Exploring nalbuphine loaded chitosan nanoparticles for effective pain management through intranasal administration: a comparative study.

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Journal of Drug Targeting Pub Date : 2025-01-01 Epub Date: 2024-09-04 DOI:10.1080/1061186X.2024.2397800
Kushagra Khanna, Nitin Sharma, Ritu Karwasra, Abhishek Kumar, Dhruv Kumar Nishad, Ashok Kumar Janakiraman, Ravishankar Ram Mani, Mogana Rajagopal, Saad Tayyab, Bhawna Goel
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引用次数: 0

Abstract

Background: Intranasal drug delivery shows potential for brain access via olfactory and trigeminal routes.

Purpose: This work aimed to ensure brain availability of nalbuphine via the nasal route.

Method: Chitosan based nanoparticles loaded with nalbuphine were successfully prepared using ionic gelation method and characterised.

Result: SEM results revealed that the nanoparticles were spherical in shape, with an average size of 192.4 ± 11.6 nm. Zeta potential and entrapment efficiency was found 32.8 mV and 88.43 ± 7.75%, respectively. The X-ray diffractometry and DSC results unravel a profound understanding on the physical and thermal characteristics. The in-vitro release of nalbuphine from the nanoparticles was biphasic, with an initial burst release followed by a slow-release profile. In-vitro cell study on HEK-293 cells and microscopic images of brain tissue confirmed the safety profile of formulation. In-vivo efficacy studies on animal confirmed the effectiveness of developed intranasal formulation as compared to the standard therapy. The in-vivo pharmacokinetic studies showed that the prepared nanoparticles were able to efficiently deliver nalbuphine to the brain in comparison to the other body organs. Gamma scintigraphy images showed retention of the drug in the brain. Furthermore, the efficacy studies confirmed that the nanoparticles were found significantly more effective than the marketed formulation in pain management.

探索通过鼻内给药有效镇痛的纳布啡载壳聚糖纳米颗粒:一项比较研究。
背景:鼻内给药具有通过嗅觉和三叉神经途径进入大脑的潜力:鼻内给药显示了通过嗅觉和三叉神经途径进入大脑的潜力。目的:这项工作旨在确保纳布啡通过鼻腔途径进入大脑:方法:采用离子凝胶法成功制备了负载纳布啡的壳聚糖基纳米颗粒,并对其进行了表征:扫描电镜结果显示,纳米颗粒呈球形,平均粒径为 192.4 ± 11.6 nm。Zeta 电位和夹带效率分别为 32.8 mV 和 88.43 ± 7.75%。X 射线衍射仪和 DSC 结果揭示了对物理和热特性的深刻理解。纳布啡从纳米颗粒中的体外释放是双相的,最初是突然释放,随后是缓慢释放。HEK-293 细胞的体外细胞研究和脑组织的显微图像证实了该制剂的安全性。对动物进行的体内药效研究证实,与标准疗法相比,所开发的鼻内配方非常有效。体内药代动力学研究表明,与其他身体器官相比,所制备的纳米颗粒能够有效地将纳布啡输送到大脑。伽马闪烁图显示了药物在大脑中的保留情况。此外,药效研究证实,纳米颗粒在镇痛方面的效果明显优于市场上销售的制剂。
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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
期刊介绍: Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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