Curcumin- β-Cyclodextrin Molecular Inclusion Complex: A Water-Soluble Complex in Fast-dissolving Tablets for the Treatment ofNeurodegenerative Disorders.

Q2 Pharmacology, Toxicology and Pharmaceutics Pharmaceutical nanotechnology Pub Date : 2024-01-01 DOI:10.2174/0122117385273171231120051021

Sruthi Laakshmi Mugundhan, Purushothaman Balasubramaniyan, Damodharan Narayanasamy, Mothilal Mohan

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Abstract

Background: Orally disintegrating tablets (ODTs) have become an excellent choice for delivering drugs as their palatability is greatly improved. In this work, β-cyclodextrin has been used to improve the solubility of curcumin by encapsulating it into the hydrophobic cavity for the treatment of neurodegenerative disorders.

Objectives: The current study aimed to present the design, formulation, and optimisation of fastdissolving oral tablets of curcumin- β-cyclodextrin molecular inclusion complex using a 3²-factorial design.

Methods: The drug-excipient compatibility was studied by FTIR spectroscopy. The inclusion complex of curcumin-β-cyclodextrin was prepared using solvent casting and confirmed using XRD studies. Powder blends were evaluated for flow properties. Tablets prepared by direct compression were evaluated for post-compression parameters. Further, the effect of formulation variables, such as sodium starch glycolate (X1) and Neusilin^® ULF2 (X2), on various responses, including disintegration time and dissolution at 2 hours, was studied using statistical models.

Results: Post-compression parameters, i.e., hardness (4.4-5 kg/cm²), thickness (3.82-3.93 mm), weight variation (±7.5%), friability (< 1%), wetting time (51-85 seconds) and drug content (96.28- 99.32%) were all found to be within the permissible limits and the disintegration time of tablets with super-disintegrants ranged between 45-58 seconds. The in-vitro dissolution profile of tablets showed that higher SSG and Neuslin^® ULF2 levels promoted drug release. For statistical analysis, the 2FI model was chosen. Optimised variables for formulation have been determined and validated with the experimental findings based on the significant desirability factor.

Conclusion: The current study reveals the validated curcumin-β-cyclodextrin inclusion complex fastdissolving tablets with SSG and Neusilin^® ULF2 to be an ideal choice for effectively treating neurodegenerative disorders.

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姜黄素-β-环糊精分子包合物：用于治疗神经退行性疾病的速溶片剂水溶性复合物。

背景：口腔崩解片（ODTs）的适口性大大提高，因此已成为一种极佳的给药选择。在这项研究中，β-环糊精通过将姜黄素包裹在疏水性空腔中来提高姜黄素的溶解度，用于治疗神经退行性疾病：本研究旨在以淀粉乙醇酸钠（SSG）和 Neusilin® ULF2 为独立因素，采用 32 因子设计法设计、配制和优化姜黄素-β-环糊精分子包合物速溶口服片剂：傅立叶变换红外光谱法研究了药物与辅料的相容性。采用溶剂浇铸法制备姜黄素-β-环糊精包合物，并通过 XRD 研究加以确认。对混合粉末的流动性能进行了评估。对直接压片法制备的片剂进行了压片后参数评估。此外，还使用统计模型研究了淀粉乙醇酸钠（X1）和 Neusilin® ULF2（X2）等制剂变量对各种反应（包括崩解时间和 2 小时溶出度）的影响：结果：压缩后的参数，即硬度（4.4-5 kg/cm2）、厚度（3.82-3.93 mm）、重量变化（±7.5%）、易碎性（结论：压缩后的产品具有较好的稳定性和可塑性：目前的研究表明，经过验证的含有 SSG 和 Neusilin® ULF2 的姜黄素-β-环糊精包合物速溶片剂是有效治疗神经退行性疾病的理想选择。

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来源期刊

Pharmaceutical nanotechnology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

4.20

自引率

0.00%

发文量

期刊介绍： Pharmaceutical Nanotechnology publishes original manuscripts, full-length/mini reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.