scholarly journals Design andIn VitroEvaluation of a New Nano-Microparticulate System for Enhanced Aqueous-Phase Solubility of Curcumin

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Diana Guzman-Villanueva ◽  
Ibrahim M. El-Sherbiny ◽  
Dea Herrera-Ruiz ◽  
Hugh D. C. Smyth
Keyword(s):  
Therapeutic Potential ◽  
Curcuma Longa ◽  
Aqueous Solubility ◽  
Release Profile ◽  
Free Form ◽  
Phase Solubility ◽  
Ionotropic Gelation ◽  
Anticancer Properties ◽  
Freeze Dried

Curcumin, a yellow polyphenol derived from the turmericCurcuma longa, has been associated with a diverse therapeutic potential including anti-inflammatory, antioxidant, antiviral, and anticancer properties. However, the poor aqueous solubility and low bioavailability of curcumin have limited its potential when administrated orally. In this study, curcumin was encapsulated in a series of novel nano-microparticulate systems developed to improve its aqueous solubility and stability. The nano-microparticulate systems are based entirely on biocompatible, biodegradable, and edible polymers including chitosan, alginate, and carrageenan. The particles were synthesized via ionotropic gelation. Encapsulating the curcumin into the hydrogel nanoparticles yielded a homogenous curcumin dispersion in aqueous solution compared to the free form of curcumin. Also, thein vitrorelease profile showed up to 95% release of curcumin from the developed nano-microparticulate systems after 9 hours in PBS at pH 7.4 when freeze-dried particles were used.

scholarly journals Cyclodextrin Inclusion Complexes of Auranofin and Its Iodido Analog: A Chemical and Biological Study

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 727
Author(s):  
Damiano Cirri ◽  
Ida Landini ◽  
Lara Massai ◽  
Enrico Mini ◽  
Francesca Maestrelli ◽  
...  
Keyword(s):  
Binary Systems ◽  
Current Knowledge ◽  
Aqueous Solubility ◽  
Biological Study ◽  
Phase Solubility ◽  
Cyclodextrin Complex ◽  
Nmr Studies ◽  
Anticancer Properties

Auranofin (AF) and its iodido analog, i.e., Au(PEt3) I (AFI), were reported to exhibit very promising anticancer properties both in vitro and in vivo. However, both these gold compounds have a scarce aqueous solubility that hampers their pharmaceutical use. Here, we explore whether encapsulation of these metallodrugs inside hydroxypropyl-beta–cyclodextrin (HPβ–CD) may lead to an improved biopharmaceutical profile for the resulting adducts. Phase solubility studies, performed at 25 °C in an aqueous buffer, revealed, in both cases, the formation of a 1:1 drug to cyclodextrin complex; a far greater apparent stability constant (K1:1) was measured for AFI compared to AF (331 M−1 versus ca. 30 M−1). NMR studies conducted on the AFI/HPβ–CD system confirmed the formation of a stable 1:1 adduct. Then, binary systems of AF and AFI with HPβ–CD were prepared by colyophilization and characterized by DSC and PXRD. The results revealed the occurrence of drug complexation and/or amorphization for the AFI/HPβ–CD binary system. Afterwards, the antiproliferative properties of the two cyclodextrin adducts and of the corresponding free drugs were comparatively evaluated in vitro in three representative ovarian cancer cell lines, i.e., A2780, SKOV3, and IGROV-1. The results, in all cases, point out that CD complexation of the two gold drugs does not substantially affect their biological activity. The implications of these findings are discussed in the frame of the current knowledge of AF and its analogs.

scholarly journals A study of deregulated MMR pathways and anticancer potential of curcuma derivatives using computational approach

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Priyanjali Bhattacharya ◽  
Trupti N. Patel
Keyword(s):  
Mismatch Repair ◽  
Protein Function ◽  
Curcuma Longa ◽  
Signaling Cascades ◽  
Altered Expression ◽  
Anticancer Properties ◽  
Medicinal Properties ◽  
Multiple Signaling

AbstractPlant derived products have steadily gained momentum in treatment of cancer over the past decades. Curcuma and its derivatives, in particular, have diverse medicinal properties including anticancer potential with proven safety as supported by numerous in vivo and in vitro studies. A defective Mis-Match Repair (MMR) is implicated in solid tumors but its role in haematologic malignancies is not keenly studied and the current literature suggests that it is limited. Nonetheless, there are multiple pathways interjecting the mismatch repair proteins in haematologic cancers that may have a direct or indirect implication in progression of the disease. Here, through computational analysis, we target proteins that are involved in rewiring of multiple signaling cascades via altered expression in cancer using various curcuma derivatives (Curcuma longa L. and Curcuma caesia Roxb.) which in turn, profoundly controls MMR protein function. These biomolecules were screened to identify their efficacy on selected targets (in blood-related cancers); aberrations of which adversely impacted mismatch repair machinery. The study revealed that of the 536 compounds screened, six of them may have the potential to regulate the expression of identified targets and thus revive the MMR function preventing genomic instability. These results reveal that there may be potential plant derived biomolecules that may have anticancer properties against the tumors driven by deregulated MMR-pathways.

