The aim of this study was the development of griseofulvin (GRI) loaded β-cyclodextrin (β–CD) based nanosponges for bitter taste masking, improving dissolution rate and oral bioavailability. Plain NS (NS1 NS2 and NS3) were fabricated by reacting β-CD with the cross-linker diphenyl carbonate at different molar ratios (1:2, 1:4 and 1:6, respectively) using ultrasonication method. The NS2 provided both highest %yield and GRI solubilization enhancement. Thus, the drug was loaded in NS2 at different NS2: drug weight ratios in presence or absence of 0.25%w/w polyvinylpyrolidone (PVP k30). The GRI loaded NS (F1) that provided highest drug loading capacity and entrapment efficiency (47.20 ± 0.38%, 84.91 ± 0.30%, respectively) was morphologically examined using scanning electron microscopy (SEM). Also, Particle size, zeta potential, differential scanning calorimetry (DSC), Fourier transform infra-red (FT-IR), nuclear magnetic resonance (NMR) spectroscopy, in-vitro release, taste masking potential were evaluated. Moreover, in-vivo Pharmacokinetic studies were performed on rats. The F1 showed particle size 665.9 ± 13.8 nm and zeta potential −21.5 ± 0.7 mV. The DSC and FT-IR analysis confirmed the complexation of GRI with NS2. Nanosponges (F1) provided 3.19, folds increase in dissolution efficiency %, 2.13 and 3.78 folds increase in C_max and AUC_0-48 compared to plain GRI. Taste masking evaluation confirmed the potential of GRI nanosponges (F1) in masking the bitter taste of GRI completely. The study confirmed that complexation of GRI with NS would be a viable approach for masking the bitter taste of GRI and improving oral bioavailability, that Cmax, Tmax and AUC 0–48 were significantly higher for the developed formulation (F1).

本研究的目的是开发负载灰黄霉素 (GRI) 的 β-环糊精 (β-CD) 基纳米海绵，用于掩蔽苦味、提高溶解速率和口服生物利用度。普通 NS（NS1 NS2 和 NS3）是通过使用超声波法以不同的摩尔比（分别为 1:2、1:4 和 1:6）使 β-CD 与交联剂碳酸二苯酯反应制造的。NS2 提供了最高的产率百分比和 GRI 增溶增强。因此，在存在或不存在 0.25%w/w 聚乙烯吡咯烷酮 (PVP k30) 的情况下，药物以不同的 NS2：药物重量比加载到 NS2 中。GRI 负载 NS (F1) 提供最高的载药能力和包封效率 (47.20  ± 使用扫描电子显微镜 (SEM) 进行形态学检查，分别为 0.38%、84.91 ± 0.30%。此外，还评估了粒径、zeta 电位、差示扫描量热法 (DSC)、傅里叶变换红外 (FT-IR)、核磁共振 (NMR) 光谱、体外释放、掩味潜力。此外，对大鼠进行了体内药代动力学研究。F1 的粒径为 665.9 ± 13.8 nm，zeta 电位为 -21.5 ± 0.7 mV。DSC 和 FT-IR 分析证实了 GRI 与 NS2 的络合。_{Nanosponges (F1) 提供 3.19 倍的溶解效率 %，C max}和 AUC的 2.13 和 3.78 倍增加_0-48与普通 GRI 相比。掩味评估证实了 GRI 纳米海绵 (F1) 在完全掩盖 GRI 苦味方面的潜力。该研究证实，GRI 与 NS 的络合将是掩盖 GRI 苦味和提高口服生物利用度的可行方法，开发的配方 (F1) 的 Cmax、Tmax 和 AUC 0-48 显着更高。