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

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• 作者：Juliana T. Clemente-Napimoga^a ; Juscelaine A. Moreira^b ; Renato Grillo^c ; ^d ; Nathalie F.S. de Melo^c ; ^d ; Leonardo F. Fraceto^c ; ^d ; Marcelo H. Napimoga^e ; ^{marcelo.napimoga@gmail.com} ; ^{napimogamh@yahoo.com}
• 关键词：15d-PGJ2 ; PPAR-gamma ; Nociception ; Temporomandibular joint ; Inflammation
• 刊名：Life Sciences
• 出版年：2012
• 期刊代码：62_00243205
• 类别：imm
• 出版时间：14 June, 2012
• 卷：90
• 期：23-24
• 页码：944-949
• 文件大小：582 K

摘要

Aims

To verify whether the nanoencapsulation of 15d-PGJ₂ in poly(d,l-lactide-co-glycolide) (PLGA) nanocapsules (15d-PGJ₂-NC) might potentialize its antinociceptive activity into rats鈥?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-PGJ₂ or 15d-PGJ₂-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-1尾 measurements.

Key finding

TEM and AFM analyses showed that 15d-PGJ₂-NC is spherical without any aggregates or adhesion confirming that this formulation is a good drug carrier system for 15d-PGJ₂. Pretreatment with 15d-PGJ₂-NC (100 and 1000 pg/TMJ), but not unloaded 15d-PGJ₂, was found to significantly decrease the release of IL-1尾 cytokine and the animals鈥?nociceptive behavioral response induced by intra-TMJ injection of formalin.

Significance

The compound 15d-PGJ₂-NC might be used as a potential antinociceptive and anti-inflammatory agent to treat temporomandibular disorders in clinical practice.