The fullerene core's capacity to scavenge free radicals is determined by its high affinity for electron donors. Conversely, the C60 molecule exhibits effective absorption of UV and visible light, accompanied by a subsequent transition to the first singlet excited state, a long-lived triplet excited state, and finally, an energy transfer to the singlet oxygen that yields molecular oxygen with a quantum yield that is nearly 100%[1].

Absorption, Distribution and Excretion
This study aimed to determine the distribution of sup>14CC₆₀ in pregnant rats and fetuses, lactating rats, and offspring. On day 15 of gestation (gd 15), four gestational rats were administered sup>14CC₆₀ at a dose of 0.28 mg/kg body weight (approximately 3 μCi per rat) via tail vein injection, dissolved in 5% polyvinylpyrrolidone saline (PVP); the other four gestational rats were injected with PVP only. Urine (0–24 hours) and tissues (24 hours) were collected from the gestational rats. On day 8 postnatal (pnd 8), eight lactating rats were injected with sup>14CC₆₀ at a dose of 0.36 mg/kg body weight, dissolved in PVP, and were sacrificed 24 or 48 hours after administration. In pregnant mice, radioactive material was distributed in the placenta (approximately 2% of the dose), fetus (1.0%), and female reproductive tract (3.0%). In lactating rats, radioactive material was distributed in milk (<1%) and mammary tissue (<1%), while in pups it was distributed in the gastrointestinal tract (<1%) and liver (<1%). In pregnant mice, radioactive material was distributed in urine (<2%), feces (2%), blood (0.9%/mL) and plasma (1.7%/mL), brain (<1%), lungs (<1%), heart (<1%), liver (approximately 43%), and spleen (4%). Compared with pregnant mice, lactating rats showed similar distribution of radioactivity in blood and plasma 24 hours after exposure (decreasing by 50% after 48 hours), with higher distribution in the lungs and lower distribution in the liver. Urinary metabolomics analysis showed that exposure to C60 in maternal mice resulted in decreased levels of metabolites originating from the tricarboxylic acid cycle and increased levels of metabolites originating from the urea cycle or glycolysis; simultaneously, the levels of some sulfur-containing amino acids and purine/pyrimidine metabolites were also altered. This study demonstrates that C60 can cross the placenta and be passed from mother to offspring via breast milk. Percutaneously harvested porcine skin was fixed to a flexion device, and a 33.5 mg/mL aqueous solution of a fullerene-substituted phenylalanine (Baa) derivative with a nuclear-localized peptide sequence (Baa-Lys(FITC)-NLS) was applied topically. The skin was flexed for 60 or 90 minutes, or left unflexed (control group). Confocal microscopy revealed that in skin flexed for 60 and 90 minutes, nanoparticles penetrated into the dermis after 8 hours; while in unflexed skin, Baa-Lys(FITC)-NLS required 24 hours to penetrate the dermis. Transmission electron microscopy analysis revealed that the fullerene-peptide complex was localized within the intercellular spaces of the granular layer. We used microscopic imaging and biological techniques to investigate the transmembrane transport of [C60(C(COOH)2)2]n nanoparticles and their intracellular transport in 3T3 L1 and RH-35 live cells. Fullerene nanoparticles were rapidly internalized by cells and entered the cytoplasm in a point-like manner. After entering the cell, they synchronized with lysosomal-like vesicles. The entry of [C60(C(COOH)2)2]n nanoparticles into cells was primarily via endocytosis, a process that was time-, temperature-, and energy-dependent. The study found that the cellular uptake of [C60(C(COOH)2)2]n nanoparticles was mediated by clathrin-mediated endocytosis, rather than caveolin-mediated endocytosis… This paper summarizes the nanostructures and physicochemical properties of fullerene drug derivatives. The biological behavior of fullerene derivatives demonstrates their potential in medical applications, as C60 is rapidly absorbed by tissues and excreted through the urinary system and intestines, with both in vitro and in vivo studies showing low toxicity. Nanomedicine has become one of the most promising areas of nanotechnology, with many claiming its potential for treating cancer, HIV infection, and neurodegenerative diseases. Chemically modified water-soluble C60 fullerene derivatives exhibit significantly enhanced bioactivity. The blood-brain barrier (BBB) is a physical barrier formed by tight junctions of endothelial cells, limiting permeability to cells. A major challenge in neuropharmacology is finding compounds that can cross the bloodstream to the brain. Fullerene C60 has been shown to cross the blood-brain barrier through binary hybridization with bioactive groups, providing a promising clue for the drug treatment of neurological diseases. /C60 Fullerene Derivatives/
Pristine fullerene (C60) will be used in many industrial and pharmaceutical production and derivatization processes in various solvents. This report investigates the effects of different types of industrial solvents (toluene, cyclohexane, chloroform, and mineral oil) on the skin permeability of C60. Yorkshire weaned piglets (n=3) were topically treated with 500 μL of a 200 μg/mL C60 solution (dissolved in a specific solvent) for 24 hours, followed by repeated application daily for four consecutive days to simulate worst-case occupational exposure. The application sites were peeled off with tape, and skin biopsies were performed after 26 peels for quantitative analysis. When toluene, cyclohexane, or chloroform was used as solvents, pristine fullerenes were able to penetrate deep into the stratum corneum, the skin's main barrier. A higher concentration of C60 was detected in the stratum corneum when chloroform was used as a solvent compared to toluene or cyclohexane. No fullerenes were detected in the skin when mineral oil was used as a solvent. This is the first direct evidence of the effect of solvents on the skin permeability of pristine fullerenes. In vitro isolated stratum corneum also confirmed the penetration of C60 into the stratum corneum. The effect of solvents on C60 uptake by the stratum corneum is consistent with the results observed in vivo. In vitro flow-through diffusion cell experiments were conducted on pig skin, and fullerenes were not detected in the receptor solution within 24 hours. The detection limit for fullerenes in 2 mL of receptor solution was 0.001 μg/mL.
Biological Half-Life
Fullerenes…are spherical molecules composed of carbon atoms (C(x)) that can have side chains added to form compounds with very different properties. …Absorption, distribution, and excretion largely depend on the nature of the side chains. Pure C60 has an extremely long biological half-life, while most water-soluble derivatives are cleared from the exposed animals within weeks.
…Male rats were exposed to C60 fullerene nanoparticles (2.22 mg/m³, diameter 55 nm) and microparticles (2.35 mg/m³, diameter 0.93 μm) for 3 hours daily for 10 consecutive days using a nasal-only exposure system. The nanoparticles were prepared using an aerosol vaporization and condensation process. High-performance liquid chromatography (HPLC), X-ray diffraction (XRD), and scanning laser Raman spectroscopy (SLR) analyses of the nanoparticles and microparticles showed that C60 fullerenes underwent no chemical modification during aerosol formation. The lung half-lives of the C60 fullerene nanoparticles and microparticles were 26 days and 29 days, respectively.

