scholarly journals Poly(ethylene glycol)-poly(ε-caprolactone)-based micelles for solubilization and tumor-targeted delivery of silibinin

Bioimpacts ◽  
2019 ◽  
Vol 10 (2) ◽  
pp. 87-95 ◽  
Author(s):  
Ashkan Hassankhani Rad ◽  
Farshid Asiaee ◽  
Sevda Jafari ◽  
Ali Shayanfar ◽  
Afsaneh Lavasanifar ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Targeted Delivery ◽  
Water Solubility ◽  
Polymeric Micelles ◽  
Inhibitory Effect ◽  
Water Soluble ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
The One ◽  
Dialysis Bag

Introduction: Silibinin is a naturally occurring compound with known positive impacts on prevention and treatment of many types of human illnesses in general and cancer in particular. Silibinin is poorly water soluble which results in its insufficient bioavailability and lack of therapeutic efficacy in cancer. Here, we proposed to examine the potential of micelles composed of poly(ethylene glycol) (PEG) as the hydrophilic block and poly(ε-caprolactone) (PCL), poly(α-benzylcarboxylate-ε-caprolactone) (PBCL), or poly(lactide)-(PBCL) (PLA-PBCL) as hydrophobic blocks for enhancing the water solubility of silibinin and its targeted delivery to tumor. Methods: Co-solvent evaporation method was used to incorporate silibinin into PEG-PCL based micelles. Drug release profiles were assessed using dialysis bag method. MTT assay also was used to analyze functional activity of drug delivery in B16 melanoma cells. Results: Silibinin encapsulated micelles were shown to be less than 60 nm in size. Among different structures under study, the one with PEG-PBCL could incorporate silibinin with the highest encapsulation efficiency being 95.5%, on average. PEG-PBCL micelles could solubilize 1 mg silibinin in 1 mL water while the soluble amount of silibinin was found to be 0.092 mg/mL in the absence of polymeric micelles. PEG-PBCL micelles provided the sustained release of silibinin indicated with less than 30% release of silibinin within 24 hours. Silibinin encapsulated in PEG-PBCL micelles resulted in growth inhibitory effect in B16 cancer cells which was significantly higher than what observed with free drug. Conclusion: Our findings showed that PEG-PBCL micellar nanocarriers can be a useful vehicle for solubilization and targeted delivery of silibinin.

Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice

2019 ◽  
Vol 14 (3) ◽  
pp. 280-291 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Farshid Hassanzadeh ◽  
Batool Hashemi-Beni ◽  
Mohsen Minaiyan ◽  
Saeedeh Enteshari
Keyword(s):  
Side Effects ◽  
Antitumor Activity ◽  
Ethylene Glycol ◽  
Tissue Distribution ◽  
Tumor Cells ◽  
Maleic Acid ◽  
Polymeric Micelles ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ether Ester

Background: Due to the low water solubility of Docetaxel (DTX), it is formulated with ethanol and Tween 80 with lots of side effects. For this reason, special attention has been paid to formulate it in new drug nano-carriers. Objective: The goal of this study was to evaluate the safety, antitumor activity and tissue distribution of the novel synthesized Raloxifene (RA) targeted polymeric micelles. Methods: DTX-loaded RA-targeted polymeric micelles composed of poly(styrene-maleic acid)- poly(amide-ether-ester-imide)-poly(ethylene glycol) (SMA-PAEE-PEG) were prepared and their antitumor activity was studied in MC4-L2 tumor-bearing mice compared with non-targeted micelles and free DTX. Safety of the micelles was studied by Hematoxylin and Eosin (H&E) staining of tumors and major organs of the mice. The drug accumulation in the tumor and major organs was measured by HPLC method. Results: The results showed better tumor growth inhibition and increased survival of mice treated with DTX-loaded in targeted micelles compared to the non-targeted micelles and free DTX. Histopathological studies, H&E staining of tumors and immunohistochemical examination showed the potential of DTX-loaded RA-targeted micelles to inhibit tumor cells proliferation. The higher accumulation of the DTX in the tumor tissue after injection of the micelles compared to the free DTX may indicate the higher uptake of the targeted micelles by the G-Protein-Coupled Estrogen Receptors (GPER). Conclusion: The results indicate that RA-conjugated polymeric micelles may be a strong and effective drug delivery system for DTX therapy and uptake of the drug into tumor cells, and overcome the disadvantages and side effects of conventional DTX.

