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

IF 2.1 4区 生物学 Q3 BIOTECHNOLOGY & APPLIED MICROBIOLOGY
H. Mahajan, V. Jadhao, Sachin M. Chandankar
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引用次数: 5

摘要

目前的工作寻求使用Pullulan和Pluronic F-127 (PF-127),一种新的凝胶形成材料,用于枸橼酸西地那非(SLC)的鼻内给药。采用冷法制备了一种基于热可逆聚合物PF-127和黏附聚合物pululan的负载slc的原位凝胶。基于Pullulan的原位凝胶系统对环境刺激(如电荷、pH值、温度、光和氧化还原)做出智能反应。为了在生理温度下实现凝胶化,对配方进行了改性,使凝胶化温度低于34.1℃。物理外观和流变学测量用于计算凝胶温度。随着普鲁兰添加量的增加,凝胶温度下降(8% w/v、10% w/v和12% w/v 0.5%普鲁兰时为34.1℃)。在山羊鼻粘膜中,普鲁兰浓度在剥离应力方面增加了黏附力。体外对山羊鼻黏膜的药物渗透试验结果表明,普鲁兰含量在0.5%以上的原位胶凝制剂可显著提高药物的有效渗透系数。经组织学检查,该制剂对鼻黏膜是安全的。总之,普鲁兰和PF-127可能是鼻内给药SLC的合适载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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.
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来源期刊
Journal of Bioactive and Compatible Polymers
Journal of Bioactive and Compatible Polymers 工程技术-材料科学:生物材料
CiteScore
3.50
自引率
0.00%
发文量
27
审稿时长
2 months
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).
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