Poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) Biopolyester Based Nanoparticles as NVP-BEZ235 Delivery Vehicle for Tumor Targeting Therapy.,Biomacromolecules

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Poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) Biopolyester Based Nanoparticles as NVP-BEZ235 Delivery Vehicle for Tumor Targeting Therapy.
Biomacromolecules ( IF 5.5 ) Pub Date : 2019-06-26 , DOI: 10.1021/acs.biomac.9b00505
Fan Fan ₁ , Dan Tan ₁ , Sen Shang ₁ , Xingjuan Wu ₁ , Jiping Zhao ₁ , Ganqiao Ran ₁ , Xiaoyun Lu ₁

Affiliation

As a biopolyester with excellent properties, the potential biomedical applications of poly(3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHHx) have gained extensive attention. In this research, PHBHHx was fabricated into nanoparticles (NPs) to encapsulate NVP-BEZ235 (BEZ), an efficient kinase inhibitor/antitumor agent, for tumor targeting therapy. The resulting BEZ-NPs displayed a regularly spherical form with an appropriate diameter at 76.0 ± 3.6 nm. The encapsulation efficiency of BEZ was 83.7 ± 3.6%, and the sustained release profiles showed that almost 97% of BEZ could be gradually unrestricted from PHBHHx NPs within 72 h. The nanotoxicity studies revealed a satisfactory biosafety of PHBHHx NPs. PHBHHx NPs presented significantly improved cellular uptake in human prostate cancer cell line PC3, thereby enhancing the antiproliferation ability and kinase inhibitory activity of BEZ in vitro. More importantly, the in vivo real-time imaging demonstrated the adequate tumor targeting and accumulation capability of PHBHHx NPs. The remarkably delayed tumor growth, increased tumor necrosis, and reduced tumor proliferation in PC3 tumor xenograft mice further confirmed the antitumor efficacies of BEZ-loaded PHBHHx NPs. The above results suggest that PHBHHx NPs might be a promising drug delivery vehicle, safe and effective, for tumor targeting therapy.

中文翻译：

聚（3-羟基丁酸酯-co-3-羟基己酸酯）生物聚酯基纳米颗粒作为NVP-BEZ235运载体，用于肿瘤靶向治疗。

作为具有优异性能的生物聚酯，聚（3-羟基丁酸酯-co-3-羟基己酸酯）（PHBHHx）的潜在生物医学应用受到了广泛关注。在这项研究中，PHBHHx被制成纳米颗粒（NPs）以封装NVP-BEZ235（BEZ），一种有效的激酶抑制剂/抗肿瘤剂，用于肿瘤靶向治疗。所得的BEZ-NP呈规则球形，其合适的直径为76.0±3.6 nm。BEZ的包封效率为83.7±3.6％，持续释放曲线显示，近97％的BEZ可以在72小时内逐渐不受PHBHHx NP的限制。纳米毒性研究表明，PHBHHx NP具有令人满意的生物安全性。PHBHHx NPs显着改善了人类前列腺癌细胞系PC3中的细胞摄取，从而增强了BEZ的体外抗增殖能力和激酶抑制活性。更重要的是，体内实时成像证明了PHBHHx NP具有足够的肿瘤靶向性和蓄积能力。PC3肿瘤异种移植小鼠中肿瘤生长明显延迟，肿瘤坏死增加和肿瘤增殖减少，进一步证实了BEZ负载的PHBHHx NP的抗肿瘤功效。以上结果表明，PHBHHx NPs可能是一种有前途的，安全有效的靶向药物，可用于肿瘤靶向治疗。PC3肿瘤异种移植小鼠体内肿瘤的减少和肿瘤增殖的减少进一步证实了BEZ加载的PHBHHx NP的抗肿瘤作用。以上结果表明，PHBHHx NPs可能是一种有前途的，安全有效的靶向药物，可用于肿瘤靶向治疗。PC3肿瘤异种移植小鼠体内肿瘤的减少和肿瘤增殖的减少进一步证实了BEZ加载的PHBHHx NP的抗肿瘤作用。以上结果表明，PHBHHx NPs可能是一种有前途的，安全有效的靶向药物，可用于肿瘤靶向治疗。

更新日期：2019-06-14

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