Cannabidiol as Self-Assembly Inducer for Anticancer Drug-Based Nanoparticles

Colombo, Eleonora; Coppini, Davide Andrea; Polito, Laura; Ciriello, Umberto; Paladino, Giuseppe; Hyeraci, Mariafrancesca; Paolo, Maria Luisa Di; Nordio, Giulia; Via, Lisa Dalla; Passarella, Daniele

doi:10.3390/molecules28010112

Cited by 5 publications

(8 citation statements)

References 33 publications

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“…The seven drugs 7 – 13 confirmed their cytotoxicity towards tumor cells, as GI 50 in the low micromolar or nanomolar range were obtained in all cell lines taken into consideration, also in accordance with our earlier data [ 31 ]. In detail, podophyllotoxin ( 12 ) and thiocolchicine ( 13 ) exerted the lowest antiproliferative effect with GI 50 values ranging from 0.011 to 0.030 μM, whereas cabazitaxel ( 8 ) and docetaxel ( 9 ) appear as the most effective drugs, showing GI 50 values from 0.7 to 2.0 nM.…”

Section: Resultssupporting

confidence: 90%

2-Hydroxyoleic Acid as a Self-Assembly Inducer for Anti-Cancer Drug-Centered Nanoparticles

et al. 2023

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A potent nontoxic antitumor drug, 2-hydroxyoleic acid (6, 2OHOA) used for membrane lipid therapy, was selected as a self-assembly inducer due to its ability to form nanoparticles (NPs) in water. For this purpose, it was conjugated with a series of anticancer drugs through a disulfide-containing linker to enhance cell penetration and to secure drug release inside the cell. The antiproliferative evaluation of the synthesized NP formulations against three human tumor cell lines (biphasic mesothelioma MSTO-211H, colorectal adenocarcinoma HT-29, and glioblastoma LN-229) showed that nanoassemblies 16–22a,bNPs exhibit antiproliferative activity at micromolar and submicromolar concentrations. Furthermore, the ability of the disulfide-containing linker to promote cellular effects was confirmed for most nanoformulations. Finally, 17bNP induced intracellular ROS increase in glioblastoma LN-229 cells similarly to free drug 8, and such elevated production was decreased by pretreatment with the antioxidant N-acetylcysteine. Also, nanoformulations 18bNP and 21bNP confirmed the mechanism of action of the free drugs.

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Section: Resultssupporting

confidence: 90%

2-Hydroxyoleic Acid as a Self-Assembly Inducer for Anti-Cancer Drug-Centered Nanoparticles

et al. 2023

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“…Furthermore, the research suggests that it may be possible to adjust the activity of anticancer drugs by changing the type of linker. 145 …”

Section: What Do We Know About Clinically Important Cannabinoids?mentioning

confidence: 99%

How Biodegradable Polymers Can be Effective Drug Delivery Systems for Cannabinoids? Prospectives and Challenges

Sobieraj,

Strzelecka,

Sobczak

et al. 2024

IJN

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Cannabinoids are compounds found in and derived from the Cannabis plants that have become increasingly recognised as significant modulating factors of physiological mechanisms and inflammatory reactions of the organism, thus inevitably affecting maintenance of homeostasis. Medical Cannabis popularity has surged since its legal regulation growing around the world. Numerous promising discoveries bring more data on cannabinoids’ pharmacological characteristics and therapeutic applications. Given the current surge in interest in the medical use of cannabinoids, there is an urgent need for an effective method of their administration. Surpassing low bioavailability, low water solubility, and instability became an important milestone in the advancement of cannabinoids in pharmaceutical applications. The numerous uses of cannabinoids in clinical practice remain restricted by limited administration alternatives, but there is hope when biodegradable polymers are taken into account. The primary objective of this review is to highlight the wide range of indications for which cannabinoids may be used, as well as the polymeric carriers that enhance their effectiveness. The current review described a wide range of therapeutic applications of cannabinoids, including pain management, neurological and sleep disorders, anxiety, and cancer treatment. The use of these compounds was further examined in the area of dermatology and cosmetology. Finally, with the use of biodegradable polymer-based drug delivery systems (DDSs), it was demonstrated that cannabinoids can be delivered specifically to the intended site while also improving the drug’s physicochemical properties, emphasizing their utility. Nevertheless, additional clinical trials on novel cannabinoids’ formulations are required, as their full spectrum therapeutical potential is yet to be unravelled.

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“…HepG2 cell line, a good in vitro model to toxicity studies also for cannabis and derivatives, was employed [27,28].…”

Section: Effect Of Cannabis Sativa L Extracts On Viability Of Hepatob...mentioning

confidence: 99%

Legal Cannabis sativa L. Dried Inflorescences: Cannabinoids Content and Cytotoxic Activity against Human HepG2 Cell Line

Acquavia

Tesoro

Pascale³

et al. 2023

Applied Sciences

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Cannabis sativa L. has health benefits, principally due to the levels and ratios of two important cannabinoids, Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD). THC:CBD ratio affects their pharmacological interaction for the treatment of different diseases as well as its modulation allows for a custom-made product that utilizes the distinguishing effects of CBD, THC, or both, for a peculiar patient or clinical effect. This study aims to investigate the total content of THC, CBD, and their ratio in 34 dried inflorescence legally sold in physical and online stores, by using a validated liquid chromatography-ultraviolet (HPLC-UV) method, after cannabinoids identification performed through MSn studies. Cannabinol (CBN) content was also monitored to evaluate hemp age or conservation status. CBN content always resulted lower than limit of quantification, thus confirming well-stored fresh hemp. All investigated samples showed a total THC amount below 0.59% w/w, thus responding to legal requirements.. The total CBD amount ranged from 2.62 to 20.27% w/w and it was not related to THC level. THC:CBD ranged among 1:3 and 1:26, thus ascertaining their suitability for different target pharmacological uses. In vitro studies using human hepatoblastoma cell line HepG2 suggested that hemp extracts with THC:CBD ratios of 1:9 exhibited higher toxicity than pure cannabinoids.

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Cannabidiol as Self-Assembly Inducer for Anticancer Drug-Based Nanoparticles

Cited by 5 publications

References 33 publications

2-Hydroxyoleic Acid as a Self-Assembly Inducer for Anti-Cancer Drug-Centered Nanoparticles

2-Hydroxyoleic Acid as a Self-Assembly Inducer for Anti-Cancer Drug-Centered Nanoparticles

How Biodegradable Polymers Can be Effective Drug Delivery Systems for Cannabinoids? Prospectives and Challenges

Legal Cannabis sativa L. Dried Inflorescences: Cannabinoids Content and Cytotoxic Activity against Human HepG2 Cell Line

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