Formulation Of Curcumin Research Articles

Curcumin‐loaded nanomedicines as therapeutic strategy in malaria management

AbstractMalaria, a parasitic protozoan disease widespread in tropical climates, is transmitted by Plasmodium spp. Many people are affected by this significant public health disease, which has a high incidence of illness and mortality worldwide. Because drug‐resistant parasites are on the rise, there are not enough controls on mosquitoes, and there are not any malaria vaccinations. Malaria is particularly challenging in developing countries. Antimalarial drugs approved by Food and Drug Administration are the main options for combating and preventing malaria; also the control of transmission at the level of mosquitoes is important. Current antimalarial chemotherapeutic therapies have significant clinical flaws such as Plasmodium resistance, the drugs that call for the development of novel drug candidates. To combat malaria, nanotechnology may give a viable alternative that is both more effective and safer than current treatment options. Nanotechnology‐based curcumin formulations have proved to overcome the limitations of current therapies in terms of optimum therapeutic benefits, safety, and cost‐efficiency, which increases a patient's capacity to adhere to prescribed medicine. The limits of current malaria therapies and the need to employ nanotechnological curcumin to treat malaria were addressed and discussed in this paper.

Simulation of optimal dose regimens of photoactivated curcumin for antimicrobial resistance pneumonia in COVID-19 patients: A modeling approach.

Secondary antimicrobial resistance bacterial (AMR) pneumonia could lead to an increase in mortality in COVID-19 patients, particularly of geriatric patients with underlying diseases. The comedication of current medicines for AMR pneumonia with corticosteroids may lead to suboptimal treatment or toxicities due to drug-drug interactions (DDIs). This study aimed to propose new promising dosage regimens of photoactivated curcumin when co-administered with corticosteroids for the treatment of antimicrobial resistance (AMR) pneumonia in COVID-19 patients. A whole-body physiologically-based pharmacokinetic (PBPK) with the simplified lung compartments model was built and verified following standard model verification (absolute average-folding error or AAFEs). The pharmacokinetic properties of photoactivated were assumed to be similar to curcumin due to minor changes in physiochemical properties of compound by photoactivation. The acceptable AAFEs values were within 2-fold. The verified model was used to simulate new regimens for different formulations of photoactivated curcumin. The AAFEs was 1.12-fold. Original formulation (120 mg once-daily dose) or new intramuscular nano-formulation (100 mg with a release rate of 10/h given every 7 days) is suitable for outpatients with MRSA pneumonia to improve patient adherence. New intravenous formulation (2000 mg twice-daily doses) is for hospitalized patients with both MRSA and VRSA pneumonia. The PBPK models, in conjunction with MIC and applied physiological changes in COVID-19 patients, is a potential tool to predict optimal dosage regimens of photoactivated curcumin for the treatment of co-infected AMR pneumonia in COVID-19 patients. Each formulation is appropriate for different patient conditions and pathogens.

Research progress on drug delivery systems for curcumin in the treatment of gastrointestinal tumors.

Curcumin is a natural compound with a diketone structure, which can control the growth, metastasis, recurrence, neovascularization, invasion, and drug resistance of gastrointestinal tumors by inhibiting nuclear factor κB, overexpression of tumor cells, vascular endothelial growth factor, etc. However, due to the low bioavailability of curcumin formulation, it did not fully exert its pharmacological effects, and its application and development in the treatment of various malignant tumors are still limited. This review summarizes the research on drug delivery systems of curcumin combating digestive tract tumors in order to further reduce the toxic side effects of curcumin-containing drugs and fully exert their pharmacological activities, and improve their bioavailability and clinical value.

