Enzymatically Degradable Synthetic Polymers

1995 ◽  
Vol 394 ◽  
Author(s):  
Wen Shao ◽  
Kam W. Leong
Keyword(s):  
Interfacial Polymerization ◽  
Controlled Drug Delivery ◽  
Gel Permeation Chromatography ◽  
Synthetic Polymers ◽  
Complex Coacervation ◽  
Terephthaloyl Chloride ◽  
Carbon Backbone ◽  
Gel Permeation ◽  
Charged Component ◽  
Diaminopropionic Acid

AbstractComplex coacervation is an appealing method of microencapsulating delicate proteins for controlled drug delivery. Natural polyelectrolytes, such as collagen, gelatin, hyaluronic acid, and chondroitin sulfate, are popular choices for formulating the microspheres. For advantage of versatility, synthetic systems are attractive. Typical synthetic polyelectrolytes are composed of a carbon-carbon backbone that is nonbiodegradable. To design synthetic polyelectrolytes that are biodegradable, we synthesized diamines containing dipeptide or tripeptide sequences that are enzymatically degradable. The enzymatically degradable linkages comprised gly-phe, gly-phe-phe, or gly-gly-phe, and lysine and 2,3-diaminopropionic acid co-monomers served as the charged component. Using an interfacial polymerization technique, these monomers were condensed with diacyl chlorides, including succinyl, adipoyl, or terephthaloyl chloride to form polyamides. Results of gel permeation chromatography and ninhydrin assays showed that the polymers degraded in PBS containing α-chymotrypsin.

scholarly journals New Poly(Hydroxylauric-co-Lactic Acid) Liquid Polymer for Dissolving Lipophilic Drugs

KIMIKA ◽  
2017 ◽  
Vol 28 (1) ◽  
pp. 20-25
Author(s):  
Florentino C. Sumera ◽  
Shienna Marie A. Pontillas ◽  
Josanelle Angela V. Bilo ◽  
John Marty Mateo
Keyword(s):  
Lactic Acid ◽  
1H Nmr Spectroscopy ◽  
Controlled Drug Delivery ◽  
Gel Permeation Chromatography ◽  
Metal Catalyst ◽  
Pharmaceutical Companies ◽  
Molecular Weights ◽  
Liquid Polymer ◽  
Gel Permeation ◽  
Ft Ir

A liquid, biocompatible polyester based polymer, which could facilitate injectable formulations by simple mixing with the active substance (drug) is much needed by the pharmaceutical companies. A favourite candidate is polylactic acid (PLA) which is biocompatible and biodegradable. However PLA is solid with high crystallinity. Thus, in this research, hydroxylauric acid (HOLA) was copolymerized with lactic acid (LA) in different ratios by polycondensation technique at 180 °C, without a metal catalyst and avoiding the formation of interfering lactides, to provide a liquid polyester. The copolymers molecular weights were determined by Gel Permeation Chromatography (GPC) and their physical states indicated as solid or liquid were noted. The structures as polyesters were confirmed by FT-IR and 1H NMR spectroscopy. Poly(HOLA:LA)  products from reactant ratios 0:100 is solid, while ratios of 20:80, 40:60 are mixed (paste) and 60:40, 80:20 and 100:0 are liquids. Thus, the liquid polyesters from the polycondensation of HOLA and LA without catalyst  were picked as potential candidates for dissolving hydrophobic drugs that could be used as injectables in controlled drug delivery experiments.

