Self-Assembled Folic Acid-Targeted Pectin-Multi-Arm Polyethylene Glycol Nanoparticles for Tumor Intracellular Chemotherapy

Abstract

Ursolic acid is widely used as an effective anticancer drug for the treatment of various cancers. However, its poor water solubility, short circulation time in vivo, and lack of targeting have made it a burden for clinical applications. We report a self-assembled folatemodified pectin nanoparticle for loading ursolic acid (HCPT@F-Pt-PU NPs) and embed the anticancer drug hydroxycamptothecin to achieve synergistic treatment with ursolic acid. In addition, the galactose residue of the pectin molecule can be recognized by the asialoglycoprotein receptor on the surface of the liver cancer cell, promoting the rapid penetration and release of HCPT@F-Pt-PU NPs intracellularly. In particular, the introduction of multiarm polyethylene glycol can improve the uniformity (106 nm) and concealment of the nanoparticles and avoid the early release of the drug or the toxicity to normal cells. HCPT@F-Pt-PU NPs have a high drug loading (7.27 wt %) and embedding efficiency (19.84 wt %) and continuous circulation up to 80 h, leading to more apoptosis (91.

Nanoparticles use for Delivering Ursolic Acid in Cancer Therapy: A Scoping Review

“…From the results of relative body weight calculations contained in Table 6, no significant differences existed in the weight of the mice, proving that nanoparticle administration neither caused side effects nor produced symptoms of toxicity (Poudel et al, 2020;Liu et al, 2021;Fu et al, 2021). This result is also supported by other toxicity data presented in Table 7, which shows that there was no clear cell damage and no morphological changes in the major organs i.e.…”

“…The concentration of NP HCPT@F-Pt-PU in the bloodstream, still detectable at 80 h, is higher than that of native UA (7 h) and HCPT (8 h). The concentration of NP HCPT @F-Pt-PU in plasma is higher than that of np F-Pt-PU, possibly because the conjugation of HCPT into polymers increases the strength of the hydrophobic bonds in the particle cores, thereby reducing the hydrolysis rate of nanoparticles (Liu et al, 2021).…”

“…V 0.5xy 2 where x is the longest and y the shortest diameter (Hattori et al, 2014;Yang et al, 2014;Wang et al, 2016;Miatmoko et al, 2017;Liu et al, 2021). In this study, the relative tumor volume is calculated using the following formulas:…”

“…Other toxicity data on the in vivo studies was derived by data recapitulation that included: tissue histopathology, increased levels of ALT and AST, and the amount of WBC as an indicator of hematological toxicity (Zhao et al, 2018;Li et al, 2019;Liu et al, 2021).…”

Targeted Delivery Methods for Anticancer Drugs

“…As pectins contain carboxyl groups, it is possible to use them to create negatively charged particles that retain drugs thanks to electrostatic interactions [228]. Moreover, pectin has been used to create self-organizing polymer nanoparticles to deliver ursolic acid [229].…”