Healing potential of curcumin nanomicelles in cutaneous burn wounds: an in vitro and in vivo study

ABSTRACT Purpose/Aim of the study Curcumin is the active substance of turmeric and has been shown to enhance the healing potential of burn wounds. However, its high hydrophobicity and rapid degradability are great challenges for its clinical applications. The development of new curcumin formulations may provide a potential solution to these issues. Methods and Results In this study, we investigated the use of curcumin nanomicelles for wound dressing and evaluated their effects on fibroblast migration and proliferation in vitro. We found that the application of curcumin nanomicelles to the wounds significantly improved wound contraction and increased the expression of transforming growth factor-1 and basic fibroblast growth factor at day 14 of the healing process. Furthermore, curcumin nanomicelles reduced the expression of interleukin-1 at days 7 and 14 post-wounding. Histopathological analysis revealed that the curcumin nanomicelles-treated burn wounds exhibited more organized granulation tissue, improved angiogenesis, and enhanced re-epithelialization. Additionally, the curcumin treatment led to increased hydroxyproline content and enhanced TGF-β1 expression level in the wounds. The in vitro studies also demonstrated that the curcumin nanomicelles induced proliferation and migration of fibroblasts. Conclusion Overall, our findings suggest that curcumin nanomicelles can be a promising candidate for the treatment of burn wounds.

Custom-modified oligolactide-cyclodextrin derivatives for electrospun drug formulations

Custom-synthesized cyclodextrin-oligolactide derivatives (CDLA) were used to produce electrospun nanofibers. The modified cyclodextrins were obtained through solution ring-opening oligomerization initiated by α-, β-, or γ-cyclodextrin in the presence of 4-dimethylaminopyridine. Following the NMR spectroscopy and mass spectrometry structural characterization, the CDLA derivatives are described as low molecular weight compounds having the lactate monomer units placed on the smaller rim of cyclodextrins as multiple short chains. The electrospinning (ESP) of the α-, β- and γ-CDLA homologous series was optimized for the use of high-concentration water/ethanol feed solutions. Scanning electron microscopy was employed for the morphology investigation of the nanofibrous webs, while the dynamic vapor sorption revealed the hygroscopicity changes induced through the ESP process. Further, the applicative potential was investigated by preparing α-, β- and γ-CDLA/curcumin nanofibrous webs. FTIR and NMR spectroscopy characterization, and thermogravimetric analysis were used to describe the particularities of curcumin association with CDLA in ESP process. The preservation of the curcumin antioxidative potential upon the ESP processing was tested, showing that β- and γ-CDLA/curcumin nanofibrous webs are better suited for curcumin formulations.

Formulation and evaluation of curcumin loaded ethosomes as novel drug delivery system

Formulation and evaluation of curcumin loaded ethosomes as novel drug delivery system

Targeting Spike Glycoprotein S1 Mediated by NLRP3 Inflammasome Machinery and the Cytokine Releases in A549 Lung Epithelial Cells by Nanocurcumin.

Chronic inflammation and tissue damage can result from uncontrolled inflammation during SARS-CoV-2 or COVID-19 infections, leading to post-acute COVID conditions or long COVID. Curcumin, found in turmeric, has potent anti-inflammatory properties but limited effectiveness. This study developed nanocurcumin, a curcumin nanoparticle, to enhance its physical and chemical stability and investigate its in vitro anti-inflammatory properties upon CoV2-SP induction in lung epithelial cells. Nanocurcumin was prepared by encapsulating curcumin extract in phospholipids. The particle size, polydispersity index, and zeta potential of nanocurcumin were measured using dynamic light scattering. The encapsulated curcumin content was determined using HPLC analysis. The encapsulation efficiency of curcumin was 90.74 ± 5.35% as determined by HPLC. Regarding the in vitro release of curcumin, nanocurcumin displayed a higher release content than non-nanoparticle curcumin. Nanocurcumin was further investigated for its anti-inflammatory properties using A549 lung epithelial cell line. As determined by ELISA, nanocurcumin showed inhibitory effects on inflammatory cytokine releases in CoV2-SP-stimulated conditions, as evidenced by a significant decrease in IL-6, IL-1β and IL-18 cytokine secretions compared with the spike-stimulated control group (p < 0.05). Additionally, as determined by RT-PCR, nanocurcumin significantly inhibited the CoV2-SP-stimulated expression of inflammatory genes (IL-6, IL-1β, IL-18, and NLRP3) compared with the spike-stimulated control group (p < 0.05). Regarding the inhibition of NLRP3 inflammasome machinery proteins by Western blot, nanocurcumin decreased the expressions of inflammasome machinery proteins including NLRP3, ASC, pro-caspase-1, and the active form of caspase-1 in CoV2-SP-stimulated A549 cells compared with the spike-stimulated control group (p < 0.05). Overall, the nanoparticle formulation of curcumin improved its solubility and bioavailability, demonstrating anti-inflammatory effects in a CoV2-SP-induced scenario by inhibiting inflammatory mediators and the NLRP3 inflammasome machinery. Nanocurcumin shows promise as an anti-inflammatory product for preventing COVID-19-related airway inflammation.

