文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期,新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

基于 SLNs 的透皮凝胶制剂中卢立康唑的皮肤滞留时间延长有助于改善抗真菌活性。

Prolonged Skin Retention of Luliconazole from SLNs Based Topical Gel Formulation Contributing to Ameliorated Antifungal Activity.

机构信息

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, 143005, India.

Department of Chemistry, Panjab University, Chandigarh, Punjab, 160014, India.

出版信息

AAPS PharmSciTech. 2024 Oct 1;25(7):229. doi: 10.1208/s12249-024-02945-0.


DOI:10.1208/s12249-024-02945-0
PMID:39354184
Abstract

The development of effective therapy is necessary because the patients have to contend with long-term therapy as skin fungal infections usually relapse and are hardly treated. Despite being a potent antifungal agent, luliconazole (LCZ) has certain shortcomings such as limited skin penetration, low solubility in aqueous medium, and poor skin retention. Solid Lipid Nanoparticles (SLNs) were developed using biodegradable lipids by solvent injection method and were embodied into the gel base for topical administration. After in-vitro characterizations of the formulations, molecular interactions of the drug with excipients were analyzed using in-silico studies. Ex-vivo release was determined in contrast to the pure LCZ and the commercial formulation followed by in-vivo skin localization, skin irritation index, and antifungal activity. The prepared SLNs have an average particle size of 290.7 nm with no aggregation of particles and homogenous gels containing SLNs with ideal rheology and smooth texture properties were successfully prepared. The ex-vivo LCZ release from the SLN gel was lower than the commercial formulation whereas its skin deposition and skin retention were higher as accessed by CLSM studies. The drug reaching the systemic circulation and the skin irritation potential were found to be negligible. The solubility and drug retention in the skin were both enhanced by the development of SLNs as a carrier. Thus, SLNs offer significant advantages by delivering long lasting concentrations of LCZ at the site of infection for a complete cure of the fungal load together with skin localization of the topical antifungal drug.

摘要

因为皮肤真菌感染通常会复发且难以治疗,所以需要开发有效的治疗方法。尽管卢立康唑(LCZ)是一种有效的抗真菌药物,但它也存在一些缺点,如皮肤穿透性有限、在水介质中的溶解度低以及皮肤滞留性差。固体脂质纳米粒(SLN)是通过溶剂注入法用可生物降解的脂质开发的,并被嵌入到局部给药的凝胶基质中。在对制剂进行体外特性评估后,使用计算机模拟研究分析了药物与赋形剂的分子相互作用。与纯 LCZ 和市售制剂相比,测定了体外释放情况,随后进行了体内皮肤定位、皮肤刺激性指数和抗真菌活性测定。所制备的 SLN 的平均粒径为 290.7nm,没有粒子聚集,并且成功制备了含有 SLN 的均匀凝胶,具有理想的流变学和光滑的质地特性。通过 CLSM 研究发现,从 SLN 凝胶中释放的 LCZ 低于市售制剂,但其皮肤沉积和皮肤滞留更高。通过计算机模拟研究发现,到达体循环的药物量和皮肤刺激性潜力可以忽略不计。通过开发 SLN 作为载体,可以提高药物的溶解度和在皮肤中的滞留性。因此,SLN 提供了显著的优势,能够在感染部位持续释放长时间的 LCZ 浓度,从而彻底清除真菌负荷,并使局部抗真菌药物在皮肤中定位。

相似文献

[1]
Prolonged Skin Retention of Luliconazole from SLNs Based Topical Gel Formulation Contributing to Ameliorated Antifungal Activity.

AAPS PharmSciTech. 2024-10-1

[2]
Luliconazole vesicular based gel formulations for its enhanced topical delivery.

J Liposome Res. 2020-12

[3]
Sucrose ester stabilized solid lipid nanoparticles and nanostructured lipid carriers. II. Evaluation of the imidazole antifungal drug-loaded nanoparticle dispersions and their gel formulations.

Nanotechnology. 2014-2-14

[4]
Fluconazole-loaded solid lipid nanoparticles topical gel for treatment of pityriasis versicolor: formulation and clinical study.

Drug Deliv. 2018-11

[5]
Polymeric micelle gel with luliconazole: in vivo efficacy against cutaneous candidiasis in Wistar rats.

Naunyn Schmiedebergs Arch Pharmacol. 2024-9

[6]
Nanoemulsion gel-based topical delivery of an antifungal drug: in vitro activity and in vivo evaluation.

Drug Deliv. 2016

[7]
Solid lipid nanoparticles (SLNs) gels for topical delivery of aceclofenac in vitro and in vivo evaluation.

Curr Drug Deliv. 2013-12

[8]
Preparation and in vivo evaluation of solid lipid nanoparticles of griseofulvin for dermal use.

J Biomed Nanotechnol. 2013-4

[9]
Histological assessment of follicular delivery of flutamide by solid lipid nanoparticles: potential tool for the treatment of androgenic alopecia.

Drug Dev Ind Pharm. 2016

[10]
Formulation and optimization of nanoemulsion using antifungal lipid and surfactant for accentuated topical delivery of Amphotericin B.

Drug Deliv. 2016-10

引用本文的文献

[1]
An Updated Perspective on Skin Disease Therapy: From Conventional Methods to Nanocarrier Innovations.

AAPS PharmSciTech. 2025-8-8

[2]
Zinc Oxide Nanoparticles in Modern Science and Technology: Multifunctional Roles in Healthcare, Environmental Remediation, and Industry.

Nanomaterials (Basel). 2025-5-17

[3]
Insights into Liposomal and Gel-Based Formulations for Dermatological Treatments.

Gels. 2025-3-26

本文引用的文献

[1]
Application of ensemble machine learning approach to assess the factors affecting size and polydispersity index of liposomal nanoparticles.

Sci Rep. 2023-10-21

[2]
Development of Soft Luliconazole Invasomes Gel for Effective Transdermal Delivery: Optimization to In-Vivo Antifungal Activity.

Gels. 2023-8-3

[3]
New Insights in Topical Drug Delivery for Skin Disorders: From a Nanotechnological Perspective.

ACS Omega. 2023-5-19

[4]
and Effect of the Imidazole Luliconazole against and spp.

Microbiol Spectr. 2023-6-15

[5]
Current Advances in Lipid Nanosystems Intended for Topical and Transdermal Drug Delivery Applications.

Pharmaceutics. 2023-2-15

[6]
Solid lipid nanoparticles for phytosterols delivery: The acyl chain number of the glyceride matrix affects the arrangement, stability, and release.

Food Chem. 2022-11-15

[7]
The global, regional, and national burden of fungal skin diseases in 195 countries and territories: A cross-sectional analysis from the Global Burden of Disease Study 2017.

JAAD Int. 2020-11-30

[8]
AutoDock Vina 1.2.0: New Docking Methods, Expanded Force Field, and Python Bindings.

J Chem Inf Model. 2021-8-23

[9]
Dermatokinetic assessment of luliconazole-loaded nanostructured lipid carriers (NLCs) for topical delivery: QbD-driven design, optimization, and in vitro and ex vivo evaluations.

Drug Deliv Transl Res. 2022-5

[10]
SLN and NLC for topical, dermal, and transdermal drug delivery.

Expert Opin Drug Deliv. 2020-2-17

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索