Antibiotic release from biodegradable PHBV microparticles
Antibiotic release from biodegradable PHBV microparticles
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DOI：
10.1016/s0168-3659(98)00195-3
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发表时间：
1999-05-20
影响因子：
10.8
通讯作者：
Hasirci, V
中科院分区：
文献类型：
--
作者：
Sendil, D;Gürsel, I;Hasirci, V
对于牙周病的治疗，控释系统的设计似乎是非常合适的一个有效的，长期的结果。在这项研究中，一种新的，可生物降解的微生物聚酯，聚（3-羟基丁酸酯-co-3-羟基戊酸酯），PHBV的各种戊酸含量含有一个完善的抗生素，四环素，已知是有效的对许多牙周病相关的微生物，被用于建设的控制释放系统。四环素以其酸性形式（TC）和中性形式（TCN）负载在PHBV微球和微胶囊中。采用w/o/w复相乳液法在不同条件下制备了PHBV微胶囊，并对其包封率、载药量、释放特性和形态学等进行了研究。结果表明，乳化剂聚乙烯醇（PVA）和明胶的浓度（0-4%）对包封率有一定的影响。为了增加包封效率（从获得的18.1-30.1%的范围）和减缓释放的高度可溶性四环素。HCl，用NaOH中和。由于在包封过程中使用的药物的不溶性形式，中和四环素的包封效率高得多（51.9-65.3%）。两种药物的释放行为均不为零级。相反，这些趋势与Higuchi的球形微球释放方法相当吻合。生物降解性不是从微胶囊中释放的可感知参数，因为在观察到任何降解迹象之前释放已经完成。(C)1999 Elsevier Science B. V.保留所有权利。
For the treatment of periodontal diseases, design of a controlled release system seemed very appropriate for an effective, long term result. In this study a novel, biodegradable microbial polyester, poly(3-hydroxybutyrate-co-3-hydroxyvalerate), PHBV of various valerate contents containing a well established antibiotic, tetracycline, known to be effective against many of the periodontal disease related microorganisms, was used in the construction of a controlled release system. Tetracycline was loaded in the PHBV microspheres and microcapsules both in its acidic (TC) and in neutral form (TCN). Microcapsules of PHBV were prepared under different conditions using w/o/w double emulsion and their properties such as encapsulation efficiency, loading, release characteristics, and morphological properties were investigated. It was found that concentration of emulsifiers polyvinyl alcohol (PVA) and gelatin (varied between 0-4%) influenced the encapsulation efficiency appreciably. In order to increase encapsulation efficiency (from the obtained range of 18.1-30.1%) and slow down the release of the highly soluble tetracycline. HCl, it was neutralized with NaOH. Encapsulation efficiency of neutralized tetracycline was much higher (51.9-65.3%) due to the insoluble form of the drug used during encapsulation. The release behaviour of neither of the drugs was found to be of zero order. Rather the trends fitted reasonably well to Higuchi's approach for release from spherical micropheres. Biodegradability was not an appreciable parameter in the release from microcapsules because release was complete before any signs of degradation were observed. (C) 1999 Elsevier Science B.V. All rights reserved.