Artemisinin emulgel ameliorates cartilage degradation in knee osteoarthritis: in vitro and in vivo studies.

IF 3 Q2 PHARMACOLOGY & PHARMACY
Samiksha Thote, Atul Mourya, Shristi Arya, Hoshiyar Singh, Prashanth Kumar, Santosh Kumar Guru, Jitender Madan
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Abstract

Aim: Laboratory scale-up of artemisinin-loaded emulgel (ART-emulgel) was carried out and characterized for therapeutic performance in osteoarthritis (OA).Materials & methods: The solubility of ART in various oils, surfactants and co-surfactants were screened for construction of pseudo ternary phase diagram (TPD), followed by scale-up of artemisinin loaded nanoemulsion (ART-NE). ART-NE was amalgamated with Carbopol Ultrez 10-NF to prepare ART-emulgel that was later characterized in vitro and in vivo to analyze therapeutic efficacy in monosodium-iodoacetate (MIA) induced knee OA.Results: The droplet diameter of ART-NE was estimated to be 104.3 ± 2.593 nm with a polydispersity index of 0.245 ± 0.019 in addition to ζ-potential of 0.434 ± 0.028 mV. Steady-state flux and permeability coefficient for ART-emulgel were estimated to be 0.651 ± 0.031 µg.cm2/h and 0.245 ± 0.011 cm/h, respectively. ART-emulgel demonstrated 43.18% reduction in COX-2 level; 52.28% drop in IL-1β, and 88.78% alleviation of Tumor Necrosis Factor-α (TNF-α) level when compared with monosodium-iodoacetate induced OA rats. ART-emulgel and injectable ART (intra-articular; I.A) portrayed minor synovial erosion compared with blank and diclofenac emulgel. Histopathological evidences indicated restoration of cartilage integrity followed by reduction of OARSI scores in ART-emulgel when compared with disease control animals.Conclusion: ART-emulgel is a potential dosage form for translating into a clinically viable product for the management of OA.

青蒿素凝胶改善膝关节骨关节炎软骨退化:体外和体内研究
目的:对青蒿素载体凝胶(ART-emulgel)进行实验室放大,并对其在骨关节炎(OA)中的治疗性能进行表征:筛选了青蒿素在各种油类、表面活性剂和辅助表面活性剂中的溶解度,构建了伪三元相图(TPD),随后对青蒿素负载纳米乳液(ART-NE)进行了放大。ART-NE与Carbopol Ultrez 10-NF混合制备成ART-emulgel,然后对其进行体外和体内表征,分析其对碘乙酸钠(MIA)诱导的膝关节OA的疗效:ART-NE 的液滴直径估计为 104.3 ± 2.593 nm,多分散指数为 0.245 ± 0.019,ζ电位为 0.434 ± 0.028 mV。估计 ART-emulgel 的稳态通量和渗透系数分别为 0.651 ± 0.031 µg.cm2/h 和 0.245 ± 0.011 cm/h。与碘乙酸钠诱导的 OA 大鼠相比,ART 胶体可降低 COX-2 水平 43.18%;IL-1β 降低 52.28%;肿瘤坏死因子-α(TNF-α)水平降低 88.78%。与空白和双氯芬酸凝胶相比,ART凝胶和注射用ART(关节内;I.A)的滑膜侵蚀程度较轻。组织病理学证据表明,与疾病对照组动物相比,ART-栓剂恢复了软骨的完整性,OARSI评分也随之降低:ART-emulgel 是一种潜在的剂型,可转化为临床上可行的产品用于治疗 OA。
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来源期刊
Therapeutic delivery
Therapeutic delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.50
自引率
0.00%
发文量
25
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.
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