Abstract
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.
Highlights
Gambogenic acid (GNA), as a kind of weakly acidic ingredient, extracted from Chinese traditional medicine Gamboge, has been proved with outstanding inhibition on proliferation and growth of various tumor cell [1,2,3]
We have developed a novel amphiphilic block copolymer poly-b-polycaprolactone (PAA-b-PCL) synthesized via successive reactions of reversible addition-fragmentation chain transfer (RAFT), ring-opening polymerization (ROP) and hydrolytic reaction
A novel amphiphilic block copolymer poly-b-polycaprolactone (PAAb-PCL) with excellent pH-triggered morphological transition performance has been successfully synthesized through successive reactions of RAFT, ROP, and hydrolytic reaction
Summary
Gambogenic acid (GNA), as a kind of weakly acidic ingredient, extracted from Chinese traditional medicine Gamboge, has been proved with outstanding inhibition on proliferation and growth of various tumor cell [1,2,3]. Great limits have been found in its potential applications, such as inflammation to blood vessel, low solubility, deficient bioavailability, or property of toxicity [5,6] To conquer these problems mentioned above, much effort has been devoted to explore effective carriers, such as PEGylated Niosomes [7], solid lipid nanoparticles [8], and nanostructured lipid carriers [9]. The drug loading efficiency (DLE) and drug loading capacity (DLC) of nanocarriers obtained through those strategies are still limited. Polymer micelles (PMs), composed of an outer hydrophilic shell and inner lipophilic core, have appealed arousing attention due to its unique performances when performed as nanocarriers, for Polymers 2019, 11, 820; doi:10.3390/polym11050820 www.mdpi.com/journal/polymers
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