Gold nanoparticles generated and stabilized by water soluble curcumin–polymer conjugate: Blood compatibility evaluation and targeted drug delivery onto cancer cells

• Published in: Journal of colloid and interface science Vol. 368; no. 1; pp. 144 - 151
• Main Authors: Manju, S., Sreenivasan, K.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Inc 15-02-2012; Elsevier
• Subjects: Antineoplastic Agents - pharmacology; bioavailability; Biocompatibility; Biocompatible Materials; Blood; Blood Coagulation - drug effects; Cancer; Cell Proliferation - drug effects; Chemistry; Colloidal state and disperse state; Confocal; confocal microscopy; curcumin; Curcumin - pharmacology; cytotoxicity; Dose-Response Relationship, Drug; Drug Delivery Systems; Drug Screening Assays, Antitumor; Exact sciences and technology; Flow cytometry; folic acid; Folic acid conjugated polyethylene glycol; General and physical chemistry; Gold; Gold - chemistry; Gold nanoparticle; HeLa Cells; Hemocompatibility; Humans; Hyaluronic acid; Hyaluronic Acid - chemistry; Magnetics; Membranes, Artificial; Metal Nanoparticles; nanocarriers; nanogold; Nanoparticles; Nanostructure; neoplasm cells; Physical and chemical studies. Granulometry. Electrokinetic phenomena; Solubility; Structure-Activity Relationship; Surface Properties; Tumor Cells, Cultured; Water - chemistry; Water soluble curcumin; Folic acid conjugated polyethylene glycol; Water soluble curcumin; Hyaluronic acid; Hemocompatibility; Gold nanoparticle; Water; Drug; Gold; Nanoparticle; Solubility; Confocal microscopy; Polymer; Transition metal; Blood; Design; Assay; Ethylene oxide polymer; Particle; Instability
• ISSN: 0021-9797; 1095-7103
• DOI: 10.1016/j.jcis.2011.11.024

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► Curcumin conjugated AuNPs were synthesized using hyaluronic acid-curcumin conjugates. ► HA–Cur@AuNPs were further HA–Cur@AuNPs modified with folate conjugated PEG to improve the cancer cell targeting. ► PF.HA–Cur@AuNPs exhibited better dose dependent cytotoxicity toward different cancer cell lines. ► PF.HA–Cur@AuNPs demonstrated enhanced targeting efficacy of 95.4%.
Curcumin (Cur) shows low anticancer activity in vivo due to its reduced systemic bioavailability stemmed from its poor aqueous solubility and instability. Suitably functionalized nanocarriers designed to empty the drug specifically at tumor sites can potentially enhance the antitumor activity of Cur. We devised a simple method for the fabrication of water soluble Cur conjugated gold nanoparticles to target various cancer cell lines. Cur was conjugated to hyaluronic acid (HA) to get a water soluble conjugate (HA–Cur). We generated gold nanoparticles (AuNPs) by reducing chloroauric acid using HA–Cur, which played the dual role of a reducing and stabilizing agent and subsequently anchored folate conjugated PEG. These entities were probed using different analytical techniques, assayed the blood compatibility and cytotoxicity. Their interaction with cancer cell lines (HeLa cells, glyoma cells and Caco 2 cells) was followed by flow cytometry and confocal microscopy. Blood–materials interactions studies showed that the nanoparticles are highly hemocompatible. Flow cytometry and confocal microscopy results showed significant cellular uptake and internalization of the particles by cells. HA–Cur@AuNPs exhibited more cytotoxicity comparing to free Cur. The strategy, we adopted here, resulted the formation blood compatible Cur conjugated AuNPs with enhanced targeting and improved efficacy.