Prodrug Strategies for Paclitaxel

Meng, Ziyuan; Lv, Quanxia; Lü, Jun; Yao, Houzong; Lv, Xiaoqing; Jiang, Feng; Lu, Aiping; Zhang, Ge

doi:10.3390/ijms17050796

Cited by 77 publications

(67 citation statements)

References 140 publications

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“…On the other hand, the OH group at C-2 is binding site between paclitaxel and microtubules. Although C-7 to C-10 do not interacted directly, but affects the affinity of Pglycoprotein [11].…”

Section: Mechanism Of Paclitaxel Kill Cancermentioning

confidence: 95%

“…CELLS Paclitaxel has a rigid center ring and flexible side chains [11]. Paclitaxel put to death cancer cells by inhibiting chromosomes separation on metaphase [12].…”

Section: Mechanism Of Paclitaxel Kill Cancermentioning

confidence: 99%

“…2. [11,16] Based on Structure activities relationships OH group at C-1 and C-2 benzoloksi are vital groups on anticancer activity of paclitaxel. Additionally,the Flexible of C-2 and C-3 also affect paclitaxel activity.…”

Section: Mechanism Of Paclitaxel Kill Cancermentioning

confidence: 99%

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The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

Nahrowi

Setiawan

Noviany

et al. 2019

JESR

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Paclitaxel is one of the cancer drugs that often used. These drug kills cancer cells byinhibiting mitotic cycle. The efficiency of paclitaxel is increased by the use ofnanomaterials as a carrier of paclitaxel. Nanomaterials can enhance encapsulationefficiency, improve the drug release to the target cell following nanomaterialdegradation, and improve local accumulation of drug in the cell through endocytosisreceptor. Nanomaterial that often used forencapsulation of paclitaxel is a polymerderived from natural resources such as cellulose. The advantages of cellulose as acarrier of paclitaxel are nontoxic, biodegradable, and very abundant from varioussources. One of the potential sources of cellulose for drug delivery system is cassavabaggase.Keywords: Paclitaxel, encapsulation, cell viability, nanocellulose

show abstract

Section: Mechanism Of Paclitaxel Kill Cancermentioning

confidence: 95%

“…CELLS Paclitaxel has a rigid center ring and flexible side chains [11]. Paclitaxel put to death cancer cells by inhibiting chromosomes separation on metaphase [12].…”

Section: Mechanism Of Paclitaxel Kill Cancermentioning

confidence: 99%

See 1 more Smart Citation

The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

Nahrowi

Setiawan

Noviany

et al. 2019

JESR

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“…Recently, many new drug delivery platforms for PTX, including prodrugs, 11 liposomes, 12 solid lipid nanoparticles 13 and polymeric micelles, 14 have emerged to circumvent the drawbacks of PTX. Polymeric micelles have been regarded as an effective nanoplatform because of their ability to encapsulate hydrophobic agents into their "coreshell" structure and deliver these agents to tumor regions by the enhanced permeability and retention (EPR) effect.…”

Section: Introductionmentioning

confidence: 99%

<p>Dual Receptor-Targeted and Redox-Sensitive Polymeric Micelles Self-Assembled from a Folic Acid-Hyaluronic Acid-SS-Vitamin E Succinate Polymer for Precise Cancer Therapy</p>

