Brain delivery of buspirone hydrochloride chitosan nanoparticles for the treatment of general anxiety disorder
Brain delivery of buspirone hydrochloride chitosan nanoparticles for the treatment of general anxiety disorder
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DOI：
10.1016/j.ijbiomac.2015.07.041
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发表时间：
2015-11-01
影响因子：
8.2
通讯作者：
Ali, Javed
中科院分区：
文献类型：
--
作者：
Bari, Naimat Kalim;Fazil, Mohammad;Ali, Javed
本工作讨论了盐酸丁螺环酮（BUH）的巯基化壳聚糖纳米粒（TCS-NPs）的制备、表征和经鼻脑内给药的体内评价。TCS NPs通过离子凝胶化方法制备并表征各种参数。形成的NP具有226.7 +/-2.52nm的粒度，PDI为0.483 +/-0.031。发现药物包封率（EE）和负载容量（LC）为81.13 +/- 2.8和49.67 +/-5.5%。药物经鼻粘膜的累积渗透百分率为76.21%。在猪粘蛋白上进行的生物粘附研究显示生物粘附效率为90.218 +/-0.134%。通过共聚焦激光扫描显微镜（CLSM）技术使用罗丹明-123作为标记物研究安慰剂NP的鼻-脑递送。鼻内给药TCS-NP后达到的脑浓度为797.46 +/- 35.76 ng/ml，t（max）为120 min，显著高于静脉内给药BUH溶液后达到的384.15 +/- 13.42 ng/ml和t（max）为120 min，鼻内给药BUH溶液后达到的417.77 +/- 19.24 ng/ml。ml和t（max）60 min。（C）2015 Elsevier B. V.保留所有权利。
The present work discusses the preparation, characterization and in vivo evaluation of thiolated chitosan nanoparticles (TCS-NPs) of buspirone hydrochloride (BUH) for brain delivery through intranasal route. TCS NPs were prepared by ionic gelation method and characterized for various parameters. The NPs formed were having particle size of 226.7 +/- 2.52 nm with PDI 0.483 +/- 0.031. Drug entrapment efficiency (EE) and loading capacity (LC) were found to be 81.13 +/- 2.8 and 49.67 +/- 5.5%. The cumulative percentage drug permeation through nasal mucosa was 76.21%. Bioadhesion study carried out on porcine mucin and showed a bioadhesion efficiency of 90.218 +/- 0.134%. Nose-to-brain delivery of placebo NPs was investigated by confocal laser scanning microscopy (CLSM) technique using rhodamine-123 as a marker. The brain concentration achieved after intranasal administration of TCS-NPs was 797.46 +/- 35.76 ng/ml with t(max) 120 min which was significantly higher than achieved after intravenous administration on BUH solution 384.15 +/- 13.42 ng/ml and t(max) of 120 min and intranasal administration of BUH solution 417.77 +/- 19.24 ng/ml and t(max) 60 min. (C) 2015 Elsevier B.V. All rights reserved.