Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 06100, Tandogan- Ankara, Turkey.
Curr Drug Deliv. 2014;11(1):98-111. doi: 10.2174/15672018113109990055.
Biodegradable spray-dried chitosan microparticles loaded with clindamycin phosphate (CDP) were formulated to deliver drugs locally into the periodontal pocket. The effects of spray dryer conditions, drug/polymer ratio, and added amounts of glutaraldehyde (GA) solution on the characterization of microparticles were investigated by determining process yield, encapsulation efficiency, particle size and size distribution, surface morphology, drug release, release kinetics, thermal analysis, and antimicrobial efficacy of formulations. Burst release was obtained for all formulations due to the water solubility of the drug, but the increased amount of chitosan decreased the drug release rates. Microparticles with a more wrinkled surface were obtained by increasing the amount of the drug. Incorporation efficiencies higher than 80% were obtained for all preparation conditions. The addition of GA caused higher viscosity of the chitosan solution, leading to larger particles with more spherical and smooth surface characteristics. However, the increased GA amount did not significantly influence the drug release. The data obtained from in vitro release experiments were best fitted to the Weibull and Higuchi models. The amorphous nature of the drug-loaded microparticles was detected by differential scanning calorimetric (DSC) thermographs. A delayed drug release of more than one week could be obtained by loading the drug into the chitosan microparticles. Antimicrobial efficacy studies reflected a positive drug release profile. These results indicate that spray-dried clindamycin-loaded microparticles with sustained antimicrobial efficacy appear to be a promising periodontal therapy for drug delivery into the periodontal pocket.
可生物降解的喷雾干燥壳聚糖载克林霉素磷酸酯（CDP）微球被制成局部递送至牙周袋的药物。通过测定工艺产率、包封效率、粒径和粒径分布、表面形态、药物释放、释放动力学、热分析和制剂的抗菌功效，研究了喷雾干燥条件、药物/聚合物比以及加入的戊二醛（GA）溶液量对微球特性的影响。由于药物的水溶性，所有制剂均获得了突释，但壳聚糖的用量增加会降低药物释放率。通过增加药物的用量，可以获得表面更皱缩的微球。对于所有制备条件，均获得了高于 80%的包封效率。GA 的加入会导致壳聚糖溶液的粘度增加，从而得到具有更球形和光滑表面特征的较大颗粒。然而，GA 用量的增加并没有显著影响药物的释放。体外释放实验得到的数据最符合 Weibull 和 Higuchi 模型。药物负载微球的无定形性质通过差示扫描量热法（DSC）热图检测到。通过将药物载入壳聚糖微球中，可以获得超过一周的延迟药物释放。抗菌功效研究反映了药物释放的积极模式。这些结果表明，具有持续抗菌功效的喷雾干燥克林霉素载药微球似乎是一种有前途的牙周病治疗方法，可将药物递送至牙周袋。
