以乙醇体为基础递送甜菜素和姜黄素提高抗炎疗效。

IF 3.9 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Sangameshwar B Kanthale, Vaibhav Bharad, Prakash Kendre, Ashish Tale, Sachin Borikar, Shirish Jain
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引用次数: 0

摘要

天然植物成分如甜菜素和姜黄素因其显著的抗氧化和抗炎特性而引起了人们的兴趣。它们的治疗效果明显受到生物利用度不足和皮肤渗透性降低的限制。目前的研究开发了一种基于乙醇体的凝胶系统,用于输送甜菜素和姜黄素,目的是改善透皮渗透并提供持续的抗炎作用。采用冷法制备脂质体,并对粒径、zeta电位和包封效率等理化特性进行了优化。优化后的配方平均粒径为202.8 nm, zeta电位为-56.4 mV,对甜菜素和姜黄素的包封效率分别为80%和85%。SEM和FT-IR表征证实了酶质体的成功包封和结构完整性。该酶体凝胶的最佳pH值为6.5,具有假塑性粘度和优异的涂抹性,适合外用。体外扩散研究表明,缓释谱持续8小时。皮肤刺激试验证实了它的生物相容性。采用卡拉胶炎症模型对大鼠体内抗炎效果进行了评价,结果表明,乙醇体凝胶能明显减轻动物的炎症。这些发现表明,醇质体制剂是一种很有前途的增强抗炎功效的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Ethosome-based delivery of betanin and curcumin for improved anti-inflammatory efficacy.

Natural phytoconstituents such as betanin and curcumin have attracted interest for their significant antioxidant and anti-inflammatory properties. Their therapeutic efficacy is notably constrained by inadequate bioavailability and reduced skin permeability. The current study developed an ethosome-based gel system for the delivery of betanin and curcumin, with the objective of improving transdermal penetration and providing sustained anti-inflammatory effects. Ethosomes were formulated by cold method and optimised for physicochemical characteristics including particle size, zeta potential and entrapment efficiency. The optimised formulation exhibited a mean particle size of 202.8 nm, a zeta potential of -56.4 mV and high entrapment efficiencies of 80% for betanin and 85% for curcumin. The characterisation using SEM and FT-IR confirmed the successful encapsulation and structural integrity of the ethosomes. The ethosomal gel demonstrated an optimal pH of 6.5, pseudoplastic viscosity and superior spreadability, making it appropriate for topical use. In vitro diffusion studies demonstrated a sustained release profile lasting 8 h. Skin irritation tests confirmed its biocompatibility. The in vivo anti-inflammatory efficacy was assessed in rats by utilising carrageenan model of inflammation, results showed that ethosomal gel significantly attenuated inflammation in animals. These findings indicate that the ethosome preparation represents a promising approach for enhancing anti-inflammatory efficacy.

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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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