Gold nanoparticles capped with benzalkonium chloride and poly (ethylene imine) for enhanced loading and skin permeability of 5-fluorouracil

Safwat, Mohamed; Soliman, Ghareb M.; Sayed, Douaa; Attia, Mohamed A.

doi:10.1080/03639045.2017.1339082

Cited by 23 publications

(17 citation statements)

References 68 publications

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“…After that ratio, the increase in the actually loaded drug amount was not proportional to the increase in the initially used drug concentration leading to deceased drug encapsulation efficiency. This behavior is commonly observed for several other nanocarriers after achieving maximum drug encapsulation efficiency [36,46,47]. It is notable that, although formulations F4-F6 have high drug loading capacity, they have little practical importance due to nanoparticle size increase and aggregation as outlined above in the UV-Vis studies ( Figure 2).…”

Section: Effect Of Egcg/haucl 4 Molar Ratio On Drug Loading Propertiessupporting

confidence: 52%

“…This is a commonly observed behavior for nanoparticles due to the dry status of nanoparticles used in TEM measurements, which probably results in nanoparticle shrinkage. In contrast, the size obtained by DLS represents hydrated nanoparticles in solution, which explains their bigger size [35,36].…”

Section: Preparation Of Egcg-gnpsmentioning

confidence: 94%

“…EGCG release from its GNPs aqueous solution was studied using the dialysis bag method, a widely used technique to characterize drug release from drug-loaded GNPs [25,36,41]. Aqueous solution of EGCG alone was used as a control to make sure that the drug could easily diffuse through the dialysis membrane.…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 99%

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Epigallocatechin-3-Gallate-Loaded Gold Nanoparticles: Preparation and Evaluation of Anticancer Efficacy in Ehrlich Tumor-Bearing Mice

et al. 2020

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Epigallocatechin-3-gallate (EGCG) is a pleiotropic compound with anticancer, anti-inflammatory, and antioxidant properties. To enhance EGCG anticancer efficacy, it was loaded onto gold nanoparticles (GNPs). EGCG-GNPs were prepared by a simple green synthesis method and were evaluated using different techniques. Hemocompatibility with human blood and in vivo anticancer efficacy in Ehrlich ascites carcinoma-bearing mice were evaluated. EGCG/gold chloride molar ratio had a marked effect on the formation and properties of EGCG-GNPs where well-dispersed spherical nanoparticles were obtained at a molar ratio not more than 0.8:1. The particle size ranged from ~26 to 610 nm. High drug encapsulation efficiency and loading capacity of ~93 and 32%, respectively were obtained. When stored at 4 °C for three months, EGCG-GNPs maintained over 90% of their drug payload and had small changes in their size and zeta potential. They were non-hemolytic and had no deleterious effects on partial thromboplastin time, prothrombin time, and complement protein C3 concentration. EGCG-GNPs had significantly better in vivo anticancer efficacy compared with pristine EGCG as evidenced by smaller tumor volume and weight and higher mice body weight. These results confirm that EGCG-GNPs could serve as an efficient delivery system for EGCG with a good potential to enhance its anticancer efficacy.

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Section: Effect Of Egcg/haucl 4 Molar Ratio On Drug Loading Propertiessupporting

confidence: 52%

Section: Preparation Of Egcg-gnpsmentioning

confidence: 94%

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Epigallocatechin-3-Gallate-Loaded Gold Nanoparticles: Preparation and Evaluation of Anticancer Efficacy in Ehrlich Tumor-Bearing Mice

et al. 2020

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“…The better SP permeability, flux, and skin deposition observed for the LeciPlex gel might be attributed to several factors. Cationic surface charge of LeciPlex facilitates their interaction with the negatively charged cell surface, which in turn leads to better drug uptake and permeation through the skin [64][65][66]. Further, the small particle size of the LeciPlexes is another important factor that contributes to their enhanced skin permeation.…”

