Hyaluronic acid - dihydroartemisinin conjugate: Synthesis, characterization and in vitro evaluation in lung cancer cells

Kumar, Robin; Singh, Mamta; Meena, Jairam; Singhvi, Priyank; Thiyagarajan, Durairaj; Saneja, Ankit; Panda, Amulya K.

doi:10.1016/j.ijbiomac.2019.04.124

Cited by 51 publications

(24 citation statements)

References 32 publications

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“…A variety of nanotechnology has been developed in the past years to improve the solubility and bioavailability of ART. [23][24][25][26] ART loaded liposomes were reported with glioma targeting capabilities with enhanced toxicity towards glioma U87 cells. 27 Jin et al reported artesunate nanoliposomes, prepared with cholesterol and an appropriate amount of lecithin via thin film hydration method, showing stronger antitumor effect on HepG2 cells than that of free artesunate.…”

Section: Introductionmentioning

confidence: 99%

<p>pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer</p>

Hao

Xie

et al. 2020

IJN

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In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(βamino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model. Methods: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core. Results: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%±1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor. Conclusion: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.

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Section: Introductionmentioning

confidence: 99%

<p>pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer</p>

Hao

Xie

et al. 2020

IJN

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“…HA and CIP were conjugated by following the protection of acidic group of CIP for removing amphoteric ions and aided solubility as well as simplest and reproducible carbodiimide chemistry using EDAC/NHS via amide bond formation between the carboxylic group of polymer HA and amino group of CIP [ 39 ], as shown in Figure 1 A. The successful conjugation of the HA and CIP was confirmed via size exclusion chromatography ( Figure 1 B) and FTIR ( Figure 1 C).…”

Section: Resultsmentioning

confidence: 99%

A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection

et al. 2021

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Ciprofloxacin (CIP), a potent anti-bacterial agent of the fluroquinolone family, shows poor solubility and permeability, thus leading to the development of intracellular pathogens induced multi-drug resistance and biofilms formation. To synergistically improve the biopharmaceutical parameters of CIP, a hyaluronic acid (FDA approved biocompatible polymer) functionalized self-nano emulsifying drug delivery system (HA-CIP-SNEDDS) was designed in the present study. SNEDDS formulations were tested via solubility, droplet size, zeta potential, a polydispersity index, thermodynamic stability, surface morphology, solid-state characterization, drug loading/release, cellular uptake, and biocompatibility. The final (HA-CIP-SNEDDS) formulation exhibited a mean droplet size of 50 nm with the 0.3 poly dispersity index and negative zeta potential (−11.4 mV). HA-based SNEDDS containing CIP showed an improved ability to permeate goat intestinal mucus. After 4 h, CIP-SNEDDS showed a 2-fold and HA-CIP-SNEDDS showed a 4-fold permeation enhancement as compared to the free CIP. Moreover, 80% drug release of HA-CIP-SNEDDS was demonstrated to be superior and sustained for 72 h in comparison to free CIP. However, anti-biofilm activity of HA-CIP-SNEDDS against Salmonella typhi was higher than CIP-SNEDDS and free CIP. HA-CIP-SNEDDS exhibited increased biocompatibility and improved oral pharmacokinetics as compared to free CIP. Taken together, HA-CIP-SNEDDS formulation seems to be a promising agent against Salmonella typhi with a strong targeting potential.

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“…After ART loading, the spectrum of the MNP-ART exhibited new band in the 1740 cm −1 region, which belongs to C = O in δ-lactone of ART. In the same way, the absorption peaks at 3378 and 1740 cm −1 belong to O-H of DHA and C = O of AS, respectively (Ding et al, 2018;Kumar et al, 2019). The loading ratios of the three drugs were further measured by the UV-vis spectra.…”

Section: Preparation and Characterization Of Drug-loaded Mnpmentioning

confidence: 97%

Dihydroartemisinin-Loaded Magnetic Nanoparticles for Enhanced Chemodynamic Therapy

et al. 2020

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Recently, chemodynamic therapy (CDT) has represented a new approach for cancer treatment with low toxicity and side effects. Nonetheless, it has been a challenge to improve the therapeutic effect through increasing the amount of reactive oxygen species (ROS). Herein, we increased the amount of ROS agents in the Fenton-like reaction by loading dihydroartemisinin (DHA) which was an artemisinin (ART) derivative containing peroxide groups, into magnetic nanoparticles (MNP), thereby improving the therapeutic effect of CDT. Blank MNP were almost non-cytotoxic, whereas three MNP loading ART-based drugs, MNP-ART, MNP-DHA, and MNP-artesunate (MNP-AS), all showed significant killing effect on breast cancer cells (MCF-7 cells), in which MNP-DHA were the most potent. What's more, the MNP-DHA showed high toxicity to drug-resistant breast cancer cells (MCF-7/ADR cells), demonstrating its ability to overcome multidrug resistance (MDR). The study revealed that MNP could produce ferrous ions under the acidic condition of tumor microenvironment, which catalyzed DHA to produce large amounts of ROS, leading to cell death. Further experiments also showed that the MNP-DHA had significant inhibitory effect on another two aggressive breast cancer cell lines (MDA-MB-231 and MDA-MB-453 cells), which indicated that the great potential of MNP-DHA for the treatment of intractable breast cancers.

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Hyaluronic acid - dihydroartemisinin conjugate: Synthesis, characterization and in vitro evaluation in lung cancer cells

Cited by 51 publications

References 32 publications

<p>pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer</p>

<p>pH-Responsive Artesunate Polymer Prodrugs with Enhanced Ablation Effect on Rodent Xenograft Colon Cancer</p>

A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection

Dihydroartemisinin-Loaded Magnetic Nanoparticles for Enhanced Chemodynamic Therapy

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