Treatment of Psoriasis with the Help of Curcumin Hydrogel

Psoriasis is a chronic inflammatory skin disorder that affects millions of people worldwide. Current treatments for psoriasis include topical corticosteroids, immunomodulators, and phototherapy, but these treatments may have limited efficacy or cause side effects. Curcumin, a natural compound with anti-inflammatory and antioxidant properties, has been shown to have potential as an alternative treatment for psoriasis. However, the low solubility and bioavailability of curcumin limit its effectiveness when administered orally or topically. Curcumin hydrogel, a topical formulation of curcumin, has been developed to address these limitations. In this review, we summarize the current research on the use of curcumin hydrogel in the treatment of psoriasis. We discuss the pharmacological properties of curcumin, the formulation of curcumin hydrogel, and the preclinical and clinical studies investigating the efficacy and safety of curcumin hydrogel in psoriasis. Overall, the available evidence suggests that curcumin hydrogel may be a promising alternative treatment for psoriasis, with potential benefits in reducing inflammation, promoting wound healing, and improving overall quality of life for psoriasis patients. Further research is needed to fully elucidate the mechanism of action of curcumin hydrogel and to optimize its formulation and delivery for maximum efficacy.

Exploring the Contribution of Curcumin to Cancer Therapy: A Systematic Review of Randomized Controlled Trials.

Although the anticancer role of curcumin has been extensively addressed in preclinical research, only a few studies were carried out in humans, with conflicting results. The aim of this systematic review is to collate together the results of the therapeutic effect of curcumin in cancer patients. A literature search was carried out in Pubmed, Scopus, and the Cochrane Central Register of Controlled Trials up to 29 January 2023. Only randomized controlled trials (RCTs) designed to evaluate the effects of curcumin on cancer progression, patient survival, or surgical/histological response were included. Seven out of 114 articles, published between 2016 and 2022, were analyzed. They evaluated patients with locally advanced and/or metastatic prostate, colorectal, and breast cancers, as well as multiple myeloma and oral leucoplakia. Curcumin was given as an add-on therapy in five studies. Cancer response was the most investigated primary endpoint and curcumin issued some positive results. On the contrary, curcumin was ineffective in improving overall or progression-free survival. The curcumin safety profile was favorable. In conclusion, available clinical evidence is not strong enough to support the therapeutic use of curcumin in cancer. New RCTs exploring the effects of different curcumin formulations in early-stage cancers would be welcome.

Efficacy of curcumin for amelioration of radiotherapy-induced oral mucositis: a preliminary randomized controlled clinical trial

