Estrone-targeted liposomes for mitoxantrone delivery via estrogen receptor: In vivo targeting efficacy, antitumor activity, acute toxicity and pharmacokinetics

Tang, Huan; Chen, Jing‐Lin; Zhu, Ming; Xie, Yizhuo; Li, Yao; Hao, Qiang; Sun, Yuxin; Cong, Dengli; Qin, Meng; Ren, Zhihui; Li, Qianwen; Bao, Haikun; Lv, Zhe; Yan, Li; Pei, Jin

doi:10.1016/j.ejps.2021.105780

Cited by 7 publications

(5 citation statements)

References 46 publications

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“…Later, the in vivo study on balb/c mice manifested superior suppression in tumor growth when treated with ES-SSL-OX without inducing significant side effects. Similarly, another study by the same research team has prepared mitoxantrone (MTO) loaded PEGylated liposomes for the targeted delivery of MTO to the gastric cancer cells via ESRs [137]. The results revealed that the PEGylated liposomes enhanced the in vivo circulation time of the drug leading to reduced drug metabolism and prolonged antitumor effect.…”

Section: Liposomesmentioning

confidence: 99%

Novel Drug Delivery Systems as an Emerging Platform for Stomach Cancer Therapy

et al. 2022

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Cancer has long been regarded as one of the world’s most fatal diseases, claiming the lives of countless individuals each year. Stomach cancer is a prevalent cancer that has recently reached a high number of fatalities. It continues to be one of the most fatal cancer forms, requiring immediate attention due to its low overall survival rate. Early detection and appropriate therapy are, perhaps, of the most difficult challenges in the fight against stomach cancer. We focused on positive tactics for stomach cancer therapy in this paper, and we went over the most current advancements and progressions of nanotechnology-based systems in modern drug delivery and therapies in great detail. Recent therapeutic tactics used in nanotechnology-based delivery of drugs aim to improve cellular absorption, pharmacokinetics, and anticancer drug efficacy, allowing for more precise targeting of specific agents for effective stomach cancer treatment. The current review also provides information on ongoing research aimed at improving the curative effectiveness of existing anti-stomach cancer medicines. All these crucial matters discussed under one overarching title will be extremely useful to readers who are working on developing multi-functional nano-constructs for improved diagnosis and treatment of stomach cancer.

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Section: Liposomesmentioning

confidence: 99%

Novel Drug Delivery Systems as an Emerging Platform for Stomach Cancer Therapy

et al. 2022

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“…The formed precipitate was separated and dried to get Egen-COOH (1265.5 mg, 92% yield). 34 Conjugation of CS with Activated Egen-COOH. Carbodiimide chemistry was used for the preparation of the Egen-COOH conjugated CS (CS-g-Egen) graft polymer.…”

Section: T H I S C O N T E N T I S O N L Y L I C E N S E D F O R C O ...mentioning

confidence: 99%

Chitosan-g-estrone Nanoparticles of Palbociclib Vanished Hypoxic Breast Tumor after Targeted Delivery: Development and Ultrasound/Photoacoustic Imaging