Anti-giardial therapeutic potential of dichloromethane extracts of Zingiber officinale and Curcuma longa in vitro and in vivo

2016 ◽  
Vol 115 (7) ◽  
pp. 2637-2645 ◽  
Author(s):  
Ahmad K. Dyab ◽  
Doaa A. Yones ◽  
Zedan Z. Ibraheim ◽  
Tasneem M. Hassan
Keyword(s):  
Therapeutic Potential ◽  
Curcuma Longa ◽  
Zingiber Officinale

scholarly journals Improving the Solubilization and Bioavailability of Arbidol Hydrochloride by the Preparation of Binary and Ternary β-Cyclodextrin Complexes with Poloxamer 188

2021 ◽  
Vol 14 (5) ◽  
pp. 411
Author(s):  
Md. Khalid Anwer ◽  
Muzaffar Iqbal ◽  
Mohammad Muqtader Ahmed ◽  
Mohammed F. Aldawsari ◽  
Mohd Nazam Ansari ◽  
...  
Keyword(s):  
Antiviral Agent ◽  
Aqueous Solubility ◽  
Phase Solubility ◽  
Pharmacokinetic Studies ◽  
Solubility Curve ◽  
Cyclodextrin Complexes ◽  
Poloxamer 188 ◽  
The Stability

In the current study, the effect of poloxamer 188 on the complexation efficiency and dissolution of arbidol hydrochloride (ADL), a broad-spectrum antiviral agent, with β-cyclodextrin (β-CD) was investigated. Phase solubility studies confirmed a stoichiometry of a 1:1 ratio for both ADL:β-CD and ADL/β-CD with a 1% poloxamer 188 system with an AL type of phase solubility curve. The stability constants (K1:1) calculated from the AL type diagram were 550 M-1 and 2134 M-1 for AD:β-CD and ADL/β-CD with 1% poloxamer 188, respectively. The binary ADL/β-CD and ternary ADL/β-CD with 1% poloxamer 188 complexes were prepared by kneading and a solvent evaporation method and were characterized by aqueous solubility, FTIR, PXRD, DSC and SEM in vitro studies. The solubility (13.1 fold) and release of ADL were markedly improved in kneaded ternary ADL/β-CD with 1% poloxamer 188 (KDB). The binding affinity of ADL and β-CD was confirmed by 1H NMR and 2D ROSEY studies. The ternary complex (KDB) was further subjected for in vivo pharmacokinetic studies in rats and a significant improvement in the bioavailability (2.17 fold) was observed in comparison with pure ADL. Therefore, it can be concluded that the solubilization and bioavailability of ADL can be remarkably increased by ADL/β-CD complexation in the presence of a third component, poloxamer 188.

scholarly journals Curcuma longa Is Able to Induce Apoptotic Cell Death of Pterygium-Derived Human Keratinocytes

2017 ◽  
Vol 2017 ◽  
pp. 1-9
Author(s):  
Silvia Sancilio ◽  
Silvio Di Staso ◽  
Stefano Sebastiani ◽  
Lucia Centurione ◽  
Nick Di Girolamo ◽  
...  
Keyword(s):  
Cultured Cells ◽  
Therapeutic Potential ◽  
Apoptotic Cell ◽  
Curcuma Longa ◽  
Annexin V ◽  
Surgical Excision ◽  
Human Keratinocytes ◽  
Alcoholic Extract ◽  
Treatment And Prevention

Pterygium is a relatively common eye disease that can display an aggressive clinical behaviour. To evaluate the in vitro effects of Curcuma longa on human pterygium-derived keratinocytes, specimens of pterygium from 20 patients undergoing pterygium surgical excision were collected. Pterygium explants were put into culture and derived keratinocytes were treated with an alcoholic extract of 1.3% Curcuma longa in 0.001% Benzalkonium Chloride for 3, 6, and 24 h. Cultured cells were examined for CAM5.2 (anti-cytokeratin antibody) and CD140 (anti-fibroblast transmembrane glycoprotein antibody) expression between 3th and 16th passage to assess cell homogeneity. TUNEL technique and Annexin-V/PI staining in flow cytometry were used to detect keratinocyte apoptosis. We showed that Curcuma longa exerts a proapoptotic effect on pterygium-derived keratinocytes already after 3 h treatment. Moreover, after 24 h treatment, Curcuma longa induces a significant increase in TUNEL as well as Annexin-V/PI positive cells in comparison to untreated samples. Our study confirms previous observations highlighting the expression, in pterygium keratinocytes, of nuclear VEGF and gives evidence for the first time to the expression of nuclear and cytoplasmic VEGF-R1. All in all, these findings suggest that Curcuma longa could have some therapeutic potential in the treatment and prevention of human pterygium.

