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 was conducted to determine the distribution of (14)C-C60 in the pregnant rat and fetus, and in the lactating rat and off-spring. Four dams were dosed via tail vein injection on gestational day (gd) 15 with 0.28 mg/kg body weight (14)C-C60 (~ 3 uCi per rat) prepared in 5% polyvinylpyrrolidone in saline (PVP), and four dams were dosed with PVP alone. Urine (0-24 hr) and tissues (24 hr) were collected from the dams. Eight lactating rats were dosed on postnatal day (pnd) 8 with 0.36 mg/kg (14)C-C 60 prepared in PVP, and sacrificed at 24 hr or 48 hr after exposure. In the pregnant dams, radioactivity was distributed to the placenta (approximately 2% of the dose), to the fetus (1.0%), and to the female reproductive tract (3.0%). Radioactivity was distributed to the milk (< 1%) and mammary tissue (<1%) in the lactating rats, and to the GI tract (<1%) and liver of the pup (< 1%). For the pregnant dam, radioactivity was distributed to the urine (<2%), feces (2%), blood (0.9% per mL) and plasma (1.7% per mL), brain (< 1%), lung (<1%), heart (<1%), liver (~43%), spleen (4%). In comparison to the pregnant dam, lactating rats had a similar radioactivity distribution to the blood and plasma at 24 hr after exposure (with a 50% decrease by 48 hr), a higher distribution to the lung, and a decreased distribution to the liver. Metabolomics analysis of urine indicated that dams exposed to C60 had a decrease in metabolites derived from the Krebs cycle and an increase in metabolites derived from the urea cycle or glycolysis; with alterations in the levels of some sulfur-containing amino acids and purine/pyrimidine metabolites. This study indicated that C60 can cross the placenta and can be transmitted from mother to offspring via milk.
Dermatomed porcine skin was fixed to a flexing device and topically dosed with 33.5 mg/mL of an aqueous solution of a fullerene-substituted phenylalanine (Baa) derivative of a nuclear localization peptide sequence (Baa-Lys(FITC)-NLS). Skin was flexed for 60 or 90 min or left unflexed (control). Confocal microscopy depicted dermal penetration of the nanoparticles at 8 hr in skin flexed for 60 and 90 min, whereas Baa-Lys(FITC)-NLS did not penetrate into the dermis of unflexed skin until 24 hr. TEM analysis revealed fullerene-peptide localization within the intercellular spaces of the stratum granulosum.
...Both microscopic imaging and biological techniques /were used/ to explore the processes of [C60(C(COOH)2)2]n nanoparticles across cellular membranes and their intracellular translocation in 3T3 L1 and RH-35 living cells. The fullerene nanoparticles are quickly internalized by the cells and then routed to the cytoplasm with punctate localization. Upon entering the cell, they are synchronized to lysosome-like vesicles. The [C60(C(COOH)2)2]n nanoparticles entering cells are mainly via endocytosis with time-, temperature- and energy-dependent manners. The cellular uptake of [C60(C(COOH)2)2]n nanoparticles was found to be clathrin-mediated but not caveolae-mediated endocytosis...