Mehata

Singh

Vikas

et al. 2023

ACS Appl. Mater. Interfaces

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Breast cancer is the leading cause of death among women globally. Approximately 80% of all breast cancers diagnosed are overexpressed with estrogen receptors (ERs). In this study, we have developed an estrone (Egen)-grafted chitosan-based polymeric nanocarrier for the targeted delivery of palbociclib (PLB) to breast cancer. The nanoparticles (NPs) were prepared by solvent evaporation using the ionic gelation method and characterized for particle size, zeta potential, polydispersity, surface morphology, surface chemistry, drug entrapment efficiency, cytotoxicity assay, cellular uptake, and apoptosis study. The developed PLB-CS NPs and PLB-CS-g-Egen NPs had a particle size of 116.3 ± 1.53 nm and 141.6 ± 1.97 nm, respectively. The zeta potential of PLB-CS NPs and PLB-CS-g-Egen NPs was found to be 18.70 ± 0.416 mV and 12.45 ± 0.574 mV, respectively. The morphological analysis demonstrated that all NPs were spherical in shape and had a smooth surface. An in vitro cytotoxicity assay was performed in estrogen receptor (ER)-expressing MCF7 cells and T47D cells, which suggested that targeted NPs were 57.34-and 30.32-fold more cytotoxic compared to the pure PLB, respectively. Additionally, cell cycle analysis confirmed that cell cycle progression from the G1 into S phase was blocked more efficiently by targeted NPs compared to nontargeted NPs and PLB in MCF7 cells. In vivo pharmacokinetic studies demonstrated that entrapment of the PLB in the NPs improved the half-life and bioavailability by ∼2−3-fold. Further, ultrasound and photoacoustic imaging of DMBA induced breast cancer in the Sprague-Dawley (SD) rat showed that targeted NPs completely vanished breast tumor, reduced hypoxic tumor volume, and suppressed tumor angiogenesis more efficiently compared to the nontargeted NPs and free PLB. Further, in vitro hemocompatibility and histopathology studies suggested that NPs were biocompatible and safe for clinical use.

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“…The synthesis of liposomes with estrone as a targeting moiety was reported in many studies to selectively target breast cancer cells [24]- [26]. For example, estrone-targeted liposomes were used for in vivo drug delivery to the tumor site with increased circulation time and reduced side effects of the drug [27]. Also, Estradiol-Associated Stealth-Liposomes were used for the delivery of an anticancer gene to breast cancer cells [28].…”

Section: Introductionmentioning

confidence: 99%

Production of Targeted Estrone Liposomes Using a Herringbone Micromixer

Agam,

Paul,

Abdelgawad

et al. 2024

IEEE Trans.on Nanobioscience

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Liposomes are spherical vesicles formed from bilayer lipid membranes that are extensively used in targeted drug delivery as nanocarriers to deliver therapeutic reagents to specific tissues and organs in the body. Recently, we have reported using estrone as an endogenous ligand on doxorubicinencapsulating liposomes to target estrogen receptor (E.R.)-positive breast cancer cells. Estrone liposomes were synthesized using the thin-film hydration method, which is a long, arduous, and multistep process. Here, we report using a herringbone micromixer to synthesize estrone liposomes in a simple and rapid manner. A solvent stream containing the lipids was mixed with a stream of phosphate buffer saline (PBS) inside a microchannel integrated with herringbone-shaped ridges that enhanced the mixing of the two streams. The small scale involved enabled rapid solvent exchange and initiated the self-assembly of the lipids to form the required liposomes. The effect of different parameters on liposome size, such as the ratio between the flow rate of the solvent and the buffer solutions (FRR), total flow rate, lipid concentrations, and solvent type, were investigated. Using this commercially available chip, we obtained liposomes with a radius of 66.1 ± 11.2 nm (mean ± standard deviation) and a polydispersity of 22% in less than 15 minutes compared to a total of ~11 hours using conventional techniques. Calcein was encapsulated inside the prepared liposomes as a model drug and was released by applying ultrasound at different powers. The size of the prepared liposomes was stable over a period of one month. Overall, using microfluidics to synthesize Estrone-liposomes simplified the procedure considerably and improved the reproducibility of the resulting liposomes.

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Estrone-targeted liposomes for mitoxantrone delivery via estrogen receptor: In vivo targeting efficacy, antitumor activity, acute toxicity and pharmacokinetics

Cited by 7 publications

References 46 publications

Novel Drug Delivery Systems as an Emerging Platform for Stomach Cancer Therapy

Novel Drug Delivery Systems as an Emerging Platform for Stomach Cancer Therapy

Chitosan-g-estrone Nanoparticles of Palbociclib Vanished Hypoxic Breast Tumor after Targeted Delivery: Development and Ultrasound/Photoacoustic Imaging

Production of Targeted Estrone Liposomes Using a Herringbone Micromixer

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