Improvement of a liposomal formulation with a native molecule: calcitriol

Many studies have been conducted to improve liposome's potency towards cancer treatment. Recently, modifications of liposomal formulations turned towards either dual loading of anticancer agents to minimize the dose of each agent or the use of targeting moieties to target them to or near cancer cells for minimizing side effects with maximum treatment. In this study, a natural molecule, calcitriol, was used to improve the effectiveness of doxorubicin loaded liposomes by co-loading approach. Calcitriol treatment alone was reported to create an anti-proliferative effect on several carcinoma cell lines. However, to create an antiproliferative effect, a high dose of calcitriol needs to be used which might result in hypercalcemia. Therefore, co-loading calcitriol into liposomes will improve its efficiency on cells besides increasing hydrophobic calcitriol's chemical stability in circulation. At first, possible doxorubicin cytotoxicity improvement against Namalwa cells by calcitriol pretreatment was investigated. The enhancing effect created was over 40% after 72 hours of calcitriol pretreatment. Upon co-loading into liposomes, enhanced and early cytotoxicity was observed even after 24 hours. Hence, the synergistic effect of calcitriol and doxorubicin on Namalwa cells was shown both in free and liposomal forms for the first time. A confocal study confirmed that early cytotoxicity was related with cell internalization. This potency ended when liposomes targeted non-internalizing antigen, CD20. Liposome co-loading of calcitriol and doxorubicin increases the effectiveness of their synergistic activity by creating a dual delivery system. Liposomal co-loaded calcitriol delivery would overcome calcitriol dose limitation problems and decrease possible side effects of both therapeutic agents.


Preparation and labeling of surface-modified magnetoferritin protein cages with a rhenium(I) carbonyl complex for magnetically targeted radiotherapy
Aslan, Tugba Nur; Asik, Elif; Volkan, Mürvet (Royal Society of Chemistry (RSC), 2016-01-01)
New rhenium radiolabeled compounds are of general interest due to their nuclear characteristics which allow radiotherapy and in situ monitoring of tumor uptake. Biocompatible magnetic nanoparticles capable of transporting radionuclides, providing MRI contrast agent properties for imaging and a therapeutic effect in the target tissue simultaneously, are highly desirable. Herein we describe the preparation of magnetoferritin samples, and their labeling with rhenium in the form of the low oxidation state rheni...
Preparation of polyethylene glycol coated magnetic nanoparticles for targeting of cancer cells
Keskin, Tuğba; Gündüz, Ufuk; Department of Biology (2012)
Conventional cancer chemotherapies cannot differentiate between healthy and cancer cells, and lead to severe side effects and systemic toxicity. In the last decades, different kinds of controlled drug delivery systems have been developed to overcome these shortcomings of chemotherapeutics. Magnetic nanoparticles (MNP) are potentially important in cancer treatment since they can be targeted to tumor site by an externally applied magnetic field. In this study, it is aimed to synthesize folic acid conjugated; ...
Investigation and scale-up of hot-melt coating of pharmaceuticals in fluidized beds
Külah, Görkem (Elsevier BV, 2011-03-10)
This study was performed to investigate and scale-up the hot-melt coating process in fluidized beds. A series of well-designed experiments was carried out in a pilot scale unit with 20 kg product capacity to investigate the effects of process variables on the efficiency of the coating of Cefuroxime Axetil with stearic acid. Results showed that the efficiency is at the highest when the fluidization air flow rate is adjusted by considering the changes in the amount of materials present in the unit as well as ...
Enhancing oxidative stability of walnuts by using gallic acid loaded lentil flour based electrospun nanofibers as active packaging material
Aydogdu, Ayca; Yıldız, Eda; Aydogdu, Yildirim; Şümnü, Servet Gülüm; Şahin, Serpil; Ayhan, Zehra (Elsevier BV, 2019-10-01)
The objective of this study was to enhance oxidative stability of walnuts present in active packages produced by electrospinning technology. Gallic acid was encapsulated into lentil flour/polyethylene oxide (PEO) nanofibers. To promote the solubility of lentil proteins, pH of solutions was adjusted to pH 1 and pH 10 which were far away from isoelectric point of lentil proteins. While acidic solutions had lower viscosity values than alkaline solutions, their electrical conductivity values were significantly ...
Chemical characterization and anticholinesterase effects of essential oils derived from Salvia species
TEMEL, HALİDE EDİP; Demirci, Betul; Demirci, Fatih; CELEP, FERHAT; KAHRAMAN, AHMET; Doğan, Musa; Baser, Kemal Husnu Can (Informa UK Limited, 2016-01-01)
Inhibitory effect of Salvia species herbal preparations on acetylcholinesterase (AChE) and butylcholinesterase (BuChE) activitiy may contribute to regulation of cognitive performance and impaired cholinergic functions in patients with Alzheimer's disease. This functional role of Salvia species and their components makes the investigations on Salvia valuable in medicine-related plant research. Within this work it was aimed to investigate the in vitro anti-cholinesterase effect of essential oils derived from ...
Citation Formats
A. D. Dalgıç, A. Tezcaner, F. ARPACI, F. AVCU, and D. Keskin, “Improvement of a liposomal formulation with a native molecule: calcitriol,” RSC ADVANCES, pp. 80158–80167, 2016, Accessed: 00, 2020. [Online]. Available: