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Open AccessArticle

Development and In Vitro Evaluation of Linear PEI-Shelled Heparin/Berberine Nanoparticles in Human Osteosarcoma U-2 OS Cells

Department of Chemistry, National Tsing Hua University, 30013 Hsinchu, Taiwan
Department of Biological Science and Technology, China Medical University, 40402 Taichung, Taiwan
Department of Agronomy, National Chung Hsing University, 40227 Taichung, Taiwan
Department of Medical Research, China Medical University Hospital, 40402 Taichung, Taiwan
Author to whom correspondence should be addressed.
Molecules 2018, 23(12), 3121;
Received: 3 October 2018 / Revised: 22 November 2018 / Accepted: 27 November 2018 / Published: 28 November 2018
Berberine (BBR), a natural isoquinoline alkaloid derived from Chinese herbs, exerts many biological effects, including antiviral, antimicrobial, antidiarrhea, anti-inflammatory, and antitumor effects. In this study, a novel berberine nanoparticle (NP) consisting of heparin (HP) and BBR with or without being shelled with linear polyethyleneimine (LPEI) was developed to enhance its antitumor activity on osteosarcoma U-2 OS cells. With varying ratios of HP to BBR, HP/BBR NPs had a size ranging from 218.4 ± 3.9 to 282.0 ± 5.1 nm and zeta potential from −35.7 ± 0.4 to −51.9 ± 1.8 mV. After shelling with LPEI, the resultant NPs (HP/BBR/LPEI) possessed a size ranging from 226.3 ± 3.0 to 405.7 ± 85.2 nm and zeta potential from −46.5 ± 0.3 to −35.6 ± 0.5 mV; the encapsulation rate of BBR was close to 80%. The release profiles of both NPs were revealed to be slower than that of BBR solution. Results also showed that BBR and its two derived NPs reduced the viability of U-2 OS cells, and BBR NPs increased the cellular uptake of BBR. Cells were arrested at the G1 phase when treated individually with BBR and the two NPs (HP/BBR and HP/BBR/LPEI) and DNA condensation was induced. In addition, BBR and BBR NPs reduced the expression of mouse double minute 2 homolog (MDM2) but increased that of p53, and BBR NPs enhanced apoptotic effects. In short, heparin-based nanoparticles could be potential carriers for osteosarcoma treatment. View Full-Text
Keywords: Berberine; linear PEI; heparin; osteosarcoma; apoptosis Berberine; linear PEI; heparin; osteosarcoma; apoptosis
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Hsu, H.-K.; Hsu, K.-H.; Cheng, Y.-M.; Suen, H.-Y.; Peng, S.-F. Development and In Vitro Evaluation of Linear PEI-Shelled Heparin/Berberine Nanoparticles in Human Osteosarcoma U-2 OS Cells. Molecules 2018, 23, 3121.

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