甲磺酸多沙唑嗪的口服生物利用度增强:纳米悬浮液与自纳米乳化给药系统

IF 3.4 Q2 CHEMISTRY, MEDICINAL ADMET and DMPK Pub Date : 2023-11-03 DOI:10.5599/admet.2022
Al Zahraa G. Al Ashmawy, Mohammad H. Alyami, Noura G. Eissa, Gehan F. Balata, Hanan M. El Nahas
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引用次数: 0

摘要

背景和目的:甲磺酸多沙唑嗪(DOX)是一种抗高血压药物,水溶性差,因此释放性差。纳米悬浮液和自纳米乳化给药系统(SNEDDS)正在成为提高不同药物水溶性的纳米技术。实验方法:本研究的目的是通过比较DOX纳米混悬液和SNEDDS在液体和固体形态下的粒径、zeta电位、包裹效率、释放速率和主动脉血压等物理特性,确定能够增强DOX释放和降压效果的最佳给药系统。关键结果:DOX纳米混悬剂的粒径为385±13 nm,多分散指数为0.049±3,zeta电位为50±4 mV, 20 min后药物释放率为91±0.43%。SNEDDS液滴尺寸为224±15 nm,多分散性指数为(0.470±0.01),zeta电位为-5±0.10 mV, DR20min为93±4%。固体SEDDS的粒径为79±14 nm,多分散性指数为1±0.00,zeta电位为-18±0.26 mv, DR20min为100±2.72%。结论:最后,在降低平均动脉血压方面,固体SNEDDS的效果优于液体SNEDDS和纳米混悬液(P >0.05)。
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Oral bioavailability enhancement of doxazosin mesylate: Nanosuspension versus self-nanoemulsifying drug delivery systems
Background and purpose: Doxazosin mesylate (DOX) is an antihypertensive drug that possesses poor water solubility and, hence, poor release properties. Both nanosuspensions and self-nanoemulsifying drug delivery systems (SNEDDS) are becoming nanotechnology techniques for the enhancement of water solubility of different drugs. Experimental approach: The study's goal was to identify the best drug delivery system able to enhance the release and antihypertensive effect of DOX by comparing the physical characteristics such as particle size, zeta potential, entrapment efficiency, release rate, and main arterial blood pressure of DOX-loaded nanosuspensions and SNEDDS in liquid and solid form. Key results: DOX nanosuspension preparation had a particle size of 385±13 nm, poly-dispersity index of 0.049±3, zeta potential of 50 ± 4 mV and drug release after 20 min (91±0.43 %). Liquid SNEDDS had a droplet size of 224±15 nm, poly-dispersity index of (0.470±0.01), zeta potential of -5±0.10 mV and DR20min of 93±4 %. Solid SEDDS showed particle size of 79±14 nm, poly-dispersity index of 1±0.00, a zeta potential of -18 ±0.26 mv and DR20min of 100 ±2.72 %. Conclusion: Finally, in terms of the mean arterial blood pressure lowering, solid SNEDDS performed better effect than both liquid SNEDDS and nanosuspension (P >0.05).
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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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