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目的 制备新型叶酸靶向紫杉醇聚合物纳米囊泡,研究其理化性质、细胞毒性和体内抗肿瘤活性。方法 以两亲性三嵌段共聚物聚己内酯-b-聚乙二醇-b-聚己内酯(PCL-b-PEG-b-PCL)、甲氧基聚乙二醇二硬脂酰磷脂酰乙醇胺(mPEG2000-DSPE)、偶联叶酸的磷脂DSPE-PEG(2000) Folate共混物为载体材料,通过薄膜-超声分散法制备出叶酸靶向紫杉醇聚合物纳米囊泡并对其进行形态、粒径及其分布、Zeta电位、载药量及包封率、体外释放等表征,用CCK-8法研究了聚合物纳米囊泡对H1299肺癌细胞的细胞毒性,并评价其在BALB/c小鼠EMT-6乳腺癌模型中的抗肿瘤效果。结果 叶酸靶向紫杉醇聚合物纳米囊泡呈球形,具有明显的核-壳结构,粒径均匀。随着紫杉醇投药量的增加,纳米囊泡的粒径增大,包封率降低。载药30%的叶酸靶向紫杉醇聚合物纳米囊泡的平均粒径为311 nm,多分散系数为0.171,Zeta电位为-30.3 mV,包封率为91.16%。体外释放研究表明,载紫杉醇聚合物纳米囊泡基本无药物突释现象,具有缓释特性。细胞毒性研究表明,当紫杉醇浓度为25 μg·mL-1时,叶酸靶向紫杉醇聚合物纳米囊泡的细胞毒性低于相应浓度的紫杉醇/聚氧乙烯蓖麻油注射剂。体内抗肿瘤活性实验研究表明,叶酸靶向紫杉醇聚合物纳米囊泡对小鼠EMT-6乳腺癌具有明显抑制作用,具有与紫杉醇/聚氧乙烯蓖麻油注射剂相似的抑制肿瘤作用。结论 叶酸靶向紫杉醇聚合物纳米囊泡具有高载药量及包封率、均匀的粒径及分布、缓释特性、低毒和较好的抗肿瘤作用,是一种有潜力的紫杉醇缓控释新剂型用于提高紫杉醇的药效并且降低不良反应。 相似文献
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Objective To develop paclitaxol (PTX)-loaded polymersomes based on poly (ε-caprolactone)-block-poly (ethylene glycol)-block-poly (ε-caprolactone)(PCL-b-PEG-b-PCL, PCEP) amphiphilic triblock copolymers. Methods A series of PCEP copolymers was synthesized by ring-opening polymerization of ε-caprolactone initiated by PEG. The block copolymers were characterized by FT-IR、1H NMR and GPC. PTX-loaded polymersomes were prepared by thin-film and ultrasonic dispersion method and characterized in terms of morphology,particle size and size distribution, encapsulation efficiency and in vitro release. The effect of different hydrophilic and hydrophobic chain length on the drug-loading content, entrapment efficiency, size and size distribution and in vitro release were also investigated. Results The PTX-loaded polymersomes showed nanometer size and spherical morphology with core and shell. The sizes of PTX-loaded polymersomes increased with the increasing of the molecular weight of PCEP. The PTX-loaded polymersomes showed a continuous and steady release of PTX without initial burst release. The release rate increased with the increasing of hydrophilic PEG chain content and decreased with the increasing of hydrophobic PCL chain content. Conclusion For the first time, a novel PTX-loaded polymersomes was developed based on PCL-b-PEG-b-PCL amphiphilic triblock copolymers. The PTX-loaded polymersomes showed nanometer size, narrow size distribution and high drug encapsulation efficiency.These results indicate that PTX-loaded polymersomes could be a promising novel controlled release dosage form to increase therapeutic effect with decreased toxic and side effect of PTX. 相似文献
