基于5-氟尿嘧啶和lepidin的纳米乳凝胶:体外和皮肤动力学评价。

IF 3.9 4区 医学 Q1 PHARMACOLOGY & PHARMACY
Zeba Usmani, Samreen Jahan, Zakiya Usmani, Abdul Ahad, Mohd Akhtar, Mohd Aqil, Mohd Mujeeb
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引用次数: 0

摘要

皮肤癌是最普遍的恶性肿瘤,发病率和发病率都在上升,尤其是在白人人群中。本研究旨在开发一种含有5-氟尿嘧啶(5-FU)和lepidine (LPD)的双重载药纳米乳凝胶,以促进角质层和真皮层的药物沉积,从而改善皮肤癌的治疗。以薄荷油、Tween 80和PEG-400为原料,采用水相滴定法制备水包油纳米乳,并通过拟三元相图进行优化。优化后的双载药纳米乳粒径为131.7±3.21 nm, PDI为0.21±0.005,zeta电位为-26.24±1.532 mV。然后将该纳米乳液分散到1%卡波波尔934凝胶中用于局部应用。体外和离体研究表明,该药物可显著增强药物沉积和延长释放时间(**p
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Bipartite 5-fluorouracil and lepidine-based nanoemulsion gel: in vitro and dermatokinetic evaluation.

Skin cancer is the most prevalent malignancy, with rising incidence and morbidity, particularly among the white population. This study aims to develop a dual drug-loaded nanoemulsion (NE) gel incorporating 5-fluorouracil (5-FU) and lepidine (LPD) to enhance drug deposition in the stratum corneum and dermal layer for improved skin cancer therapy. Oil-in-water (o/w) NEs were prepared using peppermint oil, Tween 80 and PEG-400 via aqueous phase titration method and optimised through pseudo-ternary phase diagrams. The optimised dual drug-loaded NE showed particle size of 131.7 ± 3.21 nm, PDI of 0.21 ± 0.005 and zeta potential of -26.24 ± 1.532 mV. This NE was then dispersed into a 1% carbopol 934 gel for topical application. In vitro and ex vivo studies demonstrated significantly enhanced drug deposition and prolonged release (**p < .001) compared to a conventional gel. Furthermore, dermatokinetic and CLSM studies confirmed enhanced skin permeation and deeper drug distribution. Skin irritation studies indicated that the NE gel was safe and non-irritant. It is concluded that the developed 5-FU and LPD co-loaded NE gel enhances topical drug delivery against skin cancer by improving drug absorption and distribution between the epidermis and dermis in rodent skin model, which could represent promising strategy for the management of skin cancer.

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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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