scholarly journals Melatonin/Cyclodextrin Inclusion Complexes: A Review

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 445
Author(s):  
Aikaterini Sakellaropoulou ◽  
Angeliki Siamidi ◽  
Marilena Vlachou

Melatonin (MLT) is involved in many functions of the human body, mainly in sleeping-related disorders. It also has anti-oxidant potential and has been proven very effective in the treatment of seasonal affective disorders (SAD), which afflict some people during short winter days. Melatonin has been implicated in a range of other conditions, including Parkinson’s disease, Alzheimer’s and other neurological conditions, and in certain cancers. Its poor solubility in water leads to an insufficient absorption that led scientists to investigate MLT inclusion in cyclodextrins (CDs), as inclusion of drugs in CDs is a way of increasing the solubility of many lipophilic moieties with poor water solubility. The aim of this review is to gather all the key findings on MLT/CD complexes. The literature appraisal concluded that MLT inclusion leads to a 1:1 complex with the majority of CDs and increases the solubility of the hormone. The interactions of MLT with CDs can be studied by a variety of techniques, such as NMR, FT-IR, XRD and DCS. More importantly, the in vivo experiments showed an increase in the uptake of MLT when included in a CD.

1998 ◽  
Vol 5 (4) ◽  
pp. 179-188 ◽  
Author(s):  
Dick de Vos ◽  
Rudolph Willem ◽  
Marcel Gielen ◽  
Kyra E. van Wingerden ◽  
Kees Nooter

An overview of the development of anti-tumor organotin derivatives in selected classes of compounds is presented and discussed. High to very high in vitro activity has been found, sometimes equaling that of doxorubicin. Solubility in water is an important issue, dominating the in vivo testing of compounds with promising in vitro properties. The cytotoxicity of the compounds was increased by the presence of a bulky group, an active substituent or one or more polar substituents. Polar substituents may also improve the water solubility. Although organotin derivatives constitute a separate class of compounds, the comparison with cisplatin is inevitable. Among the observed toxicities, neurotoxicity, known from platinum cytostatics, and gastrointestinal toxicity, typical for many oncology drugs, have been detected. Further research to develop novel, useful organotin anti-tumor compounds should be carried out.


Planta Medica ◽  
2019 ◽  
Vol 85 (16) ◽  
pp. 1233-1241
Author(s):  
Michael Kirchinger ◽  
Lara Bieler ◽  
Julia Tevini ◽  
Michael Vogl ◽  
Elisabeth Haschke-Becher ◽  
...  

AbstractThe chroman-like chalcone Xanthohumol C, originally found in hops, was demonstrated to be a potent neuroregenerative and neuroprotective natural product and therefore constitutes a strong candidate for further pharmaceutical research. The bottleneck for in vivo experiments is the low water solubility of this chalcone. Consequently, we developed and validated a suitable formulation enabling in vivo administration. Cyclodextrins were used as water-soluble and nontoxic complexing agents, and the complex of Xanthohumol C and 2-hydroxypropyl-β-cyclodextrin was characterized using HPLC, HPLC-MS, NMR, and differential scanning calorimetry. The water solubility of Xanthohumol C increases with increasing concentrations of cyclodextrin. Using 50 mM 2-hydroxypropyl-β-cyclodextrin, solubility was increased 650-fold. Furthermore, in vitro bioactivity of Xanthohumol C in free and complexed form did not significantly differ, suggesting the release of Xanthohumol C from 2-hydroxypropyl-β-cyclodextrin. Finally, a small-scaled in vivo experiment in a rat model showed that after i. p. administration of the complex, Xanthohumol C can be detected in serum, the brain, and the cerebrospinal fluid at 1 and 6 h post-administration. Mean (± SD) Xanthohumol C serum concentrations after 1, 6, and 12 h were determined as 463.5 (± 120.9), 61.9 (± 13.4), and 9.3 (± 0.8) ng/mL upon i. v., and 294.3 (± 22.4), 45.5 (± 0.7), and 13 (± 1.0) ng/mL after i. p. application, respectively. Accordingly, the formulation of Xanthohumol C/2-hydroxypropyl-β-cyclodextrin is suitable for further in vivo experiments and further pharmaceutical research aiming for the determination of its neuroregenerative potential in animal disease models.


