Formulation and Characterization of Nanoparticulate Drug Carrier System for Lacidipine.

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Assay and drug development technologies Pub Date : 2023-10-01 DOI:10.1089/adt.2023.023
Ashveta Anant Dessai, Mrunali Navin Kantak, Cleona Elizabeth Mary DCruz, Lalit Kumar, Prashant Jivaji Bhide, Rupesh Kalidas Shirodkar
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Abstract

Lacidipine, a calcium channel antagonist, is primarily used to treat hypertension. It is classified as a Biopharmaceutics Classification System Class II drug and exhibits an oral bioavailability of 10% due to its extensive hepatic first-pass metabolism. This research study focused on formulating lacidipine-loaded cubosomal nanovesicles developed into rapidly dissolving oral films as an alternative to overcome the downsides faced by conventional antihypertensive therapy. Lacidipine-loaded cubosomes were prepared utilizing a top-down technique using lipid and surfactant and were further developed into fast dissolving oral films. Box-Behnken design was used for the optimization of process variables to achieve minimum particle size and greater entrapment efficiency of the nanovesicles, and response data were statistically evaluated. The optimized cubosomal dispersions upon characterization reported particle size within nanorange (116.8-341 nm) and an entrapment efficiency of 88.15%-97.1%, with 91.72% of total drug content. Morphological studies revealed uniformly dispersed vesicles with cubic to spherical shape. Oral rapidly dissolving films, after evaluation, were reported to have transparent to opaque appearance with a highly porous nature, which was confirmed by scanning electron microscopic imaging and displayed uniformity in weight and thickness and reported optimum mechanical strength and considerable flexibility, with disintegration time of 37.67 ± 3.68 s and exhibited 91.44% ± 1.65% in vitro drug release after 6 min. Short-term stability studies conducted on films at 25°C ± 2°C and 60% ± 5% relative humidity for 3 months demonstrated no significant variation in morphological and mechanical properties. Therefore, lacidipine-loaded cubosomal rapid dissolving oral films may be a promising formulation approach for the management of hypertension.

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拉西地平纳米药物载体体系的制备与表征。
拉西地平是一种钙通道拮抗剂,主要用于治疗高血压。它被归类为生物制药分类系统II类药物,由于其广泛的肝脏首过代谢,口服生物利用度为10%。这项研究的重点是将负载拉西地平的立方体纳米囊泡配制成快速溶解的口腔膜,作为克服传统降压治疗所面临不利影响的替代方案。利用脂质和表面活性剂自上而下的技术制备了负载拉西地平的立方体,并进一步发展为快速溶解的口腔膜。Box-Behnken设计用于优化过程变量,以实现纳米囊泡的最小粒径和更高的包封效率,并对响应数据进行统计评估。表征后优化的立方体分散体的粒径在纳米范围内(116.8-341 包封率为88.15%-97.1%,占总药物含量的91.72%。形态学研究显示,囊泡均匀分散,呈立方体至球形。经评估,口服快速溶解薄膜具有透明至不透明的外观,具有高度多孔性,扫描电子显微镜成像证实了这一点,显示出重量和厚度的均匀性,并报告了最佳机械强度和相当大的柔韧性,崩解时间为37.67 ± 3.68 s,显示91.44% ± 6天后1.65%的体外药物释放 最小25°C下对薄膜进行的短期稳定性研究 ± 2°C和60% ± 5%的相对湿度持续3个月,表明形态和机械性能没有显著变化。因此,拉西地平负载的立方体快速溶解口服膜可能是治疗高血压的一种很有前途的制剂方法。
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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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