Synthesis and colloidal characterization of folic acid-modified PEG-b-PCL Micelles for methotrexate delivery

Brandt, João Victor; Piazza, Rodolfo Debone; Santos, Caio Carvalho dos; Vega-Chacón, Jaime; Amantéa, Bruno Estevam; Pinto, Gabriel Cardoso; Magnani, Marina; Piva, Henrique Luís; Tedesco, Antônio Cláudio; Primo, Fernando Lucas; Jafelicci, Miguel; Marques, Rodrigo Fernando Costa

doi:10.1016/j.colsurfb.2019.02.008

Cited by 49 publications

(25 citation statements)

References 33 publications

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“…A fraction of the load associated with the head groups in the presence of APBA ( Figure 4 ). A similar association has been reported at the surface between folic acid (targeting ligand) and methotrexate in PEG-PCL micelles [ 30 ].…”

Section: Resultssupporting

confidence: 80%

“…For example, the average size of TPGS-2000 micelles shifted from 30 to 51 nm upon attachment of folic acid [ 29 ]. Similarly, Brandt and coworkers [ 30 ] recorded a 50% higher size of micelles after functionalization of the block copolymer with folic acid. Moreover, folic acid imparted negative zeta potential to the micelles, which was sustained in the low pH (3–6) region as well.…”

Section: Resultsmentioning

confidence: 82%

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Synthesis, Colloidal Characterization and Targetability of Phenylboronic Acid Functionalized α-Tocopheryl Polyethylene Glycol Succinate in Cancer Cells

et al. 2020

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This study reports targetable micelles developed after covalent functionalization of α-tocopheryl polyethylene glycol succinate (TPGS) with amino phenylboronic acid (APBA). Nuclear magnetic resonance (NMR) and infrared (IR) spectroscopic results showed successful attachment of APBA to the hydrophilic segment of TPGS. Dynamic light scattering and small-angle neutron scattering studies revealed that the conjugate self-assembled in water to produce spherical core-shell micelles (14–20 nm) which remained stable against temperature (ca. 25–45 °C) and pH changes. The micelles could solubilize a high payload of paclitaxel (PLX) without exhibiting changes in the average size. However, at the saturation solubility, drug molecules migrated from the core to the shell region and engaged with APBA groups via π–π stacking interaction. Confocal microscopy and cell sorting analyses verified the effective translocation ability of TPGS-APBA micelles in sialic acid (SA) expressing MDA-MB-453 cells. At equivalent PLX dose, TPGS-APBA micelles showed about a twofold improvement in apoptotic death among the cells exposed for 2 h. Our findings indicate that the attachment of APBA can be a potential strategy for improving the intra-cellular localization of carriers among cancer cells expressing SA residues.

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Section: Resultssupporting

confidence: 80%

Section: Resultsmentioning

confidence: 82%

Synthesis, Colloidal Characterization and Targetability of Phenylboronic Acid Functionalized α-Tocopheryl Polyethylene Glycol Succinate in Cancer Cells

et al. 2020

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“…Methotrexate (MTX) is a well-known cytotoxic agent, which competitively and irreversibly inhibits dihydrofolate reductase, an enzyme that participates in tetrahydrofolate synthesis [14,15]. It is currently used in lung cancer treatment alone or along with other chemotherapeutic agents by oral and parenteral routes.…”

Section: Introductionmentioning

confidence: 99%

Co-Loaded Curcumin and Methotrexate Nanocapsules Enhance Cytotoxicity against Non-Small-Cell Lung Cancer Cells