Interactions
This study evaluated the radioprotective effects of fullerene nanoparticles DF-1, possessing antioxidant properties, on zebrafish embryos. Zebrafish embryos were exposed to different doses of ionizing radiation ranging from 20 to 80 Gy in the presence or absence of DF-1. The toxicity and radioprotective effects of DF-1 were evaluated by monitoring overall survival and morphology, as well as by assessing organ function using methods that detect renal excretion and sensory nerve cell (neurohymala) development. Furthermore, the antioxidant properties of DF-1 in whole fish were assessed. Results: Within the tested concentration range (1–1000 μmol/L), DF-1 had no significant adverse effects on the morphology or survival of normal zebrafish. Ionizing radiation (10–40 Gy) caused time- and dose-dependent disturbances in the normal morphology and physiological development of zebrafish, particularly midline developmental defects, resulting in dorsal bending of the body axis (“curling”), neurotoxicity, excretory dysfunction, and reduced survival of exposed embryos. Administration of DF-1 (100 μmol/L) within 3 hours before or 15 minutes after radiation exposure significantly reduced radiation-induced overall and organ-specific toxicity. Conversely, administration of DF-1 30 minutes after ionizing radiation had no protective effect. ... The protective effect of DF-1 against radiation-related toxicity in zebrafish embryos was associated with a significant reduction in radiation-induced reactive oxygen species.