BackgroundOral mucositis (OM) is one of the main problems in almost all patients undergoing head and neck radiotherapy (RT). Owning to the antioxidant and anti-inflammatory properties of curcumin, the effect of both oral and topical formulations of curcumin was assessed on radiation-induced OM (ROM) in this study.MethodsThe safety and efficacy of curcumin mouthwash 0.1% (w/v) and curcumin-nanocapsule were evaluated in ameliorating severity and pain/burning associated with OM during RT. The current randomized, placebo-controlled trial was conducted on 37 patients with head and neck cancers. Patients with grades 1 to 3 of ROM were randomized to receive one of the three interventions: curcumin mouthwash (0.1% w/v); Sinacurcumin soft gel containing 40 mg curcuminoids as nano-micelles (SinaCurcumin®40); or placebo mouthwash with a similar transparent appearance to curcumin mouthwash for 1 min three times daily during RT. Study evaluations were conducted at baseline and weekly thereafter for up to 3 weeks using the Numeric rating scale (NRS) and world health organization (WHO) scale.ResultsAmong the 45 patients randomized, 37 (mean (SD) age of 53.36 (15.99) years; 14 [37.8%] women) completed the treatment according to the protocol. Patients treated with either oral or topical curcumin showed a significantly reduced severity and burning related to OM during the first 3 weeks after administration (P-Value < 0.001) as compared with the placebo. At study termination, more than 33% of subjects utilizing curcumin mouthwash and 15% of patients utilizing curcumin-nanocapsule remained ulcer free while all of the placebo-receiving subjects had OM. The reduction of NRS and WHO scale between curcumin groups was comparable without significant differences.ConclusionBoth curcumin mouthwash and nanocapsule were effective, safe, and well-tolerated in the treatment of radiation-induced OM. Higher doses of curcumin and larger sample sizes can be used for further investigation in future studies.Trial registration:https://irct.ir/ IRCT20190810044500N17 (13/08/2021).

A Comparative In Vitro Study: Cytotoxicity Effect of Curcumin Vs Biodegradable Nanoparticles/PVA Against HNO97 And Effect of Curcumin on Cell Cycle Phases

Purpose: This study evaluated that curcumin and biodegradable nanoparticles with PVA as capping material, in terms of cytotoxicity followed by cell cycle analysis against the HNO97 cell line (tongue carcinoma). Material and methods: 5mg of pure curcumin, 7.5 mg of Nano curcumin formulation, and SRB for IC50 done on five concentrations. A flow cytometry test was carried on to evaluate the effect of curcumin on the HNO97 cell line. Results: This study postulated that curcumin had the highest cytotoxicity effect against cell line (HNO97) with IC50=1.59 µg/ml in comparison to curcumin nanoparticles/PVA showed low cytotoxicity owing to the pH (7.4) and surface charges of PVA. Also, the cell cycle test for curcumin showed that the percentage of cells in G2/M phase was significantly increased (p=0.003). Conclusion: The study showed that curcumin has a powerful anticancer effect against in vitro tongue carcinoma. Generally, these results reported that curcumin can in vitro inhibit cancer cells.

A Comparative In Vitro Study: Cytotoxicity Effect of Curcumin Vs Biodegradable Nanoparticles/PVA Against HNO97 And Effect of Curcumin on Cell Cycle Phases

Purpose: This study evaluated that curcumin and biodegradable nanoparticles with PVA as capping material, in terms of cytotoxicity followed by cell cycle analysis against the HNO97 cell line (tongue carcinoma). Material and methods: 5mg of pure curcumin, 7.5 mg of Nano curcumin formulation, and SRB for IC50 done on five concentrations. A flow cytometry test was carried on to evaluate the effect of curcumin on the HNO97 cell line. Results: This study postulated that curcumin had the highest cytotoxicity effect against cell line (HNO97) with IC50=1.59 µg/ml in comparison to curcumin nanoparticles/PVA showed low cytotoxicity owing to the pH (7.4) and surface charges of PVA. Also, the cell cycle test for curcumin showed that the percentage of cells in G2/M phase was significantly increased (p=0.003). Conclusion: The study showed that curcumin has a powerful anticancer effect against in vitro tongue carcinoma. Generally, these results reported that curcumin can in vitro inhibit cancer cells.

Selective Cellular Uptake and Cytotoxicity of Curcumin-encapsulated SPC and HSPC Liposome Nanoparticles on Human Bladder Cancer Cells.

