Article
Medicine, Research & Experimental
Priyanka S. Radadiya, Mackenzie M. Thornton, Rajni Puri, Sireesha Yerrathota, Johnny Dinh-Phan, Brenda Magenheimer, Dharmalingam Subramaniam, Pamela Tran, Hao Zhu, Subhashini Bolisetty, James P. Calvet, Darren P. Wallace, Madhulika Sharma
Summary: Ciclopirox or its olamine salt inhibits cyst growth in PKD mice by inducing ferritin degradation, suggesting its potential as a treatment for autosomal dominant PKD.
Article
Chemistry, Multidisciplinary
Jeffrey Lin, Maryam Zangi, Tanguturi Venkata Narayana Hajay Kumar, Makala Shakar Reddy, Lingala Vijaya Raghava Reddy, Subir Kumar Sadhukhan, Daniel P. Bradley, Brenda Moreira-Walsh, Tiffany C. Edwards, Austin T. O'Dea, John E. Tavis, Marvin J. Meyers, Maureen J. Donlin
Summary: Ciclopirox olamine, an N-hydroxypyridone, has shown broad fungicidal activity against various fungi, including Cryptococcus neoformans and Candida albicans. The structure-activity relationship study suggests that a lipophilic functional group at position six of the N-hydroxypyridone ring is necessary, and further substitution at positions four and six may be tolerated for enhanced efficacy. These findings provide a promising starting point for the development of novel antifungal therapies.
Article
Chemistry, Medicinal
Xinyan Wan, Junqi Xiang, Hui Fan, Ying Jiang, Yiting Lu, Chundong Zhang, Ying Zhang, Quanmei Chen, Yunlong Lei
Summary: Hepatocellular carcinoma is a prevalent and deadly cancer, but early identification and diagnosis remain challenging. The synthetic antifungal agent, Ciclopirox olamine (CPX), has shown potential as an anti-cancer drug for hepatocellular carcinoma, although its specific mechanisms of action have not been fully elucidated. This study demonstrates that CPX inhibits HCC cell proliferation by arresting the cell cycle, while also triggering ROS accumulation and downregulating DJ-1. CPX also induces complete autophagic flux, although this can mitigate its anti-cancer effects, and it induces glycogen clustering in HCC cells. Overall, this research provides new insights into the molecular mechanisms of CPX as an anti-cancer therapy for hepatocellular carcinoma.
Article
Biochemistry & Molecular Biology
Yiying Zhu, Zhangxun Zhao, Minggao Xue, Dan Wang, Guifeng Su, Xiaoman Ju, Qihong Yang, Shaohua Zhang, Dongmei Fan, Huifang Zhu, Min Yu, Yan Li, Lingmei Kong, Hongyu Zhou
Summary: Activation of the NKG2D receptor can enhance the sensitivity of leukemia cells to NK cell cytotoxicity, and this can be achieved through the use of drugs such as Ciclopirox Olamine (CPX). CPX can increase the expression of NKG2D ligands (NKG2DLs) on leukemia cells, thereby enhancing the efficacy of NK cell-mediated immunotherapy.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Instruments & Instrumentation
Ma. Florencia Peralta, Nadina A. Usseglio, Ma. Estefania Bracamonte, Ma. Laura Guzman, Ma. Eugenia Olivera, J. Diego Marco, Paola A. Barroso, Dolores C. Carrer
Summary: Topical treatment with dispersions containing miltefosine and different liposome compositions has shown to be effective in treating cutaneous leishmaniasis. Fluid liposomes can accelerate lesion healing and reduce the time needed to eliminate viable parasites from the lesion site.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Article
Oncology
Jie Yin, Gang Che, Kan Jiang, Ziyang Zhou, Lingyun Wu, Mengyou Xu, Jian Liu, Senxiang Yan
Summary: This study demonstrates that ciclopirox olamine (CPX) exhibits antitumor effects in lung adenocarcinoma (LUAD) cells by targeting TOP2A. CPX inhibits LUAD proliferation, induces reactive oxygen species (ROS) production, causes DNA damage, and activates the ATR-CHK1-P53 pathway. Furthermore, CPX significantly suppresses in vivo LUAD xenograft growth without toxicity or side effects.
FRONTIERS IN ONCOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Lingbo Shen, Guihua Fang, Bo Tang, Qiang Zhu
Summary: Topical corticosteroids are the primary treatment for ocular inflammation, and factors such as drug properties and administration strategies affect drug bioavailability in the eye. Currently, there is a lack of rational and dynamic approaches to strategy selection.
