{"title":"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。","authors":"Kushagra Khanna, Nitin Sharma, Ritu Karwasra, Abhishek Kumar, Dhruv Kumar Nishad, Ashok Kumar Janakiraman, Ravishankar Ram Mani, Mogana Rajagopal, Saad Tayyab, Bhawna Goel","doi":"10.1080/1061186X.2024.2397800","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Intranasal drug delivery shows potential for brain access via olfactory and trigeminal routes.</p><p><strong>Purpose: </strong>This work aimed to ensure brain availability of nalbuphine via the nasal route.</p><p><strong>Method: </strong>Chitosan based nanoparticles loaded with nalbuphine were successfully prepared using ionic gelation method and characterised.</p><p><strong>Result: </strong>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 <i>in-vitro</i> release of nalbuphine from the nanoparticles was biphasic, with an initial burst release followed by a slow-release profile. <i>In-vitro</i> cell study on HEK-293 cells and microscopic images of brain tissue confirmed the safety profile of formulation. <i>In-vivo</i> efficacy studies on animal confirmed the effectiveness of developed intranasal formulation as compared to the standard therapy. The <i>in-vivo</i> 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.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"99-110"},"PeriodicalIF":4.3000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Exploring nalbuphine loaded chitosan nanoparticles for effective pain management through intranasal administration: a comparative study.\",\"authors\":\"Kushagra Khanna, Nitin Sharma, Ritu Karwasra, Abhishek Kumar, Dhruv Kumar Nishad, Ashok Kumar Janakiraman, Ravishankar Ram Mani, Mogana Rajagopal, Saad Tayyab, Bhawna Goel\",\"doi\":\"10.1080/1061186X.2024.2397800\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Intranasal drug delivery shows potential for brain access via olfactory and trigeminal routes.</p><p><strong>Purpose: </strong>This work aimed to ensure brain availability of nalbuphine via the nasal route.</p><p><strong>Method: </strong>Chitosan based nanoparticles loaded with nalbuphine were successfully prepared using ionic gelation method and characterised.</p><p><strong>Result: </strong>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 <i>in-vitro</i> release of nalbuphine from the nanoparticles was biphasic, with an initial burst release followed by a slow-release profile. <i>In-vitro</i> cell study on HEK-293 cells and microscopic images of brain tissue confirmed the safety profile of formulation. <i>In-vivo</i> efficacy studies on animal confirmed the effectiveness of developed intranasal formulation as compared to the standard therapy. The <i>in-vivo</i> 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.</p>\",\"PeriodicalId\":15573,\"journal\":{\"name\":\"Journal of Drug Targeting\",\"volume\":\" \",\"pages\":\"99-110\"},\"PeriodicalIF\":4.3000,\"publicationDate\":\"2025-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Drug Targeting\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/1061186X.2024.2397800\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/9/4 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Targeting","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/1061186X.2024.2397800","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/9/4 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Exploring nalbuphine loaded chitosan nanoparticles for effective pain management through intranasal administration: a comparative study.
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.
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.