设计配方的体外表征和体内抗糖尿病研究:纳米海绵和纳米糖晶体

IF 3 Q2 PHARMACOLOGY & PHARMACY
Preeti Aneja, Rajender Guleria, Dev Prakash Dahiya
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引用次数: 0

摘要

糖尿病是世界范围内死亡的主要根源,也是到2030年死亡的主要原因。随着全球医疗格局的变化,糖尿病对标准治疗方法提出了严峻的挑战。用于治疗的口服胰岛素有一些缺点,包括由于降解酶和低吸收导致胃肠道系统不稳定,从而导致相对较差的吸收。纳米技术通过靶向和精确的给药,为糖尿病治疗带来了巨大的可能性。在各种纳米剂型中,纳米海绵和纳米晶体被认为是最适合糖尿病治疗的策略。本研究旨在通过将伏糖糖包埋在伏糖糖纳米海绵制剂(V-NSF)和伏糖糖纳米晶体制剂(V-NCF)中来提高伏糖糖的生物利用度。采用Box-Behnken设计成功地进行了实验设计。对响应参数(主要是粒径、捕获效率和PDI)进行了推测,然后利用粒径分析仪和捕获效率方法获得了观测值。采用体外释药、FTIR、热分析(DSC和XRD)、表面形貌(SEM)等表征参数对结果进行分析,并对优化后的制剂进行稳定性研究,并对Sprague-Dawley大鼠进行体内研究。结果V-NSF的粒径为270.63±5.9 nm, PDI值为0.165±0.027。捕集效率为78±0.32%。V-NCF的粒径为131±0.31 nm, PDI值为0.140±0.006,包封效率为74±0.28%。通过FTIR、SEM、DSC、XRD和体外释放度等方法对其理化表征参数进行了验证。结论v - nsf和V-NCF粒径分布受限,多分散指数可接受,捕获效率值较大。药效学研究表明,与V-NCF相比,V-NSF具有显著的降糖作用,与voglibose相比,其降糖作用中等。优化配方的数据可用于临床意义,并提示V-NSF和V-NCF可有效治疗糖尿病。图形抽象
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro characterization and in vivo antidiabetic studies of designed formulations: nanosponges and nanocrystals of voglibose

Background

Diabetes mellitus is the main root of mortality worldwide and a major cause of death by 2030. As the global medical landscape shifts, diabetes presents a serious challenge to standard treatment methods. Orally administered insulin, used for treatment, has drawbacks including instability in the gastrointestinal system due to degrading enzymes and low absorption, resulting in comparatively poor uptake. Nanotechnology introduces remarkable possibilities for diabetes treatment through targeted and accurate drug delivery. Among various nanodosage forms, nanosponges and nanocrystals are considered the most appropriate strategy for diabetes care. The study intends to enhance the bioavailability of voglibose by encapsulating it in a voglibose nanosponges formulation (V-NSF) and a voglibose nanocrystals formulation (V-NCF). Design of experimentation was successfully carried out using the Box–Behnken design. The response parameters, essentially particle size, entrapment efficiency and PDI, have been speculated, followed by observed values using a particle size analyzer and entrapment efficiency methods. Various characterization parameters, such as in vitro drug release, FTIR, thermal analysis (DSC and XRD) and surface morphology (SEM), were used to analyze the results, accompanied by stability studies of the optimized formulation and in vivo studies performed using Sprague–Dawley rats.

Results

The particle size of V-NSF was 270.63 ± 5.9 nm, and the PDI value was 0.165 ± 0.027. Entrapment efficiency was 78 ± 0.32%. In case of V-NCF, particle size was analyzed as 131 ± 0.31 nm, PDI value of NCF was 0.140 ± 0.006, and entrapment efficiency was 74 ± 0.28%. All physical and chemical characterization parameters were confirmed by FTIR, SEM, DSC, XRD and in vitro release.

Conclusion

V-NSF and V-NCF exhibited confined size distribution, acceptable polydispersity index and greater value of entrapment efficiency. The pharmacodynamic studies showed that V-NSF elicits a remarkable antidiabetic effect compared to V-NCF, with moderate efficacy than voglibose itself. The data of optimized formulations can be useful for clinical implications and suggest that V-NSF and V-NCF could be effective in diabetic management.

Graphical abstract

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来源期刊
自引率
0.00%
发文量
44
审稿时长
23 weeks
期刊介绍: Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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