scholarly journals Dissolution Enhancement of Flurbiprofen by Solid Dispersion Adsorbate Technique

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Sohansinh S. Vaghela ◽  
Samkit M. Shah ◽  
Sanjesh G. Rathi ◽  
Shrenik K. Shah
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Dissolution Enhancement ◽  
Phase Solubility ◽  
Fusion Method ◽  
Poloxamer 188 ◽  
X Ray ◽  
Solubility Study ◽  
Phase Solubility Study

Flurbiprofen solid dispersion Adsorbate (SDA) has been prepared using PEG 4000 and Poloxamer 188 as carrier and Neusilin as adsorbent material. The SDA of Flurbiprofen was prepared by using Fusion method in various drugs to carrier ratios. The phase solubility study concludes that both polymers have ability to improve the aqueous solubility of flurbiprofen. Pure API Flurbiprofen and final formulation samples of SDA are characterized by FTIR, DSC and X-ray diffraction spectroscopy. X-ray powder diffraction and DSC study indicated that the drug was present in amorphous form. FTIR study revealed that the characteristic peaks in spectra of pure Flurbiprofen are also present in spectra of SDA’s. Drug found compatible with the excipients. The highest improvement in solubility and in-vitro drug release were observed in solid dispersion prepared with Poloxamer 188 (F14) by fusion method. The increased dissolution rate of drug from solid dispersion adsorbates may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion adsorbates with the Poloxamer carrier in 1:2 ratio considered as most satisfactory among all solid dispersion adsorbates.

scholarly journals Development and Evaluation of Ginkgo biloba L. Extract Loaded into Carboxymethyl Cellulose Sublingual Films

2020 ◽  
Vol 11 (1) ◽  
pp. 270
Author(s):  
Laura Rimkiene ◽  
Juste Baranauskaite ◽  
Mindaugas Marksa ◽  
Laurynas Jarukas ◽  
Liudas Ivanauskas
Keyword(s):  
Mechanical Properties ◽  
Carboxymethyl Cellulose ◽  
In Vitro Release ◽  
Release Profile ◽  
Flavonoid Glycosides ◽  
Disintegration Time ◽  
Chemical Complexity ◽  
Freeze Dried ◽  
Physicochemical Evaluation

Oral bioavailability of flavonoids, including G. biloba extract, is limited due to their chemical complexity, which determines slow dissolution in vitro behavior of the extract. The overall research objective was to compare the effect of increasing freeze-dried G. biloba extract (GFD) concentrations in carboxymethyl cellulose (CMC) films on their mechanical properties, release profile of flavonoid glycosides, stability and disintegration time. Physicochemical evaluation of films was performed by SEM and FTIR. The mechanical properties and in vitro release profile of flavonoid glycosides from the prepared films were characterized in the study. The higher elongation at break and tensile strength values, quick release of flavonoids and good stability were observed in formulation, coded FRG—15 (the film contained 0.4 g of GFD, 0.3 g of glycerol and 2 g of 2% CMC), (p < 0.05). Dissolution rate tests showed that approximately 85% of loaded flavonoid glycosides had been released; the release profile of flavonoid glycosides from FRG-15 had levelled off after only 15 min. The results could lay the groundwork for further studies, concerning the development of sublingual films as G. biloba extract-based dosage forms, which might increase the multifunctional properties and pharmacological activity closer to the desired level.

A review on chemistry, source and therapeutic potential of lambertianic acid

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Md Shahinozzaman ◽  
Moutushi Islam ◽  
Bristy Basak ◽  
Arifa Sultana ◽  
Rashiduzzaman Emran ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Therapeutic Potential ◽  
Bioactive Compound ◽  
Cancer Cell Proliferation ◽  
Neuroprotective Effects ◽  
Potential Health ◽  
Anticancer Properties ◽  
Toxicological Profile ◽  
Lambertianic Acid

