他沙罗汀治疗痤疮乳状剂的设计、优化及体内评价。

IF 3.9 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Amit Pratap Singh, Sushil Kumar Kashaw, Vandana Soni
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引用次数: 0

摘要

寻常痤疮是一种常见的皮肤疾病,目前的治疗方法通常局限于皮肤渗透性差、不稳定、刺激和治疗效果不佳。迫切需要先进的药物输送系统来克服这些挑战并提高治疗效果。在此背景下,目前的研究是开发和优化一种新型的他zarotene负载凝胶制剂,它融合了乳液和凝胶的优点,以实现药物释放控制,提高稳定性,以及局部痤疮治疗的卓越临床性能。采用掺入法制备该制剂,并通过Box-Behnken统计设计(BBD)进行优化。以Carbopol 940 (X1)、Span 80 (X2)、Tween 80 (X3)三个自变量评价其对药物释放(Y1)和黏度(Y2)的影响。优化后的配方pH: 6.6±0.3,粘度:28,945 cPs,铺展性:6.17±0.02 cm2,挤压性:18±2.49 gm/cm2,药物含量:85.46±4.02%。体外释药研究表明,7小时内释药87.59±2.6%。小鼠皮肤刺激试验证实了其皮肤安全性,没有出现红斑或水肿的迹象。使用痤疮丙酸杆菌诱导的小鼠模型评估抗痤疮功效,与将痤疮病变从4.6 mm减少到2.3 mm的市售凝胶相比,优化后的乳液显着将痤疮病变从4.5 mm减少到0 mm。这些结果突出了他zarotene负载乳液作为一个有前途的和安全的局部治疗痤疮,提供优越的功效比市售配方。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, optimisation and in vivo evaluation of tazarotene loaded emulgel formulation for the treatment of acne.

Acne vulgaris is a common dermatological disorder, with current treatments often limited to poor skin penetration, instability, irritation and suboptimal therapeutic outcomes. There is a pressing need for advanced drug delivery systems that can overcome these limitations and enhance treatment efficacy. This study aimed to develop and optimise a novel tazarotene-loaded emulgel formulation, combining the advantages of emulsions and gels to achieve controlled drug release, improved stability and superior clinical performance in topical acne therapy. The formulation was prepared using the incorporation method and optimised through the Box-Behnken statistical design (BBD). Three independent variables, such as Carbopol 940 (X1), Span 80 (X2) and Tween 80 (X3), were assessed for their effects on drug release (Y1) and viscosity (Y2). The optimised formulation exhibited desirable characteristics, including pH: 6.6 ± 0.3, viscosity: 28,945 cPs, spreadability: 6.17 ± 0.02 cm2, extrudability: 18 ± 2.49 g/cm2 and drug content: 85.46 ± 4.02%. In vitro studies demonstrated 87.59 ± 2.6% drug release over 7 h. A skin irritation test in mice confirmed its dermatological safety, with no signs of erythema or oedema. Anti-acne efficacy, evaluated using a Propionibacterium acnes-induced murine model, revealed complete lesion clearance, outperforming a marketed gel. These findings firmly establish the tazarotene-loaded emulgel as a safe, effective, and superior topical treatment for acne.

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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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