Curcumin is a main bioactive constituent of turmeric (Curcuma longa L.) with pleiotropic health beneficial effects. However, poor bioavailability is the major barrier to the efficient pharmacological effects of curcumin in humans. The present study aimed to develop liposome formulations based on soybean phosphatidylcholine (SPC) and hydrogenated SPC (HSPC) to enhance the bioavailability of curcumin in bladder cancer cells. Curcumin was encapsulated in HSPC and SPC liposome nanoparticles using the solvent evaporation method. Physical properties, encapsulation efficiency (%), stability, and in vitro drug release of the prepared liposome formulations have been evaluated. The cellular uptake and cytotoxicity of curcumin-encapsulated nanoliposomes on bladder carcinoma HTB9 cell line and normal fibroblast L929 cell line were studied. DNA fragmentation, apoptosis, and genotoxicity assessments have been carried out to determine the molecular mechanisms underlying the cytotoxic effects of liposomal curcumin formulations on bladder cancer cells. The results indicated that curcumin could be efficiently encapsulated in the HSPC and SPC liposome formulations. The liposomal curcumin formulations have shown shelf-life stability for 14 weeks at 4°C. The accelerated stability testing showed that curcumin encapsulated in nanoliposomes was significantly (p < 0.001) more stable than free curcumin at various pH degrees ranging from alkaline to acidic pH. The in vitro drug release study showed curcumin to be sustainably released from the liposome nanoparticles. Of note, SPC and HSPC nanoliposome formulations significantly increased the cellular uptake and cytotoxicity of curcumin on bladder cancer HTB9 cells. Mechanistically, liposomal curcumin was found to exert a selective inhibitory effect on the viability of cancer cells by inducing apoptosis and DNA damage. In conclusion, SPC and HSPC liposome nanoparticles can significantly increase the stability and bioavailability of curcumin, which are important for improving its pharmacological effect.

Curcumin-based Nanoformulations to Target Breast Cancer: Current Trends and Challenges

: Breast cancer remains one of the most common cancers in women worldwide, and despite significant improvements in treatment modalities, the prognosis of this cancer is still poor. Herbs and plant extracts have been associated with various health benefits, and traditional folk medicine is still receiving great interest among patients as proven by accumulated records, tolerable side effects of herbal compounds compared to their synthetic counterparts, and low cost. Curcumin is a polyphenol identified as the main active ingredient in turmeric and has been used in the treatment of various diseases and ailments. Additionally, the pharmacological activities of curcumin on many cancers have been investigated substantially due to its ability to regulate many signaling pathways involved in cancer tumorigenesis and metastasis. However, the low solubility and bioavailability of curcumin limit its benefits, urging the need for new curcumin formulations and delivery systems. Nanotechnology has been widely publicized in cancer treatment not only to overcome the limitations of poorly soluble and physiologically unstable compounds but also to improve the delivery of the drug to the diseased site and cellular uptake. In this review, we summarized the main anti-tumor effect of curcumin and its mode of action on breast cancer and focused on the anticancer efficacy of various and recent curcumin nanoformulations and delivery systems. Such nanotechnological systems could pave the way to address a new future direction in this research area, enhancing the therapeutic potential of curcumin in the treatment of breast cancer. In the next few years, there will be more focus on developing curcumin-based materials for breast cancer treatment.

Curcumin Formulations for Better Bioavailability: What We Learned from Clinical Trials Thus Far?

Curcumin has been credited with a wide spectrum of pharmacological properties for the prevention and treatment of several chronic diseases such as arthritis, autoimmune diseases, cancer, cardiovascular diseases, diabetes, hemoglobinopathies, hypertension, infectious diseases, inflammation, metabolic syndrome, neurological diseases, obesity, and skin diseases. However, due to its weak solubility and bioavailability, it has limited potential as an oral medication. Numerous factors including low water solubility, poor intestinal permeability, instability at alkaline pH, and fast metabolism contribute to curcumin's limited oral bioavailability. In order to improve its oral bioavailability, different formulation techniques such as coadministration with piperine, incorporation into micelles, micro/nanoemulsions, nanoparticles, liposomes, solid dispersions, spray drying, and noncovalent complex formation with galactomannosides have been investigated with in vitro cell culture models, in vivo animal models, and humans. In the current study, we extensively reviewed clinical trials on various generations of curcumin formulations and their safety and efficacy in the treatment of many diseases. We also summarized the dose, duration, and mechanism of action of these formulations. We have also critically reviewed the advantages and limitations of each of these formulations compared to various placebo and/or available standard care therapies for these ailments. The highlighted integrative concept embodied in the development of next-generation formulations helps to minimize bioavailability and safety issues with least or no adverse side effects and the provisional new dimensions presented in this direction may add value in the prevention and cure of complex chronic diseases.