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目的 以两亲性三嵌段共聚物聚己内酯-聚乙二醇-聚己内酯(PCL-b-PEG-b-PCL)为载体材料,制备包载抗肿瘤药物阿霉素(DOX)的聚合物纳米粒,并对其进行体内外性能研究.方法 以PCL-b-PEG-b-PCL作为载体材料,通过薄膜水化超声分散法制备出载DOX的聚合物纳米粒,并对其形态、粒径及其分布、载药量及包封率等理化性能进行表征.采用MTS法研究载DOX聚合物纳米粒对EMT6乳腺癌细胞的细胞毒性,激光扫描共聚焦显微镜(CLSM)观察EMT6细胞对纳米粒的细胞吞噬,离体脏器荧光成像研究纳米粒在荷EMT6乳腺癌小鼠的组织分布.结果 通过薄膜水化超声分散法成功制备出载DOX聚合物纳米粒,透射电镜和扫描电镜结果表明,该纳米粒呈球形,大小均匀,具有明显的核壳结构.粒度分析表明,载DOX聚合物纳米粒的平均粒径为130.8 nm,且粒径分布较窄(多分散系数为0.200).DOX在聚合物纳米粒中的包封率和载药量分别为(86.71±2.05)%和(8.71±0.57)%.细胞毒性研究发现,空白纳米粒对EMT6细胞无毒性,而载入DOX后,DOX-NPs的细胞毒性具有时间和剂量依赖性;在DOX质量浓度较高(20 μg/ml和40μg/ml)和孵育时间较长(72 h)时,载DOX聚合物纳米粒与游离DOX的细胞毒性相当,差异无统计学意义(P>0.05).CLSM观察发现,EMT6乳腺癌细胞与载DOX聚合物纳米粒共同孵育后,DOX的荧光在细胞质和细胞核中均有分布,但与游离DOX共同孵育后,DOX的红色荧光主要出现在细胞核中.离体脏器荧光成像研究表明,分别对荷EMT6乳腺癌小鼠尾静脉注射载DOX聚合物纳米粒及游离DOX后,载DOX聚合物纳米粒可通过增强渗透和滞留效应(EPR)在肿瘤部位有效聚集.结论 载DOX聚合物纳米粒具有适合静脉注射的粒径、高载药量和包封率及良好的被动靶向特性,是一种在肿瘤治疗中具有潜在应用前景的纳米药物递送系统. 相似文献
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目的制备新型可注射用载紫杉醇聚己内酯-聚乙二醇-聚己内酯(PCl-PEG-PCL)胶束,并评价和比较其与市售紫杉醇注射液在大鼠体内的药代动力学性质。方法以PCL-PEG-PCL为载体材料,通过薄膜-水化-超声法制备出载紫杉醇PCl-PEG-PCL胶束,并对其进行表征。以市售紫杉醇注射液为对照.采用SD大鼠尾静脉注射后观察载紫杉醇PCL-PEG-PCL胶束的体内药代动力学.并用DAS2.0药代动力学数据软件计算相关参数。结果载紫杉醇PCL-PEG-PCL胶束呈大小均匀的球形,具有明显的核壳结构;平均粒径为93nm,多分散系数为0.19;载药量为28.98%,药物包封率为94.36%。体外释放研究表明.载紫杉醇PCL-PEG-PCL胶束具有缓释效果。药代动力学研究表明.两种制剂均符合二房室模型.市售紫杉醇注射液和紫杉醇聚合物胶束消除半衰期(t1/2)分别为(1.96±0.27)h和(12.65±1.77)h,平均滞留时间(MRT)分别为(0.93±0.19)h和(11.18±1.41)h,体内总清除率(CL)分别为(0.44±0.05)L·kg/h和(0.10±0.01)L·kg/h,药-时曲线下面积(AUC0-∞)分别为(17.15±2.35)mg·h/L和(73.82±10.38)mg.h/L。结论成功制备了新型可注射用载紫杉醇PCL-PEG-PCL胶束.药代动力学研究表明.所研制的载紫杉醇PCL-PEG-PCL胶束明显延长紫杉醇在血液中的循环时间及消除半衰期.显著提高生物利用度,是一种有潜力的紫杉醇缓控释新剂型。 相似文献
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目的 以聚己内酯-b-聚乙二醇-6-聚己内酯(PCEP)两亲性三嵌段共聚物为载体研制紫杉醇聚合物纳米囊泡.方法 以不同分子量的聚乙二醇(PEG)引发合成不同亲水段、疏水段链长的PCEP并进行FT-IR、1H NMR和GPC表征,以合成的嵌段聚合物PCEP为载体,通过薄膜-超声分散法制备紫杉醇聚合物纳米囊泡,用透射电子显微镜(TEM)表征其形态和构造,用粒度分析仪测定其粒径及分布,用高效液相色谱(HPLC)法测定其载药量及包封率,用透析袋法研究药物体外释放;同时,研究不同亲水链长、疏水链长对紫杉醇聚合物囊泡载药量、包封率、粒径及体外释放紫杉醇药物的影响.结果 研制的紫杉醇聚合物囊泡呈核-壳结构球形,粒径为纳米级,随着PCEP共聚物相对分子质量的增加而增大;紫杉醇聚合物囊泡体外释放无突释现象,能稳定缓慢释放紫杉醇,且释放速率随共聚物中亲水段PEG含量增加而增大,随疏水段PCL含量增大而减小.结论 以PCEP两亲性三嵌段共聚物为载体制备的紫杉醇聚合物纳米囊泡,其粒径小且分布均匀,包封率较高,有望成为一种用于提高紫杉醇的药效且降低不良反应的新的紫杉醇缓控释剂型. 相似文献
