Optimization and Fabrication of Curcumin Loaded Solid Lipid Nanoparticles using Box-Behnken Design for Nasal Delivery

S. Bhatt, Sherry, Jai Bharti Sharma, M. Nireekshan Kumar
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Abstract

To prepare curcumin loaded solid lipid nanoparticles for nasal administration using Box-Behnken design. The effectiveness of curcumin in neurological disorders is widely studied by various researchers, but its use is limited due to its poor bioavailability. The brain-targeting efficiency of curcumin can be improved using solid lipid nanoparticles via nasal administration. In present work, Curcumin loaded solid lipid nanoparticles (CUR-SLN) were formulated and optimized for nasal administration. In the present work, Curcumin loaded solid lipid nanoparticles (CUR-SLN) were formulated and optimized for nasal administration. On the basis of solubility, cetostearyl alcohol as lipid and Poloxamer 407 as surfactant were selected for further studies. Box-Behnken design (BBD) was used to analyze effects of drug to lipid ratio (X1), surfactant concentration (X2) and homogenization time (X3) on particle size (Y1) & % entrapment efficiency (Y2). The CUR-SLN were formulated by high shear homogenization method. The optimized formulation was evaluated for DSC, TEM, drug release & ex-vivo studies. Based on solubility studies, cetostearyl alcohol and poloxamer 407 were selected as lipid and surfactant, respectively. Box-Behnken design (BBD) was used to analyze the effects of drug-to-lipid ratio (X1), surfactant concentration (X2) and homogenization time (X3) on particle size (Y1) and % entrapment efficiency (Y2). The CUR-SLN were formulated by the high shear homogenization method. The optimized formulation was evaluated for DSC, TEM, drug release and ex-vivo studies. Good results were obtained for the particle size and entrapment efficiency analyzed using BBD. The optimized formulation of CUR-SLN obtained using BBD was observed with a particle size of 96.09 nm and % EE of 78.23. In-vitro release of the drug was found to be 82.93± 0.15% after 8 hours. DSC studies revealed that crystalline form of curcumin changed to an amorphous form in SLN. TEM results of optimized CUR-SLN were in correlation with the results obtained using a zeta sizer. No harmful effects were observed on nasal mucosa in the histopathology study. Good results were obtained for the particle size and entrapment efficiency analyzed using the BBD. The optimized formulation of CUR-SLN obtained using BBD was observed with particle size of 96.09 nm The SLN can be safely utilized for the intranasal administration of curcumin. The SLN can be safely utilized for the nasal administration of the curcumin. Nasal administration of curcumin-loaded SLN
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基于Box-Behnken设计的姜黄素固体脂质纳米颗粒鼻腔给药优化制备
采用box - behnken设计制备含姜黄素的固体脂质纳米颗粒鼻腔给药。姜黄素治疗神经系统疾病的有效性已被众多研究者广泛研究,但由于其生物利用度较差,其应用受到限制。固体脂质纳米颗粒可通过鼻腔给药提高姜黄素的脑靶向效率。本研究制备了姜黄素固体脂质纳米粒(curc - sln),并对其鼻腔给药进行了优化。本研究制备了姜黄素固体脂质纳米粒(curr - sln),并对其鼻腔给药方式进行了优化。在溶解度的基础上,选择鲸脂醇作为脂质,poloxam407作为表面活性剂进行进一步的研究。采用Box-Behnken设计(BBD)分析药脂比(X1)、表面活性剂浓度(X2)和均质时间(X3)对颗粒大小(Y1)和%包埋效率(Y2)的影响。采用高剪切均质法制备了cu - sln。对优化后的制剂进行了DSC、TEM、药物释放和离体研究。基于溶解度的研究,选择乙醇硬脂醇和poloxam407分别作为脂质和表面活性剂。采用Box-Behnken设计(BBD)分析药脂比(X1)、表面活性剂浓度(X2)和均质时间(X3)对颗粒大小(Y1)和包裹率(Y2)的影响。采用高剪切均质法制备了cu - sln。对优化后的制剂进行DSC、TEM、药物释放和离体研究。采用BBD法对颗粒粒径和捕集效率进行了分析,得到了较好的结果。采用BBD法制备的CUR-SLN最佳配方粒径为96.09nm, EE %为78.23。8 h后的体外释放度为82.93±0.15%。dsc研究表明,姜黄素在SLN中结晶形态转变为无定形形态。优化后的cu - sln的TEM结果与zeta浆料机的结果具有较好的相关性。组织病理学检查未见对鼻黏膜有不良影响。利用BBD对颗粒大小和捕集效率进行了分析,得到了较好的结果。采用BBD法制备的curc -SLN的最佳配方粒径为96.09 nm,可安全用于姜黄素的鼻内给药。SLN可以安全地用于姜黄素的鼻腔给药。姜黄素负载SLN的鼻腔给药
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来源期刊
Nanoscience and Nanotechnology - Asia
Nanoscience and Nanotechnology - Asia Engineering-Engineering (all)
CiteScore
1.90
自引率
0.00%
发文量
35
期刊介绍: Nanoscience & Nanotechnology-Asia publishes expert reviews, original research articles, letters and guest edited issues on all the most recent advances in nanoscience and nanotechnology with an emphasis on research in Asia and Japan. All aspects of the field are represented including chemistry, physics, materials science, biology and engineering mainly covering the following; synthesis, characterization, assembly, theory, and simulation of nanostructures (nanomaterials and assemblies, nanodevices, nano-bubbles, nano-droplets, nanofluidics, and self-assembled structures), nanofabrication, nanobiotechnology, nanomedicine and methods and tools for nanoscience and nanotechnology.
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