Water-soluble polyesters from long chain alkylesters of citric acid and poly(ethylene glycol)

2007 ◽  
Vol 43 (4) ◽  
pp. 1288-1301 ◽  
Author(s):  
Fabienne Barroso-Bujans ◽  
Ricardo Martínez ◽  
Mehrdad Yazdani-Pedram ◽  
Pedro Ortiz ◽  
Holger Frey
Keyword(s):  
Citric Acid ◽  
Ethylene Glycol ◽  
Water Soluble ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Long Chain

Tracing the transport of organic colloids in porous media using tailored poly(ethylene glycol)

2021 ◽  
Author(s):  
Thomas Ritschel ◽  
Katharina Lehmann ◽  
Michaela Brunzel ◽  
Jürgen Vitz ◽  
Ivo Nischang ◽  
...  
Keyword(s):  
Porous Media ◽  
Ethylene Glycol ◽  
Water Solubility ◽  
Size Range ◽  
Large Fraction ◽  
Colloid Interface ◽  
Poly Ethylene Glycol ◽  
Polymer Backbone ◽  
Colloidal Transport ◽  
Poly Ethylene

<p>A large fraction of organic matter in natural aqueous soil solutions is given by molecules in sizes above one nanometer, which classifies them as colloids according to the IUPAC definition. Such colloids feature discernable mobility in soils and their transport is decisive for the cycling of carbon as well as the migration of nutrients or contaminants. Yet, their size-dependent hydrodynamics and functional diversity result in transport phenomena that are specific to colloids and, thus, largely differ from those observed for smaller substances. Still, tracers that appropriately represent small organic colloids are not available and the investigation of their transport in laboratory column experiments, in dependence of size and chemistry, remains difficult. To overcome this limitation, we tested if well-defined synthetic polymers in the colloidal size range are suitable as non-conventional tracers of colloidal transport. As polymer backbone, we selected poly(ethylene glycol) (PEG) due to its high water-solubility and established pathway of synthesis that permits tailoring of functional moieties to the fullest extent. An easy and sensitive detection in the aqueous phase became possible by using a fluorophore as starting group. After full characterization, we studied PEG adsorption to quartz, illite, goethite, and their mixtures in batch and column transport experiments. In numerical simulations, we successfully reconstructed and predicted PEG transport based on its physicochemical as well as hydrodynamic properties and, thus, show that PEG transport can be comprehensively and quantitatively studied. Considering also its low adverse effect on the environment, functional PEG therefore presents as promising candidate to be used as organic tracer, designable in the size range of natural organic (macro-)molecules (Ritschel et al., 2021).</p><p>References</p><p>Ritschel, T., Lehmann, K., Brunzel, M., Vitz, J., Nischang, I., Schubert, U., Totsche, K. U. (2021) <strong>Well-defined poly(ethylene glycol) polymers as non-conventional reactive tracers of colloidal transport in porous media</strong>.<em> J. Colloid Interface Sci.</em> 548, 592-601, doi: 10.1016/j.jcis.2020.09.056.</p>

scholarly journals The Importance of Poly(ethylene glycol) and Lipid Structure in Targeted Gene Delivery to Lymph Nodes by Lipid Nanoparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1068 ◽  
Author(s):  
Danijela Zukancic ◽  
Estelle J. A. Suys ◽  
Emily H. Pilkington ◽  
Azizah Algarni ◽  
Hareth Al-Wassiti ◽  
...  
Keyword(s):  
Lymph Node ◽  
Gene Delivery ◽  
Ethylene Glycol ◽  
Lymph Nodes ◽  
Injection Site ◽  
Targeted Delivery ◽  
Lipid Nanoparticles ◽  
Tween 20 ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene

Targeted delivery of nucleic acids to lymph nodes is critical for the development of effective vaccines and immunotherapies. However, it remains challenging to achieve selective lymph node delivery. Current gene delivery systems target mainly to the liver and typically exhibit off-target transfection at various tissues. Here we report novel lipid nanoparticles (LNPs) that can deliver plasmid DNA (pDNA) to a draining lymph node, thereby significantly enhancing transfection at this target organ, and substantially reducing gene expression at the intramuscular injection site (muscle). In particular, we discovered that LNPs stabilized by 3% Tween 20, a surfactant with a branched poly(ethylene glycol) (PEG) chain linking to a short lipid tail, achieved highly specific transfection at the lymph node. This was in contrast to conventional LNPs stabilized with a linear PEG chain and two saturated lipid tails (PEG-DSPE) that predominately transfected at the injection site (muscle). Interestingly, replacing Tween 20 with Tween 80, which has a longer unsaturated lipid tail, led to a much lower transfection efficiency. Our work demonstrates the importance of PEGylation in selective organ targeting of nanoparticles, provides new insights into the structure–property relationship of LNPs, and offers a novel, simple, and practical PEGylation technology to prepare the next generation of safe and effective vaccines against viruses or tumours.

Sign in / Sign up

Export Citation Format

Share Document