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纳米胶囊载入 15d-PGJ2 增强了对大鼠颞下颌部痛觉过敏的镇痛作用。

15d-PGJ2-loaded in nanocapsules enhance the antinociceptive properties into rat temporomandibular hypernociception.

机构信息

Laboratory of Orofacial Pain, Department of Physiology, Piracicaba Dental School, State University of Campinas, Brazil.

出版信息

Life Sci. 2012 Jun 14;90(23-24):944-9. doi: 10.1016/j.lfs.2012.04.035. Epub 2012 Apr 27.

DOI:10.1016/j.lfs.2012.04.035
PMID:22564409
Abstract

AIMS

To verify whether the nanoencapsulation of 15d-PGJ(2) in poly(D,L-lactide-co-glycolide) (PLGA) nanocapsules (15d-PGJ(2)-NC) might potentialize its antinociceptive activity into rats' temporomandibular joint (TMJ).

MAIN METHODS

Transmission electron microscopy (TEM) and atomic force microscopy (AFM) were used to evaluate the morphology and suspension of the PLGA nanocapsules. Rats were pretreated (15 min) with an intra-TMJ injection of unloaded 15d-PGJ(2) or 15d-PGJ(2)-NC at concentrations of 10, 100 or 1000 pg followed by an ipsilateral intra-TMJ injection of 1.5% formalin. The nociceptive behavioral response was observed during 45 min; animals were then sacrificed and the periarticular tissue was removed for IL-1β measurements.

KEY FINDING

TEM and AFM analyses showed that 15d-PGJ(2)-NC is spherical without any aggregates or adhesion confirming that this formulation is a good drug carrier system for 15d-PGJ(2). Pretreatment with 15d-PGJ(2)-NC (100 and 1000 pg/TMJ), but not unloaded 15d-PGJ(2), was found to significantly decrease the release of IL-1β cytokine and the animals' nociceptive behavioral response induced by intra-TMJ injection of formalin.

SIGNIFICANCE

The compound 15d-PGJ(2)-NC might be used as a potential antinociceptive and anti-inflammatory agent to treat temporomandibular disorders in clinical practice.

摘要

目的

验证 15d-PGJ(2)包埋于聚(D,L-丙交酯-共-乙交酯)(PLGA)纳米囊(15d-PGJ(2)-NC)中是否可能增强其对大鼠颞下颌关节(TMJ)的镇痛活性。

主要方法

使用透射电子显微镜(TEM)和原子力显微镜(AFM)评估 PLGA 纳米囊的形态和悬浮状态。大鼠预先经 TMJ 内注射未负载的 15d-PGJ(2)或 15d-PGJ(2)-NC(浓度为 10、100 或 1000pg),15min 后于同侧 TMJ 内注射 1.5%甲醛。在 45 分钟内观察到疼痛行为反应;然后处死动物,取出关节周围组织测量 IL-1β。

主要发现

TEM 和 AFM 分析表明 15d-PGJ(2)-NC 呈球形,无任何聚集或粘连,证实该制剂是 15d-PGJ(2)的良好药物载体系统。与未负载的 15d-PGJ(2)相比,预注射 15d-PGJ(2)-NC(100 和 1000pg/TMJ)可显著减少 TMJ 内注射甲醛引起的 IL-1β细胞因子释放和动物的疼痛行为反应。

意义

化合物 15d-PGJ(2)-NC 可作为一种有潜力的镇痛和抗炎药物,用于临床治疗颞下颌关节紊乱。

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