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米诺环素包封壳聚糖纳米颗粒的中枢镇痛活性。

Minocycline encapsulated chitosan nanoparticles for central antinociceptive activity.

机构信息

Division of Research and Development, Lovely Professional University, Punjab 144411, India.

Department of Pharmaceutical Sciences, Guru Jambeshwar University of Science & Technology, Hisar, Haryana, 125001, India.

出版信息

Int J Biol Macromol. 2015 Jan;72:131-5. doi: 10.1016/j.ijbiomac.2014.07.055. Epub 2014 Aug 9.

DOI:10.1016/j.ijbiomac.2014.07.055
PMID:25111492
Abstract

The purpose of the study is to explore the central anti-nociceptive activity of brain targeted nanoparticles (NP) of minocycline hydrochloride (MH). The NP were formulated using the modified ionotropic gelation method (MHNP) and were coated with Tween 80 (T80) to target them to brain (cMHNP). The formulated nanoparticles have already been characterized for particle size, zeta potential, drug entrapment efficiency and in vitro drug release. The nanoparticles were then evaluated for pharmacodynamic activity using thermal methods. The pure drug and the formulation, MHNP were not able to show a statistically significant central analgesic activity. cMHNP on the other hand evidenced a significant central analgesic activity. Animal models evidenced that brain targeted nanoparticles may be utilized for effective delivery of central anti-nociceptive effect of MH. Further clinical studies are required to explore the activity for mankind.

摘要

本研究旨在探索盐酸米诺环素(MH)脑靶向纳米粒子(NP)的中枢抗伤害作用。NP 采用改良的离子凝胶法(MHNP)进行制剂,并采用吐温 80(T80)进行包被以靶向脑部(cMHNP)。已对所制备的纳米粒子的粒径、Zeta 电位、药物包封效率和体外药物释放进行了表征。然后使用热法评估了纳米粒子的药效学活性。纯药物和制剂 MHNP 均不能显示出统计学上显著的中枢镇痛活性。另一方面,cMHNP 表现出显著的中枢镇痛活性。动物模型表明,脑靶向纳米粒子可用于有效递送至 MH 的中枢抗伤害作用。需要进一步的临床研究来探索对人类的活性。

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