Antitumor gemcitabine conjugated micelles from amphiphilic comb-like random copolymers

Wang, Jianfeng; Zhang, Xiaomin; Cen, Yixin; Lin, Xianfu; Wu, Qi

doi:10.1016/j.colsurfb.2016.07.027

Cited by 10 publications

(8 citation statements)

References 34 publications

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“…These PEGylated polymeric micelles had effective anticancer activities against A549 cells due to efficient internalization. In vivo studies using A549 tumor borne nude mice verified an improved antitumor efficiency of gemcitabine-containing micelles compared to free gemcitabine owing to the prevention of rapid plasma degradation of gemcitabine [93] . However, the release of parent gemcitabine was usually restricted from these gemcitabine conjugated micelles with an ester bond or amide bond.…”

Section: Nano-drug Strategies Using Nanocarriersmentioning

confidence: 90%

“…Gemcitabine could also be conjugated to the polymer to obtain gemcitabine-polymer conjugate micelle with extremely high drug loading, enabling gemcitabine to prevent rapid plasma degradation [93] , prolong cytotoxicity [94] , and enhance antitumor efficacy [95] . In a typical example, gemcitabine and PEG were grafted to comb-like amphiphilic polymers, which could further self-assemble to obtain micelles ( Fig.…”

Section: Nano-drug Strategies Using Nanocarriersmentioning

confidence: 99%

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Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy

Han

Zhong

et al. 2022

Asian Journal of Pharmaceutical Sciences

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Section: Nano-drug Strategies Using Nanocarriersmentioning

confidence: 90%

Section: Nano-drug Strategies Using Nanocarriersmentioning

confidence: 99%

Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy

Han

Zhong

et al. 2022

Asian Journal of Pharmaceutical Sciences

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“…On the structural bases, the polymers are divided into three categories that are widely utilized to synthesize polymer-drug conjugates: (i) comb-like copolymers [19]; (ii) block copolymers [20]; and (iii) dendritic copolymers [21]. These copolymers have common advantageous characteristics such as: it contains numerous functional sites on the polymer skeleton, and anticarcinogen molecules are mainly cross-linked to the polymer as branched chains to achieve high drug loading efficiency.…”

Section: Types Of Prodrug-based Nanomedicinesmentioning

confidence: 99%

Stimuli-responsive prodrug-based cancer nanomedicine

et al. 2020

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The rapid development of nanotechnology results in the emergence of nanomedicines, but the effective delivery of drugs to tumor sites remains a great challenge. Prodrug-based cancer nanomedicines thus emerged due to their unique advantages, including high drug load efficiency, reduced side effects, efficient targeting, and real-time controllability. A distinctive characteristic of prodrug-based nanomedicines is that they need to be activated by a stimulus or multi-stimulus to produce an anti-tumor effect. A better understanding of various responsive approaches could allow researchers to perceive the mechanism of prodrugbased nanomedicines effectively and further optimize their design strategy. In this review, we highlight the stimuli-responsive pathway of prodrug-based nanomedicines and their anticancer applications. Furthermore, various types of prodrug-based nanomedicines, recent progress and prospects of stimuli-responsive prodrug-based nanomedicines and patient data in the clinical application are also summarized. Additionally, the current development and future challenges of prodrug-based nanomedicines are discussed. We expect that this review will be valuable for readers to gain a deeper understanding of the structure and development of prodrug-based cancer nanomedicines to design rational and effective drugs for clinical use.

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“…Thus, various attempts have been made to deliver GEM with the aim to improve pharmacokinetics and tumor delivery of this compound for more effective chemotherapy. GEM has been studied in different polymeric systems such as magnetic poly ε-caprolactone nanoparticles [14], micelles [15], and gold nanoparticles for pancreatic cancer treatment [16]. Several liposomal formulations have also been prepared and evaluated, e.g., pH-sensitive stearoyl-PEG-poly(methacryloyl sulfadimethoxine)-coated liposomes [17] and hyaluronic acid-coated liposomes for pancreatic adenocarcinoma cells [18].…”

Section: Introductionmentioning

confidence: 99%

SYNTHESIS AND OPTIMIZATION OF GEMCITABINE-LOADED MIL-101NH2 (Fe) NANOCARRIERS: RESPONSE SURFACE METHODOLOGY APPROACH

Kush

Madan

Kumar

2019

Asian J Pharm Clin Res

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Objective: The objective of the present study is to synthesize and optimize gemcitabine (GEM)-loaded MIL-101NH2 (Fe) nanocarriers. The design of experiments is used to optimize the formulation for higher encapsulation efficiency (EE) for effective drug delivery. Materials and Methods: MIL-101NH2 (Fe) was synthesized by microwave-assisted hydrothermal method. Central composite design (CCD) under response surface methodology was used for the optimization of GEM encapsulation into the MIL-101NH2 (Fe). The most influential variable that affects the EE was investigated by Perturbation plot. Validation of the design was carried out by performing the experiments under optimal conditions. Further optimized formulation was physicochemically characterized for particle size, surface charge, and surface morphology using zetasizer and scanning electron microscopy (SEM), respectively. Structural integrity of the optimized formulation was carried out by Powder X ray crystallography (PXRD). Fourier-transform infrared (FTIR) spectroscopy was used for the confirmation of GEM loading. Accelerated storage stability analysis was also performed to find out the related parameters. Results: Here in this work, crystalline MIL-101NH2 (Fe) has been successfully synthesized by microwave radiation method. The optimization result revealed that process variables such as GEM concentration, pH, and time significantly affect the desired constraint, EE. Perturbation plot evidenced that among all the variables, pH is the most significant factor followed by drug concentration and time. The optimized formulation exhibited 76.4 ± 7% EE and average particle size of 252.9 ± 9.23 nm. PXRD and SEM results demonstrated that the optimized formulation was crystalline in nature. FTIR spectroscopy confirms the presence of drug inside the MIL-101NH2 (Fe). In vitro release profile revealed that MIL-101NH2 (Fe)-GEM exhibited the sustained release up to 72 h in comparison to the native GEM. Storage-stability studies also indicate that MIL-101NH2 (Fe)-GEM has a shelf life of 6 months. Conclusion: The EE of GEM in MIL-101NH2 (Fe) can be altered by varying the drug concentration and pH during the impregnation.

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Antitumor gemcitabine conjugated micelles from amphiphilic comb-like random copolymers

Cited by 10 publications

References 34 publications

Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy

Emerging pro-drug and nano-drug strategies for gemcitabine-based cancer therapy

Stimuli-responsive prodrug-based cancer nanomedicine

SYNTHESIS AND OPTIMIZATION OF GEMCITABINE-LOADED MIL-101NH2 (Fe) NANOCARRIERS: RESPONSE SURFACE METHODOLOGY APPROACH

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