Heparin–deoxycholic acid chemical conjugate as an anticancer drug carrier and its antitumor activity

Park, Kyeongsoon; Lee, Gee Young; Kim, Yoo Shin; Yu, Mikyung; Park, Rang Woon; Kim, In San; Kim, Sang Yoon; Byun, Youngro

doi:10.1016/j.jconrel.2006.05.017

Cited by 150 publications

(108 citation statements)

References 24 publications

Supporting

Mentioning

104

Contrasting

Order By: Relevance

“…They can be defined as biodegradable colloidal systems that include spherical nano-sized polymeric particles, where cytotoxic drugs can be encapsulated or physically entrapped within a polymeric matrix (nanospheres) or entrapped into a cavity surrounded by a polymeric membrane (nanocapsules), being also possible the conjugation of the anticancer drug to the surface or the core of the particles [198,400]. In the case of insoluble drugs, it is possible to produce a hydrophobic interaction between the drug and the core of the particle, increasing its solubility [401]. When a drug is conjugated to the particle, the properties of the linkers play a crucial role in the pharmacological properties of the complex, for example, they can make them stable in the bloodstream at pH=7 and be decomposed at pH=5.5, the typical pH in tumors, or be stable in blood, but be cleaved by lysosomal enzymes in the tumors [402].…”

Section: Polymeric Nanocarriersmentioning

confidence: 99%

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

Pérez-Herrero

Fernández‐Medarde

2015

European Journal of Pharmaceutics and Biopharmaceutics

1,465

754

View full text Add to dashboard Cite

Cancer is the second worldwide cause of death, exceeded only by cardiovascular diseases. It is characterized by uncontrolled cell proliferation and an absence of cell death that, except for hematological cancers, generates an abnormal cell mass or tumor. This primary tumor grows thanks to new vasculatization and, in time, adquires metastatic potential and spreads to other body sites, which causes metastasis and finally death. Cancer is caused by damage or mutations in the genetic material of the cells due to environmental or inherited factors. While surgery and radiotherapy are the primary treatment used for local and non-metastatic cancers, anti-cancer drugs (chemotherapy, hormone and biological therapies) are the choice currently used in metastasic cancers. Chemotherapy is based on the inhibition of the division of rapidly growing cells, which is a characteristic of the cancerous cells, but unfortunately, it also affects normal cells with fast proliferation rates, like the hair follicles, bone marrow and gastrointestinal tract cells, generating the characteristic side effects of chemotherapy. The indiscriminate destruction of normal cells, the toxicity of conventional chemotherapeutic Código de campo cambiado

show abstract

Section: Polymeric Nanocarriersmentioning

confidence: 99%

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

Pérez-Herrero

Fernández‐Medarde

2015

European Journal of Pharmaceutics and Biopharmaceutics

1,465

754

View full text Add to dashboard Cite

show abstract

“…[35][36][37] In this study, SA (an aminated fatty acid) was conjugated to LMWH to produce an amphiphilic polymer, which is to form the self-assembled nanoparticles in aqueous environment ( Figure 1A). As shown in Figure 1B, the amine group of SA was covalently coupled to the carboxylic group of LMWH in the presence of EDC and NHS, thus producing amphiphilic LHSA conjugates.…”

Section: Synthesis and Characterization Of Lhsa Conjugatesmentioning

confidence: 99%

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Kim¹,

Termsarasab²,

Cho³

et al. 2014

IJN

View full text Add to dashboard Cite

Low-molecular-weight heparin (LMWH)–stearylamine (SA) conjugates (LHSA)-based self-assembled nanoparticles were prepared for intravenous delivery of docetaxel (DCT). 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide and N -hydroxysuccinimide were used as coupling agents for synthesis of LHSA conjugates. The physicochemical properties, in vitro antitumor efficacy, in vitro cellular uptake efficiency, in vivo antitumor efficacy, and in vivo pharmacokinetics of LHSA nanoparticles were investigated. The LHSA nanoparticles exhibited a spherical shape with a mean diameter of 140–180 nm and a negative surface charge. According to in vitro release and in vivo pharmacokinetic test results, the docetaxel-loaded LHSA5 (LMWH:SA =1:5) nanoparticles exhibited sustained drug release profiles. The blank LHSA nanoparticles demonstrated only an insignificant cytotoxicity in MCF-7 and MDAMB 231 human breast cancer cells; additionally, higher cellular uptake of coumarin 6 (C6) in MCF-7 and MDAMB 231 cells was observed in the LHSA5 nanoparticles group than that in the C6 solution group. The in vivo tumor growth inhibition efficacy of docetaxel-loaded LHSA5 nanoparticles was also significantly higher than the Taxotere ® -treated group in the MDAMB 231 tumor-xenografted mouse model. These results indicated that the LHSA5-based nanoparticles could be a promising anticancer drug delivery system.

show abstract

“…Dispersed nanoparticles in a film DOCA (HD) dispersed in polyurethane Heparin [63] In vitro, Release of drugs into endothelial cell (HUVEC) In vivo, Anti-proliferative effects on old male C3H/HeN mice Nanoparticles PLGA-NP Cyclosporine [64] In vitro, Release of drug into heparinized blood from SD rats. In vivo, Effect of drug in male SD rats.…”

Section: In Vivo Anticoagulant Effect In Rabbitmentioning

confidence: 99%

Functionalized Polymers for Enhance Oral Bioavailability of Sensitive Molecules

et al. 2016

View full text Add to dashboard Cite

Currently, many sensitive molecules have been studied for effective oral administration. These substances are biologically active compounds that mainly suffer early degradation in the gastrointestinal tract (GIT) and physicochemical instability, inactivation and poor solubility and permeability. The sensibility of the biomolecules has limited their oral administration in the body and today is an important research topic to achieve desired effects in medicine field. Under this perspective, various enhancement approaches have been studied as alternatives to increase their oral bioavailability. Some of these strategies include functionalized polymers to provide specific useful benefits as protection to the intestinal tract by preventing its degradation by stomach enzymes, to increase their absorption, permeability, stability, and to make a proper release in the GIT. Due to specific chemical groups, shapes and sizes, morphologies, mechanical properties, and degradation, recent advances in functionalized polymers have opened the door to great possibilities to improve the physicochemical characteristics of these biopharmaceuticals. Today, many biomolecules are found in basic studies, preclinical steps, and others are late stage clinical development. This review summarizes the contribution of functionalized polymers to enhance oral bioavailability of sensitive molecules and their application status in medicine for different diseases. Future trends of these polymers and their possible uses to achieve different formulation goals for oral delivery are also covered in this manuscript.

show abstract

Heparin–deoxycholic acid chemical conjugate as an anticancer drug carrier and its antitumor activity

Cited by 150 publications

References 24 publications

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Functionalized Polymers for Enhance Oral Bioavailability of Sensitive Molecules

Contact Info

Product

Resources

About