用于雾化的自纳米乳化给药系统:用于阿托伐他汀全身给药的制造和评估。

IF 3.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Muhammad Danish Saeed, Kifayat Ullah Shah, Muhammad Fahad, Shefaat Ullah Shah, Syed Faisal Badshah, Hassan Shah, Irfan Anjum, Gamal A Shazly, Mohammed Bourhia
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引用次数: 0

摘要

本研究开发了一种阿托伐他汀自纳米乳化给药系统(SNEDDS),以提高其生物利用度。研究人员使用油酸、吐温 80 和斯盘 80 通过自发乳化法制成了 SNEDDS。对 SNEDDS 的粒度分布、zeta 电位、形态、药物含量、表面张力、粘度和药物释放进行了评估。使用安徒生级联冲击器评估了 SNEDDS 的空气动力学性能,并使用 "Microlab 300 "分析仪测定了 SNEDDS 在 Wistar 大鼠体内的降脂潜力。SNEDDS 的粒径范围为 36 至 311 nm,多分散指数(PDI)为 0.25 至 0.40。SNEDDS 的 zeta 电位在 - 29.22 至 - 38.26 mV 之间波动,F5 的 zeta 电位降至 - 4.55 mV。与其他制剂(F1-F4)相比,壳聚糖包衣制剂(F5)表现出更高的粘度(22.12 mPa s)和更低的表面张力(0.056 dyne/cm)。与包衣制剂(F5)相比,非包衣制剂表现出明显较高的猝发释药率,随后出现持续释药模式(p ≤ 0.05)。雾化 SNEDDS 的分散度达到 87% 至 97%,其中 F4 的气溶胶分散度明显更高,这归因于其较小的粒径和圆度。雾化 SNEDDS 的吸入率为 74-87%。在雾化过程中,SNEDDS 液滴的大小是影响 SNEDDS 空气动力学性能的主要决定因素。壳聚糖包衣的SNEDDS比市场上销售的片剂具有更高的降血脂效果,这表明F5适用于通过肺部有效地全身给药阿托伐他汀。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Self-nanoemulsifying drug delivery system for nebulization: fabrication and evaluation for systemic delivery of atorvastatin.

The study undertakes the development of an atorvastatin-loaded self-nanoemulsifying drug delivery system (SNEDDS) to improve its bioavailability. The SNEDDS were fabricated using oleic acid, Tween 80, and Span 80 by spontaneous emulsification. The SNEDDS were assessed for their particle size distribution, zeta potential, morphology, drug content, surface tension, viscosity, and drug release. The aerodynamic performance of the SNEDDS was evaluated using an Andersen cascade impactor, while the lipid-lowering potential of the SNEDDS was determined in Wistar rats using the analyzer "Microlab 300." The particle size of the SNEDDS ranged from 36 to 311 nm, with a polydispersity index (PDI) of 0.25-0.40. The zeta potential of the SNEDDS fluctuated from - 29.22 to - 38.26 mV, which declined to - 4.55 mV in the case of F5. The chitosan-coated formulation (F5) exhibited a higher viscosity (22.12 mPa s) and lower surface tension (0.056 dyne/cm) than other formulations (F1-F4). The non-coated formulation exhibited a significantly higher burst drug release, followed by a sustained drug release pattern (p ≤ 0.05) as compared to the coated formulation (F5). The nebulized SNEDDS achieved a dispersed fraction of 87 to 97%, where notably higher aerosol dispersion from F4 was attributed to its smaller particle size and circularity. The inhaled fraction of nebulized SNEDDS was 74-87%. The size of the SNEDDS droplets was the primary determinant affecting the aerodynamic performance of the SNEDDS during nebulization. The chitosan-coated SNEDDS achieved a higher antihyperlipidemic effect than marketed tablets, which shows the suitability of F5 for effective systemic delivery of atorvastatin through the lung.

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来源期刊
CiteScore
6.20
自引率
5.60%
发文量
142
审稿时长
4-8 weeks
期刊介绍: Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.
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