Copaiba essential oil carried in a self-nanoemulsifying drug delivery system improves adjuvant-induced arthritis in rats.

IF 2.8 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Ana Paula Ames-Sibin, Any Carolina Chagas-Almeida, Ana Beatriz P Souza, Ana Paula M Andrade, Juliana C Castro, Sabrina B S Ferreira, Francielli Maria S Silva-Comar, Roberto K N Cuman, Marcos L Bruschi, Maria Raquel M Natali, Anacharis B Sá-Nakaninhi, Lívia Bracht, Adelar Bracht, Jurandir F Comar
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Abstract

Objectives: Copaiba essential oil (CEO) is obtained through the distillation of copaiba balsam and has been used in the traditional medicine to treat inflammatory conditions. However, the highly lipophilic nature of CEO restricts its pharmaceutical use. This study evaluated the effect of CEO, carried in a self-nanoemulsifying drug delivery system (SNEDDS), on articular and systemic inflammation and liver changes in Holtzman rats with Freund's adjuvant-induced arthritis.

Methods: Healthy and arthritic rats received orally for 18 days the non-formulated CEO and the one carried in a self-nanoemulsifying drug delivery system (FSNEDDS), both at doses of 50 and 100 mg/kg. The oral bioavailability of FSNEDDS was determined in healthy rats by quantifying the levels of β-caryophyllene in the plasma.

Key findings: FSNEDDS exhibited more than three times greater oral bioavailability compared to non-formulated CEO. This phenomenon allowed FSNEDDS (100 mg/kg) to effectively reduce adjuvant-induced articular and systemic inflammation and oxidative stress in arthritic rats at a dose four times lower than copaiba balsam and β-caryophyllene. Furthermore, FSNEDDS did not alter the serum markers of liver damage, hepatic morphometry, and liver gluconeogenesis in healthy rats.

Conclusion: FSNEDDS was effective against arthritis in rats, and unlike copaiba balsam, it does not exhibit hepatotoxicity, suggesting it could serve as a phytotherapeutic alternative in the treatment of rheumatoid arthritis.

自纳米乳化给药系统中携带的可可巴精油可改善佐剂诱导的大鼠关节炎。
目的:Copaiba精油(CEO)是通过Copaiba香脂的蒸馏得到的,在传统医学中用于治疗炎症。然而,其高度亲脂性限制了其在医药上的应用。本研究评估了在自纳米乳化药物递送系统(SNEDDS)中携带的CEO对患有弗氏佐剂诱导关节炎的Holtzman大鼠关节和全身炎症以及肝脏变化的影响。方法:健康大鼠和关节炎大鼠分别以50和100 mg/kg的剂量口服未配制的CEO和自纳米乳化给药系统(FSNEDDS)。通过测定大鼠血浆中β-石竹烯的含量,测定FSNEDDS的口服生物利用度。主要发现:与非配方CEO相比,FSNEDDS的口服生物利用度高出三倍以上。这一现象使得FSNEDDS (100 mg/kg)以比copaiba香脂和β-石竹烯低4倍的剂量有效减轻佐剂诱导的关节炎大鼠关节和全身炎症和氧化应激。此外,FSNEDDS没有改变健康大鼠的肝损伤血清标志物、肝脏形态测定和肝糖异生。结论:FSNEDDS对大鼠关节炎有一定的治疗作用,且与copaiba香脂不同,FSNEDDS不具有肝毒性,提示其可作为一种治疗类风湿性关节炎的植物疗法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
6.60
自引率
0.00%
发文量
91
审稿时长
3 months
期刊介绍: JPP keeps pace with new research on how drug action may be optimized by new technologies, and attention is given to understanding and improving drug interactions in the body. At the same time, the journal maintains its established and well-respected core strengths in areas such as pharmaceutics and drug delivery, experimental and clinical pharmacology, biopharmaceutics and drug disposition, and drugs from natural sources. JPP publishes at least one special issue on a topical theme each year.
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