Safety of surfactant excipients in oral drug formulations

Maher, Sam; Geoghegan, Caroline; Brayden, David J.

doi:10.1016/j.addr.2023.115086

Cited by 12 publications

(2 citation statements)

References 323 publications

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“…By adding a phosphanium chain to caffeic acid, we prepared four substances with surfactant properties. Surfactants as pharmaceuticals are well-known for topical application, although some surfactants within acceptable dose limits are considered safe for human consumption and could be used in oral pharmaceutical products [46]. According to our results, the prepared caffeic acid phosphanium derivatives exhibited a high cytotoxic effect against the control cell line.…”

Section: Anti-acanthamoeba Activitymentioning

confidence: 63%

Caffeic Acid Phosphanium Derivatives: Potential Selective Antitumor, Antimicrobial and Antiprotozoal Agents

Lukáč,

Slobodníková,

Mrva

et al. 2024

IJMS

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Caffeic acid (CA) is one of the most abundant natural compounds present in plants and has a broad spectrum of beneficial pharmacological activities. However, in some cases, synthetic derivation of original molecules can expand their scope. This study focuses on the synthesis of caffeic acid phosphanium derivatives with the ambition of increasing their biological activities. Four caffeic acid phosphanium salts (CAPs) were synthesized and tested for their cytotoxic, antibacterial, antifungal, and amoebicidal activity in vitro, with the aim of identifying the best area for their medicinal use. CAPs exhibited significantly stronger cytotoxic activity against tested cell lines (HeLa, HCT116, MDA-MB-231 MCF-7, A2058, PANC-1, Jurkat) in comparison to caffeic acid. Focusing on Jurkat cells (human leukemic T cell lymphoma), the IC50 value of CAPs ranged from 0.9 to 8.5 μM while IC50 of CA was >300 μM. Antimicrobial testing also confirmed significantly higher activity of CAPs against selected microbes in comparison to CA, especially for Gram-positive bacteria (MIC 13–57 μM) and the yeast Candida albicans (MIC 13–57 μM). The anti-Acanthamoeba activity was studied against two pathogenic Acanthamoeba strains. In the case of A. lugdunensis, all CAPs revealed a stronger inhibitory effect (EC50 74–3125 μM) than CA (>105 µM), while in A. quina strain, the higher inhibition was observed for three derivatives (EC50 44–291 μM). The newly synthesized quaternary phosphanium salts of caffeic acid exhibited selective antitumor action and appeared to be promising antimicrobial agents for topical application, as well as potential molecules for further research.

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Section: Anti-acanthamoeba Activitymentioning

confidence: 63%

Caffeic Acid Phosphanium Derivatives: Potential Selective Antitumor, Antimicrobial and Antiprotozoal Agents

Lukáč,

Slobodníková,

Mrva

et al. 2024

IJMS

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“…The selection of surfactants was informed by a thorough literature evaluation of their safety profiles, effectiveness in nanoparticle stabilization, and the possibility of enhancing the absorption of CBD. Such criteria ensured our formulation's alignment with the existing literature on oral applications [37][38][39].…”

Section: Particle Size (Ymentioning

confidence: 99%

Cannabidiol-Loaded Solid Lipid Nanoparticles Ameliorate the Inhibition of Proinflammatory Cytokines and Free Radicals in an In Vitro Inflammation-Induced Cell Model

Alcantara,

Malabanan,

Nalinratana

et al. 2024

IJMS

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Cannabidiol (CBD) is a non-psychoactive compound derived from Cannabis sativa. It has demonstrated promising effects in combating inflammation and holds potential as a treatment for the progression of chronic inflammation. However, the clinical application of CBD is limited due to its poor solubility and bioavailability. This study introduces an effective method for preparing CBD-loaded solid lipid nanoparticles (CBD-SLNs) using a combination of low-energy hot homogenization and ultrasonication. We enhanced this process by employing statistical optimization with response surface methodology (RSM). The optimized CBD-SLN formulation utilizes glyceryl monostearate as the primary lipid component of the nanocarrier. The CBD-SLN formulation is screened as a potential tool for managing chronic inflammation. Stable, uniformly dispersed spherical nanoparticles with a size of 123 nm, a surface charge of –32.1 mV, an encapsulation efficiency of 95.16%, and a drug loading of 2.36% were obtained. The CBD-SLNs exhibited sustained release properties, ensuring prolonged and controlled CBD delivery, which could potentially amplify its therapeutic effects. Additionally, we observed that CBD-SLNs significantly reduced both reactive oxygen and nitrogen species and proinflammatory cytokines in chondrocyte and macrophage cell lines, with these inhibitory effects being more pronounced than those of free CBD. In conclusion, CBD-SLNs demonstrated superiority over free CBD, highlighting its potential as an effective delivery system for CBD.

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Preparation and biochemical evaluation of daily-thiosulfinate/polyoxyethylene conjugated pH-responsive micelle with enhanced stability, hydrosolubility and antibacterial properties

Bhattacharya,

DasChowdhury

2024

Colloid Polym Sci

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Safety of surfactant excipients in oral drug formulations

Cited by 12 publications

References 323 publications

Caffeic Acid Phosphanium Derivatives: Potential Selective Antitumor, Antimicrobial and Antiprotozoal Agents

Caffeic Acid Phosphanium Derivatives: Potential Selective Antitumor, Antimicrobial and Antiprotozoal Agents

Cannabidiol-Loaded Solid Lipid Nanoparticles Ameliorate the Inhibition of Proinflammatory Cytokines and Free Radicals in an In Vitro Inflammation-Induced Cell Model

Preparation and biochemical evaluation of daily-thiosulfinate/polyoxyethylene conjugated pH-responsive micelle with enhanced stability, hydrosolubility and antibacterial properties

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