国际生物医学工程杂志
國際生物醫學工程雜誌
국제생물의학공정잡지
INTERNATIONAL JOURNAL OF BIOMEDICAL ENGINEERING
2011年
1期
1-4,10,后插4
,共6页
温敏水凝胶%PCL-PEG-PCL共聚物%紫杉醇%控制释放%生物降解能力
溫敏水凝膠%PCL-PEG-PCL共聚物%紫杉醇%控製釋放%生物降解能力
온민수응효%PCL-PEG-PCL공취물%자삼순%공제석방%생물강해능력
Thermosensitive hydrogels%PCL1250-PEG1500-PCL1250copolymers%Paclitaxel%Controlled release%Biodegradability
目的 利用聚己内酯-聚乙二醇-聚己内酯(PCL1250-PEG1500-PCL1250)两亲性聚合物温敏凝胶作为载体材料,构建疏水性抗肿瘤药物紫杉醇的载药体系.方法 以辛酸亚锡为催化剂、聚乙二醇为引发剂,引发己内酯单体开环聚合,合成PCL1250-PEG1500-PCL1250三嵌段共聚物.通过核磁共振氢谱及凝胶渗透色谱对其组成、结构及分子量进行表征:制备不同凝胶浓度及初始载药量的载药温敏凝胶,并对其相转变性能、体外药物释放行为以及体内的生物降解性能进行考察.结果 核磁共振及凝胶渗透色谱测定结果表明:合成的共聚物组成与初始投料比一致,符合设计的PCL1250-PEG1500-PCL1250嵌段聚合物结构;该凝胶在15%～30%浓度区间内,具备温敏性溶胶-凝胶相转变能力;该温敏凝胶对紫杉醇具有可控的药物缓释能力,通过改变凝胶浓度及初始载药量可调节药物释放速率和维持释放的时间.小鼠背部皮下注射PCL1250-PEG1500-PCL1250溶胶后在体内迅速原位凝胶化,凝胶随植入时间逐渐降解至45 d时基本降解完全.结论 PCL1250-PEG1500-PCL1250温敏凝胶作为紫杉醇载药体系具有良好的药物控释能力和体内生物降解性能.
目的 利用聚己內酯-聚乙二醇-聚己內酯(PCL1250-PEG1500-PCL1250)兩親性聚閤物溫敏凝膠作為載體材料,構建疏水性抗腫瘤藥物紫杉醇的載藥體繫.方法 以辛痠亞錫為催化劑、聚乙二醇為引髮劑,引髮己內酯單體開環聚閤,閤成PCL1250-PEG1500-PCL1250三嵌段共聚物.通過覈磁共振氫譜及凝膠滲透色譜對其組成、結構及分子量進行錶徵:製備不同凝膠濃度及初始載藥量的載藥溫敏凝膠,併對其相轉變性能、體外藥物釋放行為以及體內的生物降解性能進行攷察.結果 覈磁共振及凝膠滲透色譜測定結果錶明:閤成的共聚物組成與初始投料比一緻,符閤設計的PCL1250-PEG1500-PCL1250嵌段聚閤物結構;該凝膠在15%～30%濃度區間內,具備溫敏性溶膠-凝膠相轉變能力;該溫敏凝膠對紫杉醇具有可控的藥物緩釋能力,通過改變凝膠濃度及初始載藥量可調節藥物釋放速率和維持釋放的時間.小鼠揹部皮下註射PCL1250-PEG1500-PCL1250溶膠後在體內迅速原位凝膠化,凝膠隨植入時間逐漸降解至45 d時基本降解完全.結論 PCL1250-PEG1500-PCL1250溫敏凝膠作為紫杉醇載藥體繫具有良好的藥物控釋能力和體內生物降解性能.
목적 이용취기내지-취을이순-취기내지(PCL1250-PEG1500-PCL1250)량친성취합물온민응효작위재체재료,구건소수성항종류약물자삼순적재약체계.방법 이신산아석위최화제、취을이순위인발제,인발기내지단체개배취합,합성PCL1250-PEG1500-PCL1250삼감단공취물.통과핵자공진경보급응효삼투색보대기조성、결구급분자량진행표정:제비불동응효농도급초시재약량적재약온민응효,병대기상전변성능、체외약물석방행위이급체내적생물강해성능진행고찰.결과 핵자공진급응효삼투색보측정결과표명:합성적공취물조성여초시투료비일치,부합설계적PCL1250-PEG1500-PCL1250감단취합물결구;해응효재15%～30%농도구간내,구비온민성용효-응효상전변능력;해온민응효대자삼순구유가공적약물완석능력,통과개변응효농도급초시재약량가조절약물석방속솔화유지석방적시간.소서배부피하주사PCL1250-PEG1500-PCL1250용효후재체내신속원위응효화,응효수식입시간축점강해지45 d시기본강해완전.결론 PCL1250-PEG1500-PCL1250온민응효작위자삼순재약체계구유량호적약물공석능력화체내생물강해성능.
Objective To construct an injectable controlled delivery system of paclitaxel based on thermosensitive PCL1250-PEG1500-PCL1250 hydrogels. Methods A thermosensitive PCL1250-PEG1500-PCL1250 triblock copolymer was synthesized by ring-opening polymerization of e-CL using PEG (Mw=l 500) as the initiator and Sn(Oct)2 as the catalyst. The synthesized PCL1250-PEG1500-PCL1250 copolymers were characterized for their composition,structure, and molecular weight via 1H NMR and GPC techniques. A series of Paclitaxel loaded hydrogels with various predesigned hydrogel concentrations and initial drug loadings were prepared to investigate their gelation ability, in vitro drug release behavior and in vivo biodegradability. Results The results calculated from 1H NMR and GPC indicated that EG/CL ratio(1.55) was consistent with the initial feed ratio(1.6), which offered a strong proof to their composition and molecular structure. The thermosensitive PCL1250-PEG1500-PCL1250 hydrogels exhibited a desirable sol-gel transition ability within the concentration range of 15%-30%. The in vitro release rate of paclitaxel from the paclitaxel/PCL1250-PEG1500-PCL1250 hydrogels was controllable by altering the hydrogel concentrations and initial drug loadings. The PCL1250-PEG1500-PCL1250 hydrogels showed a good in situ gelation ability after subcutaneously injected into mouse back. The in situ formed hydrogels gradually degradated with time and almost disappeared after 45 days in vivo. Conclusion Both the controllable drug release behavior and promising biodegradability of this new thermosensitive PCL1250-PEG1500-PCL1250 hydrogels paved a way to develop a novel delivery system for paclitaxel.
