策略性优化的perphenazine负载纳米脂质载体鼻-脑靶向的体内药代动力学评估和体外表征

IF 3.1 4区 材料科学 Q3 MATERIALS SCIENCE, MULTIDISCIPLINARY
Yogeeta O Agrawal, Tulshidas S Patil, Kiran D Patil, Nayan A Gujarathi, Amit Gangwal, Sameer N Goyal
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引用次数: 0

摘要

奋那嗪(Perphenazine, PPZ)是一种普遍用于治疗精神分裂症的抗精神病药物。然而,口服治疗后,它显示出大量的首过代谢和降低的生物利用度。本研究的目的是将PPZ纳入纳米结构脂质载体,从而提高其生物利用度和脑靶向性(PPZ- nlcs)。采用加热条件下高压均质法制备PPZ-NLCs,并采用23全因子设计进行优化。优化后的PPZ-NLCs粒径为167.5 nm, PDI为0.277,Zeta电位为-28.8 mV, EE为98.6%。在体外实验中,PPZ-NLCs的药物释放表现出最符合Higuchi动力学模型的药物缓释谱。PPZ-NLCs在体内药代动力学中观察到t1/2、AUC0-∞和Cmax显著增加,这表明PPZ-NLCs的生物利用度更高,消除量更少(Kel)。这些结果表明NLCs在提高PPZ药物的生物利用度方面具有优势,适合于成功的脑靶向治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In-vivo Pharmacokinetic Assessment and In-vitro Characterization of Strategically Optimized Perphenazine-loaded Nanostructured Lipid Carriers for Nose-to-brain Targeting.

Background: Perphenazine (PPZ) is a prevalent antipsychotic medication used to treat schizophrenia. After oral treatment, however, it shows substantial first-pass metabolism and decreased bioavailability.

Objective: The goal of this research was to incorporate PPZ into nanostructured lipid carriers and thereby improve its bioavailability and brain targeting (PPZ-NLCs).

Methods: PPZ-NLCs were formulated by a high-pressure homogenization methodology under heated conditions and optimized by applying a 23-full factorial design.

Results: The optimized PPZ-NLCs showed particle size 167.5 nm, PDI 0.277, Zeta Potential of -28.8 mV, and 98.6% EE. The drug release during In-vitro experiments of PPZ-NLCs exhibited a prolonged release profile of the drug best fitted into the Higuchi kinetic model. PPZ-NLCs when examined In-vivo pharmacokinetically a significant increase in t1/2, AUC0-∞, and Cmax was observed which indicates a greater bioavailability and a lesser elimination (Kel).

Conclusion: These results suggested the superiority of NLCs in enhancing the bioavailability of PPZ drug and their suitability for successful brain targeting, which could be subject to a patent application to protect the novel formulation.

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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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