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(a) Preparation of the CaCit NPs using the coprecipitation method; (b) incorporation of FITC into the CaCit NPs.
Source publication
In this work, the preparation of novel calcium citrate (CaCit) nanoparticles (NPs) has been disclosed and the use of these NPs as “Trojan” carriers has been demonstrated. The concentration ratio between calcium ions and citrate ions was optimized, yielding spherical NPs with size in the range of 100–200 nm. Additionally, a fluorescent dye, fluoresc...
Contexts in source publication
Context 1
... we attempted to prepare the CaCit NPs using the coprecipitation method between calcium and citrate ions ( Figure 2a). The effect of the concentration ratio between the two ions on the morphologies of the resulting CaCit particles was first investigated. ...
Context 2
... could be achieved by premixing calcium ions with the anionic FITC generated under basic conditions. Next, the mixture was then mixed with the citrate ion at the previously described optimum conditions, leading to the formation of CaCit-based FITC NPs (CaCit-FITC), as illustrated in Figure 2b. Using this coprecipitation method, we surmised that the FITC is chemisorbed evenly throughout the CaCit NPs, hence allowing the prolonged release of the embedded molecules. ...
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Citations
... Building on these findings, our previous study demonstrated a novel slow-release transdermal drug delivery system using calcium citrate nanoparticles (CaCitNPs), which have been shown to be effective drug carriers [25][26][27]. Therefore, the use of a transdermal patch loaded with CaCitNPs-encapsulated ALA has promising potential for improving the efficacy of subcutaneous fat reduction. ...
... The use of nanoparticle formulations can significantly improve the stability and controlled release of ALA, ensuring prolonged exposure to the target tissues [37]. The nanoparticle-based delivery system used in this study has been reported to be outstanding materials for drug delivery due to their high availability, low cost, safety, biocompatibility, and slow biodegradability [25][26][27]. Nanoparticles with smaller particle sizes, such as the CaCitNPs used in this study, are effective in crossing the stratum corneum and reaching subcutaneous fat tissue, which could enhance bioavailability and therapeutic efficacy [26]. Although the penetration mechanisms of the compounds in this transdermal patch are still unknown, our in vitro drug release investigation revealed sustained release of ALA from the patch at pH 4.5 and 5.4, which is the natural skin pH [38]. ...
Background
Combating obesity is challenging, as anti-obesity compounds lose effectiveness or cause severe side effects when delivered via conventional routes. Thus, there is a need for new, effective treatment routes that are home-based and safe for long-term use. This double-blind, placebo-controlled clinical trial aimed to investigate the efficacy of a biocellulose transdermal patch containing α-lipoic acid (ALA), an anti-obesity compound, in reducing subcutaneous fat accumulation.
Methods
One hundred and sixteen overweight participants (average age 37.96 ± 7.80 years) were recruited for the study. They were randomly assigned to apply either the calcium citrate nanoparticle-encapsulated ALA transdermal patch or a placebo on their arm. The participants’ body weight, height, blood lipid profile (cholesterol, triglyceride, low-density lipoprotein, and high-density lipoprotein), arm circumference, triceps skin fold, and subcutaneous fat thickness were recorded at baseline and at the 2-week follow-up.
Results
The mean arm circumference did not show any significant difference from baseline, whereas the triceps skinfold and subcutaneous fat thickness showed a significant reduction. The 2-week treatment did not significantly alter the plasma LDL, HDL, and triglyceride levels of the participants, but it significantly reduced the total cholesterol level.
Conclusion
This study reports the successful reduction of subcutaneous fat of the calcium citrate nanoparticle-encapsulated ALA transdermal patches. The transdermal patches could be used as a safe and effective home-based solution for combating obesity.
... The synthesis of cisplatin-loaded calcium citrate nanoparticles conjugated with epidermal growth factor (CaCit@CDDP-EGF NPs) was achieved through a coprecipitation method involving calcium and citrate ions in a bottom-up process, enabling control over the cisplatin loading capacity. 15 The epidermal growth factor receptor (EGFR) is predominantly expressed in carcinoma cells and plays a crucial role in activating tyrosine kinase activity, which regulates cell proliferation and apoptosis. EGF is presented as a commonly detected binding specific ligand in humans with good binding affinity through the size of the molecule around 6.1 kDa. ...
