senescent cell population. Briefly, we used two established human fibroblast cell lines (MRC-5 and/or BJ) as model systems to induce senescence, via chronic treatment with a DNA-damaging agent, namely BrdU (at a concentration of 100 μM for 8 days). Cell viability was then monitored by using the SRB assay, to measure protein content. As a consequence of this streamlined screening strategy, we identified Azithromycin and Roxithromycin as two novel clinically-approved senolytic drugs. However, Erythromycin – the very closely-related parent compound – did not show any senolytic activity, highlighting the dramatic specificity of these interactions. Interestingly, we also show that Azithromycin treatment of human fibroblasts was indeed sufficient to strongly induce both aerobic glycolysis and autophagy. However, the effects of Azithromycin on mitochondrial oxygen consumption rates (OCR) were bi-phasic, showing inhibitory activity at 50 μM and stimulatory activity at 100 μM. These autophagic/metabolic changes induced by Azithromycin could mechanistically explain its senolytic activity. We also independently validated our findings using the xCELLigence real-time assay system, which measures electrical impedance. Using this approach, we see that Azithromycin preferentially targets senescent cells, removing approximately 97% of them with great efficiency. This represents a near 25-fold reduction in senescent cells. Finally, we also discuss our current results in the context of previous clinical findings that specifically document the anti-inflammatory activity of Azithromycin in patients with cystic fibrosis – a genetic lung disorder that results in protein mis-folding mutations that cause protein aggregation.

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“…Some formulations can enhance antibiotic efficiency by improving bioavailability, thus, allowing oral [ 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 ], intramuscular [ 67 ], pulmonary [ 68 , 69 ], skin [ 70 , 71 , 72 ] or subcutaneous [ 73 , 74 ] drug administration. Other groups have demonstrated that SLNs can increase antibiotic activity by facilitating drug permeation through different barriers in the eye [ 75 , 76 , 77 , 78 , 79 , 80 ], through the mucosal barrier [ 81 , 82 ], or even through the blood–brain barrier [ 83 ].…”

Section: Solid Lipid Nanoparticle To Improve Drug Deliverymentioning

confidence: 99%

Incorporation of Antibiotics into Solid Lipid Nanoparticles: A Promising Approach to Reduce Antibiotic Resistance Emergence

2021

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Antimicrobial resistance is one of the biggest threats to global health as current antibiotics are becoming useless against resistant infectious pathogens. Consequently, new antimicrobial strategies are urgently required. Drug delivery systems represent a potential solution to improve current antibiotic properties and reverse resistance mechanisms. Among different drug delivery systems, solid lipid nanoparticles represent a highly interesting option as they offer many advantages for nontoxic targeted drug delivery. Several publications have demonstrated the capacity of SLNs to significantly improve antibiotic characteristics increasing treatment efficiency. In this review article, antibiotic-loaded solid lipid nanoparticle-related works are analyzed to summarize all information associated with applying these new formulations to tackle the antibiotic resistance problem. The main antimicrobial resistance mechanisms and relevant solid lipid nanoparticle characteristics are presented to later discuss the potential of these nanoparticles to improve current antibiotic treatment characteristics and overcome antimicrobial resistance mechanisms. Moreover, solid lipid nanoparticles also offer new possibilities for other antimicrobial agents that cannot be administrated as free drugs. The advantages and disadvantages of these new formulations are also discussed in this review. Finally, given the progress of the studies carried out to date, future directions are discussed.

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Roxithromycin-loaded lipid nanoparticles for follicular targeting

Cited by 36 publications

References 25 publications

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

The Improvement of Skin Whitening of Phenylethyl Resorcinol by Nanostructured Lipid Carriers

Azithromycin and Roxithromycin define a new family of “senolytic” drugs that target senescent human fibroblasts

Incorporation of Antibiotics into Solid Lipid Nanoparticles: A Promising Approach to Reduce Antibiotic Resistance Emergence

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