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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Enhancing drug incorporation into tetracycline-loaded chitosan microspheres for periodontal therapy
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Enhancing drug incorporation into tetracycline-loaded chitosan microspheres for periodontal therapy

机译：增强药物掺入四环素壳聚糖微球的牙周治疗

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Purpose:To identify optimal formulation parameters for enhancing the incorporation of tetracycline hydrochloride into chitosan microspheres for periodontal therapy.Methods:Tetracycline-loaded chitosan microspheres were prepared by ionotropic gelation.Various formulation parameters(salt form of drug,aqueous phase pH,anion structure,inorganic salts and electrolytes,preparation method)were investigated for their influence on drug incorporation efficiency.Microspheres were assessed in terms of drug entrapment and content,microsphere recovery,particle size and morphology.Results:Although drug incorporation efficiency was increased marginally,the use of a dihydrate form of the drug was not considered feasible due to the lowered microsphere recovery and higher costs.A decrease in the aqueous pH from 9 to 6 enhanced drug incorporation efficiency without an adverse effect on microsphere morphology.The use of inorganic salts/electrolytes and other approaches of microsphere preparation did not significantly enhance drug incorporation efficiency and these approaches also adversely affected microsphere morphology.The ionotropic preparation method in terms of the drug loading technique significantly affected drug incorporation efficiencies.Conclusions:This study has shown that formulation variables can be exploited in order to enhance the incorporation of a water soluble drug into chitosan microspheres using the ionotropic gelation technique.Based on a comparison of all results obtained with the different approaches,the modification of the aqueous phase to pH 6 was identified as the most feasible approach.
机译：目的：确定最佳的配方参数，以增强盐酸四环素掺入壳聚糖微球中用于牙周治疗。方法：通过离子凝胶法制备负载四环素的壳聚糖微球。各种配方参数（药物的盐形式，水相pH，阴离子结构，研究了无机盐和电解质（制备方法）对药物掺入效率的影响。从药物截留量，含量，微球回收率，粒径和形态等方面对微球进行了评估。结果：尽管药物掺入效率略有提高，但使用由于降低了微球的回收率和增加了成本，因此认为二水合形式的药物不可行。将pH值从9降低到6可以提高药物的掺入效率，而对微球的形态没有不利影响。使用无机盐/电解质和微球制备的其他方法没有成功显着提高药物掺入效率，这些方法也对微球形态产生不利影响。就药物加载技术而言，离子型制备方法显着影响了药物掺入效率。通过离子化凝胶技术将水溶性药物溶解到壳聚糖微球中。基于对不同方法获得的所有结果的比较，将水相改性至pH 6被认为是最可行的方法。

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