Nguyen Dinh Trung, Dinh Van Thoai, Dang Le Hang, Nguyen Dang Nam, Giang Bach Long, Nguyen Cong Truc, Nguyen Thi Bich Tram, Thu Le Van, Tran Ngoc Quyen
Institute of Research and Development, Duy Tan University, Da Nang City 550000, Vietnam.
Institute of Applied Materials Science, VAST, TL29, ThanhLoc Ward, Dist. 12, Ho Chi Minh City 700000, Vietnam.
Polymers (Basel). 2019 May 7;11(5):814. doi: 10.3390/polym11050814.
Herein, a new process to manufacture multicore micelles nanoparticles reinforced with co-assembly via hydrophobic interaction and electrostatic interaction under the help of ultrasonication was developed. The precise co-assembly between negative/hydrophobic drug and positive charged amphiphilic copolymer based pluronic platform allows the formation of complex micelles structures as the multicore motif with predefined functions. In this study, curcumin was selected as a drug model while positively charged copolymer was based on a pluronic-conjugated gelatin with different hydrophobicity length of Pluronic F87 and Pluronic F127. Under impact of dual hydrophobic and electrostatic interactions, the nCur-encapsulated core-shell micelles formed ranging from 40 nm to 70 nm and 40-100 nm by transmission electron microscopy (TEM) and Dynamic Light Scattering (DLS), respectively. It is found that the structures emerged depended on the relative lengths of the hydrophobic blocks in pluronic. Regarding g2(τ) behavior from DLS measurement, the nanogels showed a high stability in spherical form. Surprisingly, the release profiles showed a sustainable behavior of Cur from this system for drug delivery approaches. In vitro study exhibited that nCur-encapsulated complex micelles increased inhibitory activity against cancer cells growth with IC is 4.02 ± 0.11 mg/L (10.92 ± 0.3 µM) which is higher than of free curcumin at 9.40 ± 0.17 mg/L (25.54 ± 0.18 µM). The results obtained can provide the new method to generate the hierarchical assembly of copolymers with incorporated loading with the same property.
在此,开发了一种新的工艺,即在超声作用下,通过疏水相互作用和静电相互作用共组装来制造多核胶束纳米颗粒。基于普朗尼克平台的带负电荷/疏水性药物与带正电荷的两亲共聚物之间的精确共组装,能够形成具有预定义功能的多核基序的复合胶束结构。在本研究中,选择姜黄素作为药物模型,而带正电荷的共聚物基于具有不同普朗尼克F87和普朗尼克F127疏水长度的普朗尼克共轭明胶。在双重疏水和静电相互作用的影响下,通过透射电子显微镜(TEM)和动态光散射(DLS)分别形成了粒径范围为40 nm至70 nm和40 - 100 nm的包载nCur的核壳胶束。研究发现,所形成的结构取决于普朗尼克中疏水嵌段的相对长度。关于DLS测量的g2(τ)行为,纳米凝胶呈球形且具有高稳定性。令人惊讶的是,释放曲线表明该系统在药物递送方法中姜黄素具有持续释放行为。体外研究表明,包载nCur的复合胶束对癌细胞生长的抑制活性增强,其IC50为4.02±0.11 mg/L(10.92±0.3 µM),高于游离姜黄素的9.40±0.17 mg/L(25.54±0.18 µM)。所得结果可为生成具有相同性质的负载型共聚物分级组装提供新方法。