Development of sustained-release curcumin and piperine co-encapsulated electro-sprayed multilayer chitosan microparticles

IF 2.3 4区 化学 Q3 CHEMISTRY, PHYSICAL
Ngoc-Hanh Cao-Luu, Huynh-Vu-Thanh Luong, Duy Toan Pham, Bich-Thuyen Nguyen-Thi, Ngoc-Mai Ngo-Truong, Huynh-Giao Dang, Tuong-Vy Nguyen
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引用次数: 0

Abstract

Curcumin (CCM) is a natural compound with strong tumor-inhibiting activity. However, CCM is not widely used for cancer treatment because of its poor water solubility, penetration, and bioavailability. In this study, CCM and piperine (PPR), a bio-enhancer, were co-encapsulated within chitosan (CS) by co-axial electro-spraying method aiming to increase CCM bioavailability. Two formulation approaches have been proposed, including (1) co-encapsulation of CCM and PPR in microparticle core (e.g., CCM/PPR@CS) and (2) separate encapsulation of CCM and PPR in two different CS layers (e.g., CCM@PPR@CS). The optimal electro-spraying parameters were investigated and found to have applied a voltage of 15 kV, flow-rate of 0.1/0.2 mL h−1 (core/shell), and needle tip-to-collector distance of 10 cm for CCM/PPR@CS microparticle; and applied voltage of 19 kV, flow rate of 0.1/0.2/0.3 mL h−1 (inner-layer/middle-layer/outer-layer), and working distance of 14 cm for CCM@PPR@CS formulation. The obtained particles were non-agglomerated, spherical, and possessed core–shell structure with clear boundaries, relatively wide distribution with mean diameters of 366 ± 136 nm for CCM/PPR@CS and 784 ± 139 nm for CCM@PPR@CS. The in vitro CCM and PPR cumulative releases were considerably high (70–80%) and the diffusion of drugs through polymer network was the primary release mechanism, adhering to the Korsmeyer-Peppas kinetics model. Remarkably, the CCM@PPR@CS formulation improved the cell viability when comparing to free CCM with impressive half-maximal inhibitory concentration (IC50). In conclusion, the CCM@PPR@CS structure could be utilized as a potential drug delivery system for decreasing denaturation and enhancing the absorption of CCM.

Abstract Image

姜黄素与胡椒碱共包封电喷涂多层壳聚糖缓释微粒的研制
姜黄素(Curcumin, CCM)是一种具有较强肿瘤抑制活性的天然化合物。然而,CCM由于其水溶性、渗透性和生物利用度差,并没有广泛应用于癌症治疗。本研究采用同轴电喷涂方法,将CCM与生物增强剂胡椒碱(PPR)共包被壳聚糖(CS),以提高CCM的生物利用度。提出了两种配方方法,包括:(1)CCM和PPR在微粒核心中共包封(例如,CCM/PPR@CS)和(2)CCM和PPR在两个不同的CS层中单独包封(例如,CCM@PPR@CS)。对CCM/PPR@CS微粒的最佳电喷涂参数进行了研究,发现电压为15 kV,流速为0.1/0.2 mL h - 1(芯/壳),针尖至收集器距离为10 cm;,施加电压19 kV,流速0.1/0.2/0.3 mL h−1(内层/中间层/外层),CCM@PPR@CS配方工作距离14 cm。所得颗粒无团聚,呈球形,具有边界清晰的核壳结构,分布较宽,CCM/PPR@CS和CCM@PPR@CS的平均直径分别为366±136 nm和784±139 nm。CCM和PPR体外累积释放量相当高(70-80%),药物通过聚合物网络扩散是主要释放机制,符合Korsmeyer-Peppas动力学模型。值得注意的是,与游离CCM相比,CCM@PPR@CS配方提高了细胞活力,具有令人印象深刻的半最大抑制浓度(IC50)。综上所述,CCM@PPR@CS结构可以作为一种潜在的药物传递体系,用于降低CCM的变性和增强其吸收。
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来源期刊
Colloid and Polymer Science
Colloid and Polymer Science 化学-高分子科学
CiteScore
4.60
自引率
4.20%
发文量
111
审稿时长
2.2 months
期刊介绍: Colloid and Polymer Science - a leading international journal of longstanding tradition - is devoted to colloid and polymer science and its interdisciplinary interactions. As such, it responds to a demand which has lost none of its actuality as revealed in the trends of contemporary materials science.
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