Abstract
Conventional delivery of anticancer drugs is less effective due to pharmacological drawbacks such as lack of aqueous solubility and poor cellular accumulation. This study reports the increased drug loading, therapeutic delivery, and cellular accumulation of silibinin (SLB), a poorly water-soluble phenolic compound using a hydrophobically-modified chitosan nanoparticle (pCNP) system. In this study, chitosan nanoparticles were hydrophobically-modified to confer a palmitoyl group as confirmed by 2,4,6-Trinitrobenzenesulfonic acid (TNBS) assay. Physicochemical features of the nanoparticles were studied using the TNBS assay, and Attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR) analyses. The FTIR profile and electron microscopy correlated the successful formation of pCNP and pCNP-SLB as nano-sized particles, while Dynamic Light Scattering (DLS) and Field Emission-Scanning Electron Microscopy (FESEM) results exhibited an expansion in size between pCNP and pCNP-SLB to accommodate the drug within its particle core. To evaluate the cytotoxicity of the nanoparticles, a Methylthiazolyldiphenyl-tetrazolium bromide (MTT) cytotoxicity assay was subsequently performed using the A549 lung cancer cell line. Cytotoxicity assays exhibited an enhanced efficacy of SLB when delivered by CNP and pCNP. Interestingly, controlled release delivery of SLB was achieved using the pCNP-SLB system, conferring higher cytotoxic effects and lower IC50 values in 72-h treatments compared to CNP-SLB, which was attributed to the hydrophobic modification of the CNP system.
Highlights
IntroductionRadiation, chemotherapy and surgery have become important methods to treat cancer patients
Over the last decade, radiation, chemotherapy and surgery have become important methods to treat cancer patients
Silibinin is preferentially advantageous for development as a candidate therapeutic agent as it is considered remarkably safe in cytotoxicity studies, as it confers low toxicity even in acute administration dosages in both humans and animals, and there are no LD50 values for the flavonolignan reported in laboratory studies
Summary
Radiation, chemotherapy and surgery have become important methods to treat cancer patients Among these methods, chemotherapy remains the most significant treatment, with synthetic drugs being the most potent chemotherapeutic drugs used [1]. Known as silybin, is a major active constituent obtained from the seeds of the milk thistle plant, Silybum marianum. It exists as a polyphenolic flavonolignan with hepatoprotective and antioxidant activity. Its widespread application in medical therapy has been marred by its low bioavailability due to low solubility in water (0.4 mg/mL) [15,16,17,18] This restriction was due to its multiple ring structure, which is too large to be absorbed by simple diffusion, which leads to poor water solubility, poor bioavailability and poor intestinal absorption [19]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
