Hybrid bicelles as a pH-sensitive nanocarrier for hydrophobic drug delivery

RSC Advances ◽  
2016 ◽  
Vol 6 (83) ◽  
pp. 79811-79821 ◽  
Author(s):  
Li Lin ◽  
Xiaoyou Wang ◽  
Yanyu Guo ◽  
Kuan Ren ◽  
Xiaoda Li ◽  
...  

Stabilized disc-like hybrid bicelles provide pH-sensitive release, preferable cellular uptake, tumor accumulation and therapeutic effect in vitro and in vivo.

2020 ◽  
Author(s):  
Ye Yuan ◽  
Jia-Xing Song ◽  
Mei-Na Zhang ◽  
Baoshan Yuan

Abstract Present study was planned for the development of pH sensitive lipid polymer hybrid nanoparticles (pHS-LPHNPs) loaded with docetaxel (DTX) for guided and target specific cytosolic-delivery delivery of docetaxel (DTX). pHS-LPHNPs were formulated to entrap DTX by self-assembled nano-precipitation technique and characterised with respect to zeta potential, particle-size, entrapment efficiency, PDI as well as invitro drug release. The cell viability, apoptosis, cellular-uptake, pharmacokinetics, bio-distribution in vital organs, % changes in tumour volume and survival of breast cancer bearing animals were used for the evaluation of efficacy of the formulation. In-vitro studies showed increased cytotoxicity at lower IC50 and better cellular-uptake of pHS-LPHNPs mediated drug by breast cancer cell lines. We saw the better rate of apoptosis of breast cancer cells via Annexin V/Propidium iodide staining. Moreover, in-vivo studies demonstrated improved pharmacokinetics and targetability with minimum drug circulation in deep-seated organs upon delivery of DTX via pHS-LPHNPs in comparison with LPHNPs-DTX and free DTX. We observed sizeable % reduction in tumour-burden with pHS-LPHNPs-DTXthan that withLPHNPs-DTX &free DTX. In brief, pHS-LPHNPs mediated delivery of DTX exhibited promising approach for developing therapeutic-interventions against breast-cancer.


2016 ◽  
Vol 31 (4) ◽  
pp. 568-581 ◽  
Author(s):  
Huijuan Zhang ◽  
Yandan Ji ◽  
Qianqian Chen ◽  
Xing Zhu ◽  
Xiaoge Zhang ◽  
...  

Author(s):  
Antony Thomas ◽  
Paige Baldwin ◽  
Yaling Liu

Ultrasound in the presence of microbubbles brings in transient increase in cell membrane permeability, which allows the entry of foreign molecules into cells. This platform has been applied in in vitro and in vivo gene delivery studies in recent years[1–2]. The frequently used microbubbles are air or inert gas encapsulated in a protein, lipid or polymer which is commonly used as FDA approved contrast agents in diagnostic ultrasound. On exposure to ultrasound the microbubbles lead to formation of small pores on the cell membrane. This work concentrates on application of this platform to enhance cellular uptake of nanoparticles and thereby achieve enhanced drug delivery. Nanoparticles can be manipulated at the nano level and have been applied in the realm of cancer detection and treatment for imaging, targeting tumors, and drug delivery purposes [2].


Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1833 ◽  
Author(s):  
Kyoung-Ran Kim ◽  
Pascal Röthlisberger ◽  
Seong Kang ◽  
Kihwan Nam ◽  
Sangyoup Lee ◽  
...  

Rolling circle amplification (RCA) is a robust way to generate DNA constructs, which are promising materials for biomedical applications including drug delivery because of their high biocompatibility. To be employed as a drug delivery platform, however, the DNA materials produced by RCA need to be shaped into nanoparticles that display both high cellular uptake efficiency and nuclease resistance. Here, we showed that the DNA nanoparticles (DNPs) can be prepared with RCA and modified nucleotides that have side-chains appended on the nucleobase are capable of interacting with the DNA strands of the resulting RCA products. The incorporation of the modified nucleotides improved cellular uptake efficiency and nuclease resistance of the DNPs. We also demonstrated that these DNPs could be employed as carriers for the delivery of a photosensitizer into cancer cells to achieve photodynamic therapy upon irradiation at both the in vitro and in vivo levels.


