首页|用于伤口镇痛及愈合的PLGA-PEG-PLGA热敏凝胶的制备

用于伤口镇痛及愈合的PLGA-PEG-PLGA热敏凝胶的制备

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目的 构建一种由PLGA-PEG-PLGA/甘油组成的温敏凝胶系统,用以负载盐酸布比卡因和多聚脱氧核糖核苷酸复方药物.方法 以胶凝温度作为关键响应参数,单因素法初步筛选凝胶基质浓度、药物装载量以及甘油添加量.随后,采用正交实验设计,并引入渗透压作为优化参数,以深化配方的优化过程.最后,对优选的配方进行质量评估.结果 优选配方包含16%PLGA-PEG-PLGA、5%甘油、2%盐酸布比卡因,0.4%多聚脱氧核糖核苷酸.常温下配方呈均一透明溶液态,胶凝温度33.83 ℃,胶凝时间100s,pH值3.11,渗透压836 mOsm,可注射性及黏附性良好.药物体外释放符合Ritger-peppas方程.开放型伤口模型证实了该样品能够有效促进伤口的愈合,达到镇痛的效果.结论 优选配方制备工艺简单,各项质量指标均符合要求,有望在临床中得到应用.
Preparation of PLGA-PEG-PLGA thermal gel for wound analgesics and healing
Objective To prepare a temperature-sensitive gel system composed of PLGA-PEG-PLGA/glycerol for loading bupivacaine hydrochloride and polydeoxyribonucleotide combination drugs.Methods Gelling temperature was used as the key response parameter,the gel matrix concentration,drug loading and glycerol addition were preliminarily screened by a single factor method.Subsequently,an orthogonal experiment was designed,and osmotic pressure was introduced as a parameter to optimize the formulation.Finally,the quality of the selected formulations was evaluated.Results The preferred formula contained 16%PLGA-PEG-PLGA,5%glycerol,2%bupivacaine hydrochloride,and 0.4%polydeoxyribonucleotide.The formula was a uniform transparent solution at room temperature,with gelling temperature of 33.83 ℃,gelling time of 100 s,pH value of 3.11,and osmotic pressure of 836 mOsm,with good injectability and adhesion.The drug release conformed to the Ritger-peppas equation.The open wound model confirmed that the sample effectively promoted wound healing and showed analgesic effect.Conclusion The preparation of the optimal formula is simple,and all quality indicators meet the requirements,which is expected to be used in clinical practice.

temperature-sensitive in situ gelprescription screeninganalgesiahealing promotionbupivacaine hydrochloridepolydeoxyribonucleotide

余紫依、夏方亮、张建勇、郝蕾蕾、刘洋、翟光喜、张涛

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中国海洋大学医药学院,山东 青岛 266003

滨州市检验检测中心,山东 滨州 256606

山东齐都药业有限公司,山东 淄博 255400

山东大学药学院,济南 250012

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温敏型原位凝胶 处方筛选 镇痛 促愈合 布比卡因 多聚脱氧核糖核苷酸

2024

中南药学
湖南省药学会

中南药学

CSTPCD
影响因子:0.736
ISSN:1672-2981
年,卷(期):2024.22(8)