Journal of Pharmaceutical Innovation
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2025
·Vol. 21
·期 1
·16
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IF 2.7
Jia Chaoliang,Qu Jianlu,Liu Taoning,Wu Wei,Li wenlong
Objective This research intended to establish a curcumin nanosuspension micro-pellets (CUR-NSP) delivery system combining Hummer acoustic resonance (HAR) and fluidized bed coating technologies. Methods Polyvinylpyrrolidone K30 and sodium lauryl sulfate were employed as stabilizers to optimize and scale up the preparation of curcumin nanosuspension (CUR-NS) via HAR equipment. Using CUR-NS as the coating medium, the fluidized bed coating process for CUR-NSP was optimized through experimental design methodologies. Results First, this study prepared CUR-NS, which reduced the average particle size of raw curcumin from 5.38 ± 2.46 μm to 95.9 ± 0.46 nm. Under the optimal coating conditions, the redispersed CUR-NSP exhibited an average particle size of 104.86 ± 0.34 nm, a polydispersity index of 0.180 ± 0.002, a Zeta potential of -36.24 ± 0.80 mV, and a pellets yield of 97.14 ± 0.12%. Furthermore, this study evaluated the solidification efficiencies of fluidized bed coating, freeze drying, and rotary evaporation for CUR-NS. Structural characterizations via DSC, XRD, and FTIR confirmed the interaction between curcumin and stabilizers, along with partial amorphization. Saturation solubility tests demonstrated that CUR-NSP increases the solubility of curcumin in hydrochloric acid buffer solution at pH 1.2 and phosphate buffer solution at pH 6.8 by 2221.4 and 2761.89 times, respectively. In vitro dissolution tests indicated that CUR-NSP releases rapidly within 5 min. Conclusions The combination of HAR and fluidized bed coating enables an efficient and feasible approach for preparing CUR-NSP, addressing the issue of poor solubility.
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高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2019
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IF 2.606
Ya-Nan Xia,Xiang-Hui Li,Jie-Hong Xu,Li-Qing Chen,Atef Mohammed Qasem Ahmed,Dingyun Cao,Huan-Huan Du,Yibin Deng,Qing-Ri Cao
Traditional dosage forms of dexibuprofen extremely limit their clinical applications because of the bitter taste and the frequent drug administration caused by the relatively short half-life of the drug. This study aims to design novel sustained release (SR) supermicro-pellet based dry suspensions that load dexibuprofen, and also optimize the formulations in terms of morphology, release rate, flowability, and physicochemical stability of dosage forms. Drug-loaded pellets were prepared by using a bottom spray fluid bed coating technique using microcrystalline cellulose supermicro-pellets as the core and PVP K30 or Poloxamer 188 as the binder. The drug-loaded pellets were further coated with Kollicoat SR 30D to form SR pellets. The optimal SR dry suspensions are composed of SR pellets, diluent granules, and suspending agents. PVP K30- and Poloxamer 188-based SR pellets release the drug molecules in a SR manner over 8 h and show a high release profile for Poloxamer 188-based pellets. The drug release profile is not affected by the rotation speed of the paddle but shows a distinct pH-responsive behavior. The physical property of dexibuprofen has been changed during the preparation process. The SR dry suspensions (F5, with high amount of xanthan gum in suspending agents and low amount of poloxamer 188 in diluent granules) show high physical stability with the sedimentation rate of 0.8 (Hu/H) within 5 min and good flowability with the angle of repose (θ) at 27°. Low content variations were observed with a value of A+1.80SD ≤ 15, and no significant change was found in the drug content under high humidity and strong light. In conclusion, novel SR supermicro-pellet based dry suspensions have been successfully prepared, and the optimal formulation shows excellent SR, good flowability, content uniformity, and physicochemical stability.
研究领域:
药剂学
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药物释放系统
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生物药剂学
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高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Li Wang,Jianlu Qu,Zixuan Yan,Cunhao Li,Xingchu Gong,Wenlong Li
Curcumin (CUR) exhibits broad pharmacological activities, including anti-inflammatory, antibacterial, and antioxidant effects, and shows promising therapeutic potential in diseases such as diabetes and liver injury. However, its poor water solubility and low stability significantly limit clinical application. Conventional nanoemulsion solidification techniques, such as spray-drying and lyophilization, often involve high energy input, drug degradation, and poor redispersibility, making it challenging to achieve both stability and performance. In this study, we developed a novel strategy combining design-of-experiments (DoE) optimized curcumin nanoemulsions (CUR-NE) with fluidized bed coating to systematically enhance solubility and stability. Plackett-Burman design was used to screen key variables, and Box-Behnken design further optimized these factors, revealing that formulation parameters exert a more pronounced effect on particle size and polydispersity index (PDI) than process variables. The optimized CUR-NE exhibited an extremely small droplet size (Z-Ave = 13.48 ± 0.20 nanometers) and uniform distribution (PDI = 0.064 ± 0.013), and maintained a low redispersibility index (109.95 ± 1.18 percent) when coated onto pellets (CUR-Ps). Structural characterization using FT-IR and XRD confirmed negligible drug and excipient interactions and partial amorphization of CUR. Unlike conventional solidification methods, fluidized bed coating significantly improved the storage stability of the nanoemulsion while preserving its excellent solubility. This approach not only provides a new technical pathway for the development of curcumin delivery systems but also offers an innovative reference for the industrial production and application of poorly soluble drugs.
研究领域:
药剂学
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药物递送系统
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纳米技术
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制剂科学
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制药技术
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）