Abstract Lambertianic acid (LA) is a diterpene bioactive compound mainly purified from different species of Pinus. It is an optical isomer of another natural compound daniellic acid and was firstly purified from Pinus lambertiana. LA can be synthesized in laboratory from podocarpic acid. It has been reported to have potential health benefits in attenuating obesity, allergies and different cancers including breast, liver, lung and prostate cancer. It exhibits anticancer properties through inhibiting cancer cell proliferation and survival, and inducing apoptosis, targeting major signalling components including AKT, AMPK, NFkB, COX-2, STAT3, etc. Most of the studies with LA were done using in vitro models, thus warranting future investigations with animal models to evaluate its pharmacological effects such as antidiabetic, anti-inflammatory and neuroprotective effects as well as to explore the underlying molecular mechanisms and toxicological profile. This review describes the chemistry, source, purification and therapeutic potentials of LA and it can therefore be a suitable guideline for any future study with LA.

scholarly journals Studies on Preparation and Evaluation of Soluble 1:1 Stoichiometric Curcumin Complex for Colorectal Cancer Treatment

2021 ◽  
Vol 18 (24) ◽  
pp. 1403
Author(s):  
Jamal Moideen Muthu Mohamed ◽  
Fazil Ahmad ◽  
Ali Alqahtani ◽  
Taha Lqahtani ◽  
Venkatesan Krishna Raju ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
In Vitro Cytotoxicity ◽  
Phase Solubility ◽  
In Vitro Drug Release ◽  
Enhanced Solubility ◽  
Ft Ir ◽  
First Time ◽  
Preparation And Evaluation ◽  
Colorectal Cancer Treatment

This study investigates the complex of curcumin (CMN), which has enhanced solubility and hence, higher cytotoxicity compared to free CMN. Insilco molecular modelling and phase solubility (PS) studies were performed with the drug and carriers for interaction. The complex was characterized by in vitro drug release, FT-IR, PXRD, TGA, DSC, SEM, DLS, and functionalized dyeing test. The result showed that the CMN-PEG6000 complex produced significant properties of solubility (≈ 190 folds) and dissolution (80.68 % at 30 min), with stability constants equivalent to 309 and 377 M-1 at 25 and 37 °C, respectively. It exhibited AL type of isotherm indicating 1:1 stoichiometry. The result from the in vitro cytotoxicity showed that 50 % inhibition (IC50) was achieved on the SW480 and Caco-2 cells at an amount of complex that was considerably lesser than free CMN. Apoptosis study showed that the cells underwent cell death mainly by apoptosis with a small number by necrosis. HIGHLIGHTS Enhanced curcumin solubility up to 190 fold higher than pure curcumin was investigated The phase solubility results of curcumin range from 5.7×10-4 M-1 and 7.8×10-4 M-1 at 25 and 37 °C, respectively First time of novel dyeing test was performed with complex of curcumin, signified its solubility This study provides useful approach for obtaining curcumin products with maximum aqueous solubility GRAPHICAL ABSTRACT

scholarly journals Preparation of Soluble Complex of Curcumin for the Potential Antagonistic Effects on Human Colorectal Adenocarcinoma Cells

2021 ◽  
Vol 14 (9) ◽  
pp. 939
Author(s):  
Jamal Moideen Muthu Mohamed ◽  
Ali Alqahtani ◽  
Barkat A. Khan ◽  
Adel Al Fatease ◽  
Taha Alqahtani ◽  
...  
Keyword(s):  
Aqueous Solubility ◽  
In Vitro Cytotoxicity ◽  
Phase Solubility ◽  
Soluble Complex ◽  
Zebrafish Model ◽  
Adenocarcinoma Cells ◽  
Hot Melt ◽  
Central Composite

This study was designed to investigate the effects of curcumin (CMN) soluble complex (SC) prepared by melt casting (HM) and hot-melt extrusion (HME) technology. Phase solubility (PS) study, in silico molecular modeling, aqueous solubility, drug release, and physicochemical investigation including a novel dyeing test was performed to obtain an optimized complex by a central composite design (CCD). The results show that the HME-SC produces better improvements towards solubility (0.852 ± 0.02), dissolution (91.87 ± 0.21 % at 30 min), with an ideal stability constant (309 and 377 M−1 at 25 and 37 °C, respectively) and exhibits AL type of isotherm indicating 1:1 stoichiometry. Intermolecular hydrogen bonding involves the formation of SC, which does not undergo any chemical modification, followed by the complete conversion of the amorphous form which was identified by XRD. The in vitro cytotoxicity showed that IC50 was achieved in the SW480 (72 µM.mL−1) and Caco-2 (40 µM.mL−1) cells while that of pure CMN ranged from 146 to 116 µM/mL−1. Apoptosis studies showed that cell death is primarily due to apoptosis, with a low rate of necrosis. In vivo toxicity, confirmed by the zebrafish model, exhibited the safety of the HME-SC. In conclusion, the HME-SC potentially enhances the solubility and cytotoxicity to the treatment of colorectal cancer (CRC).

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