[1]. D Franskevych,et al. Fullerene C 60 Penetration into Leukemic Cells and Its Photoinduced Cytotoxic Effects. Nanoscale Res Lett.2017 Dec;12(1):40.

C60 fullerene is a type of fullerene. It has anti-aging properties. Buckminster fullerene is a nanoparticle characterized by its spherical geometry and hollow interior, composed of 60 carbon atoms. This structure is the most common type of fullerene. Buckminster fullerene is a mineral. Fullerene is a mineral with the chemical formula C60. It is a polyhedral carbon structure composed of approximately 60-80 carbon atoms arranged in pentagons and hexagons. It is named after Buckminster Fuller because its structure resembles a geodesic dome. Fullerenes can be prepared at high temperatures, such as by arc discharge in an inert atmosphere. See also: Fullerenes (note moved to).

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Therapeutic Uses
/Experimental Therapies:/ Fullerene (C60) is the third allotrope of carbon and a classic engineered material with potential applications in the biomedical field. One of the most important biological properties of C60 is its ability to quench a variety of free radicals, acting like a "free radical sponge." Conversely, photosensitization of C60 leads to its transition to a long-lived triplet excited state, subsequently transferring energy or electrons to molecular oxygen, generating highly reactive singlet oxygen (¹O₂) or superoxide anion (O₂⁻), respectively. These reactive oxygen species (ROS) can react with a variety of biological targets and participate in cell signaling and cell damage. Therefore, the dual nature of fullerenes—both quenching and generating cell-damaging ROS—holds promise for the development of cell-protective or cytotoxic anticancer/antibacterial drugs. However, attempts to achieve this goal have been hampered by the extremely low water solubility of C60 and the fact that solubilization processes significantly affect the reactive oxygen species (ROS) generation/scavenging properties of C60 (whether through chemical modification or the formation of complex nanoparticles with different photophysical properties)...
/Experimental Therapy: Gadolinium metal fullerol nanoparticles [Gd@C82(OH)22]n (22 nm in physiological saline) at doses as low as 10⁻⁷ mol/kg showed extremely high antitumor efficacy (approximately 60%) in mice. Increasing the dose by 1 × 10⁻⁷ mol/kg increased the tumor inhibition rate by 26%. [Gd@C82(OH)22]n particles possess a strong ability to enhance immunity and interfere with tumor invasion of normal muscle cells, and exhibit virtually no toxicity in vivo or in vitro. Unlike traditional antitumor drugs, the high antitumor efficiency of nanoparticles does not stem from their cytotoxic effects, as they do not directly kill tumor cells, and only about 0.05% of the content is present in tumor tissue. The results indicate that fullerene derivatives with appropriate surface modifications and sizes hold promise for development as highly effective and low-toxicity chemotherapy drugs for tumors. /Gadolinium metal fullerenol nanoparticles/
/Experimental therapy:/ This is the first report on the targeted delivery of low-toxicity fullerene-based nanocational particles (a porphyrin adduct of cyclohexylfullerene-C60) to treat hypoxia-induced mitochondrial dysfunction in mammalian myocardium. ……The magnetic isotope effect generated by the paramagnetic (25)Mg2+ released by these nanoparticles selectively stimulated the overproduction of ATP in hypoxic cells. ……Since the nanoparticles are membrane-affinity cations, they only release overactivated paramagnetic cations when the acidic environment is altered in a hypoxia-induced manner. The resulting changes in cardiomyocyte energy metabolism resulted in a recovery rate of approximately 80% of the damaged myocardium within 24 hours after a single injection (0.03-0.1 LD50). …Pharmacokinetics and pharmacodynamics of nanoparticles suggest they are suitable for safe and effective use in single or multiple-injection (acute or chronic) treatment regimens to prevent and treat clinical conditions involving myocardial hypoxia. /Experimental Therapy:/ Oxidative stress plays a significant role in acne formation, suggesting that oxygen free radical scavengers are potential therapeutic agents. Fullerenes are spherical carbon molecules with strong free radical sponge activity; therefore, researchers investigated the efficacy of fullerene gel in treating acne vulgaris. Researchers conducted an open-label trial, applying fullerene gel twice daily; at weeks 4 and 8, the mean number of inflammatory lesions (erythematous papules and pustules) was significantly reduced (P < 0.05), from 16.09 ± 9.08 to 12.36 ± 7.03 (reduction rate 23.2%) and 10.0 ± 5.62 (reduction rate 37.8%), respectively. The number of pustules formed by neutrophil aggregation was also significantly reduced (P < 0.05), from 1.45 ± 1.13 to 0.18 ± 0.60 (reduction rate 87.6%). Further in vitro sebum production experiments using hamster sebaceous cells showed that 75 μM polyvinylpyrrolidone-fullerene inhibited sebum production, suggesting that fullerene inhibits acne by reducing neutrophil infiltration and sebum production. After 8 weeks of treatment, skin hydration significantly increased (P < 0.05), from 51.7 ± 7.9 units to 60.4 ± 10.3 units. Therefore, fullerene gel may help control acne vulgaris and has skin-care benefits.