... An overview of the nanostructure and the physical and chemical characteristics of fullerene-drug derivatives is given. The biological behavior of fullerene derivatives shows their potential to medical application fields because C(60) is rapidly absorbed by tissues and is excreted through urinary tract and enterons, which reveals low toxicity in vitro and in vivo studies. Nanomedicine has become one of the most promising areas of nanotechnology, while many have claimed its therapeutic use against cancer, human immunodeficiency virus (HIV), and neurodegenerative disorders. Water-soluble C(60) fullerene derivatives that come from chemical modification largely enhance the biological efficacy. The blood-brain barrier (BBB) is a physical barrier composed of endothelial tight junctions that restrict the paracellular permeability. A major challenge facing neuropharmacology is to find compounds that can be delivered into the brain through the bloodstream. Fullerene C(60) was demonstratively able to cross the BBB by hybridizing a biologically active moiety dyad, which provides a promising clue as a pharmacological therapy of neural disorders. /C(60) Fullerene derivatives/
Pristine fullerenes (C60) in different solvents will be used in many industrial and pharmaceutical manufacturing and derivatizing processes. This report explores the impact of solvents on skin penetration of C60 from different types of industrial solvents (toluene, cyclohexane, chloroform and mineral oil). Yorkshire weanling pigs (n=3) were topically dosed with 500 uL of 200 ug/mL C60 in a given solvent for 24 hr and re-dosed daily for 4 days to simulate the worst scenario in occupational exposures. The dose sites were tape-stripped and skin biopsies were taken after 26 tape-strips for quantitative analysis. When dosed in toluene, cyclohexane or chloroform, pristine fullerenes penetrated deeply into the stratum corneum, the primary barrier of skin. More C60 was detected in the stratum corneum when dosed in chloroform compared to toluene or cyclohexane. Fullerenes were not detected in the skin when dosed in mineral oil. This is the first direct evidence of solvent effects on the skin penetration of pristine fullerenes. The penetration of C60 into the stratum corneum was verified using isolated stratum corneum in vitro; the solvent effects on the stratum corneum absorption of C60 were consistent with those observed in vivo. In vitro flow-through diffusion cell experiments were conducted in pig skin and fullerenes were not detected in the receptor solutions by 24 hr. The limit of detection was 0.001 ug/mL of fullerenes in 2 mL of the receptor solutions.

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Biological Half-Life
Fullerenes ... are spherical molecules consisting entirely of carbon atoms (C(x)) to which side chains can be added, furnishing compounds with widely different properties. ... Absorption, distribution and excretion strongly depend on the properties of the side chains. The pristine C(60) has a very long biological half-life, whereas the most water-soluble derivatives are eliminated from the exposed animals within weeks.
... Male rats /were exposed/ to C60 fullerene nanoparticles (2.22 mg/cu m, 55 nm diameter) and microparticles (2.35 mg/cu m, 0.93 um diameter) for 3 hr a day, for 10 consecutive days using a nose-only exposure system. Nanoparticles were created utilizing an aerosol vaporization and condensation process. Nanoparticles and microparticles were subjected to high-pressure liquid chromatography (HPLC), XRD, and scanning laser Raman spectroscopy, which cumulatively indicated no chemical modification of the C60 fullerenes occurred during the aerosol generation. ... Lung half-lives for C60 fullerene nanoparticles and microparticles were 26 and 29 days, respectively...

Interactions
The radioprotective effect of the nanoparticle DF-1, a fullerene with antioxidant properties, /was evaluated. in zebrafish embryos. Zebrafish embryos were exposed to different doses of ionizing radiation ranging from 20 to 80 Gy in the presence and absence of DF-1. Toxicity and radioprotective effects were assessed by monitoring overall survival and morphology as well as organ functions by employing assays to measure kidney excretory function and development of sensory nerve cells (neuromasts). Antioxidant properties of DF-1 were assessed in whole fish. RESULTS: DF-1 had no apparent adverse effects on normal zebrafish morphology or viability throughout the concentration range tested (1-1,000 umol/L). Ionizing radiation (10-40 Gy) caused time-dependent and dose-dependent perturbations of normal zebrafish morphology and physiology, notably defective midline development resulting in dorsal curvature of the body axis ("curly-up"), neurotoxicity, impaired excretory function, and decreased survival of the exposed embryos. DF-1 (100 umol/L) markedly attenuated overall and organ-specific radiation-induced toxicity when given within 3 hours before or up to 15 minutes after radiation exposure. By contrast, DF-1 afforded no protection when given 30 minutes after ionizing radiation. ... Protection against radiation-associated toxicity using DF-1 in zebrafish embryos was associated with marked reduction of 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 fullerene. It has a role as a geroprotector.
Buckyball is a nanoparticle characterized by a spherical geometry and hollow interior that is comprised of 60 carbon atoms. This configuration is the most common type of fullerene.
buckminsterfullerene is a mineral.
Fullerite is a mineral with formula of C60.
A polyhedral CARBON structure composed of around 60-80 carbon atoms in pentagon and hexagon configuration. They are named after Buckminster Fuller because of structural resemblance to geodesic domes. Fullerenes can be made in high temperature such as arc discharge in an inert atmosphere.