JOURNAL OF CONTROLLED RELEASE
(2021)
Review
Pharmacology & Pharmacy
Victor Hmingthansanga, Nidhi Singh, Superna Banerjee, Sivakumar Manickam, Ravichandiran Velayutham, Subramanian Natesan
Summary: Delivery of drugs via transdermal routes offers advantages, but overcoming the skin's barrier properties remains challenging. Chemical permeation enhancers (CPEs) can improve transdermal drug delivery, but may have side effects. With advancements in analytical techniques, synthetic chemistry, and combinatorial studies, CPEs-aided transdermal drug delivery is expected to reach its full potential.
Review
Pharmacology & Pharmacy
Abhinav Thareja, Helen Hughes, Carmen Alvarez-Lorenzo, Jenni J. Hakkarainen, Zubair Ahmed
Summary: There is a clinical need for efficient eye drop formulations to treat posterior ocular segment diseases non-invasively. Cell penetrating peptides (CPPs), TAT, and penetratin are inferred as the most efficient penetration enhancers for drug delivery to the fundus oculi via topical eye drop instillation, but further high-quality experimental studies are needed for quantitative efficacy confirmation.
Article
Polymer Science
Agne Mazurkeviciute, Inga Matulyte, Marija Ivaskiene, Modestas Zilius
Summary: Emulsions are unstable systems and it is difficult to produce biphasic formulations with large amounts of oil. This study aimed to prepare biphasic formulations with 1% ciclopirox olamine and investigate the influence of oil incorporation method on the properties of the formulations. The results showed that using poloxamer 407 gel as the hydrophase could lead to stable formulations regardless of the oil incorporation method, while the addition of emulsifier improved the stability of the formulations.
Article
Pharmacology & Pharmacy
Tao Jiang, Shuangshuang Ma, Yangyang Shen, Yuwen Li, Ruirui Pan, Huaixin Xing
Summary: Various strategies, including functionalized nanostructures, have been developed to overcome the stratum corneum barrier for topical anesthesia and pain relief. A novel compound PB-PEG-DSPE was synthesized and used to design TAT/PB LID NLC for the delivery of lidocaine hydrochloride, showing superior percutaneous penetration ability and anesthetic effect.
Article
Biochemistry & Molecular Biology
Agota Peto, Dora Kosa, Adam Haimhoffer, Daniel Nemes, Palma Feher, Zoltan Ujhelyi, Miklos Vecsernyes, Judit Varadi, Ferenc Fenyvesi, Adina Frum, Felicia Gabriela Gligor, Laura Gratiela Vicas, Eleonora Marian, Tunde Jurca, Annamaria Pallag, Mariana Eugenia Muresan, Zoltan Toth, Ildiko Bacskay
Summary: The study aimed to explore the medicinal value of Philadelphus coronarius and develop topical ointments. The composition and excipients of the ointments were found to greatly impact drug release, texture, and bioavailability. Despite being effective against Escherichia coli and Staphylococcus aureus, the P. coronarius leaf did not significantly decrease IL-4 production in HaCaT cells. The topical application of P. coronarius could be a valuable addition to antimicrobial therapy.
Review
Polymer Science
Aneta Ostrozka-Cieslik
Summary: Hormones have gained significant attention as potential drugs for treating various diseases, but formulating hormone-containing drug forms has limitations. This review discusses the development of hydrogels as potential hormone carriers and factors affecting the efficacy of hormones applied to the skin.
Article
Chemistry, Physical
Katarzyna Mielech-Lukasiewicz, Milena Domalewska
Summary: This study proposed a method for detecting ciclopirox olamine using a BDDE electrode, which was validated through optimization and the use of cyclic voltammetry and square wave voltammetry. The results demonstrated good sensitivity and repeatability of the method, making it successful for the detection of ciclopirox olamine in pharmaceutical preparations.
Article
Pharmacology & Pharmacy
Ekaterina P. Vasyuchenko, Philipp S. Orekhov, Grigoriy A. Armeev, Marine E. Bozdaganyan
Summary: The cutaneous delivery route is increasingly common for drug administration, with the use of chemical penetration enhancers (CPEs) to facilitate drug transport through skin layers. The creation of a CPE-DB database allows for the classification and identification of new enhancers, as well as the prediction of biological activity using machine-learning applications.