... CaCit NPs were selected as CDDP carriers due to their biocompatibility and wide availability in various applications. 13,15 In our study, calcium nitrate and trisodium citrate dihydrate were used as sources of calcium and citrate ions, respectively. 17,18 We achieved the formation of thermodynamically stable CaCit NPs with a needlelike crystal shape at a Ca 2+ :C 6 H 5 O 7 3− ratio of 1.5:1.0 ...
... The resulting white precipitates of nanoparticles were collected, washed five times with DI water, and then frozen and dried at −80°C to halt the reaction. 15 NPs). 800 mg of CaCit@CDDP NPs were dispersed in 1 mL of DI water and subjected to ultrasonication. ...
Lung cancer is the leading cause of cancer-related deaths worldwide with high incidence rates for new cases. Conventional cisplatin (CDDP) therapy has limitations due to severe side effects from nonspecific targeting. To address this challenge, nanomedicine offers targeted therapies. In this study, cisplatin-loaded calcium citrate nanoparticles conjugated with epidermal growth factor (CaCit@CDDP-EGF NPs) were synthesized. The resulting nanodrug had a size below 350 nm with a cation charge. Based on density functional theory (DFT), the CaCit@CDDP NP model containing two citrates substituted on two chlorides exhibited a favorable binding energy of −5.42 eV, and the calculated spectrum at 261 nm closely matched the experimental data. CaCit@CDDP-EGF NPs showed higher inhibition rates against EGFR-expressed and mutant carcinoma cells compared to those of cisplatin while displaying lower cytotoxicity to lung fibroblast cells. Integrating in vitro experiments with in silico studies, these nanoparticles hold promise as a novel nanomedicine for targeted therapy in clinical applications.
... In a recent study, our research group had successfully synthesized a novel type of NP based on calcium citrate NPs (CaCit NPs), which presented a high stability and biocompatibility for drug delivery applications. 19 Following the advancement, the main objective of this work is to investigate the potential use of CaCit NPs as a vehicle for the topical application of eugenol. Novel eugenol-embedded CaCit NPs (Eu-CaCit NPs) were prepared as well as the penetration ability of Eu-CaCit NPs into the human skin was determined. ...
... 30,31 We then investigated the potential application of Eu-CaCit NPs as molecular carriers for drug delivery by introducing FITC as a fluorescent probe onto the Eu-CaCit NP surface. 32 This surface modification could be achieved conveniently 19 by mixing the Eu-CaCit NP colloidal mixture with the anionic FITC generated under basic conditions for 1 h, leading to the formation of FITC-Eu-CaCit NPs. The thermal decomposition behaviors of both Eu-CaCit and FITC-Eu-CaCit NPs expressed three main regions of weight loss. ...
... In our previous study, CaCit NPs did not show any meaningful toxicity in human keratinocytes at concentrations of 0.3, 0.6, and 1.2 g/L. 19 We performed a cytotoxicity assay in order to determine nontoxic physiological concentrations of CaCit NPs and Eu-CaCit NPs in human keratinocytes and fibroblasts at concentrations of 0.3, 0.6, and 1.2 g/L. The results did not show any remarkable changes on the cell viability when compared with the control (Figures S2 and S3). ...
Eugenol is a major phenolic component derived from clove oil with potential medical applications. Of particular interest, it has been used as a therapeutic agent in topical applications because of its analgesic and local anesthetic properties. However, topical formulations of eugenol produce skin irritation, which limits its clinical applications. One promising strategy to overcome this disadvantage is by using a biocompatible material that could be an appropriate topical vehicle for eugenol. Researchers have recently focused on the development of eugenol-embedded calcium citrate nanoparticles (Eu-CaCit NPs) without adverse effects. The Eu-CaCit NPs were developed as a topical delivery system and their biocompatibility and penetration ability were evaluated. Eu-CaCit NPs at 1.2 mg/mL did not show cytotoxicity effects in human cells. Moreover, the Eu-CaCit NPs presented the ability to penetrate the dermis layer of the human intact skin following 12 h exposure. All the results concluded that Eu-CaCit NPs have shown a potential as a carrier for topical delivery of eugenol. These novel nanoparticles represent a promising alternative for topical application of local anesthetic with natural pain relievers.
