{"title":"基于Pullulan和Pluronic F-127的鼻腔内给药原位凝胶系统:开发,体外和体内评估","authors":"H. Mahajan, V. Jadhao, Sachin M. Chandankar","doi":"10.1177/08839115221110284","DOIUrl":null,"url":null,"abstract":"The current work seeks to use Pullulan and Pluronic F-127 (PF-127), a new gel-forming material, for sildenafil citrate (SLC) intranasal delivery. The cold approach was used to develop an SLC-loaded in situ gel based on thermoreversible polymer PF-127 and mucoadhesive polymer Pullulan. In situ gel systems based on Pullulan responds intelligently to environmental stimuli like charge, pH, temperature, light, and redox. To achieve gelation at physiological temperature formulations were modified to have gelation temperatures lower than 34.1°C. Physical appearance and rheological measurements were used to calculate the temperature of gelation. With the addition of increasing quantities of Pullulan, the gelation temperatures fell (from 34.1°C for 8% w/v, 10% w/v, and 12% w/v 0.5% Pullulan). In the goat nasal mucosal membrane, Pullulan concentration increased the mucoadhesive force in terms of detachment stress. The results of drug permeation testing in vitro investigations over the goat nasal mucosa showed that utilizing an in situ gelling formulation with a Pullulan content of 0.5% or higher can greatly boost the effective penetration coefficient. The formulation was shown to be safe for the nasal mucosa after a histological investigation. Conclusively, Pullulan and PF-127 may be appropriate carriers for SLC intranasal administration.","PeriodicalId":15038,"journal":{"name":"Journal of Bioactive and Compatible Polymers","volume":" 3","pages":"406 - 418"},"PeriodicalIF":2.1000,"publicationDate":"2022-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"5","resultStr":"{\"title\":\"Pullulan and Pluronic F-127 based in situ gel system for intranasal delivery: Development, in vitro and in vivo evaluation\",\"authors\":\"H. Mahajan, V. Jadhao, Sachin M. Chandankar\",\"doi\":\"10.1177/08839115221110284\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The current work seeks to use Pullulan and Pluronic F-127 (PF-127), a new gel-forming material, for sildenafil citrate (SLC) intranasal delivery. The cold approach was used to develop an SLC-loaded in situ gel based on thermoreversible polymer PF-127 and mucoadhesive polymer Pullulan. In situ gel systems based on Pullulan responds intelligently to environmental stimuli like charge, pH, temperature, light, and redox. To achieve gelation at physiological temperature formulations were modified to have gelation temperatures lower than 34.1°C. Physical appearance and rheological measurements were used to calculate the temperature of gelation. With the addition of increasing quantities of Pullulan, the gelation temperatures fell (from 34.1°C for 8% w/v, 10% w/v, and 12% w/v 0.5% Pullulan). In the goat nasal mucosal membrane, Pullulan concentration increased the mucoadhesive force in terms of detachment stress. The results of drug permeation testing in vitro investigations over the goat nasal mucosa showed that utilizing an in situ gelling formulation with a Pullulan content of 0.5% or higher can greatly boost the effective penetration coefficient. The formulation was shown to be safe for the nasal mucosa after a histological investigation. Conclusively, Pullulan and PF-127 may be appropriate carriers for SLC intranasal administration.\",\"PeriodicalId\":15038,\"journal\":{\"name\":\"Journal of Bioactive and Compatible Polymers\",\"volume\":\" 3\",\"pages\":\"406 - 418\"},\"PeriodicalIF\":2.1000,\"publicationDate\":\"2022-07-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"5\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Bioactive and Compatible Polymers\",\"FirstCategoryId\":\"5\",\"ListUrlMain\":\"https://doi.org/10.1177/08839115221110284\",\"RegionNum\":4,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"BIOTECHNOLOGY & APPLIED MICROBIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Bioactive and Compatible Polymers","FirstCategoryId":"5","ListUrlMain":"https://doi.org/10.1177/08839115221110284","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"BIOTECHNOLOGY & APPLIED MICROBIOLOGY","Score":null,"Total":0}
Pullulan and Pluronic F-127 based in situ gel system for intranasal delivery: Development, in vitro and in vivo evaluation
The current work seeks to use Pullulan and Pluronic F-127 (PF-127), a new gel-forming material, for sildenafil citrate (SLC) intranasal delivery. The cold approach was used to develop an SLC-loaded in situ gel based on thermoreversible polymer PF-127 and mucoadhesive polymer Pullulan. In situ gel systems based on Pullulan responds intelligently to environmental stimuli like charge, pH, temperature, light, and redox. To achieve gelation at physiological temperature formulations were modified to have gelation temperatures lower than 34.1°C. Physical appearance and rheological measurements were used to calculate the temperature of gelation. With the addition of increasing quantities of Pullulan, the gelation temperatures fell (from 34.1°C for 8% w/v, 10% w/v, and 12% w/v 0.5% Pullulan). In the goat nasal mucosal membrane, Pullulan concentration increased the mucoadhesive force in terms of detachment stress. The results of drug permeation testing in vitro investigations over the goat nasal mucosa showed that utilizing an in situ gelling formulation with a Pullulan content of 0.5% or higher can greatly boost the effective penetration coefficient. The formulation was shown to be safe for the nasal mucosa after a histological investigation. Conclusively, Pullulan and PF-127 may be appropriate carriers for SLC intranasal administration.
期刊介绍:
The use and importance of biomedical polymers, especially in pharmacology, is growing rapidly. The Journal of Bioactive and Compatible Polymers is a fully peer-reviewed scholarly journal that provides biomedical polymer scientists and researchers with new information on important advances in this field. Examples of specific areas of interest to the journal include: polymeric drugs and drug design; polymeric functionalization and structures related to biological activity or compatibility; natural polymer modification to achieve specific biological activity or compatibility; enzyme modelling by polymers; membranes for biological use; liposome stabilization and cell modeling. This journal is a member of the Committee on Publication Ethics (COPE).