2019 ◽  
Vol 23 (11n12) ◽  
pp. 1486-1494
Author(s):  
Nthabeleng Molupe ◽  
Balaji Babu ◽  
Earl Prinsloo ◽  
Abdessamad Y. A. Kaassis ◽  
Katharina Edkins ◽  
...  

A novel Sn(IV) meso-tetraacenaphthylporphyrin (SnTAcP) has been synthesized and characterized. SnTAcP was complexed with methyl-[Formula: see text]-cyclodextrin (m[Formula: see text]-CD), a nanocarrier that enhances water solubility, and the complexes were evaluated as PDT agents using MCF-7 breast cancer cells. A relatively low singlet oxygen quantum yield value of 0.36 was obtained in DMF, and the lowest energy Q band lies at 608 nm on the edge of the therapeutic window. SnTAcP was found to be non-toxic in the dark and phototoxic towards MCF-7 breast cancer cells with a half-maximal inhibitory concentration (IC[Formula: see text] value of 11 ± 1.1 [Formula: see text]g · mL[Formula: see text] after 30 min of irradiation with a 625 nm Thorlabs LED that provides a dose of 432 J · cm[Formula: see text]. A higher IC[Formula: see text] value of 21 ± 1.1 [Formula: see text]g · mL-1 was obtained for the m[Formula: see text]-CD inclusion complex of SnTAcP.


2021 ◽  
Vol 21 (2) ◽  
pp. 1293-1299
Author(s):  
Bo Yang ◽  
Fang Zhang ◽  
Weili Yuan ◽  
Li Du ◽  
Xuejun Jiang

Cancer is a serious threat to human health and longevity, and is an important cause of disease death. At present, cancer is mainly treated by surgery, radiotherapy, chemotherapy, etc. The existing various methods of treating tumors have their limitations. Although there are immune, genetic and other treatment methods, they are still immature. Therefore, tumor-targeted drug delivery systems have attracted more and more attention in cancer treatment. Targeted nano-drugs are selectively targeted to the tumor surface to achieve targeted drug delivery. New nano-drugs have created new hotspots in medical research. It could be a new strategy for treating cancer. Carboxymethyl chitosan (CMC) is formed by the carboxylation of chitosan. It has good water solubility and biodegradability, biocompatibility and antibacterial properties, so CMC is the best choice as a nanomaterial. Isorhamnetin (Iso) is an important anticancer drug. This article uses nanomedicine technology to construct CMC as a carrier, Iso as an antitumor drug, and using polydopamine (PDA) to modify the surface of the particles. Through in vitro and in vivo experiments, the Iso/CMC-PDA nanosphere Targeting and Growth Inhibition of Cervical Cancer Cells.


Drug Delivery ◽  
2019 ◽  
Vol 27 (1) ◽  
pp. 54-65
Author(s):  
Qing Yao ◽  
Meng-Ting Lin ◽  
Qing-Hua Lan ◽  
Zhi-Wei Huang ◽  
Ya-Wen Zheng ◽  
...  

2001 ◽  
Vol 71 (3) ◽  
pp. 325-334
Author(s):  
Andrada Iftode ◽  
Roxana Racoviceanu ◽  
Razvan Susan ◽  
Daniela Marti ◽  
Iulia Pinzaru ◽  
...  

Fluconazole is a bistriazole derivative with antifungal activity. The major weak points of fluconazole are the development of antifungal resistance and low water solubility, which impairs its administration. Binary systems between fluconazole and beta-cyclodextrin were prepared with the aim of obtaining a new delivery system that will overcome the limitations of fluconazole administration. Using two feasible laboratory methods, inclusion complexes between fluconazole and beta-cyclodextrin were obtained. Thermal and spectroscopic analyses were used to characterize the inclusion complexes.


Sign in / Sign up

Export Citation Format

Share Document