Yang¹,

Li²,

Chen³

et al. 2020

IJN

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Poor site-specific delivery and insufficient intracellular drug release in tumors are inherent disadvantages to successful chemotherapy. In this study, an extraordinary polymeric micelle nanoplatform was designed for the efficient delivery of paclitaxel (PTX) by combining dual receptor-mediated active targeting and stimuli response to intracellular reduction potential. Methods: The dual-targeted redox-sensitive polymer, folic acid-hyaluronic acid-SS-vitamin E succinate (FHSV), was synthesized via an amidation reaction and characterized by 1 H-NMR. Then, PTX-loaded FHSV micelles (PTX/FHSV) were prepared by a dialysis method. The physiochemical properties of the micelles were explored. Moreover, in vitro cytological experiments and in vivo animal studies were carried out to evaluate the antitumor efficacy of polymeric micelles. Results: The PTX/FHSV micelles exhibited a uniform, near-spherical morphology (148.8 ± 1.4 nm) and a high drug loading capacity (11.28% ± 0.25). Triggered by the high concentration of glutathione, PTX/FHSV micelles could quickly release their loaded drug into the release medium. The in vitro cytological evaluations showed that, compared with Taxol or single receptor-targeted micelles, FHSV micelles yielded higher cellular uptake by the dual receptor-mediated endocytosis pathway, thus leading to significantly superior cytotoxicity and apoptosis in tumor cells but less cytotoxicity in normal cells. More importantly, in the in vivo antitumor experiments, PTX/FHSV micelles exhibited enhanced tumor accumulation and produced remarkable tumor growth inhibition with minimal systemic toxicity. Conclusion: Our results suggest that this well-designed FHSV polymer has promising potential for use as a vehicle of chemotherapeutic drugs for precise cancer therapy.

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“…2 However, their use is limited by toxicity, including hypersensitivity reactions and peripheral neuropathy, 3 their extremely poor water solubility (0.3 µg/mL) that requires the use of toxic solvents, eg, Cremophor EL/ethanol ® , and the need of relatively high doses to provide therapeutic effects. 3,4 Advanced drug delivery systems (DDSs), such as nanoparticles (NPs), may help overcoming pharmacokinetic and pharmacodynamic limitations of anticancer drugs. 4 Different preparation procedures have been proposed for keratin NPs (KER-NPs) synthesis.…”

Section: Introductionmentioning

confidence: 99%

Anticancer activity of paclitaxel-loaded keratin nanoparticles in two-dimensional and perfused three-dimensional breast cancer models

Foglietta¹,

Spagnoli²,

Muraro³

et al. 2018

IJN

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PurposeTaxanes are highly effective cytotoxic drugs for progressing breast cancer treatment. However, their poor solubility and high toxicity urge the development of innovative formulations of potential clinical relevance.Materials and methodsBy using a simple and straightforward aggregation method, we have generated paclitaxel (PTX) loaded in keratin nanoparticles (KER-NPs-PTX). Their activities were tested against human breast cancer MCF-7 and MDA MB 231 cell lines in conventional two-dimensional (2D) cultures and in a dynamic three-dimensional (3D) model with perfused bioreactor (p3D). Moreover, KER-NPs-PTX activity was compared to free PTX and to PTX loaded in albumin nanoparticles (HSA-NPs-PTX). Cell viability, induction of apoptosis, and gene expression analysis were used as readouts.ResultsIn 2D cultures, KER-NPs-PTX was able to inhibit tumor cell viability and to induce apoptosis similarly to PTX and HSA-NPs-PTX. In the p3D model, a lower sensitivity of tumor cells to treatments was observed. Importantly, only KER-NPs-PTX was able to induce a statistically significant increase in apoptotic cell percentages following 24 h treatment for MCF-7 (16.7±4.0 early and 11.3±4.9 late apoptotic cells) and 48 h treatment for MDA MB 231 (21.3±11.2 early and 10.5±1.8 late apoptotic cells) cells. These effects were supported, at least for MCF-7 cells, by significant increases in the expression of proapoptotic BAX gene (5.8±0.5) 24 h after treatment and of cleaved caspase 3 (CC3) protein.ConclusionKER-NPs-PTX, generated by a simple procedure, is characterized by high water solubility and enhanced PTX-loading ability, as compared to HSA-NPs-PTX. Most importantly, it appears to be able to exert effective anticancer activities on breast cancer cells cultured in 2D or in p3D models.

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Prodrug Strategies for Paclitaxel

Cited by 77 publications

References 140 publications

The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

The Improvement of Paclitaxel Cytotoxicity using Nanocellulose based Nature Resources

<p>Dual Receptor-Targeted and Redox-Sensitive Polymeric Micelles Self-Assembled from a Folic Acid-Hyaluronic Acid-SS-Vitamin E Succinate Polymer for Precise Cancer Therapy</p>

Anticancer activity of paclitaxel-loaded keratin nanoparticles in two-dimensional and perfused three-dimensional breast cancer models

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