Pluronic-phosphatidylcholine mixed polymeric nanomicellar formulation for curcumin drug bioavailability: Design, fabrication, characterization and in vitro bioinvestigations

IF 2.1 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY Journal of Bioactive and Compatible Polymers Pub Date : 2023-03-17 DOI:10.1177/08839115231157098
Hemil S. Patel, Anju P. Kunjadiya, A. Rahdar, Rakesh K. Sharma
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Abstract

Curcumin (CUR), obtained from turmeric, has biological advantages, but low aqueous solubility restricts its pharmaceutical applications. In the present work, a mixed polymeric nanomicellar formulation composed of bioactive Pluronic P123, Pluronic F68, and biocompatible phosphatidylcholine (PC) was designed and examined as the nanovehicles for overcoming the major barriers of poor bioavailability related to CUR. The CUR-incorporated P123/F68/PC mixed nanomicellar formulation (CUR-PFPC) was fabricated by the thin film technique and investigated in vitro. The fabrication of CUR-PFPC was optimized through D-optimal design. CUR-PFPC morphology, size distribution, zeta potential, drug encapsulating and incorporation efficiency, compatibility, and crystallinity were characterized using DLS, TEM, FTIR, XRD, and DSC analysis. Moreover, the cumulative drug release, antioxidant assays, and antimicrobial properties of formulations were also examined. The CUR-PFPC formulation exhibited a micellar size of 67.43 nm, a zeta potential of −15.1 mV, a PDI of 0.528, and a spherical shape. The mixed micellar formulation showed excellent compatibility and stability. The in vitro release profile of the CUR-PFPC reached over 60% in comparison to the 95% release of CUR, indicating a slow and sustained release. The DPPH assay showed that the CUR-PFPC had 96% antioxidant activity. Results show that the CUR-PFPC has powerful antibacterial and antifungal properties, which separates it from the free CUR. These findings suggest that the fabricated CUR-PFPC mixed polymeric nanomicellar formulation is thermodynamically and kinetically stable and may be considered a novel nanovehicle for hydrophobic antimicrobial drugs like CUR. Graphical Abstract
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用于姜黄素药物生物利用度的pluronic -磷脂酰胆碱混合聚合物纳米束制剂:设计、制造、表征和体外生物研究
从姜黄中提取的姜黄素(Curcumin, CUR)具有生物学上的优势,但较低的水溶性限制了其在医药上的应用。本文设计了一种由Pluronic P123、Pluronic F68和生物相容性磷脂酰胆碱(PC)组成的混合聚合物纳米胶束制剂,并研究了其作为纳米载体,以克服CUR生物利用度差的主要障碍。采用薄膜技术制备了含有CUR的P123/F68/PC混合纳米胶束制剂(CUR- pfpc)。采用d -最优设计方法对cu - pfpc的制备工艺进行了优化。采用DLS、TEM、FTIR、XRD、DSC等分析手段对cu - pfpc的形貌、粒径分布、zeta电位、药物包封和掺入效率、相容性和结晶度进行了表征。此外,还考察了制剂的累积药物释放、抗氧化试验和抗菌性能。CUR-PFPC胶束尺寸为67.43 nm, zeta电位为- 15.1 mV, PDI为0.528,呈球形。混合胶束配方具有良好的相容性和稳定性。与CUR的95%的体外释放相比,CUR- pfpc的体外释放谱达到60%以上,表明其释放缓慢且持续。DPPH实验表明,CUR-PFPC具有96%的抗氧化活性。结果表明,与游离的CUR相比,CUR- pfpc具有较强的抗菌和抗真菌性能,这表明所制备的CUR- pfpc混合聚合物纳米胶束具有良好的热力学和动力学稳定性,可作为一种新型的疏水抗菌药物纳米载体
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来源期刊
Journal of Bioactive and Compatible Polymers
Journal of Bioactive and Compatible Polymers 工程技术-材料科学:生物材料
CiteScore
3.50
自引率
0.00%
发文量
27
审稿时长
2 months
期刊介绍: The use and importance of biomedical polymers, especially in pharmacology, is growing rapidly. The Journal of Bioactive and Compatible Polymers is a fully peer-reviewed scholarly journal that provides biomedical polymer scientists and researchers with new information on important advances in this field. Examples of specific areas of interest to the journal include: polymeric drugs and drug design; polymeric functionalization and structures related to biological activity or compatibility; natural polymer modification to achieve specific biological activity or compatibility; enzyme modelling by polymers; membranes for biological use; liposome stabilization and cell modeling. This journal is a member of the Committee on Publication Ethics (COPE).
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