| [PMID]: | 28457963 |
| [Au] Autor: | Nagasaki Y; Mizukoshi Y; Gao Z; Feliciano CP; Chang K; Sekiyama H; Kimura H |
| [Ad] Endereço: | Department of Material Science, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennoudai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan; Master's School of Medical Sciences, Graduate School of Comprehensive Human Sciences, University of Tsukuba, Tennoudai 1-1-1, Tsukuba, Ibaraki 305-8 |
| [Ti] Título: | Development of a local anesthetic lidocaine-loaded redox-active injectable gel for postoperative pain management. |
| [So] Source: | Acta Biomater;57:127-135, 2017 Jul 15. |
| [Is] ISSN: | 1878-7568 |
| [Cp] País de publicação: | England |
| [La] Idioma: | eng |
| [Ab] Resumo: | Although local anesthesia is commonly applied for pain relief, there are several issues such as its short duration of action and low effectiveness at the areas of inflammation due to the acidic pH. The presence of excessive amount of reactive oxygen species (ROS) is known to induce inflammation and aggravate pain. To resolve these issues, we developed a redox-active injectable gel (RIG) with ROS-scavenging activity. RIG was prepared by mixing polyamine-b-poly(ethylene glycol)-b-polyamine with nitroxide radical moieties as side chains on the polyamine segments (PMNT-b-PEG-b-PMNT) with a polyanion, which formed a flower-type micelle via electrostatic complexation. Lidocaine could be stably incorporated in its core. When the temperature of the solution was increased to 37°C, the PIC-type flower micelle transformed to gel. The continuous release of lidocaine from the gel was observed for more than three days, without remarkable initial burst, which is probably owing to the stable entrapment of lidocaine in the PIC core of the gel. We evaluated the analgesic effect of RIG in carrageenan-induced arthritis mouse model. Results showed that lidocaine-loaded RIG has stronger and longer analgesic effect when administered in inflamed areas. In contrast, while the use of non-complexed lidocaine did not show analgesic effect one day after its administration. Note that no effect was observed when PIC-type flower micelle without ROS-scavenging ability was used. These findings suggest that local anesthetic-loaded RIG can effectively reduce the number of injection times and limit the side effects associated with the use of anti-inflammatory drugs for postoperative pain management. STATEMENT OF SIGNIFICANCE: 1. We have been working on nanomaterials, which effectively eliminate ROS, avoiding dysfunction of mitochondria in healthy cells. 2. We designed redox injectable gel using polyion complexed flower type micelle, which can eliminates ROS locally. 3. We could prepare local anesthesia-loaded redox injectable gel (lido@RIG). 4. Drug release could be extended by local administration of lido@RIG. 5. Deprotonation of lidocaine improved anesthetic effect because ROS were eliminated locally by RIG. 6. Local inflammation could be also suppressed by lido@RIG. |
| [Mh] Termos MeSH primário: |
Anestésicos Locais
Lidocaína
Manejo da Dor/métodos
Dor Pós-Operatória/tratamento farmacológico
|
| [Mh] Termos MeSH secundário: |
Anestésicos Locais/química
Anestésicos Locais/farmacocinética
Anestésicos Locais/farmacologia
Animais
Preparações de Ação Retardada/química
Preparações de Ação Retardada/farmacocinética
Preparações de Ação Retardada/farmacologia
Lidocaína/química
Lidocaína/farmacocinética
Lidocaína/farmacologia
Masculino
Camundongos
Camundongos Endogâmicos ICR
Dor Pós-Operatória/fisiopatologia
|
| [Pt] Tipo de publicação: | JOURNAL ARTICLE |
[Nm] Nome de substância:
| 0 (Anesthetics, Local); 0 (Delayed-Action Preparations); 98PI200987 (Lidocaine) |
| [Em] Mês de entrada: | 1802 |
| [Cu] Atualização por classe: | 180223 |
[Lr] Data última revisão:
| 180223 |
| [Sb] Subgrupo de revista: | IM |
| [Da] Data de entrada para processamento: | 170502 |
| [St] Status: | MEDLINE |
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