Synthesis of nanocapsules blended polymeric hydrogel loaded with bupivacaine drug delivery system for local anesthetics and pain management.
Synthesis of nanocapsules blended polymeric hydrogel loaded with bupivacaine drug delivery system for local anesthetics and pain management.
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负载布比卡因药物递送系统的纳米胶囊混合聚合水凝胶的合成，用于局部麻醉和疼痛管理
DOI：
10.1080/10717544.2021.2023702
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发表时间：
2022-12
期刊：
影响因子：
6
通讯作者：
Li C
中科院分区：
文献类型：
--
作者：
Deng W;Yan Y;Zhuang P;Liu X;Tian K;Huang W;Li C
壳聚糖 - 京尼平/聚己内酯（CS - GP/PC）聚合物水凝胶体系的制备与表征
载有布比卡因（BPV）的CS - GP/PC在磷酸盐缓冲溶液（PBS）中呈现出延长的体外释放
载有BPV的CS - GP/PC聚合物水凝胶对成纤维细胞（3T3）的细胞毒性
CS - GP/PC作为一种有前景的局部麻醉药BPV皮肤给药系统的研发
局部麻醉药在临床上用于控制术后疼痛管理。本研究旨在开发以壳聚糖（CS）与京尼平（GP）水凝胶作为亲水性脂质外壳，负载聚（ε - 己内酯）（PC）纳米胶囊作为疏水性聚合物核复合物（CS - GP/PC）来递送布比卡因（BPV），以延长麻醉和缓解疼痛。CS - GP/PC聚合物水凝胶的溶胀率、体外降解和流变性能增强。通过扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）和X射线衍射（XRD）分析证实了PC纳米胶囊掺入到CS - GP水凝胶中。扫描电子显微镜结果表明，CS - GP水凝胶和CS - GP/PC聚合物水凝胶具有多孔结构，孔径不均匀，直径在25到300μm之间。CS - GP/PC聚合物水凝胶的体外药物释放曲线显示，在36小时内BPV药物释放达到99.2 ± 1.12%。使用CCK - 8法对3T3成纤维细胞进行细胞活力评估，结果表明所获得的载有BPV的CS - GP/PC聚合物水凝胶没有明显的细胞毒性。与对照组动物相比，载有BPV的CS - GP/PC聚合物水凝胶在至少7天内疼痛反应有显著改善。与BPV溶液相比，CS - GP水凝胶和CS - GP/PC聚合物水凝胶在24小时内分别使BPV的皮肤渗透率提高了3倍和5倍。体外和体内结果表明，负载PC纳米胶囊的CS - GP水凝胶可作为有效的药物载体，从而延长和增强BPV的麻醉效果。组织病理学结果表明，载有BPV的CS - GP/PC聚合物水凝胶系统在7、14和21天具有良好的生物降解性和生物相容性，且无神经毒性。
Preparation and characterization of CS-GP/PC polymeric hydrogel system. BPV-loaded CS-GP/PC exhibited prolonged in vitro release in PBS solution. Cytotoxicity of BPV-loaded CS-GP/PC polymeric hydrogel against fibroblast (3T3) cells. Development of CS-GP/PC a promising skin drug-delivery system for local anesthetic BPV. Local anesthetics are used clinically for the control of postoperative pain management. This study aimed to develop chitosan (CS) with genipin (GP) hydrogels as the hydrophilic lipid shell loaded poly(ε-caprolactone) (PC) nanocapsules as the hydrophobic polymeric core composites (CS-GP/PC) to deliver bupivacaine (BPV) for the prolongation of anesthesia and pain relief. The swelling ratio, in vitro degradation, and rheological properties enhancement of CS-GP/PC polymeric hydrogel. The incorporation of PC nanocapsules into CS-GP hydrogels was confirmed by SEM, FTIR, and XRD analysis. Scanning electron microscopy results demonstrated that the CS-GP hydrogels and CS-GP/PC polymeric hydrogels have a porous structure, the pore dimensions being non-uniform with diameters between 25 and 300 μm. The in vitro drug release profile of CS-GP/PC polymeric hydrogel has been achieved 99.2 ± 1.12% of BPV drug release in 36 h. Cellular viability was evaluated using the CCK-8 test on 3T3 fibroblast cells revealed that the obtained CS-GP/PC polymeric hydrogel with BPV exhibited no obvious cytotoxicity. The CS-GP/PC polymeric hydrogel loaded with BPV showed significant improvement in pain response compared to the control group animals for at least 7 days. When compared with BPV solution, CS-GP hydrogel and CS-GP/PC polymeric hydrogel improved the skin permeation of BPV 3-fold and 5-fold in 24 h, respectively. In vitro and in vivo results pointed out PC nanocapsules loaded CS-GP hydrogel can act as effective drug carriers, thus prolonging and enhancing the anesthetic effect of BPV. Histopathological results demonstrated the excellent biodegradability and biocompatibility of the BPV-loaded CS-GP/PC polymeric hydrogel system on 7, 14, and 21 days without neurotoxicity.
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DOI：
10.1016/j.ijbiomac.2019.06.184
发表时间：
2019-09-01
影响因子：
8.2
作者：
Lewandowska-Lancucka, Joanna;Gilarska, Adriana;Nowakowska, Maria
通讯作者：
Nowakowska, Maria
影响因子：
4.6
作者：
Hu Y;Hu S;Zhang S;Dong S;Hu J;Kang L;Yang X
通讯作者：
Yang X
影响因子：
3.7
作者：
Batista da Silva C;Volpato MC;Muniz BV;Dos Santos CP;Serpe L;Ferreira LEN;de Melo NFS;Fraceto LF;Groppo FC;Franz-Montan M
通讯作者：
Franz-Montan M
影响因子：
9.7
作者：
Khanal M;Gohil SV;Kuyinu E;Kan HM;Knight BE;Baumbauer KM;Lo KW;Walker J;Laurencin CT;Nair LS
通讯作者：
Nair LS
影响因子：
8
作者：
Frank LA;Sandri G;D'Autilia F;Contri RV;Bonferoni MC;Caramella C;Frank AG;Pohlmann AR;Guterres SS
通讯作者：
Guterres SS