Department of Pharmaceutics, PSG College of Pharmacy, Peelamedu, Coimbatore, 641004, Tamil Nadu, India.
Department of Pharmaceutics, MNR College of Pharmacy, MNR Nagar, Fasalwadi, Sangareddy, Hyderabad, 502294, Telangana, India.
Naunyn Schmiedebergs Arch Pharmacol. 2024 Nov;397(11):9007-9021. doi: 10.1007/s00210-024-03223-3. Epub 2024 Jun 15.
Nanostructured lipid carriers (NLC) have low storage and gastrointestinal stability, limiting their applicability. The work aimed to elevate the stability and behaviour of NLC in the alimentary tract by creating an alginate bead. Through the extrusion dropping procedure, Resveratrol (RES)-loaded NLC were efficiently integrated into alginate beads. The incorporation had no significant impact on the particle size, morphology, or inner structure of NLC, as assessed using DLS (Dynamic Light Scattering), SEM (Scanning Electron Microscopy), Differential Scanning Calorimetry (DSC) and FT-IR (Fourier Transform Infra-Red). Incorporating NLC into alginate beads improves its physical stability compared to dispersion of NLC as well as NLC-Sol. An in vitro release investigation found that the NLC-alginate beads released RES more slowly than optimized NLC formulation (RES-NLCs-opt) and NLC-alginate sol. Research on simulated in vitro digestive models revealed that just a small amount of integrated NLC may permeate stomach fluid due to its tiny size. The slow diffusion of NLC from alginate to intestinal fluid prevented aggregation and allowed for gentle hydrolysis of the lipid matrix. Incorporating NLC in alginate beads shows promise for improving stability, modifying gastrointestinal behaviour, and controlling release throughout the process of digestion.
纳米结构脂质载体(NLC)的储存和胃肠道稳定性较低,限制了其适用性。本工作旨在通过制备藻酸盐珠来提高 NLC 在消化道中的稳定性和行为。通过挤出滴注程序,将负载白藜芦醇(RES)的 NLC 有效地整合到藻酸盐珠中。采用动态光散射(DLS)、扫描电子显微镜(SEM)、差示扫描量热法(DSC)和傅里叶变换红外光谱(FT-IR)评估,发现整合到藻酸盐珠中的 NLC 对其粒径、形态或内部结构没有显著影响。与 NLC 分散体和 NLC-Sol 相比,将 NLC 整合到藻酸盐珠中可提高其物理稳定性。体外释放研究发现,NLC-藻酸盐珠比优化的 NLC 制剂(RES-NLCs-opt)和 NLC-藻酸盐溶胶释放 RES 的速度更慢。在模拟体外消化模型的研究中发现,由于其粒径小,只有少量整合的 NLC 可能穿透胃液。NLC 从藻酸盐缓慢扩散到肠液中,防止了聚集,并允许脂质基质温和水解。将 NLC 整合到藻酸盐珠中有望改善其在消化过程中的稳定性、胃肠道行为和控制释放。
Naunyn Schmiedebergs Arch Pharmacol. 2024-11
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