The effect of micro-particle curcumin on chronic kidney disease progression: the MPAC-CKD randomized clinical trial.

Curcumin is a commonly used herbal supplement with anti-inflammatory and anti-fibrotic properties. Animal studies and small human trials suggest that curcumin reduces albuminuria in patients with chronic kidney disease (CKD). Micro-particle curcumin is a new, more bioavailable formulation of curcumin. To determine whether micro-particle curcumin versus placebo slows the progression of albuminuric CKD we conducted a randomized, double-blind, placebo-controlled trial with 6-month follow-up. We included adults with albuminuria [a random urine albumin-to-creatinine ratio >30mg/mmol (265mg/g) or a 24-h urine collection with more than 300mg of protein] and an estimated glomerular filtration rate (eGFR) between 15 and 60mL/min/1.73 m2 within the 3months before randomization. We randomly allocated participants 1:1 to receive micro-particle curcumin capsules (90mg/day) or matching placebo for 6months. After randomization, the co-primary outcomes were the changes in albuminuria and the eGFR. We enrolled 533 participants, but 4/265 participants in the curcumin group and 15/268 in the placebo group withdrew consent or became ineligible. The 6-month change in albuminuria did not differ significantly between the curcumin and placebo groups [geometric mean ratio 0.94, 97.5% confidence interval (CI) 0.82 to 1.08, P=.32]. Similarly, the 6-month change in eGFR did not differ between groups (mean between-group difference -0.22mL/min/1.73m2, 97.5% CI-1.38 to 0.95, P=.68). Ninety milligrams of micro-particle curcumin daily did not slow the progression of albuminuric CKD over 6months. ClinicalTrials.gov Identifier: NCT02369549.

Curcumin Supplementation and Human Disease: A Scoping Review of Clinical Trials.

Medicinal properties of turmeric (Curcuma longa L.), a plant used for centuries as an anti-inflammatory, are attributed to its polyphenolic curcuminoids, where curcumin predominates. Although "curcumin" supplements are a top-selling botanical with promising pre-clinical effects, questions remain regarding biological activity in humans. To address this, a scoping review was conducted to assess human clinical trials reporting oral curcumin effects on disease outcomes. Eight databases were searched using established guidelines, yielding 389 citations (from 9528 initial) that met inclusion criteria. Half focused on obesity-associated metabolic disorders (29%) or musculoskeletal disorders (17%), where inflammation is a key driver, and beneficial effects on clinical outcomes and/or biomarkers were reported for most citations (75%) in studies that were primarily double-blind, randomized, and placebo-controlled trials (77%, D-RCT). Citations for the next most studied disease categories (neurocognitive [11%] or gastrointestinal disorders [10%], or cancer [9%]), were far fewer in number and yielded mixed results depending on study quality and condition studied. Although additional research is needed, including systematic evaluation of diverse curcumin formulations and doses in larger D-RCT studies, the preponderance of current evidence for several highly studied diseases (e.g., metabolic syndrome, osteoarthritis), which are also clinically common, are suggestive of clinical benefits.

Enhanced Pharmacokinetics and Anti-inflammatory Activity of Curcumin Using Dry Emulsion as Drug Delivery Vehicle.

