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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

The College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China
Anhui Province Key Laboratory of Advanced Catalytic Materials and Reaction Engineering, School of Chemistry and Chemical Engineering, Hefei University of Technology, Hefei 230009, China
Authors to whom correspondence should be addressed.
These authors contributed equally to the work.
Polymers 2019, 11(5), 820;
Received: 13 April 2019 / Revised: 27 April 2019 / Accepted: 29 April 2019 / Published: 7 May 2019
(This article belongs to the Special Issue Polymer Matrix Composites for Advanced Applications)
PDF [3893 KB, uploaded 7 May 2019]


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. View Full-Text
Keywords: amphiphilic block copolymer; gambogenic acid; pH-sensitive amphiphilic block copolymer; gambogenic acid; pH-sensitive

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Liu, H.; Chen, H.; Cao, F.; Peng, D.; Chen, W.; Zhang, C. 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, 11, 820.

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