{"title":"开发出一种脑部靶向粘液黏附性阿米舒必利纳米结构脂质载体","authors":"Manar Adnan Tamer","doi":"10.31925/farmacia.2023.5.18","DOIUrl":null,"url":null,"abstract":"This research aimed to create and refine intranasal mucoadhesive amisulpride-loaded nanostructured lipid carriers (AMS-MNLCs) to increase efficacy and safety by increasing nasal-mucosal adhesion and facilitating direct brain targetability. Using HPMC K4M, Carbopol 934, and Hyaluronic acid (HA), AMS-MNLCs were made by applying modified melt-emulsification and ultra-sonication procedures. The results of the pH, osmolarity, and mucoadhesive tests on the optimized formulation were 6.3 ± 0.02, 304.53 ± 2.15, and 26.07 ± 0.37, respectively. Rheological investigation, in-vitro release and ex-vivo permeation study of the optimized formulation revealed a shear-thinning behaviour, significantly higher release, and the flux of the drug from the formula was 975.2 ± 12.45. Based on the pharmacokinetic analyses in rats, intranasal AMS-MNLCs were reported to have a brain C max about 14 times higher than intravenous AMS-solution. In addition, two weeks of intranasal administration of formulation did not affect haematological parameters in the in vivo research. The histopathological investigation showed that there was no disruption of the naso-mucosal membrane structure. Therefore, the created and optimized intranasal MNLCs showed a promised venue for the efficient and secure delivery of AMS as an antiemetic drug for the prevention and treatment of preoperative nausea and vomiting (PONV).","PeriodicalId":12344,"journal":{"name":"FARMACIA","volume":null,"pages":null},"PeriodicalIF":1.4000,"publicationDate":"2023-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"THE DEVELOPMENT OF A BRAIN TARGETED MUCOADHESIVE AMISULPRIDE LOADED NANOSTRUCTURED LIPID CARRIER\",\"authors\":\"Manar Adnan Tamer\",\"doi\":\"10.31925/farmacia.2023.5.18\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"This research aimed to create and refine intranasal mucoadhesive amisulpride-loaded nanostructured lipid carriers (AMS-MNLCs) to increase efficacy and safety by increasing nasal-mucosal adhesion and facilitating direct brain targetability. Using HPMC K4M, Carbopol 934, and Hyaluronic acid (HA), AMS-MNLCs were made by applying modified melt-emulsification and ultra-sonication procedures. The results of the pH, osmolarity, and mucoadhesive tests on the optimized formulation were 6.3 ± 0.02, 304.53 ± 2.15, and 26.07 ± 0.37, respectively. Rheological investigation, in-vitro release and ex-vivo permeation study of the optimized formulation revealed a shear-thinning behaviour, significantly higher release, and the flux of the drug from the formula was 975.2 ± 12.45. Based on the pharmacokinetic analyses in rats, intranasal AMS-MNLCs were reported to have a brain C max about 14 times higher than intravenous AMS-solution. In addition, two weeks of intranasal administration of formulation did not affect haematological parameters in the in vivo research. The histopathological investigation showed that there was no disruption of the naso-mucosal membrane structure. Therefore, the created and optimized intranasal MNLCs showed a promised venue for the efficient and secure delivery of AMS as an antiemetic drug for the prevention and treatment of preoperative nausea and vomiting (PONV).\",\"PeriodicalId\":12344,\"journal\":{\"name\":\"FARMACIA\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.4000,\"publicationDate\":\"2023-10-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"FARMACIA\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.31925/farmacia.2023.5.18\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"FARMACIA","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.31925/farmacia.2023.5.18","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
THE DEVELOPMENT OF A BRAIN TARGETED MUCOADHESIVE AMISULPRIDE LOADED NANOSTRUCTURED LIPID CARRIER
This research aimed to create and refine intranasal mucoadhesive amisulpride-loaded nanostructured lipid carriers (AMS-MNLCs) to increase efficacy and safety by increasing nasal-mucosal adhesion and facilitating direct brain targetability. Using HPMC K4M, Carbopol 934, and Hyaluronic acid (HA), AMS-MNLCs were made by applying modified melt-emulsification and ultra-sonication procedures. The results of the pH, osmolarity, and mucoadhesive tests on the optimized formulation were 6.3 ± 0.02, 304.53 ± 2.15, and 26.07 ± 0.37, respectively. Rheological investigation, in-vitro release and ex-vivo permeation study of the optimized formulation revealed a shear-thinning behaviour, significantly higher release, and the flux of the drug from the formula was 975.2 ± 12.45. Based on the pharmacokinetic analyses in rats, intranasal AMS-MNLCs were reported to have a brain C max about 14 times higher than intravenous AMS-solution. In addition, two weeks of intranasal administration of formulation did not affect haematological parameters in the in vivo research. The histopathological investigation showed that there was no disruption of the naso-mucosal membrane structure. Therefore, the created and optimized intranasal MNLCs showed a promised venue for the efficient and secure delivery of AMS as an antiemetic drug for the prevention and treatment of preoperative nausea and vomiting (PONV).
期刊介绍：
FARMACIA publishes original research papers, invited topical reviews and editorial commentaries and news, with emphasis on conceptual novelty and scientific quality. Main research areas are focused on: pharmacology, toxicology, medicinal chemistry, biopharmacy, drug design, drug delivery, personalized medicine, nanostructures, nutraceuticals, biochemistry and biotechnology. Manuscripts submitted to the Journal are only accepted after the peer review precess. The papers should have not been published in any other journal. The recommendations of the Declaration of Helsinki, for humans, and the International guidelines as accepted principles for the use of experimental animals should be followed.
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