Sustained release of isoniazid from polylactide microspheres prepared using solid/oil drug loading method for tuberculosis treatment.
Polylactide (PLA) microspheres were prepared using the solid-in-oil (S/O) spray-drying method to achieve the sustained release of a hydrophilic drug for the treatment of tuberculosis, via intratracheal instillation. Isoniazid (IN), a low-molecular-weight hydrophilic drug, was used as a model drug. The effects of various sizes of micronized IN powder, different drug/polymer ratios, spray-drying process parameters, and drug-release characteristics were studied to optimize the manufacturing parameters. A high entrapment efficiency (87.3%) was obtained using this method; furthermore, the microspheres were spherical and smooth. They were individually and homogenously distributed, with a mean diameter of 5.6 μm; furthermore, they showed a satisfactory extended sustained-release phase. After administration of the microspheres to rats, pulmonary drug concentrations were maintained at a relatively stable level for up to 4 weeks.
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100193, China.
Limei
L
Zhang
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100193, China.
Ying
Y
Li
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100193, China.
Yun
Y
Zhang
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100193, China. cyzhu@implad.ac.cn.
Chunyan
C
Zhu
D000818:Animals; D000995:Antitubercular Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002152:Calorimetry, Differential Scanning; D002853:Chromatography, Liquid; D004337:Drug Carriers; D066298:In Vitro Techniques; D007538:Isoniazid / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008863:Microspheres; D051381:Rats; D014376:Tuberculosis / Q000188:drug therapy*
D000995:Antitubercular Agents; D004337:Drug Carriers; D007538:Isoniazid
intratracheal intubation; isoniazid; polylactide microspheres; solid/oil spraying method; sustained release