Enhanced bioavailability and efficacy in antimalarial treatment through QbD approach enteric encased inclusion delivery.

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-09-03 DOI:10.1080/20415990.2024.2377948

Neha Bajwa, Preet Amol Singh, Sumant Kumar, Girish Chandra Arya, Ashish Baldi

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Abstract

Aim: In this study, we aimed to prepare enteric encapsulated spheroids containing inclusion complex using quality by design approach.Methods: A Box-Behnken design was employed to determine effects of variables on selected responses. Risk assessment was conducted using Ishikawa fishbone diagram. A model with a p-value was less than 0.5 for being a significant error of model was determined based on significance 'lack of fit' value. Spheroids were formulated using the extrusion spheronization technique and were characterized using analytical techniques.Results: In vitro release was performed in both acidic (pH 1.2) and simulated intestinal (pH 6.8) conditions. Permeability studies demonstrated tenfold enhancement compared with arteether. In vivo studies further validated increase of 51.8% oral bioavailability. Ex vivo studies revealed 3.4-fold enhancement in antimalarial activity compared with arteether.Conclusion: These findings highlight effectiveness of inclusion complexation technique as a viable approach to enhance solubility and bioavailability for drugs with low aqueous solubility.

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通过 QbD 方法肠溶包合物给药提高抗疟治疗的生物利用度和疗效。

目的：在本研究中，我们旨在采用质量设计法制备含有包涵复合物的肠道包裹球。方法采用方框-贝肯设计来确定变量对选定反应的影响。使用石川鱼骨图进行风险评估。根据显著性 "不拟合 "值，确定 p 值小于 0.5 的模型为显著误差模型。使用挤压球化技术配制球体，并使用分析技术对其进行表征。结果：在酸性（pH 值为 1.2）和模拟肠道（pH 值为 6.8）条件下进行了体外释放。渗透性研究表明，与蒿甲醚相比，蒿甲醚的渗透性提高了十倍。体内研究进一步验证了口服生物利用率提高了 51.8%。体内外研究表明，与蒿甲醚相比，其抗疟活性提高了 3.4 倍。结论：这些研究结果凸显了包合复合物技术的有效性，它是提高低水溶性药物的溶解度和生物利用度的一种可行方法。

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.