Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization

Laserra, Sara; Basit, Abdul W.; Sozio, Piera; Marinelli, Lisa; Fornasari, Erika; Cacciatore, Ivana; Ciulla, Michele; Türkez, Hasan; Geyikoğlu, Fatime; Stefano, Antonio Di

doi:10.1016/j.ijpharm.2015.03.001

Cited by 64 publications

(22 citation statements)

References 47 publications

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“… 33 Another explanation explains that increasing the surfactant concentration could cause the rearrangement of the surfactant molecules to form loops and tails on the particle surface, leading to the bridging among the SLNs followed by particle aggregation. 34 On the contrary, lecithin concentration ( X 5 ) correlate inversely with the particle size when used as a co-surfactant. It was reported that 10% lecithin is sufficient to produce nanoparticles but, when used in combination with a surfactant, could yield a lower particle size than when used alone.…”

Section: Resultsmentioning

confidence: 99%

Development of Pomegranate Extract-Loaded Solid Lipid Nanoparticles: Quality by Design Approach to Screen the Variables Affecting the Quality Attributes and Characterization

et al. 2020

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The aim of this work was to study the influence of process variables on the quality attributes of pomegranate extract loaded solid lipid nanoparticles (PE-SLNs) using Plackett–Burman design. PE-SLN formulations were prepared by hot homogenization followed by ultra-sonication technique and evaluated based on the dependent variables that were analyzed utilizing Statgraphics Centurion XV software. The lipid and surfactant (type and concentration), co-surfactant concentration, sonication time, and amplitude were selected as the independent variables ( X 1 – X 7 ). The dependent parameters were particle size, polydispersity index, zeta potential, entrapment efficiency, and cumulative drug release ( Y 1 – Y 5 ). Response surface plots, Pareto charts, and mathematical equations were generated to study the influence of independent variables on the dependent quality parameters. Out of seven variables, X 1 , X 2 , and X 6 have the main significant ( p value < 0.05) effect on the entrapment efficiency, the cumulative drug release, the polydispersity index, respectively, while particle size was mainly affected by X 3 , X 6 and zeta potential by X 1 , X 3 , and X 4 . Consequently, this screening study revealed that stearic acid as lipid, Tween 80 as surfactant, as well as sonication with short time and high amplitude can be selected for the development of PE-SLN formulation with minimum particle size, maximum zeta potential, highest entrapment, and sustained drug release behavior. Meanwhile, concentrations of lipid, surfactant, and co-surfactant are planned to be scaled up for further optimization study. In conclusion, the Plackett–Burman design verified its influence and significance in determining and understanding both process and formulation variables affecting the quality of PE-SLNs.

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Section: Resultsmentioning

confidence: 99%

Development of Pomegranate Extract-Loaded Solid Lipid Nanoparticles: Quality by Design Approach to Screen the Variables Affecting the Quality Attributes and Characterization

et al. 2020

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“…While these results are of interest, invasive intraocular therapeutic administration is less desirable than noninvasive topical administration route . More recently, lipoyl–memantine‐loaded solid lipid nanoparticles and memantine–pamonic acid nanocrystalline salts have been described. Each of these formulations exhibited a sub‐200 nm size and good homogeneity but only solubilized ≈0.1 mg mL −1 of lipoyl–memantine and 0.028 mg mL −1 of memantine–pamonic acid, respectively.…”

Section: Discussionmentioning

confidence: 99%

Memantine‐Loaded PEGylated Biodegradable Nanoparticles for the Treatment of Glaucoma

Sánchez-López

Egea

Davis³

et al. 2017

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Glaucoma is a multifactorial neurodegenerative disease associated with retinal ganglion cells (RGC) loss. Increasing reports of similarities in glaucoma and other neurodegenerative conditions have led to speculation that therapies for brain neurodegenerative disorders may also have potential as glaucoma therapies. Memantine is an N-methyl-d-aspartate (NMDA) antagonist approved for Alzheimer's disease treatment. Glutamate-induced excitotoxicity is implicated in glaucoma and NMDA receptor antagonism is advocated as a potential strategy for RGC preservation. This study describes the development of a topical formulation of memantine-loaded PLGA-PEG nanoparticles (MEM-NP) and investigates the efficacy of this formulation using a well-established glaucoma model. MEM-NPs <200 nm in diameter and incorporating 4 mg mL of memantine were prepared with 0.35 mg mL localized to the aqueous interior. In vitro assessment indicated sustained release from MEM-NPs and ex vivo ocular permeation studies demonstrated enhanced delivery. MEM-NPs were additionally found to be well tolerated in vitro (human retinoblastoma cells) and in vivo (Draize test). Finally, when applied topically in a rodent model of ocular hypertension for three weeks, MEM-NP eye drops were found to significantly (p < 0.0001) reduce RGC loss. These results suggest that topical MEM-NP is safe, well tolerated, and, most promisingly, neuroprotective in an experimental glaucoma model.

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“…A control experiment was also carried out by replacing NFBTA with the same amount of DMSO (to manage any possible effects of DMSO on the cell growth). Triton X-100 (%1) and Mitomycin-C (0.09 µM) were added to the cells as positive control agents for testing of the cytotoxicity and genotoxicity [60,75].…”

Section: Methodsmentioning

confidence: 99%

NFBTA: A Potent Cytotoxic Agent against Glioblastoma

et al. 2019

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Piplartine (PPL), also known as piperlongumine, is a biologically active alkaloid extracted from the Piper genus which has been found to have highly effective anticancer activity against several tumor cell lines. This study investigates in detail the antitumoral potential of a PPL analogue; (E)-N-(4-fluorobenzyl)-3-(3,4,5-trimethoxyphenyl) acrylamide (NFBTA). The anticancer potential of NFBTA on the glioblastoma multiforme (GBM) cell line (U87MG) was determined by 3-(4,5-dimethyl-2-thia-zolyl)-2, 5-diphenyl-2H-tetrazolium bromide (MTT), and lactate dehydrogenase (LDH) release analysis, and the selectivity index (SI) was calculated. To detect cell apoptosis, fluorescent staining via flow cytometry and Hoechst 33258 staining were performed. Oxidative alterations were assessed via colorimetric measurement methods. Alterations in expressions of key genes related to carcinogenesis were determined. Additionally, in terms of NFBTA cytotoxic, oxidative, and genotoxic damage potential, the biosafety of this novel agent was evaluated in cultured human whole blood cells. Cell viability analyses revealed that NFBTA exhibited strong cytotoxic activity in cultured U87MG cells, with high selectivity and inhibitory activity in apoptotic processes, as well as potential for altering the principal molecular genetic responses in U87MG cell growth. Molecular docking studies strongly suggested a plausible anti-proliferative mechanism for NBFTA. The results of the experimental in vitro human glioblastoma model and computational approach revealed promising cytotoxic activity for NFBTA, helping to orient further studies evaluating its antitumor profile for safe and effective therapeutic applications.

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Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization

Cited by 64 publications

References 47 publications

Development of Pomegranate Extract-Loaded Solid Lipid Nanoparticles: Quality by Design Approach to Screen the Variables Affecting the Quality Attributes and Characterization

Development of Pomegranate Extract-Loaded Solid Lipid Nanoparticles: Quality by Design Approach to Screen the Variables Affecting the Quality Attributes and Characterization

Memantine‐Loaded PEGylated Biodegradable Nanoparticles for the Treatment of Glaucoma

NFBTA: A Potent Cytotoxic Agent against Glioblastoma

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