Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

Abstract

The objective of the present study was to deliver docetaxel to cancerous cells with enhanced efficacy and safety profile, using aspartic acid linked fullerenols. This aspartic acid derivatized fullerenol conjugate linked with docetaxel was characterized by UV, FT-IR and NMR spectroscopy. Studies for particle size, PDI, zeta potential and FE-SEM were also performed. The conjugate was evaluated for release kinetics, cancer cell cytotoxicity, cellular uptake using confocal laser microscopy and also for pharmacokinetic profile. Cytotoxic studies proved that there was almost 4.3 folds decrease in IC with significantly enhanced cellular uptake of the nanometric conjugates. It was observed that the bioavailability was enhanced by 5.8 folds when compared to that of pure DTX. The developed nanoconstructs were erythrocyte compatible and offered decreased protein binding. The findings are encouraging and offer a novel carrier with enhanced efficacy and safety of a drug, belonging to BCS class IV.

pH-Sensitive Co-Adsorption/Release of Doxorubicin and Paclitaxel by Carbon Nanotube, Fullerene, and Graphene Oxide in Combination with N-isopropylacrylamide: A Molecular Dynamics Study

“…Some studies have shown that encapsulation or micro-encapsulation of fullerene in special carriers such as cyclodextrins and chemical functionalization by amino acid, carboxylic acid, poly hydroxyl group, and amphiphilic polymers can enhance the hydrophilicity and drastically reduce fullerene’s toxicity. The biological efficacy of water-soluble fullerenes has been investigated in vitro, indicating its low toxicity [27,28,29,30,31].…”

Advances in Therapeutic Implications of Inorganic Drug Delivery Nano-Platforms for Cancer

“…In another study, Docetaxel (DTX) was delivered to human breast cancer cells (MDA-MB-231 cell line) with enhanced efficacy and safety using aspartic acid linked fullerenols. Cytotoxic investigations proved that conjugated NDDP has ~4.3-fold lower IC 50 with significant cellular uptake and high bioavailability of drug (~5.8-fold higher as compared to free DTX) and nano-constructs were also immuno-compatible [63]. DTX has also been delivered in another in vitro cancer model using carboxylated and acylated C 60 -fullerenes as carrier vehicles to MCF-7 and MDA-MB231 cancerous cells.…”

Synthesis of surfactant‐modified ZIF‐8 with controllable microstructures and their drug loading and sustained release behaviour

“…According to properties of nanomaterials, nano‐drug carriers can be divided into inorganic nanocarriers (such as graphene [5], carbon nanotubes [6], fullerenes [7] and oxide nanoparticles [8–10]), organic nanocarriers (such as liposomes [11], polylactic acid [12], chitosan [13]) and metal nanocarriers including Au nanoparticles [14], Pd nanosheets [15], Pd@Au nanoparticles [16] etc.). In the field of nano drugs, researchers are paying more attention to control the design and construction of nanoparticles with special morphology and topology to better use for drug delivery.…”