2020 ◽  
Vol 15 (4) ◽  
pp. 341-359
Author(s):  
Moloud Kazemi ◽  
Jaber Emami ◽  
Farshid Hasanzadeh ◽  
Mohsen Minaiyan ◽  
Mina Mirian ◽  
...  

Background: The development of biocompatible tumor-targeting delivery systems for anticancer agents is essential for efficacious cancer chemotherapy. Nanoparticles, as drug delivery cargoes for cancer therapy, are rapidly improving to overcome the limitations of conventional chemotherapeutic agents. Heparin–modified nanoparticles are currently being considered as one of the favorable carriers for the delivery of chemotherapeutics to cancer tissues. Objective: This study was aimed at evaluating the in vitro and in vivo antitumor activity of a novel targeted, pH-sensitive, heparin-based polymeric micelle loaded with the poorly water-soluble anticancer drug, docetaxel (DTX). The micelles could overcome the limited water solubility, non-specific distribution, and insufficient drug concentration in tumor tissues. Methods: DTX-loaded folate targeted micelles were prepared and evaluated for physicochemical properties, drug release, in vitro cellular uptake and cytotoxicity in folate receptor-positive and folate receptor-negative cells. Furthermore, the antitumor activity of DTX-loaded micelles was evaluated in the tumor-bearing mice. Some related patents were also studied in this research. Results: The heparin-based targeted micelles exhibited higher in vitro cellular uptake and cytotoxicity against folate receptor over-expressed cells due to the specific receptor-mediated endocytosis. DTX-loaded micelles displayed greater antitumor activity, higher anti-angiogenesis effects, and lower systemic toxicity compared with free DTX in a tumor-induced mice model as confirmed by tumor growth monitoring, immunohistochemical evaluation, and body weight shift. DTX-loaded targeting micelles demonstrated no considerable toxicity on major organs of tumor-bearing mice compared with free DTX. Conclusion: Our results indicated that DTX-loaded multifunctional heparin-based micelles with desirable antitumor activity and low toxicity possess great potential as a targeted drug delivery system in the treatment of cancer.


2010 ◽  
Vol 13 (2) ◽  
pp. 721-731 ◽  
Author(s):  
ChangYang Gong ◽  
YuJun Wang ◽  
XiuHong Wang ◽  
XiaWei Wei ◽  
QinJie Wu ◽  
...  

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 23022-23033 ◽  
Author(s):  
Jinyan Lin ◽  
Yang Li ◽  
Hongjie Wu ◽  
Xiangrui Yang ◽  
Yanxiu Li ◽  
...  

Polymer–lipid hybrid micelles co-delivered hydrophilic mitomycin C and hydrophobic 10-hydroxycamptothecin showed improved cellular uptake and cytotoxicity in vitro and enhanced tumor accumulation and antitumor activity in vivo.


Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5649
Author(s):  
Shijie Zhuo ◽  
Feng Zhang ◽  
Junyu Yu ◽  
Xican Zhang ◽  
Guangbao Yang ◽  
...  

The development of precise and personalized medicine requires novel formulation strategies to deliver the therapeutic payloads to the pathological tissues, producing enhanced therapeutic outcome and reduced side effects. As many diseased tissues are feathered with acidic characteristics microenvironment, pH-sensitive biomaterials for drug delivery present great promise for the purpose, which could protect the therapeutic payloads from metabolism and degradation during in vivo circulation and exhibit responsive release of the therapeutics triggered by the acidic pathological tissues, especially for cancer treatment. In the past decades, many methodologies, such as acidic cleavage linkage, have been applied for fabrication of pH-responsive materials for both in vitro and in vivo applications. In this review, we will summarize some pH-sensitive drug delivery system for medical application, mainly focusing on the pH-sensitive linkage bonds and pH-sensitive biomaterials.


2016 ◽  
Vol 45 (12) ◽  
pp. 5101-5110 ◽  
Author(s):  
Huiting Bi ◽  
Yunlu Dai ◽  
Ruichan Lv ◽  
Chongna Zhong ◽  
Fei He ◽  
...  

A CuS–DOX NP drug delivery system was synthesized by conjugating carboxyl-functionalized copper sulfide nanoparticles (CuS NPs) and DOX through hydrazone bonds. The platform exhibits high in vitro and in vivo anti-cancer efficacy due to the combined chemo- and photothermal therapeutic effect upon 808 nm laser irradiation.


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