Illuminating Insights: Clinical Study Harnessing Pharmacoscintigraphy for Permeation Study of Radiolabeled Nimesulide Topical Formulation in Healthy Human Volunteers.

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Assay and drug development technologies Pub Date : 2023-10-01 Epub Date: 2023-10-06 DOI:10.1089/adt.2023.053
Nitin Sharma, Kushagra Khanna, Neeraj Kumar, Ritu Karwasra, Ashok Kumar Janakiraman, Mogana Sundari Rajagopal
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Abstract

An alternative to oral administration for the delivery of therapeutic substances is the topical route, which frequently has comparable efficacy but may have a better tolerability profile. Gamma scintigraphy is a noninvasive technique that involves the application of radioactive substances to conduct biodistribution studies of therapeutic substances delivered through various routes. Nimesulide (NSD) was radiolabeled with technetium pertechnetate (Technetium99m [99mTc]) and this radiolabeled drug complex (99mTc-NSD) was used to prepare a topical gel formulation. The permeation of the radiolabeled drug from the topical gel was determined by gamma scintigraphy on human volunteers. The region of interest was calculated for the quantification of permeated radiolabeled drugs. This was observed that the mean percentage permeation of 99mTc-NSD was found to be 0.32 ± 0.22 to 36.37 ± 2.86 at 5 and 240 min. It was demonstrated that gamma scintigraphy may be a noninvasive and reliable technique for the determination of drug permeation through topical routes.
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启发性见解:利用药物闪烁扫描在健康人体志愿者中进行放射性标记尼美舒利局部制剂渗透性研究的临床研究。
用于递送治疗物质的口服给药的替代方案是局部给药途径,该途径通常具有类似的疗效,但可能具有更好的耐受性。伽马闪烁扫描是一种非侵入性技术,涉及应用放射性物质对通过各种途径输送的治疗物质进行生物分布研究。尼美舒利(NSD)用高锝酸锝(99mTc]锝)放射性标记,这种放射性标记的药物复合物(99mTc-NSD)用于制备局部凝胶制剂。放射性标记药物从局部凝胶中的渗透是通过人体志愿者的γ闪烁扫描法测定的。计算感兴趣区域,用于渗透放射性标记药物的定量。观察到99mTc-NSD的平均渗透百分比为0.32 ± 0.22至36.37 ± 2.86在5和240 min。研究表明,γ闪烁扫描法可能是一种非侵入性和可靠的技术,用于通过局部途径测定药物渗透。
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来源期刊
Assay and drug development technologies
Assay and drug development technologies 医学-生化研究方法
CiteScore
3.60
自引率
0.00%
发文量
33
审稿时长
>12 weeks
期刊介绍: ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts
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