Folic acid-decorated and PEGylated PLGA nanoparticles for improving the antitumour activity of 5-fluorouracil

El-Hammadi, Mazen M.; Delgado, A.V.; Melguizo, Consolación; Prados, José; Arias, José L.

doi:10.1016/j.ijpharm.2016.11.012

Cited by 123 publications

(64 citation statements)

References 38 publications

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“…(e) Synthesis of NHS-activated PLGA (NHS-PLGA) NHS-activated PLGA (NHS-PLGA) conjugate was synthesized using previously available literature protocol with slight modifications [21]. Organic phase was prepared by dissolving an appropriate amount of PLGA (0.12 mmol), DCC (0.24 mmol) and NHS (0.24 mmol) in 4 ml of anhyd.…”

Section: (B) Synthesis Of N-boc-ethylenediamine (Bocking)mentioning

confidence: 99%

Anti-proliferate and apoptosis triggering potential of methotrexate-transferrin conjugate encapsulated PLGA nanoparticles with enhanced cellular uptake by high-affinity folate receptors

Parmar

Jain

Uppal

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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The objective of the present study is to enhance the permeation of bioactive molecules across highly lipophilic insurmountable blood brain barrier (BBB) using folic acid (FA) functionalized poly(lactic-co-glycolic acid) (PLGA) nanoparticles (FA-PNPs) coated with non-ionic surfactant, Polysorbate 80 (P). The developed Mtx-Tf loaded folic acid anchored PNPs formulation depicted particle size, zeta potential and entrapment efficiency of 109 ± 2.3 nm, -9.38 ± 0.9 mV and 71.0 ± 0.6%, respectively. In vitro release showed biphasic release pattern with initial >35% release in 8 h followed by sustained release, up to 65% by the end of 168 h. SRB cyto-toxicity assay depicted P-Mtx-Tf-FA-PNPs possessing better cellular cyto-toxicity (C6 Glioma) as compared to counter test formulations, i.e. 100 μM nano-encapsulated drug-conjugate concentration incubated for 72 h resulted in apoptosis of ∼100% of the cellular population. Qualitatively, ∼85% of P-FITC-FA-PNPs have been found to be internalized by C6 glioma cells post 5 h of incubation. Quantitative cellular uptake assay demonstrated a collinear dependence on drug-conjugate concentration. In vivo administration of P-Mtx-Tf-FA-PNPs depicted significant decrease, i.e. 73.6% in the tumour spheroid volume. Serum analysis data pointed towards the significant relevance of P-coated FA-PNPs in lowering the drug diffusion rate by 88.4% (after 30 min) and three-fold enhanced retention time of drug in systemic circulation, thereby felicitating an effective prognostic treatment. This study clearly demonstrated reduced systemic toxicity, enhanced biocompatibility and anti-tumour efficacy of formulated NPs.

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Section: (B) Synthesis Of N-boc-ethylenediamine (Bocking)mentioning

confidence: 99%

Anti-proliferate and apoptosis triggering potential of methotrexate-transferrin conjugate encapsulated PLGA nanoparticles with enhanced cellular uptake by high-affinity folate receptors

Parmar

Jain

Uppal

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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“…Burst release phenomenon can be attributed to the drug attached to the surface of the NCs. 40 Moreover, PEG chains are hydrophilic and can be easily dissolved in an aqueous release medium which derived the water to penetrate into the oily core, allowing HK to be released. Higher content of PEG accelerated the degradation rate because it facilitates higher water penetration compared with other NCs.…”

Section: Effect Of Peg Content Of the Polymer Backbonementioning

confidence: 99%

<p>Design, Formulation and in vivo Evaluation of Novel Honokiol-Loaded PEGylated PLGA Nanocapsules for Treatment of Breast Cancer</p>

Haggag¹,

Ibrahim²,

Hafiz³

2020

IJN

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Background: Honokiol (HK) is a common herbal medicine extracted from magnolia plants. Low aqueous solubility and limited bioavailability of HK have hindered its clinical application, especially for cancer treatment. Nano-drug delivery system has the potential to enhance HK delivery and therefore, enhance its anti-cancer activity. Purpose: The study's aim is to design novel PEGylated-PLGA polymeric nanocapsules (NCs) for HK delivery to breast tumor-bearing mice after systemic administration. Methods: Formulation of different HK-loaded NCs and their physio-chemical characterization were optimized through the use of different formulation variables. The antitumor activity of the HK-loaded NCs was investigated both in vitro using MCF-7 and EAC breast cancer cell lines and in vivo using solid Ehrlich carcinoma (SEC) breast cancer model. Results: The optimum HK-loaded NCs were prepared from 15% PEG-PLGA diblock copolymer and exhibited the lowest nano size of 125 nm, smooth spherical morphology, highest drug loading of 94% and highest cellular uptake into breast cancer cells. HK-loaded PEGylated NCs can effectively inhibit the in vitro cell growth of breast cancer cells by 80.2% and 58.1% compared to 35% and 31% with free HK in the case of MCF-7 and EAC, respectively. HK-loaded NCs inhibited SEC tumor growth by 2.3 fold significantly higher than free HK, in vivo. Conclusion: The designed drug delivery system encapsulating HK exhibited a pronounced decrease in tumor growth biomarkers meanwhile proved its safety in animals. Therefore, 15% PEGylated HK-loaded NCs may act as a promising new approach for breast cancer treatment.