Aggregated, Conformationally Changed Fibrinogen Exposes the Stimulating Sites for t-PA-Catalysed Plasminogen Activation

1996 ◽  
Vol 75 (02) ◽  
pp. 326-331 ◽  
Author(s):  
Unni Haddeland ◽  
Knut Sletten ◽  
Anne Bennick ◽  
Willem Nieuwenhuizen ◽  
Frank Brosstad
Keyword(s):  
Conformational Changes ◽  
Gel Permeation Chromatography ◽  
Tissue Type ◽  
Plasminogen Activation ◽  
Chromogenic Substrate ◽  
Type Plasminogen Activator ◽  
Gel Permeation ◽  
Self Association ◽  
Fibrin Monomers ◽  
Stimulation Of

SummaryThe present paper shows that conformationally changed fibrinogen can expose the sites Aα-(148-160) and γ-(312-324) involved in stimulation of the tissue-type plasminogen activator (t-PA)-catalysed plasminogen activation. The exposure of the stimulating sites was determined by ELISA using mABs directed to these sites, and was shown to coincide with stimulation of t-PA-catalysed plasminogen activation as assessed in an assay using a chromogenic substrate for plasmin. Gel permeation chromatography of fibrinogen conformationally changed by heat (46.5° C for 25 min) demonstrated the presence of both aggregated and monomeric fibrinogen. The aggregated fibrinogen, but not the monomeric fibrinogen, had exposed the epitopes Aα-(148-160) and γ-(312-324) involved in t-PA-stimulation. Fibrinogen subjected to heat in the presence of 3 mM of the tetrapeptide GPRP neither aggregates nor exposes the rate-enhancing sites. Thus, aggregation and exposure of t-PA-stimulating sites in fibrinogen seem to be related phenomena, and it is tempting to believe that the exposure of stimulating sites is a consequence of the conformational changes that occur during aggregation, or self-association. Fibrin monomers kept in a monomeric state by a final GPRP concentration of 3 mM do not expose the epitopes Aα-(148-160) and γ-(312-324) involved in t-PA-stimulation, whereas dilution of GPRP to a concentration that is no longer anti-polymerizing, results in exposure of these sites. Consequently, the exposure of t-PA-stimulating sites in fibrin as well is due to the conformational changes that occur during selfassociation.

Cooperative Self-Assembly of Pyridine-2,6-Diimine-Linked Macrocycles into Mechanically Robust Nanotubes

2019 ◽  
Author(s):  
Michael J. Strauss ◽  
Darya Asheghali ◽  
Austin Evans ◽  
Rebecca Li ◽  
Anton Chavez ◽  
...  
Keyword(s):  
Aspect Ratio ◽  
High Aspect Ratio ◽  
Self Assembly ◽  
Gel Permeation Chromatography ◽  
Synthetic Polymers ◽  
Young’S Moduli ◽  
Structural Rigidity ◽  
Assembly Mechanism ◽  
Low Dimensionality ◽  
Harsh Conditions

<p>Nanotubes assembled from macrocyclic precursors offer a unique combination of low dimensionality, structural rigidity, and distinct interior and exterior microenvironments. Usually the weak stacking energies of macrocycles limit the length or strength of the resultant nanotubes. Imine-linked macrocycles were recently found to assemble into high-aspect ratio (>10<sup>3</sup>), lyotropic nanotubes in the presence of excess acid. Yet these harsh conditions are incompatible with many functional groups and processing methods, and lower acid loadings instead catalyze macrocycle degradation. Here we report pyridine-2,6-diimine-linked macrocycles that assemble into high-aspect ratio nanotubes in the presence of less than 1 equiv of CF<sub>3</sub>CO<sub>2</sub>H per macrocycle. Analysis by gel permeation chromatography and fluorescence spectroscopy revealed a cooperative self-assembly mechanism. Nanofibers obtained by touch-spinning the pyridinium-based nanotubes exhibit Young’s moduli of 1.48 GPa, which exceeds that of many synthetic polymers and biological filaments. These findings will enable the design of structurally diverse nanotubes from synthetically accessible macrocycles. </p>

Gel Permeation Chromatography of Polyelectrolytes

1981 ◽  
Vol 4 (8) ◽  
pp. 1297-1309 ◽  
Author(s):  
M. Rinaudo ◽  
J. Desbrières ◽  
C. Rochas
Keyword(s):  
Gel Permeation Chromatography ◽  
Gel Permeation
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