scholarly journals Amphiphilic Block Copolymer Poly (Acrylic Acid)-B-Polycaprolactone as a Novel pH-sensitive Nanocarrier for Anti-Cancer Drugs Delivery: In-vitro and In-vivo Evaluation

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 820 ◽  
Author(s):  
Huanhuan Liu ◽  
Hong Chen ◽  
Fuhu Cao ◽  
Daiyin Peng ◽  
Weidong Chen ◽  
...  

Gambogenic acid (GNA) has been demonstrated with outstanding antitumor activity as a potential antitumor drug in recent years. However, the low solubility and deficient bioavailability of GNA seriously hinder its practical application in the clinic area. In this study, a novel amphiphilic block copolymer, poly (acrylic acid)-b-polycaprolactone (PAA-b-PCL) is prepared and assembled into pH-responsive polymeric micelles (PMs) as one mold of drug delivery system (DDS) with unique properties. Relevant investigation on PMs exhibits excellent carrying potential and pH-dependent release performance for GNA. The drug loading capacity (DLC) and drug loading efficiency (DLE) for GNA-loaded PMs can be achieved as high as 15.20 ± 0.07% and 83.67 ± 0.49%, respectively. The in vitro experiments indicate that the GNA releasing time, cytotoxicity, and cellular uptake are significantly enhanced. Especially, the peak concentration (Cmax) and area under the curve (AUC) are promoted sharply in the GNA-loaded PMs concentration-time curve. This study not only provides a novel way to widen the application of anticancer GNA in the future, but also extends the potential of stimuli-responsive copolymers to biomedical applications.

2018 ◽  
Vol 42 (2) ◽  
pp. 1290-1299 ◽  
Author(s):  
Zhen Wang ◽  
Yongtao Tan ◽  
Ying Liu ◽  
Lengyuan Niu ◽  
Lingbin Kong ◽  
...  

Herein, amphiphilic block copolymer-modified film electrodes were fabricated using poly(acrylic acid)-b-poly(acrylonitrile)-b-poly(acrylic acid) as a surface modifier, polyethersulfone as a matrix polymer, and activated carbon as an active substance by the phase separation method to enhance the wettability of the electrodes.


2018 ◽  
Vol 230 ◽  
pp. 143-147 ◽  
Author(s):  
Sudhina Guragain ◽  
Nagy L. Torad ◽  
Yousef Gamaan Alghamdi ◽  
Abdulmohsen Ali Alshehri ◽  
Jeonghun Kim ◽  
...  

Author(s):  
Qurat-ul-Ain Sharif ◽  
Muhammad Sohail ◽  
Mahmood Ahmad ◽  
Muhammad Usman Minhas ◽  
Shahzeb Khan ◽  
...  

2002 ◽  
Vol 280 (1) ◽  
pp. 90-94 ◽  
Author(s):  
S.-Z. Mao ◽  
L.-Y. Zhu ◽  
T.-Z. Wang ◽  
M.-Z. Li ◽  
E.-J. Wang ◽  
...  

2021 ◽  
Author(s):  
Shaodong Sun ◽  
Chenrui Yuan ◽  
Zhulu Xie ◽  
Wen-Cong Xu ◽  
Qijin Zhang ◽  
...  

The self-assembly properties and photoresponsive behaviours of an azobenzene-containing block copolymer poly(acrylic acid-block-6-(4-(p-tolyldiazenyl)phenoxy)hexyl acrylate) (PAA-b-PAzo) are reported. As azobenzene has reversible trans–cis photoisomerization abilities, the trans PAA-b-PAzo solutions were converted...


2016 ◽  
Vol 18 (37) ◽  
pp. 26236-26244 ◽  
Author(s):  
Ye Zhu ◽  
Chenglin Yi ◽  
Qiong Hu ◽  
Wei Wei ◽  
Xiaoya Liu

In this study, a series of random copolymer poly(acrylic acid-co-styrene) (P(AA-co-St)) and block copolymer poly(acrylic acid)-b-polystyrene (PAA-b-PSt) with similar chemical composition but different chain microstructure were synthesized.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1210
Author(s):  
Xieguo Yan ◽  
Shiqiang Wang ◽  
Kaoxiang Sun

Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the optimized formulation by stepwise regression. We also assessed the crystalline changes, residual solvents, solubility and stability after sterilization, in-vivo polymer degradation, pharmacokinetics, and tissue inflammation in the case of the optimized formulation. The surface of the optimized RIS microspheres was small and hollow with 134.4 ± 3.5 µm particle size, 1.60 SPAN, 46.7% ± 2.3% implant drug loading, and 93.4% entrapment efficiency. The in-vitro dissolution behavior of RIS-IM had zero-order kinetics and stable blood concentration; no lag time was released for over three months. Furthermore, the RIS-IM was not only non-irritating to tissues but also had good biocompatibility and product stability. Long-acting RIS-IMs with microspheres and film coatings can provide a new avenue for treating schizophrenia.


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