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Objective To develop paclitaxol (PTX)-loaded polymersomes based on poly (ε-caprolactone)-block-poly (ethylene glycol)-block-poly (ε-caprolactone)(PCL-b-PEG-b-PCL, PCEP) amphiphilic triblock copolymers. Methods A series of PCEP copolymers was synthesized by ring-opening polymerization of ε-caprolactone initiated by PEG. The block copolymers were characterized by FT-IR、1H NMR and GPC. PTX-loaded polymersomes were prepared by thin-film and ultrasonic dispersion method and characterized in terms of morphology,particle size and size distribution, encapsulation efficiency and in vitro release. The effect of different hydrophilic and hydrophobic chain length on the drug-loading content, entrapment efficiency, size and size distribution and in vitro release were also investigated. Results The PTX-loaded polymersomes showed nanometer size and spherical morphology with core and shell. The sizes of PTX-loaded polymersomes increased with the increasing of the molecular weight of PCEP. The PTX-loaded polymersomes showed a continuous and steady release of PTX without initial burst release. The release rate increased with the increasing of hydrophilic PEG chain content and decreased with the increasing of hydrophobic PCL chain content. Conclusion For the first time, a novel PTX-loaded polymersomes was developed based on PCL-b-PEG-b-PCL amphiphilic triblock copolymers. The PTX-loaded polymersomes showed nanometer size, narrow size distribution and high drug encapsulation efficiency.These results indicate that PTX-loaded polymersomes could be a promising novel controlled release dosage form to increase therapeutic effect with decreased toxic and side effect of PTX. 相似文献
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健康教育作为整体护理的重要内容,它不仅推动了医疗卫生服务从观念转变到工作模式的转变,而且有利于促进病人康复,提高病人的生活质量。但由于医护职责不同及旧医学模式的影响,服务对象更乐于接受医师的指导、建议。而做为健康教育的主要实施者——护士,教育过程不易于得到服务对象的认同,从而影响了教育效果。如何尽快获得服务对象对护士健康教育的认同,使服务对象从健康教育中获得更好的自我护理和维持健康知识和技能,笔者在工作中总结了以下几点。 相似文献
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