... Vancomycin, an antibiotic drug for bone spacer application, was successfully encapsulated in the calcium citrate particles (VAN-CC) with a size of around 500 nm and an encapsulation efficiency of 28% [22]. In another work, FITC, a fluorescent agent, was encapsulated and slowly released from calcium citrate nanoparticles as experimented with human keratinocytes [23]. ...
... Despite the successful drug encapsulation in calcium citrate nanoparticles [23], the method was not applicable for the incorporation of 2a. This was due to the use of water as the only solvent in the system, leading to poor solubility of triazine drugs. ...
... Therefore, we attempted to optimise the protocol for the preparation of 1,3,5-triazines-incorporated calcium citrate nanoparticles (CaCit-triazine NPs) using EtOH-water as a binary solvent system, adjusted from the synthesis of calcium carbonate particles previously reported [30]. There are many methods to prepare calcium citrate particles, but the two most common reagents are CaCl 2 and sodium citrate [21,23,31]. In our first attempt, a solution of CaCl 2 in EtOH was slowly added to a solution of 2a and sodium citrate in EtOH-water under vigorous stirring at room temperature. ...
Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.
Cisplatin (CDDP) is an effective Platinum (Pt) based anticancer drug used in chemotherapy. However, its effectiveness is limited due to its instability in solvents, along with the side effects it causes due to DNA damage. Nanoparticles (NPs) were developed in vitro to address these issues by loading CDDP into various types of NPs, including metal, lipid, and biological NPs. Citrate was employed as a biocompatible compound in nanomedicine to reduce cytotoxicity and enhance stability. In our study, the physicochemical and electronic properties of CDDP and citrate have been investigated using density functional theory (DFT), with a comparison of their behavior in water and DMSO. Additionally, TD‐DFT was applied to analyze the UV–Vis spectra results. Six complexes have been proposed to better understand the interaction between citrate and CDDP. The results demonstrated that the CDDP could form stable complexes with citrate in both water and DMSO, and the considered complexes exhibited UV–Vis spectra within the experiment range. The frontier orbitals, electron densities mapping, and electrostatic potential analysis revealed that complex 5, where citrate di‐substituted on two chlorides, is the most likely and effective complex. In summary, our investigation sheds light on the potential of CDDP‐citrate complexes to address the limitations of CDDP, offering insights into their stability and interaction in solvents and highlighting the promising efficacy of specific complex formations for future therapeutic applications.
Biotransformation of amorphous calcium carbonate into calcite and other inorganic calcium minerals is a worldwide phenomenon in the bacterial kingdom. In this study, it showed that calcite (CaCO3) could be transformed into an organic mineral earlandite [Ca3(C6H5O7)2·4H2O], through the dissolution of calcite and subsequent crystallization by the fungus Trichoderma asperellum BDH65. Observations by light microscopy showed that the fungal induced crystal particles were deposited as irregularly granular accumulations of micro globular particles. Scanning and transmission electron microscopy revealed that each micro globular particle consists of numerous needle-like crystals with domed end assembling radially with their ends pointing outside from its centers. This is clearly different from the shapes of microsheets formed by the chemical method. The mineral phase of the fungal catalyzed crystals is identified as earlandite, which is chemically identical to calcium citrate tetrahydrate. Structure and properties of the fungal formed crystals are further characterized by Fourier transform infrared spectroscopy and thermogravimetry, showing a similar pattern with those observed for chemically synthesized calcium citrate tetrahydrate. The current result may useful for understanding bioweathering of minerals and rocks, and insight into the calcium cycling driven by fungi.