C60

720.64

720

99685-96-8

157697-67-1;147045-79-2;157697-66-0

123591

Spherical aromatic molecule with a hollow truncated-icosahedron structure, similar to a soccer ball. /C60/
Polyhedral cages made up of entirely five-and six-membered rings ... fullerenes contain 2(10+N) carbon atoms ... the smallest conceivable fullerene is C20, and all fullerenes must contain an even number of carbon atoms.
Solutions of C60 fullerene in hydrocarbon solvents are magenta ... C70 fullerene are port-wine red. In some solvents C76 /and C84/ fullerene gives yellow-green solutions ... C82 fullerene has a less greenish tinge. Solutions of C78 fullerene are golden chestnut brown

3.4±0.1 g/cm3

500-600℃ subl.

>280ºC(lit.)

94ºC

1.813

21.59

0

0

0

60

2030

0

C12C3=C4C5=C6C7C8C9=C6C6C%10=C5C5C%11=C%12C%10=C%10C%13=C%14C%15=C%16C%17=C%18C%19=C%16C%16C%20=C%15C%13=C%12C%12C%20=C%13C%15C(=C%20C(=C%19C%19C%21C(=C(C3=7)C=1C%20=%19)C=8C(=C1C9=C(C%14=C1%17)C%10=6)C%18=%21)C%13=%16)C2=C(C=54)C=%15C=%12%11

XMWRBQBLMFGWIX-UHFFFAOYSA-N

InChI=1S/C60/c1-2-5-6-3(1)8-12-10-4(1)9-11-7(2)17-21-13(5)23-24-14(6)22-18(8)28-20(12)30-26-16(10)15(9)25-29-19(11)27(17)37-41-31(21)33(23)43-44-34(24)32(22)42-38(28)48-40(30)46-36(26)35(25)45-39(29)47(37)55-49(41)51(43)57-52(44)50(42)56(48)59-54(46)53(45)58(55)60(57)59

(C60-Ih)[5,6]fullerene

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O: < 0.1 mg/mL
DMSO: < 1 mg/mL

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)