Sustained antibacterial activity of doxycycline-loaded poly(D,L-lactide-co-glycolide) and poly(ε-caprolactone) nanoparticles
Sustained antibacterial activity of doxycycline-loaded poly(D,L-lactide-co-glycolide) and poly(ε-caprolactone) nanoparticles
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DOI：
10.2217/nnm.09.28
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发表时间：
2009-07-01
期刊：
影响因子：
5.5
通讯作者：
Sahoo, Sanjeeb K.
中科院分区：
文献类型：
--
作者：
Misra, Ranjita;Acharya, Sarbari;Sahoo, Sanjeeb K.
目的：通过改变处方中聚合物比例、载药量(w/w)、溶剂选择、电解液加入量和pH等处方参数，将多西环素(Dxy)聚(D，L-丙交酯-乙交酯)：聚己内酯(PCL)纳米粒的包封率提高70%以上。方法：以不同比例的可生物降解聚合物PLGA和PCL，采用水包油包水复乳技术制备水溶性DXY纳米粒。纳米粒的物理化学表征包括尺寸和表面电荷的测量、表面形貌的扫描电子显微镜研究、傅立叶变换红外光谱研究、差示扫描量热法分析和体外释放动力学研究。结果：动态激光散射法测得纳米粒的平均粒径为230~360 mm，扫描电子显微镜证实了纳米粒的球形和光滑的表面。傅立叶变换红外光谱分析表明，纳米粒中的药物与聚合物之间没有相互作用。对载药纳米粒的差示扫描量热法分析表明，DXY在制剂中存在分子水平的分散。采用生长抑制法和菌落计数法检测了天然DXY和DXY纳米粒对一株大肠杆菌(DH5α)的抑菌活性。结果表明，由于DXY纳米粒在大肠杆菌中的持续释放，DXY纳米粒比天然DXY纳米粒更有效。
Aim: To increase the entrapment efficiency of doxycycline (DXY)-loaded poly(D,L-lactide-co-glycolide) (PLGA):poly(epsilon-caprolactone) (PCL) nanoparticles by up to 70% by varying the different formulation parameters such as polymer ratio, amount of drug loading (w/w), solvent selection, electrolyte addition and pH in the formulation. Method: Biodegradable polymers PLGA and PCL are used in various ratios for nanoparticle preparation using the water-in-oil-in-water double emulsion technique for water-soluble DXY. The physicochemical characterization of nanoparticles included size and surface charge measurement, study of surface morphology using scanning-electron microscopy, Fourier transform infrared spectroscopy study, differential scanning calorimetry analysis and in vitro release kinetics study. Results: The mean particle size ranged from 230 to 360 rim, as measured by dynamic laser light scattering, and scanning-electron microscopy confirmed the spherical nature and smooth surface of the nanoparticles. Fourier transform infrared spectroscopy analysis of void nanoparticles, drug-loaded nanoparticles and native DXY indicated no interaction between the drug and polymer in the nanoparticle. Differential scanning calorimetry analysis of drug-loaded nanoparticles indicated a molecular level dispersion of DXY in the formulation. The antibacterial activity of native DXY and DXY-loaded nanoparticles were tested using a strain of Escherichia coli (DH5 alpha) through growth inhibition and colony-counting method. The results indicated that DXY-loaded nanoparticles are more effective than native DXY due to the sustained release of DXY from nanoparticles in the E. coli strain.