基于伪三元相图的聚乙二醇化奈利唑胺纳米分散体促进伤口再生:体外和体内评价。

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Journal of Drug Targeting Pub Date : 2025-07-01 Epub Date: 2025-02-12 DOI:10.1080/1061186X.2025.2461093
Bani Kumar Jana, Ishita Singha, Nusalu Puro, Rinku Baishya, Rajat Subhra Dutta, Mohini Singh, Bhaskar Mazumder
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引用次数: 0

摘要

开放性伤口容易发生细菌浸润,其中大多数是耐甲氧西林金黄色葡萄球菌等耐药菌株,影响开放性伤口的愈合。使用精油作为纳米凝胶的局部利奈唑胺纳米分散体可以增加药物的溶解度,并避免口服给药引起的胃肠道刺激等副作用。建立伪三元相图对纳米乳进行优化。将混合液(tween20: PEG400 = 3:1)、去离子水、油混合液(丁香油:薰衣草油= 4:1)与药物进行旋流后超声处理。制备优化后的1%卡波醇凝胶纳米乳,并对其进行进一步表征,然后进行抗菌研究、HEK293细胞系细胞相容性研究和大鼠切除模型伤口愈合研究。组织学研究证实角质层和上皮组织的生长。优化后的配方粒径(244.6±178.66nm)、PDI(25%)、包封效率(92.3±3.38%)、体外释药率(87.58±4.16%)符合korsmemeyer - peppas动力学模型(R2=0.9969)。NEGF6(0.2%w/w)的黏度为5345±6cP,对MRSA具有良好的抗菌效果。在800µg/ml的浓度下,HEK293细胞存活率高达90%,显示出良好的细胞相容性。创面收缩率为99.66±0.57%,第15天每日应用1gm,创面角质层基本再生。由此可见,所研制的纳米凝胶具有潜在的抗菌作用,并能促进伤口愈合。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pseudo-ternary phase diagram based PEGylated nano-dispersion of linezolid to promote wound regeneration: an in vitro and in vivo evaluation.

Open wounds are prone to bacterial infiltration mostly resistant strains like methicillin-resistant Staphylococcus aureus (MRSA), which affects healing of open wounds. Topical linezolid nano-dispersion using essential oils as nanoemulgel can increase solubility of drug and bypass side-effects like GI-irritation of oral administration. Pseudo-ternary phase diagram was built to optimise nanoemulsion. Surfactant/co-surfactant mixture (3:1), deionised water and Oilmix (4:1) with drug were vortexed and then ultrasonicated. 1% carbopol gel of optimised nanoemulsion was prepared and characterised, exposed to antimicrobial study, cytocompatibility study using HEK293 cell-line, and in vivo wound healing study using rat excision model. Histological study was performed to confirm growth of stratum corneum. Optimised formulation has particle size (244.6 ± 178.66 nm), polydispersity index (25%), entrapment efficiency (92.3 ± 3.38%) and in vitro drug release (87.58 ± 4.16%) best fitted in Korsmeyer-Peppas kinetics model. Nanoemulgel F6 (0.2%w/w) was found with viscosity of 5345 ± 6 cP constituting a very excellent antimicrobial effect against MRSA. HEK293 cells had shown good cytocompatibility with formulation. The wound contraction rate was 99.66 ± 0.57% at day 15 on daily application of nanoemulgel and stratum corneum was almost fully regenerated. The developed nanoemulgel has potential antimicrobial efficacy and can promote wound healing.

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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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