See also: Fullerene (annotation moved to).

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Therapeutic Uses
/Experimental Therapy:/ Fullerene (C60), a third carbon allotrope, is a classical engineered material with the potential application in biomedicine. One of the biologically most relevant features of C60 is the ability to quench various free radicals, behaving as a "free radical sponge". Conversely, photosensitization of C60 leads to its transition to a long-lived triplet excited state and the subsequent energy or electron transfer to molecular oxygen, yielding highly reactive singlet oxygen (1O2) or superoxide anion (O2-), respectively. These reactive oxygen species (ROS) react with a wide range of biological targets and are known to be involved in both cellular signaling and cell damage. Therefore, the dual property of fullerenes to either quench or generate cell-damaging ROS could be potentially exploited for their development as cytoprotective or cytotoxic anticancer/antimicrobial agents. However, the attempts to that effect have been hampered by the extremely low water solubility of C60, and by the fact that solubilization procedures profoundly influence the ROS-generating/quenching properties of C60, either through chemical modification or through formation of complex nanoscale particles with different photophysical properties...
/Experimental Therapy: Gadolinium metallofullerenol nanoparticles [Gd@C82(OH)22]n particles (22 nm in a saline solution) of a dose level as low as 10-7 mol/kg exhibit a very high antineoplastic efficiency ( approximately 60%) in mice. A dose increment of 1 x 10-7 mol/kg increases the tumor inhibition rate 26%. [Gd@C82(OH)22]n particles have a strong capacity to improve immunity and interfere with tumor invasion in normal muscle cells, nearly without toxicity in vivo and in vitro. Unlike conventional antineoplastic chemicals, the high antitumor efficiency of nanoparticles is not due to toxic effects to cells because they do not kill the tumor cells directly and only about 0.05% of the used dose is found in the tumor tissues. Results suggest that fullerene derivatives with proper surface modifications and sizes may /be developed as/ tumor chemotherapeutics of high-efficacy and low-toxicity. /Gadolinium metallofullerenol nanoparticles/
/Experimental Therapy:/ This is the first report on the targeted delivery of fullerene-based low toxic nanocationite particles (porphyrin adducts of cyclohexyl fullerene-C(60)) to treat hypoxia-induced mitochondrial dysfunction in mammalian heart muscle. ... The magnetic isotope effect generated by the release of paramagnetic (25)Mg(2+) from these nanoparticles selectively stimulates the ATP overproduction in the oxygen-depleted cell. ... Because nanoparticles are membranotropic cationites, they will only release the overactivating paramagnetic cations in response to hypoxia-induced acidic shift. The resulting changes in the heart cell energy metabolism result in approximately 80% recovery of the affected myocardium in <24 hr after a single injection (0.03-0.1 LD(50)).... Pharmacokinetics and pharmacodynamics of the nanoparticles suggest their suitability for safe and efficient administration in either single or multi-injection (acute or chronic) therapeutic schemes for the prevention and treatment of clinical conditions involving myocardial hypoxia.
/Experimental Therapy:/ Oxidative stress plays a major role in acne formation, suggesting that oxygen radical scavengers are potential therapeutic agents. Fullerene is a spherical carbon molecule with strong radical sponge activity; therefore, the effectiveness of fullerene gel in treating acne vulgaris /was studied/. /Investigators/ performed an open trial using a fullerene gel twice a day; at 4 and 8 weeks, the mean number of inflammatory lesions (erythematous papules and pustules) significantly (P < 0.05) decreased 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, consisting of accumulation of neutrophils, was significantly (P < 0.05) decreased from 1.45 +/- 1.13 to 0.18 +/- 0.60 (reduction rate 87.6%), and further in vitro assays of sebum production in hamster sebocytes revealed that 75 uM polyvinylpyrrolidone-fullerene inhibits sebum production, suggesting that fullerene suppresses acne through decreasing neutrophil infiltration and sebum production. After treatment for 8 weeks, the water content of the skin significantly (P < 0.05) increased from 51.7 +/- 7.9 to 60.4 +/- 10.3 instrumental units. Therefore, the fullerene gel may help in controlling acne vulgaris with skin care benefit. ...

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.)