et al. 2020

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Background: As part of the efforts to find natural alternatives for cancer treatment and to overcome the barriers of cellular resistance to chemotherapeutic agents, polymeric nanocapsules containing curcumin and/or methotrexate were prepared by an interfacial deposition of preformed polymer method. Methods: Physicochemical properties, drug release experiments and in vitro cytotoxicity of these nanocapsules were performed against the Calu-3 lung cancer cell line. Results: The colloidal suspensions of nanocapsules showed suitable size (287 to 325 nm), negative charge (−33 to −41 mV) and high encapsulation efficiency (82.4 to 99.4%). Spherical particles at nanoscale dimensions were observed by scanning electron microscopy. X-ray diffraction analysis indicated that nanocapsules exhibited a non-crystalline pattern with a remarkable decrease of crystalline peaks of the raw materials. Fourier-transform infrared spectra demonstrated no chemical bond between the drug(s) and polymers. Drug release experiments evidenced a controlled release pattern with no burst effect for nanocapsules containing curcumin and/or methotrexate. The nanoformulation containing curcumin and methotrexate (NCUR/MTX-2) statistically decreased the cell viability of Calu-3. The fluorescence and morphological analyses presented a predominance of early apoptosis and late apoptosis as the main death mechanisms for Calu-3. Conclusions: Curcumin and methotrexate co-loaded nanocapsules can be further used as a novel therapeutic strategy for treating non-small-cell lung cancer.

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“…Nonpolar lipophilic drugs are incorporated within the lipid bicoating, while water-soluble drugs reside in the vesicle. Entrapment of antineoplastic therapies in lipophilic liposomes result in pharmacokinetic modifications and pharmacodynamics features, with a resultant decline in drug degradation and improved dose cytotoxicity [31,[51][52][53]. These lipophilic nanocarriers can be utilised for specific targeting and imaging of tumour tissues; however, ligands applied to the phospholipid coating improve cellular uptake thus enabling a pronounced therapeutic effect to the targeted specific-sites [31,[51][52][53][54].…”

Section: Critical Comparison Of Nanosystems To Nanomicelles For Oc Trmentioning

confidence: 99%

“…Schematic depicting examples of nanosized delivery systems; (a) liposomes, (b) nanomicelles, (c,d) polymer-drug conjugates, and (e) dendrimers, which are currently explored in detail for transport of chemotherapeutic agents (adapted with permission from (a) Trucillo et al[31], (b) Brandta et al[51], (c,d) Tong et al[52], (e) Huang &Wu[53].…”

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confidence: 99%

Nanodrug Delivery Systems for the Treatment of Ovarian Cancer

Pantshwa

Kondiah

Choonara

et al. 2020

Cancers

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Despite advances achieved in medicine, chemotherapeutics still has detrimental side effects with ovarian cancer (OC), accounting for numerous deaths among females. The provision of safe, early detection and active treatment of OC remains a challenge, in spite of improvements in new antineoplastic discovery. Nanosystems have shown remarkable progress with impact in diagnosis and chemotherapy of various cancers, due to their ideal size; improved drug encapsulation within its interior core; potential to minimize drug degradation; improve in vivo drug release kinetics; and prolong blood circulation times. However, nanodrug delivery systems have few limitations regarding its accuracy of tumour targeting and the ability to provide sustained drug release. Hence, a cogent and strategic approach has focused on nanosystem functionalization with antibody-based ligands to selectively enhance cellular uptake of antineoplastics. Antibody functionalized nanosystems are (advanced) synthetic candidates, with a broad range of efficiency in specific tumour targeting, whilst leaving normal cells unaffected. This article comprehensively reviews the present status of nanosystems, with particular emphasis on nanomicelles for molecular diagnosis and treatment of OC. In addition, biomarkers of nanosystems provide important prospects as chemotherapeutic strategies to upsurge the survival rate of patients with OC.

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Synthesis and colloidal characterization of folic acid-modified PEG-b-PCL Micelles for methotrexate delivery

Cited by 49 publications

References 33 publications

Synthesis, Colloidal Characterization and Targetability of Phenylboronic Acid Functionalized α-Tocopheryl Polyethylene Glycol Succinate in Cancer Cells

Synthesis, Colloidal Characterization and Targetability of Phenylboronic Acid Functionalized α-Tocopheryl Polyethylene Glycol Succinate in Cancer Cells

Co-Loaded Curcumin and Methotrexate Nanocapsules Enhance Cytotoxicity against Non-Small-Cell Lung Cancer Cells

Nanodrug Delivery Systems for the Treatment of Ovarian Cancer

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