In Vitro Evaluation of Inhalable Isoniazid-Loaded Surfactant Liposomes as an Adjunct Therapy in Pulmonary Tuberculosis
In Vitro Evaluation of Inhalable Isoniazid-Loaded Surfactant Liposomes as an Adjunct Therapy in Pulmonary Tuberculosis
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DOI：
10.1002/jbm.b.31608
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发表时间：
2010-07-01
影响因子：
3.4
通讯作者：
Banerjee, R.
中科院分区：
文献类型：
--
作者：
Chimote, G.;Banerjee, R.
在这项研究中，评估了外源性肺表面活性物质作为抗结核药物异烟肼（INH）的可吸入药物载体。异烟肼包封脂质体的二棕榈酰磷脂酰胆碱（DPPC）（最丰富的脂质肺表面活性剂和外源性表面活性剂）的开发和评价的大小，药物包封，释放，在体外肺泡沉积，生物相容性，抗分枝杆菌活性，和肺表面活性剂的行动。包封的DPPC脂质体直径约为750 nm，包封率为36.7% ± 1.8%。DPPC脂质体在24 h内持续释放INH。使用双撞击器进行的体外肺泡沉积效率显示出与使用喷射雾化器进行1分钟雾化后肺泡腔中25-27%的INH沉积相似。在37 ℃下，该制剂具有更好的肺表面活性剂功能，吸附时表面张力的降低（36.7 +/-0.4 mN/m）比DPPC脂质体（44.7 +/-0.6 mN/m）更快，并且该制剂在毛细管表面活性计中显示87%的气道通畅率。该制剂具有生物相容性和抗分枝杆菌活性。DPPC脂质体由于表面活性剂的抗肺不张作用，可增加抗结核药物INH到达肺泡的距离，从而实现肺部给药和肺泡稳定的双重目的。(C)2010 Wiley Periodicals，Inc. J Biomed Mater Res Part B：Appl Biomater 946：1-10，2010.
In this study, exogenous pulmonary surfactant was evaluated as an inhalable drug carrier for antitubercular drug isoniazid (INH). Isoniazid-entrapped liposomes of dipalmitoyl-phosphatidylcholine (DPPC) (the most abundant lipid of lung surfactant and exogenous surfactant) were developed and evaluated for size, drug entrapment, release, in vitro alveolar deposition, biocompatibility, antimycobacterial activity, and pulmonary surfactant action. Isoniazid-entrapped DPPC liposomes were about 750 nm in diameter and had entrapment efficiency of 36.7% +/- 1.8%. Sustained release of INH from DPPC liposomes was observed over 24 h. In vitro alveolar deposition efficiency using the twin impinger exhibited similar to 25-27% INH deposition in the alveolar chamber upon one minute nebulization using a jet nebulizer. At 37 degrees C, the formulation had better pulmonary surfactant function with quicker reduction of surface tension on adsorption (36.7 +/- 0.4 mN/m) than DPPC liposomes (44.7 +/- 0.6 mN/m) and 87% airway patency was exhibited by the formulation in a capillary surfactometer. The formulation was biocompatible and had antimycobacterial activity. The isoniazid-entrapped DPPC liposomes could fulfill the dual purpose of pulmonary drug delivery and alveolar stabilization due to antiatelectatic effect of the surfactant action which can improve the reach of antitubercular drug INH to the alveoli. (C) 2010 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater 946: 1-10, 2010.