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“…5-Florourasil, nükleozit metabolizmasına müdahale eden ve ribonükleik asit ve deoksiribonükleik asite dahil edilebilen geniş spektrumlu bir moleküldür, esas olarak timidilat sentaz inhibitörü olarak hareket ederek kanser hücrelerinde apoptozu aktive eder. 4 5-Florourasil'in, sitotoksik etkisini gösterebilmesi için monofosfat formu olan florodeoksiüridin monofosfat (FdUMP)'a aktive edilmelidir. Florodeoksiüridin monofosfat, kararlı bir üçlü kompleks oluşturarak timidilat sentazın güçlü irreversibl inhibitörü olarak etki gösterir.…”

Section: -Florourasi̇l (5-fu)unclassified

New Drug Combination in Colorectal Cancer Treatment: Trifluridine and Tipiracil

Avci¹,

Tunçbìlek²

2017

Turkiye Klinikleri J Med Sci

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Ö ÖZ ZE ET T Kanser önemli bir insan sağlığı problemi olup, hem gelişmekte olan hem de sanayileşmiş ülkelerdeki morbidite ve mortalitenin önde gelen nedenlerinden biridir. Kanser, dünyadaki ölümlerin önde gelen ikinci nedenidir ve global olarak, 6 ölümden yaklaşık 1 tanesi kansere bağlıdır. Kolorektal kanser dünyada üçüncü en yaygın kanser ve yılda 700.000 ölümle kanserle ilgili ölümlerde dördüncü ölüm sebebi haline gelmiştir. Cinsiyete göre ise kadınlarda ikinci sı-rada (%9.2), erkeklerde üçüncü sırada (%10) görülmektedir. 1990 yılından 2012 yılına kadar her yıl 200.000 yeni vakayla kolorektal kanser görülme sıklığı artmıştır. Kolorektal kanser vakalarının çoğu Batı ülkelerinde (%55) tespit edilmektedir. Kolorektal kanserin erken evrede tespit edilmesi tedavi için önemlidir. Tarama programları ile kolorektal kansere bağlı morbidite ve mortalitenin azaltılabildiği gözlenmiştir. Tedavide gerekli durumlarda cerrahi müdahale yapı-lırken; 5-florourasil (5-FU), irinotekan, kapesitabin, oksaliplatin gibi kemoterapötikler ile setuksimab, bevasizumab, panitumumab gibi monoklonal antikorlar da kullanılmaktadır. "Trifluridin+tipirasil" kombinasyonu 15 ve 20 mg dozlarında tablet formülasyonunda, yeni bir antineoplastik ajandır. Trifluridin, timidin nükleozit analoğu ve tipirasil, timidin fosforilaz (TP) inhibitörüdür. Metastatik kolorektal kanser hastalarının tedavisi için Amerika Birleşik Devletleri, Avrupa ve Japonya'daki ulusal sağlık otoriteleri tarafından onaylanmış yeni bir oral floropirimidin tedavisidir. Bu çalışma ile metastatik kolorektal kansere karşı kullanılmak üzere yeni bir ilaç kombinasyonu olan "trifluridin+tipirasil"in yapısı, sentezi ve biyolojik etkilerinin incelenmesi amaçlanmıştır.A An na ah ht ta ar r K Ke el li im me el le er r: : Kolorektal kanser; trifluridin; tipirasil A AB BS ST TR RA AC CT T Cancer is a major human health problem and one of the principal reasons of morbidity and mortality in both developing and industrialized countries. Cancer is the second leading cause of death worldwide and globally nearly 1 in 6 deaths is due to cancer. Colorectal cancer is third most common cancer and the fourth most common cause of cancer-related death, with 700.000 deaths per year. By gender, colorectal cancer is the second most common cancer in women (9.2%) and the third in men (10%). The incidence of colorectal cancer has risen by 200.000 new cases per year from 1990 to 2012. Most cases of colorectal cancer are detected in Western countries (55%). Early detection of colorectal cancer is important for treatment. It has been observed that morbidity and mortality due to colorectal cancer can be reduced by screening programs. Surgical intervention, chemotherapeutics such as 5-fluorouracil (5-FU), irinotecan, capecitabine, oxaliplatin and monoclonal antibodies like cetuximab, bevacizumab, panitumumab are used for treatment. The combination of "Trifluridine/tipiracil" 15 and 20 mg tablets, is a new antineoplastic agent. "Trifluridine/tipiracil" is comprised of an antineoplastic thymidine-based nucleoside ana...

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Folic acid-decorated and PEGylated PLGA nanoparticles for improving the antitumour activity of 5-fluorouracil

Cited by 123 publications

References 38 publications

Anti-proliferate and apoptosis triggering potential of methotrexate-transferrin conjugate encapsulated PLGA nanoparticles with enhanced cellular uptake by high-affinity folate receptors

Anti-proliferate and apoptosis triggering potential of methotrexate-transferrin conjugate encapsulated PLGA nanoparticles with enhanced cellular uptake by high-affinity folate receptors

<p>Design, Formulation and in vivo Evaluation of Novel Honokiol-Loaded PEGylated PLGA Nanocapsules for Treatment of Breast Cancer</p>

New Drug Combination in Colorectal Cancer Treatment: Trifluridine and Tipiracil

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