In-vitro and In-silico Examinations on Baicalein-loaded Solid Lipid Nanoparticles for Neurodegeneration

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2024-01-25 DOI:10.2174/0122103031263883231230085819
Mansi Varshney, Bhavna Kumar, Poorvi Varshney, Diwya Kumar Lal, N. Sethiya
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Abstract

In the current scenario, most of the population affected by neurogenera-tive disorders like Alzheimer's, Parkinson's, Huntington's, etc., exist among the 10% population 65 years of age group. Neurodegenerative diseases are characterised as chronic and progressive disorders that occur due to the degeneration of neurons. Baicalein is a flavonoid glycoside derived from the roots of Scutellaria baicalensis. Earlier research suggested that it could be used to treat neurodegenerative illnesses. Baicalein, which was selected for the current study, was designed in-to a solid lipid nanoparticle (SLN) formulation. The SLNs have low permeability across BBB and are delivered by the non-invasive route, i.e., through nasal delivery. The In-silico docking studies were performed to examine and compare the binding affinity of Baicalein to already established drugs on the two most viable targets of Alzheimer's disease, i.e., Beta- secretase and Acetylcho-linesterase. The current work is to formulate and evaluate the Baicalein-loaded SLN for neuro-degenerative disorders via a non-invasive route. Baicalein loaded SLN was developed by solvent emulsification diffusion method, and formulation is characterised by using different parameters such as particle size analysis, zeta po-tential, scanning electron microscope, transverse electron microscope, X-ray diffraction, Differen-tial scanning calorimetric, Fourier transforms -infrared radiations, drug entrapment, in-vitro drug release and in-silico docking studies. The particle size of Baicalein-loaded SLN was 755.2 ± 0.48 nm, the Polydispersity index was 0.06, and the zeta potential was -32.5 ± 0.36 mV. The drug entrapment and loading efficien-cy of the optimised formulation were found to be 94% ± 0.653 and 18.2% ± 0.553, respectively. Optimised formulation shows 84.6% ± 0.3% of drug release within 30 minutes, which demon-strates the sustained release of the drug. Baicalein-loaded SLN is formulated and evaluated for the treatment of neurodegen-erative disorders. SLN is an approach to overcome the challenge of bypassing the BBB by admin-istering the drug via an intranasal route. Hence, when analysed together with the results of Bai-calein-loaded SLN and in-silico studies, it was correlated that Baicalein proved to have a targeted moiety for neurodegeneration.
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用于神经退行性病变的黄芩苷载体固体脂质纳米粒子的体外和体内研究
目前,大多数神经退行性疾病(如阿尔茨海默氏症、帕金森氏症、亨廷顿氏症等)的患者都集中在 65 岁以上的人群中。神经退行性疾病的特点是由于神经元退化而导致的慢性和进行性疾病。黄芩苷是从黄芩根中提取的一种黄酮苷。早期的研究表明,它可用于治疗神经退行性疾病。本次研究选择的黄芩苷被设计成固体脂质纳米粒子(SLN)配方。这种固体脂质纳米粒子在生物BB中的渗透性很低,可通过非侵入性途径(即鼻腔给药)给药。为了研究和比较黄芩苷与阿尔茨海默氏症的两个最有效靶点--β-分泌酶和乙酰胆碱酯酶--上已有药物的结合亲和力,我们进行了硅对接研究、目前的工作是通过非侵入性途径配制和评估负载黄芩素的 SLN,以治疗神经退行性疾病。采用溶剂乳化扩散法研制出了负载黄芩素的 SLN,并利用粒度分析、zeta 电位、扫描电子显微镜、横向电子显微镜、X 射线衍射、差示扫描量热法、傅立叶变换红外辐射、药物夹带、体外药物释放和微观对接研究等不同参数对配方进行了表征。负载黄芩素的 SLN 的粒径为 755.2 ± 0.48 nm,多分散指数为 0.06,Zeta 电位为 -32.5 ± 0.36 mV。优化配方的药物夹带率和装载率分别为 94% ± 0.653 和 18.2% ± 0.553。优化配方在 30 分钟内的药物释放率为 84.6% ± 0.3%,这表明了药物的持续释放。通过鼻内给药途径,SLN 克服了绕过 BBB 的难题。因此,结合白头翁苷载体 SLN 和室内研究的结果进行分析,证明白头翁苷具有治疗神经退行性疾病的靶向分子。
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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