Section: Ex Vivo Skin Permeation Studiesmentioning

confidence: 99%

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

et al. 2019

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Spironolactone (SP), an aldosterone antagonist with anti-androgen properties, has shown promising results in the treatment of female acne. However, its systemic side effects limit its clinical benefits. This study aimed to prepare and evaluate LeciPlexes for SP topical delivery. LeciPlexes were prepared by a one-step procedure and characterized using various techniques. Optimum LeciPlex preparation was incorporated into 1% methylcellulose gel and SP permeability was tested ex vivo in Sprague-Dawley rat skin. The maximum drug encapsulation efficiency obtained was 93.6 ± 6.9% and was dependent on the drug/phospholipid and surfactant/phospholipid ratios. A zeta potential of +49.3 ± 3.5 to +57.7 ± 3.3 mV and a size of 108 ± 25.3 to 668.5 ± 120.3 nm were observed for the LeciPlexes. FT-IR and DSC studies confirmed the incorporation of SP into the LeciPlexes through hydrophobic and hydrogen bonding interactions. SP release from the LeciPlex formulations was significantly slower than from the drug suspension. Cumulative SP permeated through rat skin from LeciPlex gel was about 2-fold higher than SP control gel. Cumulative SP deposited in the stratum corneum and other skin layers from the LeciPlex gel was about 1.8- and 2.6-fold higher than SP control gel, respectively. This new SP LeciPlex formulation is a promising carrier for the treatment of female acne.

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“…Benzalkonium chloride (BAC) (its chemical structure is shown in Figure 1) is a synthetic quaternary ammonium compound with amphoteric surface-acting properties [1]. It is a mixture of several alkyldimethylbenzylammonium chlorides differing only in the length of their alkyl side chains; commercially available BAC consists of benzyldodecyldimethylammonium chloride, benzyldimethyltetradecylammonium chloride, and benzylcetyldimethylammonium chloride [2].…”

Section: Introductionmentioning

confidence: 99%

Mitochondrial Dysfunctions May Be One of the Major Causative Factors Underlying Detrimental Effects of Benzalkonium Chloride

Рогов

Goleva

Sukhanova

et al. 2020

Oxidative Medicine and Cellular Longevity

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Benzalkonium chloride (BAC) is currently the most commonly used antimicrobial preservative in ophthalmic solutions, nasal sprays, and cosmetics. However, a large number of clinical and experimental investigations showed that the topical administration of BAC-containing eye drops could cause a variety of ocular surface changes, from ocular discomfort to potential risk for future glaucoma surgery. BAC-containing albuterol may increase the risk of albuterol-related systemic adverse effects. BAC, commonly present in personal care products, in cosmetic products can induce irritation and dose-dependent changes in the cell morphology. The cationic nature of BAC (it is a quaternary ammonium) suggests that one of the major targets of BAC in the cell may be mitochondria, the only intracellular compartment charged negatively. However, the influence of BAC on mitochondria has not been clearly understood. Here, the effects of BAC on energy parameters of rat liver mitochondria as well as on yeast cells were examined. BAC, being a "weaker" uncoupler, potently inhibited respiration in state 3, diminished the mitochondrial membrane potential, caused opening of the Ca2+/Pi-dependent pore, blocked ATP synthesis, and promoted H 2 O 2 production by mitochondria. BAC triggered oxidative stress and mitochondrial fragmentation in yeast cells. BAC-induced oxidative stress in mitochondria and yeast cells was almost totally prevented by the mitochondria-targeted antioxidant SkQ1; the protective effect of SkQ1 on mitochondrial fragmentation was only partial. Collectively, these data showed that BAC acts adversely on cell bioenergetics (especially on ATP synthesis) and mitochondrial dynamics and that its prooxidant effect can be partially prevented by the mitochondria-targeted antioxidant SkQ1.

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Gold nanoparticles capped with benzalkonium chloride and poly (ethylene imine) for enhanced loading and skin permeability of 5-fluorouracil

Abstract: Based on these results, BC- and PEI-GNPs might find applications as effective topical delivery systems of 5-FU.

Cited by 23 publications

References 68 publications

Epigallocatechin-3-Gallate-Loaded Gold Nanoparticles: Preparation and Evaluation of Anticancer Efficacy in Ehrlich Tumor-Bearing Mice

Epigallocatechin-3-Gallate-Loaded Gold Nanoparticles: Preparation and Evaluation of Anticancer Efficacy in Ehrlich Tumor-Bearing Mice

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

Mitochondrial Dysfunctions May Be One of the Major Causative Factors Underlying Detrimental Effects of Benzalkonium Chloride

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