Development of Stabilized and Aqueous Dissolvable Nanosuspension Encompassing BCS Class IV Drug via Optimization of Process and Formulation Variables.

IF 2 4区 材料科学 Q3 MATERIALS SCIENCE, MULTIDISCIPLINARY
Surya Goel, Vijay Agarwal, Monika Sachdeva
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引用次数: 0

Abstract

Background: Nanosuspension has emerged as an effective, lucrative, and unequalled approach for efficiently elevating the dissolution and bioavailability of aqueous soluble drugs. Diverse challenges persist within this domain, demanding further comprehensive investigation and exploration.

Objective: This study aims to design, develop, optimise formulation and process variables, and characterise the stabilised aqueous dissolvable nanosuspension using chlorthalidone as a BCS class- IV drug.

Methods: Nanosuspensions of the chlorthalidone drug were prepared using a combination of topdown and bottom-up approaches. Various polymers such as Pluronic L-64, F-68, F-127, and Synperonic F-108 were used as stabilisers in this research. All important processes and formulation variables, such as ultrasonication intensity and time, the concentration of the drug, organic solvent, and stabilisers that may critically influence the characteristics of the nanosuspensions, were optimised. Formulation screening was performed using the optimisation of process and formulation variables, and the optimised nanosuspension formulation was assessed for particle size, PDI, surface charge, morphology, in vitro drug release, and stability.

Results: To select an optimised nanosuspension formulation, the effects of formulation and process variables were investigated. These variables critically influence the development of a stabilised nanosuspension. The outcomes revealed that the nanosuspension formulation containing pluronic F- 68 as a stabiliser in 0.6% w/v concentration and the drug in 4 mg/ml concentration were optimized. The particle size and zeta potential of the optimised preparation were 110 nm and -27.5 mV, respectively. The in-vitro drug release of chlorthalidone drug from the optimised nanoformulation was increased up to 3-fold, approximately (88% in 90 min) compared with pure chlorthalidone drug (27% in 90 min) because of the decrease in particle size. Moreover, stability studies indicated that the crafted nanoformulation was stable at cold (4℃) as well as normal room temperature (25℃) for six months.

Conclusion: From the obtained results, it was concluded that the combination of top-down and bottom- up approaches employed for the fabrication of oral nanosuspension is a remunerative and lucrative approach to successfully resolve the perplexities associated with the dissolution rate of poorly aqueous soluble BCS class-IV drug moieties such as chlorthalidone.

通过工艺和配方优化制备含BCS IV类药物的稳定水溶性纳米混悬液。
背景:纳米悬浮液作为一种有效的、有利可图的、无与伦比的提高水溶性药物溶出度和生物利用度的方法已经出现。这一领域面临着各种各样的挑战,需要进一步全面的调查和探索。目的:设计、研制、优化氯噻酮作为BCS - IV类药物的水溶纳米混悬液的配方和工艺参数,并对其进行表征。方法:采用自上而下和自下而上相结合的方法制备氯噻酮纳米混悬液。多种聚合物如Pluronic L-64、F-68、F-127和Synperonic F-108在本研究中被用作稳定剂。所有重要的工艺和配方变量,如超声强度和时间、药物浓度、有机溶剂和稳定剂,可能会严重影响纳米混悬液的特性,都进行了优化。通过优化工艺和配方变量进行配方筛选,并对优化后的纳米混悬液配方进行粒径、PDI、表面电荷、形貌、体外药物释放和稳定性评估。结果:考察了配方和工艺因素对纳米混悬液的影响,优选出最佳的纳米混悬液配方。这些变量严重影响稳定纳米悬浮液的发展。结果表明,以pluronic F- 68为稳定剂,浓度为0.6% w/v,药物浓度为4 mg/ml的纳米混悬液最优配方。优化后的材料粒径为110 nm, zeta电位为-27.5 mV。由于粒径减小,优化后的纳米制剂氯噻酮药物的体外释放量比纯氯噻酮药物(90分钟内释放量为27%)增加了约3倍(90分钟内释放量为88%)。此外,稳定性研究表明,制备的纳米制剂在低温(4℃)和常温(25℃)下稳定6个月。结论:采用自上而下和自下而上相结合的方法制备口服纳米混悬液,成功解决了氯噻酮等难溶性BCS iv类药物的溶出率问题。
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来源期刊
Recent Patents on Nanotechnology
Recent Patents on Nanotechnology NANOSCIENCE & NANOTECHNOLOGY-MATERIALS SCIENCE, MULTIDISCIPLINARY
CiteScore
4.70
自引率
10.00%
发文量
50
审稿时长
3 months
期刊介绍: Recent Patents on Nanotechnology publishes full-length/mini reviews and research articles that reflect or deal with studies in relation to a patent, application of reported patents in a study, discussion of comparison of results regarding application of a given patent, etc., and also guest edited thematic issues on recent patents in the field of nanotechnology. A selection of important and recent patents on nanotechnology is also included in the journal. The journal is essential reading for all researchers involved in nanotechnology.
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