Oral Administration of Chemotherapeutic Agents Using Complexation Hydrogels

2002 ◽  
Vol 724 ◽  
Author(s):  
James Blanchette ◽  
Kinam Park ◽  
Nicholas A Peppas
Keyword(s):  
Small Intestine ◽  
Intestinal Epithelium ◽  
Chemotherapeutic Agents ◽  
Uv Spectrophotometry ◽  
Ph Responsive ◽  
Poly Ethylene Glycol ◽  
Target Delivery ◽  
Poly Ethylene

AbstractCarriers were synthesized to target delivery of a chemotherapeutic agent, bleomycin, to the upper small intestine in response to the pH shift when entering the upper small intestine from the stomach. Complexation hydrogels capable of pH-responsive swelling were used to form these carriers. Hydrogel nanospheres composed of methacrylic acid (MAA) and poly(ethylene glycol) (PEG) were loaded with bleomycin. Loading of bleomycin was performed by in situ polymerization and release of bleomycin from the nanospheres was measured by UV spectrophotometry. Results showed that bleomycin release from the nanospheres was responsive to the pH of the environment surrounding the nanospheres. In addition to pH-responsive release of bleomycin, the hydrogel nanospheres are also able to enhance the permeability of an in vitro model of the intestinal epithelium. Increasing the permeability of the intestinal epithelium could aid in transport of bleomycin from the lumen of the small intestine out into the bloodstream.

A Tunable pH-Responsive Nanomaterials for Cancer Delivery

2013 ◽  
Vol 750-752 ◽  
pp. 1476-1479 ◽  
Author(s):  
Bin Liu ◽  
Guan Hui Gao ◽  
Peng Liu ◽  
Hu Qiang Yi ◽  
Wei Wei ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Ethylene Glycol ◽  
Potential Application ◽  
Ph Responsive ◽  
Poly Ethylene Glycol ◽  
Positive Potential ◽  
Ph Values ◽  
Drugs In Blood ◽  
Poly Ethylene

In this paper, we successfully designed a pH-responsive micelles based on hybrid polypeptide copolymers of poly (L-lysine-4-Azepan-1-yl-butyric)-b-poly (ethylene glycol)-b-poly (L-lysine-Diisopropylamide)-b-poly (L-leucine) (PLL(A)-PEG-PLL(B)-PLLeu) for efficient drug delivery. This pH-responsive nanoparticles were able to response to different pH values (pH=6.8 and 5.5). In vitro, these nanoparticles exhibited a stable and evenly distributed approximately 51 nm, a slightly positive potential about 10.3 mv at pH 7.4, which were crucial for the circulation of drugs in blood. While size and potential were about 130 nm and 34.7 mv at pH 6.8, which were good for drugs in membrane. Furthermore, the loading capability of DOX was up to 11.3%, and the pH-responsive release efficiency reached to 68.3% at pH 5.5. The results indicated that these micelles had huge potential application in cancer delivery.

A bioactive hyaluronic acid–based hydrogel cross-linked by Diels–Alder reaction for promoting neurite outgrowth of PC12 cells

2017 ◽  
Vol 32 (4) ◽  
pp. 382-396 ◽  
Author(s):  
Dongming Xing ◽  
Lie Ma ◽  
Changyou Gao
Keyword(s):  
Hyaluronic Acid ◽  
Ethylene Glycol ◽  
Neurite Outgrowth ◽  
Pc12 Cells ◽  
Alder Reaction ◽  
Poly Ethylene Glycol ◽  
Substitution Degree ◽  
Poly Ethylene

In order to improve neurite outgrowth on the in situ formed hyaluronic acid–based hydrogel, furan and methacrylate groups were grafted on hyaluronic acid successively. Furthermore, a laminin-derived peptide CQAASIKVAV was covalently immobilized via the Michael addition. The furan- and peptide-modified hyaluronic acid was then cross-linked in situ by mixing with bismaleimide poly(ethylene glycol) at 37 °C to obtain a bioactive hyaluronic acid–based hydrogel. The hyaluronic acid derivatives were characterized by 1H NMR and Fourier transform infrared spectroscopy. The gelation, swelling, and mechanical property of the hydrogels were analyzed. The modulus of the hydrogel could be tuned by changing furan substitution degree, while the peptide concentration could be changed by the ratio of furan- and peptide-modified hyaluronic acid with hyaluronic acid–furan. In vitro culture of PC12 cells showed that the longest neurite outgrowth appeared on the hyaluronic acid–poly(ethylene glycol) hydrogel with the highest peptide content (the substitution degree of peptide in furan- and peptide-modified hyaluronic acid was 23 %) and a lower threshold modulus of 4.5 kPa. The furan and methacrylate-functionalized hyaluronic acid provides a versatile platform for diverse functionalization and can be used for modulation of other cell behaviors as well.

scholarly journals Well-Defined Diblock Poly(ethylene glycol)-b-Poly(ε-caprolactone)-Based Polymer-Drug Conjugate Micelles for pH-Responsive Delivery of Doxorubicin

Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1510 ◽  
Author(s):  
Amin Jafari ◽  
Lingyue Yan ◽  
Mohamed Alaa Mohamed ◽  
Yun Wu ◽  
Chong Cheng
Keyword(s):  
Ethylene Glycol ◽  
Diblock Copolymer ◽  
Click Reaction ◽  
Ph Responsive ◽  
Poly Ethylene Glycol ◽  
Polymer Backbone ◽  
Drug Conjugate ◽  
Wide Range ◽  
Poly Ethylene

