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Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells. To overcome these shortcomings, researchers have explored a number of strategies, such as chemical structural modifications, microsphere dispersion systems, and nanodrug delivery systems. This review summarizes the structure-activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity. This review can provide evidence for further research of NCTD.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9693198 | PMC |
http://dx.doi.org/10.3390/molecules27227740 | DOI Listing |
Pharm Dev Technol
September 2025
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, wenhua Road 103, Shenyang 110016, PR China.
Nimodipine (NMP), a poorly water-soluble small-molecule agent, demonstrates notable therapeutic limitations in addressing cerebral vasospasm secondary to subarachnoid hemorrhage (SAH). Owing to its inherent physicochemical properties characterized by low oral bioavailability, rapid elimination half-life, and extensive first-pass metabolism, conventional formulations necessitate frequent dosing regimens to sustain therapeutic plasma concentrations. These pharmacological challenges collectively result in suboptimal patient adherence, marked plasma concentration fluctuations, and recurrent vascular irritation.
View Article and Find Full Text PDFMol Pharm
September 2025
Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Phytosterols are a class of natural steroids found in various plants. Commercially available phytosterols (PS) are primarily extracted from the deodorized distillate of soybean oil and consist predominantly of β-sitosterol with smaller amounts of stigmasterol and campesterol. Numerous studies have consistently demonstrated the significant lipid-lowering activity of PS.
View Article and Find Full Text PDFBioimpacts
July 2025
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
Vitiligo, a chronic autoimmune disorder characterized by the presence of depigmented skin patches, remains a therapeutic challenge due to its multifactorial pathogenesis and the absence of highly effective treatment options. Although the exact etiology of vitiligo is not fully understood, factors such as genetic factors, oxidative stress, autoimmunity, and inflammation are implicated in the destruction of melanocytes. Current therapeutic strategies primarily focus on modulating immune responses and alleviating oxidative stress.
View Article and Find Full Text PDFPest Manag Sci
September 2025
Department of Chemistry, Northeast Agricultural University, Harbin, China.
Background: Diniconazole (DCZ) is a poorly water-soluble triazole fungicide. However, the water solubility of DCZ can be significantly enhanced by inclusion complexation with cyclodextrins. In order to improve the properties and bioavailability of pesticide fungicides DCZ, a new system of nanofibers was prepared by electrospinning and cyclodextrin encapsulation.
View Article and Find Full Text PDFFood Res Int
November 2025
Department of Food Science and Technology, College of Agricultural and Environmental Sciences, University of Georgia, Griffin, GA 30223, USA. Electronic address:
Turmeric-derived curcumin offers various health benefits but has poor bioavailability due to low water solubility and rapid gastrointestinal degradation. A recently proposed raw-to-nano strategy enables the direct formulation of turmeric nanoparticles from raw turmeric, using inherent biopolymers to encapsulate and protect curcumin. However, it remains unclear how these nanoparticles enhance gastrointestinal bioavailability and how food matrices influence this process.
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