中国组织工程研究
中國組織工程研究
중국조직공정연구
Journal of Clinical Rehabilitative Tissue Engineering Research
2015年
3期
421-426
,共6页
生物材料%缓释材料%聚乳酸-羟基乙酸共聚物微球%聚乙二醇%利福平%突释%国家自然科学基金
生物材料%緩釋材料%聚乳痠-羥基乙痠共聚物微毬%聚乙二醇%利福平%突釋%國傢自然科學基金
생물재료%완석재료%취유산-간기을산공취물미구%취을이순%리복평%돌석%국가자연과학기금
Subject headings:Biocompatible Materials%Delayed-Action Preparations%Polyglactin 910
背景：聚乳酸-羟基乙酸共聚物微球具有良好的生物相容性，是优良的药物缓释载体，但缓释微球的突释问题严重影响了其临床应用。
<br> 目的：观察聚乙二醇对利福平-聚乳酸-羟基乙酸聚合物缓释微球特征、载药率、包封率、体外释放规律及突释的影响。
<br> 方法：以高分子材料聚乳酸-羟基乙酸共聚物作为载体，采用复乳化-溶剂挥发法制备聚乙二醇-利福平-聚乳酸-羟基乙酸聚合物微球(实验组)和利福平-聚乳酸-羟基乙酸聚合物微球(对照组)。扫描电子显微镜观察两组聚合物缓释微球特征，高效液相色谱法检测两组微球在不同时段模拟体液中的利福平药物浓度及累计释放量，计算两组微球的载药量、包封率。
<br> 结果与结论：与对照组比较，实验组微球表面光滑、粒径减小、分散良好，包封率和载药量明显提高。实验组微球3 h内药物释放量最大，1 d左右药物释放趋于平稳稳定状态，1 d药物累计释放量小于20%；对照组微球3 h内药物释放量最大，约为实验组的1.5倍，1 d左右药物释放也趋于平稳状态。表明聚乙二醇可改善利福平-聚乳酸-羟基乙酸聚合物缓释微球的成球率，减小其粒径，增加其载药量和包封率，控制其突释现象。
揹景：聚乳痠-羥基乙痠共聚物微毬具有良好的生物相容性，是優良的藥物緩釋載體，但緩釋微毬的突釋問題嚴重影響瞭其臨床應用。
<br> 目的：觀察聚乙二醇對利福平-聚乳痠-羥基乙痠聚閤物緩釋微毬特徵、載藥率、包封率、體外釋放規律及突釋的影響。
<br> 方法：以高分子材料聚乳痠-羥基乙痠共聚物作為載體，採用複乳化-溶劑揮髮法製備聚乙二醇-利福平-聚乳痠-羥基乙痠聚閤物微毬(實驗組)和利福平-聚乳痠-羥基乙痠聚閤物微毬(對照組)。掃描電子顯微鏡觀察兩組聚閤物緩釋微毬特徵，高效液相色譜法檢測兩組微毬在不同時段模擬體液中的利福平藥物濃度及纍計釋放量，計算兩組微毬的載藥量、包封率。
<br> 結果與結論：與對照組比較，實驗組微毬錶麵光滑、粒徑減小、分散良好，包封率和載藥量明顯提高。實驗組微毬3 h內藥物釋放量最大，1 d左右藥物釋放趨于平穩穩定狀態，1 d藥物纍計釋放量小于20%；對照組微毬3 h內藥物釋放量最大，約為實驗組的1.5倍，1 d左右藥物釋放也趨于平穩狀態。錶明聚乙二醇可改善利福平-聚乳痠-羥基乙痠聚閤物緩釋微毬的成毬率，減小其粒徑，增加其載藥量和包封率，控製其突釋現象。
배경：취유산-간기을산공취물미구구유량호적생물상용성，시우량적약물완석재체，단완석미구적돌석문제엄중영향료기림상응용。
<br> 목적：관찰취을이순대리복평-취유산-간기을산취합물완석미구특정、재약솔、포봉솔、체외석방규률급돌석적영향。
<br> 방법：이고분자재료취유산-간기을산공취물작위재체，채용복유화-용제휘발법제비취을이순-리복평-취유산-간기을산취합물미구(실험조)화리복평-취유산-간기을산취합물미구(대조조)。소묘전자현미경관찰량조취합물완석미구특정，고효액상색보법검측량조미구재불동시단모의체액중적리복평약물농도급루계석방량，계산량조미구적재약량、포봉솔。
<br> 결과여결론：여대조조비교，실험조미구표면광활、립경감소、분산량호，포봉솔화재약량명현제고。실험조미구3 h내약물석방량최대，1 d좌우약물석방추우평은은정상태，1 d약물루계석방량소우20%；대조조미구3 h내약물석방량최대，약위실험조적1.5배，1 d좌우약물석방야추우평은상태。표명취을이순가개선리복평-취유산-간기을산취합물완석미구적성구솔，감소기립경，증가기재약량화포봉솔，공제기돌석현상。
BACKGROUND:Polylactic acid as a carrier has good biocompatibility, but the burst release of microspheres seriously affects their clinical application.
<br> OBJECTIVE:To investigate the effects of polyethylene glycol on rifampicin-polylactic acid-glycolic acid microspheres in terms of morphologies, drug loading, encapsulation efficiency, in vitro release and burst release.
<br> METHODS: Polylactic acid-glycolic acid polymer was used as a carrier, and polyethylene glycol-rifampicin-polylactic acid-glycolic acid polymer microspheres (experimental group) and rifampicin-polylactic acid-glycolic acid polymer microspheres were prepared using W/O/W emulsifying-solvent evaporation technique. The characteristics of two kinds of microscopes were observed by scanning electron microscopy, drug concentration and cumulative release of rifampicin in the simulated body fluid were detected using high performance liquid chromatography during different periods, and drug loading as wel as encapsulation efficiency was also determined in the two groups.
<br> RESULTS AND CONCLUSION: Compared with the control group, in the experimental group, the microspheres were found smooth surface, even distribution, decreased particle size and good dispersion, and the drug loading and encapsulation efficiency were evidently higher. In the experimental group, the largest amount of drug release of the microspheres was within 3 hours, the drug release tended to be stable at 1 day, and the cumulative drug release was less than 20% in1 day. In the control group, the largest amount of drug release was within 3 hours, but the amount was about 1.5 times than that of the experimental group, the drug release also tended to stable at 1 day. The study has shown that polyethylene glycol can improve the peletizing ratio and reduce the particle size of rifampicin-polylactic acid-glycolic acid microspheres, increase the drug loading and encapsulation efficiency of rifampicin, and reduce the burst release in the process of rifampicin release.
