{"title":"Development of sustained-release curcumin and piperine co-encapsulated electro-sprayed multilayer chitosan microparticles","authors":"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","doi":"10.1007/s00396-025-05418-3","DOIUrl":null,"url":null,"abstract":"<div><p>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<sup>−1</sup> (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<sup>−1</sup> (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 (IC<sub>50</sub>). 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.</p></div>","PeriodicalId":520,"journal":{"name":"Colloid and Polymer Science","volume":"303 7","pages":"1331 - 1345"},"PeriodicalIF":2.3000,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Colloid and Polymer Science","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s00396-025-05418-3","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, PHYSICAL","Score":null,"Total":0}
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.
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。
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.