Self-Assembling Polymer–Drug Conjugates Nanomedicine for Drug Delivery

2020 ◽  
pp. 111-158
Author(s):  
Jasbir Singh ◽  
Harmeet Kaur
Keyword(s):  
Drug Delivery ◽  
Drug Conjugates ◽  
Self Assembling ◽  
Polymer Drug Conjugates

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

Albumin–Polymer–Drug Conjugates: Long Circulating, High Payload Drug Delivery Vehicles

2016 ◽  
Vol 5 (10) ◽  
pp. 1089-1094 ◽  
Author(s):  
Anton A. A. Smith ◽  
Kaja Zuwala ◽  
Oliver Pilgram ◽  
Karen Singers Johansen ◽  
Martin Tolstrup ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Vehicles ◽  
Drug Conjugates ◽  
Delivery Vehicles ◽  
Polymer Drug Conjugates ◽  
High Payload

Polymer-drug conjugates: manipulating drug delivery kinetics using model LCST systems

1997 ◽  
Vol 45 (1) ◽  
pp. 95-101 ◽  
Author(s):  
S.S Shah ◽  
J Wertheim ◽  
C.T Wang ◽  
C.G Pitt
Keyword(s):  
Drug Delivery ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

scholarly journals Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer

2011 ◽  
Vol 61 (4) ◽  
pp. 465-472 ◽  
Author(s):  
Marijana Končič ◽  
Branka Zorc ◽  
Predrag Novak
Keyword(s):  
Drug Delivery ◽  
Water Solubility ◽  
The Other ◽  
Amino Groups ◽  
Chemically Modified ◽  
Drug Conjugates ◽  
17Β Estradiol ◽  
Macromolecular Prodrugs ◽  
Polymer Drug Conjugates ◽  
Estradiol 17Β

Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymerTwo hydrosoluble conjugates of 17β-estradiol (ED) and estradiol-17β-valerate (EV) with polyaspartamide polymer were prepared and characterized. ED and EV were first chemically modified and bound to poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)]-poly[α,β-(N-2-aminoethyl-DL-aspartamide)] (PAHA), a hydrosoluble polyaspartamide-type copolymer bearing both hydroxyl and amino groups. ED was first converted to 17-hemisuccinate (EDS) and then bound to PAHA. In the resulting conjugate PAHA-EDS, the estradiol moiety was linked to the polymer through a 2-aminoethylhemisuccinamide spacer. On the other hand, EV was first converted to estradiol-17β-valerate-3-(benzotriazole-1-carboxylate), which readily reacted with amino groups in PAHA affording the polymer-drug conjugate PAHA-EV. In the prepared conjugate PAHA-EV, the estradiol moiety was covalently bound to the polyaspartamide backbone by carbamate linkage, through an ethylenediamine spacer. The polymer-drug conjugates were designed and prepared with the aim to increase water-solubility, bioavailability and to improve drug delivery of the lipophilic estrogen hormone.

Polymer–Drug Conjugates as Drug Delivery Systems

2019 ◽  
pp. 61-75
Author(s):  
Sauraj Singh ◽  
Ruchir Priyadarshi ◽  
Bijender Kumar ◽  
Saleheen Bano ◽  
Farha Deeba ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates
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