Many naturally available dietary molecules such as curcumin have not seen the market due to poor solubility, bioavailability, and photodegradability. Successful development of a lipid-based dry emulsion may overcome these issues and help in reaching the markets for natural dietary molecules such as curcumin. The current study aims to develop a dry emulsion formulation of curcumin using natural oil and evaluate its dissolution, photostability, pharmacokinetics, and anti-inflammatory activity. Dry emulsions were prepared using emu oil and corn oil as the lipid phase, Caproyl 90 and Cremophor RH 40 as surfactants, and dextrin as a hydrophilic carrier. Microscopic studies showed the formation of spherical porous particles, and solid-state characterization using differential scanning calorimetry and powder X-ray diffraction showed the conversion of curcumin to an amorphous form. About 80% drug release was observed from formulation, whereas pure drug showed only 50% drug release in 30min. Invivo pharmacokinetic studies showed fivefold improvement in the maximum concentration of curcumin in plasma (Cmax) and sevenfold improvement in the area under the concentration-timecurve of curcumin from emu oil formulation compared with pure curcumin. Significant differences were observed in the anti-inflammatory activity of curcumin dry emulsion and plain curcumin. Emu-oil-based formulations showed synergistic anti-inflammatory activity over corn-oil-based formulations with improved photostability. The present study suggests that the dry emulsion may enhance the bioavailability with synergistic anti-inflammatory activity and photostability of curcumin when given orally.

Development of Computational In Silico Model for Nano Lipid Carrier Formulation of Curcumin.

The oral delivery system is very important and plays a significant role in increasing the solubility of drugs, which eventually will increase their absorption by the digestive system and enhance the drug bioactivity. This study was conducted to synthesize a novel curcumin nano lipid carrier (NLC) and use it as a drug carrier with the help of computational molecular docking to investigate its solubility in different solid and liquid lipids to choose the optimum lipids candidate for the NLCs formulation and avoid the ordinary methods that consume more time, materials, cost, and efforts during laboratory experiments. The antiviral activity of the formed curcumin-NLC against SARS-CoV-2 (COVID-19) was assessed through a molecular docking study of curcumin's affinity towards the host cell receptors. The novel curcumin drug carrier was synthesized as NLC using a hot and high-pressure homogenization method. Twenty different compositions of the drug carrier (curcumin nano lipid) were synthesized and characterized using different physicochemical techniques such as UV-Vis, FTIR, DSC, XRD, particle size, the zeta potential, and AFM. The in vitro and ex vivo studies were also conducted to test the solubility and the permeability of the 20 curcumin-NLC formulations. The NLC as a drug carrier shows an enormous enhancement in the solubility and permeability of the drug.

CurQ+, a Next-Generation Formulation of Curcumin, Ameliorates Growth Plate Chondrocyte Stress and Increases Limb Growth in a Mouse Model of Pseudoachondroplasia.

Mutations in cartilage oligomeric matrix protein (COMP) causes protein misfolding and accumulation in chondrocytes that compromises skeletal growth and joint health in pseudoachondroplasia (PSACH), a severe dwarfing condition. Using the MT-COMP mice, a murine model of PSACH, we showed that pathological autophagy blockage was key to the intracellular accumulation of mutant-COMP. Autophagy is blocked by elevated mTORC1 signaling, preventing ER clearance and ensuring chondrocyte death. We demonstrated that resveratrol reduces the growth plate pathology by relieving the autophagy blockage allowing the ER clearance of mutant-COMP, which partially rescues limb length. To expand potential PSACH treatment options, CurQ+, a uniquely absorbable formulation of curcumin, was tested in MT-COMP mice at doses of 82.3 (1X) and 164.6 mg/kg (2X). CurQ+ treatment of MT-COMP mice from 1 to 4 weeks postnatally decreased mutant COMP intracellular retention, inflammation, restoring both autophagy and chondrocyte proliferation. CurQ+ reduction of cellular stress in growth plate chondrocytes dramatically reduced chondrocyte death, normalized femur length at 2X 164.6 mg/kg and recovered 60% of lost limb growth at 1X 82.3 mg/kg. These results indicate that CurQ+ is a potential therapy for COMPopathy-associated lost limb growth, joint degeneration, and other conditions involving persistent inflammation, oxidative stress, and a block of autophagy.