Neuroprotective efficiency of celecoxib vesicular bilosomes for the management of lipopolysaccharide-induced Alzheimer in mice employing 2³ full factorial design.

IF 4.6 2区医学 Q2 IMMUNOLOGY Inflammopharmacology Pub Date : 2024-12-01 Epub Date: 2024-07-17 DOI:10.1007/s10787-024-01522-y

Asmaa Badawy Darwish, Abeer Salama, Mostafa Mohammed Younis

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Abstract

The aim of this study was to develop and evaluate bilosomes loaded with Celecoxib (CXB) for the efficient treatment of Alzheimer. The thin-film hydration approach was utilized in the formulation of CXB bilosomes (CXB-BLs). The study used a 2³-factorial design to investigate the impact of several formulation variables. Three separate parameters were investigated: bile salt type (X₁), medication amount (X₂), and lipid-bile salt ratio (X₃). The dependent responses included entrapment efficiency (Y₁: EE %), particle size (Y₂: PS), and zeta potential (_Y3: ZP). The formulation factors were statistically optimized using the Design-Expert^® program. The vesicles demonstrated remarkable CXB encapsulation efficiency, ranging from 94.16 ± 1.91 to 98.38 ± 0.85%. The vesicle sizes ranged from 241.8 ± 6.74 to 352 ± 2.34 nm. The produced formulations have high negative zeta potential values, indicating strong stability. Transmission electron microscopy (TEM) revealed that the optimized vesicles had a spherical form. CXB release from BLs was biphasic, with the release pattern following Higuchi's model. In vivo studies confirmed the efficiency of CXB-BLs in management of lipopolysaccharide-induced Alzheimer as CXB-BLs ameliorated cognitive dysfunction, decreased acetylcholinesterase (AChE), and inhibited neuro-inflammation and neuro-degeneration through reducing Toll-like receptor (TLR4), and Interleukin-1β (IL-1β) levels. The findings suggested that the created CXB-BLs could be a potential drug delivery strategy for Alzheimer's treatment.

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采用23全因子设计的塞来昔布囊状双体对脂多糖诱发的小鼠阿尔茨海默病的神经保护作用。

本研究旨在开发和评估负载有塞来昔布（CXB）的双管状体，以有效治疗老年痴呆症。在配制 CXB 双糖体（CXB-BLs）时采用了薄膜水合方法。该研究采用了 23 个因子设计来研究多个制剂变量的影响。研究了三个独立的参数：胆汁盐类型（X1）、用药量（X2）和脂质-胆汁盐比例（X3）。因果反应包括夹带效率（Y1：EE %）、粒度（Y2：PS）和 zeta 电位（Y3：ZP）。使用 Design-Expert® 程序对配方因素进行了统计优化。囊泡的 CXB 包封效率非常高，从 94.16 ± 1.91% 到 98.38 ± 0.85%。囊泡尺寸从 241.8 ± 6.74 纳米到 352 ± 2.34 纳米不等。制备的制剂具有较高的负 zeta 电位值，表明其具有很强的稳定性。透射电子显微镜（TEM）显示，优化后的囊泡呈球形。CXB 从 BLs 中的释放是双相的，释放模式遵循樋口模型。体内研究证实，CXB-BLs 能有效治疗脂多糖诱发的阿尔茨海默病，因为 CXB-BLs 能改善认知功能障碍，降低乙酰胆碱酯酶（AChE），并通过降低 Toll 样受体（TLR4）和白细胞介素-1β（IL-1β）水平来抑制神经炎症和神经变性。研究结果表明，创造出的CXB-BLs可能是治疗阿尔茨海默氏症的一种潜在药物输送策略。

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来源期刊

Inflammopharmacology IMMUNOLOGYTOXICOLOGY-TOXICOLOGY

CiteScore

8.00

自引率

3.40%

发文量

200

期刊介绍： Inflammopharmacology is the official publication of the Gastrointestinal Section of the International Union of Basic and Clinical Pharmacology (IUPHAR) and the Hungarian Experimental and Clinical Pharmacology Society (HECPS). Inflammopharmacology publishes papers on all aspects of inflammation and its pharmacological control emphasizing comparisons of (a) different inflammatory states, and (b) the actions, therapeutic efficacy and safety of drugs employed in the treatment of inflammatory conditions. The comparative aspects of the types of inflammatory conditions include gastrointestinal disease (e.g. ulcerative colitis, Crohn''s disease), parasitic diseases, toxicological manifestations of the effects of drugs and environmental agents, arthritic conditions, and inflammatory effects of injury or aging on skeletal muscle. The journal has seven main interest areas: -Drug-Disease Interactions - Conditional Pharmacology - i.e. where the condition (disease or stress state) influences the therapeutic response and side (adverse) effects from anti-inflammatory drugs. Mechanisms of drug-disease and drug disease interactions and the role of different stress states -Rheumatology - particular emphasis on methods of measurement of clinical response effects of new agents, adverse effects from anti-rheumatic drugs -Gastroenterology - with particular emphasis on animal and human models, mechanisms of mucosal inflammation and ulceration and effects of novel and established anti-ulcer, anti-inflammatory agents, or antiparasitic agents -Neuro-Inflammation and Pain - model systems, pharmacology of new analgesic agents and mechanisms of neuro-inflammation and pain -Novel drugs, natural products and nutraceuticals - and their effects on inflammatory processes, especially where there are indications of novel modes action compared with conventional drugs e.g. NSAIDs -Muscle-immune interactions during inflammation [...]