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含甲硝唑-薄荷油-氨甲环酸自纳米乳化给药系统的新型含片的研制与优化用于拔牙后:体外评价与体内评估

Development and Optimization of a Novel Lozenge Containing a Metronidazole-Peppermint Oil-Tranexamic Acid Self-Nanoemulsified Delivery System to Be Used after Dental Extraction: In Vitro Evaluation and In Vivo Appraisal.

作者信息

Alissa Mohammed, Hjazi Ahmed, Abusalim Ghadah S, Aloraini Ghfren S, Alghamdi Suad A, Rizg Waleed Y, Hosny Khaled M, Alblowi Jazia A, Alkharobi Hanaa

机构信息

Department of Medical Laboratory Sciences, College of Applied Medical Sciences, Prince Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

出版信息

Pharmaceutics. 2023 Sep 19;15(9):2342. doi: 10.3390/pharmaceutics15092342.

DOI:10.3390/pharmaceutics15092342
PMID:37765310
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10535350/
Abstract

In-depth studies on essential oil-based nanoemulsions (NEs) have centered on a variety of oral health issues. NEs improve the delivery of nonpolar active agents to sites and thereby boost the dissolution and distribution of the agents. Metronidazole-peppermint oil-tranexamic acid self-nanoemulsifying drug delivery systems (MZ-PO-TX-SNEDDS) were created and loaded into novel lozenges to act as antifungal, hemostatic, antimicrobial, and analgesic dosage forms after dental extractions. The design-of-experiments approach was used in creating them. To generate the NEs, different concentrations of MZ-PO (240, 180, and 120 mg), 2% TX (600, 450, and 300 mg), and S (600, 400, and 200 mg) were used. The ideal formulation had serum levels of 1530 U/mL of interleukin-6, a minimal inhibitory concentration against bacteria of 1.5 µg/mL, a droplet size of 96 nm, and a blood coagulation time of 16.5 min. Moreover, the produced NE offered better MZ release. The adopted design was used to produce the ideal formulation; it contained 240 mg of MZ-PO, 600 mg of 2% TX, and 600 mg of S It was incorporated into lozenges with acceptable characteristics and an improved capability for drug release. These lozenges had reasonable coagulation times, IL-6 serum levels, and MIC values. All of these characteristics are desirable for managing symptoms following tooth extractions. Therefore, these lozenges loaded with MZ-PO-TX-SNEDDs might be considered a beneficial paradigm for relieving complications encountered after tooth extractions.

摘要

对基于精油的纳米乳剂(NEs)的深入研究集中在各种口腔健康问题上。纳米乳剂可改善非极性活性剂向作用部位的递送,从而促进这些活性剂的溶解和分布。甲硝唑-薄荷油-氨甲环酸自纳米乳化药物递送系统(MZ-PO-TX-SNEDDS)被制备出来,并装入新型含片,用作拔牙后的抗真菌、止血、抗菌和镇痛剂型。在制备过程中采用了实验设计方法。为了制备纳米乳剂,使用了不同浓度的MZ-PO(240、180和120毫克)、2%的TX(600、450和300毫克)以及S(600、400和200毫克)。理想配方的血清白细胞介素-6水平为1530 U/mL,对细菌的最低抑菌浓度为1.5 µg/mL,液滴大小为96纳米,凝血时间为16.5分钟。此外,所制备的纳米乳剂具有更好的甲硝唑释放效果。采用该设计制备出了理想配方;它含有240毫克的MZ-PO、600毫克的2% TX和600毫克的S。将其制成具有可接受特性且药物释放能力得到改善的含片。这些含片具有合理的凝血时间、白细胞介素-6血清水平和最低抑菌浓度值。所有这些特性对于拔牙后症状的处理都是理想的。因此,这些装载有MZ-PO-TX-SNEDDs的含片可被视为缓解拔牙后并发症的有益范例。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/cde9f33ea0ca/pharmaceutics-15-02342-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/3983601199ac/pharmaceutics-15-02342-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/d01286dc8ee8/pharmaceutics-15-02342-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/a06f177cb23c/pharmaceutics-15-02342-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/cde9f33ea0ca/pharmaceutics-15-02342-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/3983601199ac/pharmaceutics-15-02342-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/d01286dc8ee8/pharmaceutics-15-02342-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/a06f177cb23c/pharmaceutics-15-02342-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1507/10535350/cde9f33ea0ca/pharmaceutics-15-02342-g006.jpg

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