Nanoparticles have emerged as versatile carriers for various therapeutics and can potentially treat a wide range of diseases in an accurate and disease-specific manner. Polymeric biomaterials have gained tremendous attention over the past decades, owing to their tunable structure and properties. Aliphatic polyesters have appealing attributes, including biodegradability, non-toxicity, and the ability to incorporate functional groups within the polymer backbone. Such distinctive properties have rendered them as a class of highly promising biomaterials for various biomedical applications. In this article, well-defined alkyne-functionalized poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) diblock copolymer was synthesized and studied for pH-responsive delivery of doxorubicin (DOX). The alkyne-functionalized PEG-b-PCL diblock copolymer was prepared by the synthesis of an alkyne-functionalized ε-caprolactone (CL), followed by ring-opening polymerization (ROP) using PEG as the macroinitiator. The alkyne functionalities of PEG-b-PCL were modified through copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) click reaction to graft aldehyde (ALD) groups and obtain PEG-b-PCL-g-ALD. Subsequently, DOX was conjugated on PEG-b-PCL-g-ALD through the Schiff base reaction. The resulting PEG-b-PCL-g-DOX polymer-drug conjugate (PDC) self-assembled into a nano-sized micellar structure with facilitated DOX release in acidic pH due to the pH-responsive linkage. The nanostructures of PDC micelles were characterized using transmission electron microscopy (TEM) and dynamic light scattering (DLS). In vitro studies of the PDC micelles, revealed their improved anticancer efficiency towards MCF-7 cells as compared to free DOX.

In vitro and in vivo protein delivery from in situ forming poly(ethylene glycol)–poly(lactide) hydrogels

2007 ◽  
Vol 119 (3) ◽  
pp. 320-327 ◽  
Author(s):  
Christine Hiemstra ◽  
Zhiyuan Zhong ◽  
Sophie R. Van Tomme ◽  
Mies J. van Steenbergen ◽  
John J.L. Jacobs ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Protein Delivery ◽  
Poly Ethylene Glycol ◽  
In Situ Forming ◽  
Poly Ethylene

scholarly journals Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 605
Author(s):  
Marie-Emérentienne Cagnon ◽  
Silvio Curia ◽  
Juliette Serindoux ◽  
Jean-Manuel Cros ◽  
Feifei Ng ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Surface Erosion ◽  
Sustained Delivery ◽  
Trimethylene Carbonate ◽  
Poly Ethylene Glycol ◽  
In Situ Forming ◽  
Poly Ethylene ◽  
Long Acting

This article describes the utilization of (methoxy)poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) ((m)PEG–PTMC) diblock and triblock copolymers for the formulation of in situ forming depot long-acting injectables by solvent exchange. The results shown in this manuscript demonstrate that it is possible to achieve long-term drug deliveries from suspension formulations prepared with these copolymers, with release durations up to several months in vitro. The utilization of copolymers with different PEG and PTMC molecular weights affords to modulate the release profile and duration. A pharmacokinetic study in rats with meloxicam confirmed the feasibility of achieving at least 28 days of sustained delivery by using this technology while showing good local tolerability in the subcutaneous environment. The characterization of the depots at the end of the in vivo study suggests that the rapid phase exchange upon administration and the surface erosion of the resulting depots are driving the delivery kinetics from suspension formulations. Due to the widely accepted utilization of meloxicam as an analgesic drug for animal care, the results shown in this article are of special interest for the development of veterinary products aiming at a very long-term sustained delivery of this therapeutic molecule.

scholarly journals Bio-based polyurethane nanocomposite thin coatings from two comparable POSS with eight same vertex groups for controlled release urea

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Lixia Li ◽  
Meng Wang ◽  
Xiandong Wu ◽  
Wenping Yi ◽  
Qiang Xiao
Keyword(s):  
In Situ Polymerization ◽  
Polyhedral Oligomeric Silsesquioxanes ◽  
Poly Ethylene Glycol ◽  
Thin Coatings ◽  
Polyurethane Coatings ◽  
Coated Urea ◽  
Poly Ethylene ◽  
Coated Fertilizer ◽  
Polyurethane Matrix

AbstractNanocomposite modification has attracted much attention in improving properties of bio-based polymer coating material for coated fertilizer. Herein two comparable polyhedral oligomeric silsesquioxanes (POSS), with eight poly(ethylene glycol) (PEG) and octaphenyl groups attached to the cage, respectively, were successfully incorporated into thin castor oil-based polyurethane coatings via in-situ polymerization on the urea surface. The nanostructure coatings are environmentally friendly, easy to prepare, and property-tunable. The results show that the vertex group of POSS had a pronounced influence on dispersion level and interaction between polyurethane and POSS that well-tuned the release pattern and period of coated urea, even at the coating rate as low as of 2 wt%. The liquid POSS with long and flexible PEG groups had better compatibility and dispersibility in polyurethane matrix than the solid POSS with rigid octaphenyl groups, as evidenced by SEM/EDS. The unique properties were resulted from the different extents of physical crosslinkings. This modification of bio-based polyurethane coating with POSS provided an alternative method of regulating and controlling the properties of coated fertilizer.

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