Disassembly of amphiphilic small molecular prodrug with fluorescence switch induced by pH and folic acid receptors for targeted delivery and controlled release

2017 ◽  
Vol 150 ◽  
pp. 50-58 ◽  
Author(s):  
Zhigang Xu ◽  
Xiaoxiao Shi ◽  
Meili Hou ◽  
Peng Xue ◽  
Yong-E Gao ◽  
...  
2020 ◽  
Vol 22 (1) ◽  
pp. 340
Author(s):  
Ilya Nifant’ev ◽  
Andrei Siniavin ◽  
Eduard Karamov ◽  
Maxim Kosarev ◽  
Sergey Kovalchuk ◽  
...  

Despite the world’s combined efforts, human immunodeficiency virus (HIV), the causative agent of AIDS, remains one of the world’s most serious public health challenges. High genetic variability of HIV complicates the development of anti-HIV vaccine, and there is an actual clinical need for increasing the efficiency of anti-HIV drugs in terms of targeted delivery and controlled release. Tenofovir (TFV), a nucleotide-analog reverse transcriptase inhibitor, has gained wide acceptance as a drug for pre-exposure prophylaxis or treatment of HIV infection. In our study, we explored the potential of tenofovir disoproxil (TFD) adducts with block copolymers of poly(ethylene glycol) monomethyl ether and poly(ethylene phosphoric acid) (mPEG-b-PEPA) as candidates for developing a long-acting/controlled-release formulation of TFV. Two types of mPEG-b-PEPA with numbers of ethylene phosphoric acid (EPA) fragments of 13 and 49 were synthesized by catalytic ring-opening polymerization, and used for preparing four types of adducts with TFD. Antiviral activity of [mPEG-b-PEPA]TFD or tenofovir disoproxil fumarate (TDF) was evaluated using the model of experimental HIV infection in vitro (MT-4/HIV-1IIIB). Judging by the values of the selectivity index (SI), TFD exhibited an up to 14-fold higher anti-HIV activity in the form of mPEG-b-PEPA adducts, thus demonstrating significant promise for further development of long-acting/controlled-release injectable TFV formulations.


2017 ◽  
Vol 76 ◽  
pp. 743-751 ◽  
Author(s):  
Laura Jaimes-Aguirre ◽  
Enrique Morales-Avila ◽  
Blanca E. Ocampo-García ◽  
Luis Alberto Medina ◽  
Gustavo López-Téllez ◽  
...  

2016 ◽  
Vol 4 (15) ◽  
pp. 2578-2590 ◽  
Author(s):  
Jyh-Ping Chen ◽  
Chih-Hsin Liu ◽  
Hao-Lung Hsu ◽  
Tony Wu ◽  
Yu-Jen Lu ◽  
...  

Targeted delivery and triggered release of rtPA-encapsulated magnetic chitosan nanoparticles with the guidance of a magnet could be used for remote-controlled thrombolysis therapy.


2018 ◽  
Vol 15 (3) ◽  
pp. 994-1004 ◽  
Author(s):  
James A. Vassie ◽  
John M. Whitelock ◽  
Megan S. Lord

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