PAA-g-PLA amphiphilic graft copolymer: synthesis, self-assembly, and drug loading ability

2017 ◽  
Vol 8 (28) ◽  
pp. 4098-4107 ◽  
Author(s):  
Wenhao Qian ◽  
Tao Song ◽  
Mao Ye ◽  
Peicheng Xu ◽  
Guolin Lu ◽  
...  

This article reports the synthesis of a PAA-g-PLA amphiphilic polymer by the combination of RAFT polymerization and organocatalytic ROP, which could self-assemble into spheres in aqueous media for sustained release of doxorubicin.

RSC Advances ◽  
2017 ◽  
Vol 7 (86) ◽  
pp. 54562-54569 ◽  
Author(s):  
Wei Wang ◽  
Xin Zhou ◽  
Min Wei ◽  
Zude Liu ◽  
Guolin Lu ◽  
...  

This article reports the synthesis of a PAA-g-PLA amphiphilic graft polymer, which could self-assemble into large compound micelles in aqueous media for sustained release of MTX.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 904
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Xiaowei Dong

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.


RSC Advances ◽  
2017 ◽  
Vol 7 (39) ◽  
pp. 24522-24536 ◽  
Author(s):  
N. S. Serkhacheva ◽  
O. I. Smirnov ◽  
A. V. Tolkachev ◽  
N. I. Prokopov ◽  
A. V. Plutalova ◽  
...  

Hydrophilic and amphiphilic polymeric trithiocarbonates based on polyacrylic acid are able to provide polymerization-induced self-assembly in copolymerization of butyl and fluoroalkyl acrylates.


2020 ◽  
Author(s):  
Sauradip Chaudhuri ◽  
Martha Fowler ◽  
Afroz S. Mohammad ◽  
Wenqui Zhang ◽  
Cassandra Baker ◽  
...  

<p> Here, we describe a simple, efficient formulation of a novel library of β-cyclodextrin-poly (β-amino ester) networks (CDN) to achieve this goal. We observed that network architecture was a critical determinant of CDN encapsulation of candidate molecules, with a more hydrophobic core enabling effective self-assembly and a PEGylated surface enabling high loading (up to ~30% w/w), effective self assembly of the nanoparticle, and slow release of drug into aqueous media (24 days) for the model <i>HDACi</i> panobinostat. Optimized CDN nanoparticles were taken up by GL261 cells in culture, and released panobinostat was confirmed to be bioactive. Pharmacokinetic analyses demonstrated that panobinostat was delivered to the brainstem, cerebellum, and upper spinal cord following intrathecal administration via cisterna magna injection in healthy mice. We next constructed a library of CDNs to encapsulate various small, hydrophobic, ionizable molecules (panobinostat, quisinostat, dacinostat, givinostat, and bortezomib, camptothecin, nile red, and cytarabine), which yielded important insights into the structural requirements for effective drug loading and CDN self-assembly. Taken in sum, these studies present a novel nanocarrier platform for encapsulation of <i>HDACi</i> via both ionic and hydrophobic interactions, which is an important step toward better treatment of disease via <i>HDACi</i> therapy.</p>


2015 ◽  
Vol 7 (6) ◽  
pp. 2738-2746 ◽  
Author(s):  
Zhao Wang ◽  
Zhongkui Yang ◽  
Tao Gao ◽  
Jingwen He ◽  
Laijiang Gong ◽  
...  

An amphiphilic block copolymer-based colorimetric and fluorescent chemosensor for Hg2+was prepared, which was synthesized by sequential RAFT polymerization of NIPAM and R6GDM (a novel Hg2+-sensitive rhodamine monomer).


2019 ◽  
Vol 55 (66) ◽  
pp. 9829-9832 ◽  
Author(s):  
Alexandre Moquin ◽  
Ramez Hanna ◽  
Tongyue Liang ◽  
Huseyin Erguven ◽  
Evan Rizzel Gran ◽  
...  

A simple one-pot methodology provides easy access to amphiphilic PEG–pyrrole backbone polymers, which self-assemble into soft nanoparticles enabling efficient drug loading/sustained release and can be detected inside cells.


2016 ◽  
Vol 8 (14) ◽  
pp. 9454-9461 ◽  
Author(s):  
Harim Jeon ◽  
Dong Jun Kim ◽  
Min Su Park ◽  
Du Yeol Ryu ◽  
Jong Hak Kim

2020 ◽  
Author(s):  
Sauradip Chaudhuri ◽  
Martha Fowler ◽  
Afroz S. Mohammad ◽  
Wenqui Zhang ◽  
Cassandra Baker ◽  
...  

<p> Here, we describe a simple, efficient formulation of a novel library of β-cyclodextrin-poly (β-amino ester) networks (CDN) to achieve this goal. We observed that network architecture was a critical determinant of CDN encapsulation of candidate molecules, with a more hydrophobic core enabling effective self-assembly and a PEGylated surface enabling high loading (up to ~30% w/w), effective self assembly of the nanoparticle, and slow release of drug into aqueous media (24 days) for the model <i>HDACi</i> panobinostat. Optimized CDN nanoparticles were taken up by GL261 cells in culture, and released panobinostat was confirmed to be bioactive. Pharmacokinetic analyses demonstrated that panobinostat was delivered to the brainstem, cerebellum, and upper spinal cord following intrathecal administration via cisterna magna injection in healthy mice. We next constructed a library of CDNs to encapsulate various small, hydrophobic, ionizable molecules (panobinostat, quisinostat, dacinostat, givinostat, and bortezomib, camptothecin, nile red, and cytarabine), which yielded important insights into the structural requirements for effective drug loading and CDN self-assembly. Taken in sum, these studies present a novel nanocarrier platform for encapsulation of <i>HDACi</i> via both ionic and hydrophobic interactions, which is an important step toward better treatment of disease via <i>HDACi</i> therapy.</p>


2011 ◽  
Vol 233-235 ◽  
pp. 2138-2144 ◽  
Author(s):  
Fang Ping Wang ◽  
Xin Zhen Du ◽  
Hu Po Mu ◽  
Dong Xia Zhang ◽  
Yun Jun Ma

The self-assembly of the amphiphilic graft copolymer AA-C8PhEO10Ac in water was investigated by fluorescence technique using 8-anilino-1-naphthalene sulfonate(ANS) as a probe and transmission electron microscopy (TEM), the effects of inorganic salt , copolymer concentration and pH on the micellar size and structures of AA-C8PhEO10Ac were discussed. It was found that the micelle morphologies and sizes were related with the micellar preparation methods. The sizes of micelles increased with the addition of NaCl and decreased at high pH values.


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