Low Water Solubility Research Articles

Impact of Co-Spray Drying with Leucine or Trileucine on Aerosol Performance, In Vitro Dissolution, and Cellular Uptake of Colistin Powder Formulations for Inhalation

Background/Objective: Surface enrichment of hydrophobic excipients via spray drying has been demonstrated as an efficient way to protect the dry powder inhaler formulations against moisture-induced deterioration in aerosol performance. However, the impact of such surface enrichment on dissolution and cellular uptake is less investigated, which can affect the safety and efficacy of dry powder inhalers (DPIs). Methods: In the present work, hygroscopic colistin was coated with leucine or trileucine, at different weight ratios during spray drying. All the powders were exposed to 75% relative humidity for one week. The aerosol performance was compared before and after the moisture exposure. Various solid-state characterizations, including particle size, particle morphology, crystallinity, water sorption/desorption, and surface composition, were conducted to evaluate the properties of spray-dried colistin with/without leucine or trileucine. Results: The results indicated that leucine or trileucine could protect the aerosol performance of spray-dried colistin against moisture deterioration. Leucine crystallized after spray drying with colistin, and such crystal leucine could further hinder water uptake when leucine was at a 20% or higher weight ratio. Trileucine did not crystallize after spray drying with colistin nor reduce the water uptake. Interestingly, trileucine showed a superior moisture protective effect to that of leucine, which could be attributed to its better surface enrichment efficiency than that of leucine due to its lower water solubility. Conclusions: Importantly, our results showed that the surface enrichment with leucine and trileucine did not significantly affect in vitro dissolution of colistin in the Franz cell test and cellular uptake of colistin in the H441 lung epithelium cell model, which could be attributed to small particle size and incomplete surface coverage by leucine or trileucine.

Validation of RP-UHPLC Method for Quantitative Determination of Polycyclic Aromatic Hydrocarbons from Soil

Polycyclic aromatic hydrocarbons (PAHs) are ubiquitous environmental pollutants composed of two or more fused aromatic rings, which are characterized by low water solubility, low vapor pressure, and high melting and boiling points, depending on their structures. Due to the lipophilic nature of these compounds, they are strongly adsorbed by soil and sediments. The United States Environmental Protection Agency (USEPA) has declared 16 PAHs as priority pollutants in 1983 based on their existence of highest concentrations, greater exposure and toxicity. The purpose of this article is to validate a method for determining ten PAHs in soil by ultra-high pressure liquid chromatography with UV-VIS detection. The evaluated performance parameters are: selectivity, linearity, accuracy, precision, limit of detection (LOD), limit of quantification (LOQ), limit of repeatability (r), recovery (R) and uncertainty of measurement (U). LOD ranged between 0.02 mg/mL and 0.3 mg/mL, LOQ ranged between 0.2 mg/mL and 0.95 mg/mL. The recovery values ranged between 75.4% for benzo(b) fluoranthen and 89.8% for chrysene. These values were established using a soil reference material which was extracted with hexane/acetone using a Soxhlet method. The PAH compounds were separated using a nonpolar stationary phase column and were determined by liquid chromatography with Array Diode Detector at 254 nm.

Corosolic acid and its derivatives targeting MCCC1 against insulin resistance and their hypoglycemic effect on type 2 diabetic mice.

Corosolic acid (CA), a natural triterpenoid, exhibits various biological activities and is often called as plant-derived insulin due to its significant hypoglycemic effects, making it especially beneficial for individuals with diabetes or high blood glucose levels. However, CA has notable in vitro toxicity, low water solubility, and poor pharmacokinetic properties. To address these limitations, a series of CA derivatives were synthesized, resulting in the identification of derivative H26, which demonstrates a significantly enhanced hypoglycemic effect, reduced toxicity, and improved pharmacokinetic characteristics compared to CA. To identify the target protein of CA and investigate its therapeutic potential, a chemical probe derived from natural products, called CA-biotin, was designed and synthesized. By employing an avidin-biotin affinity binding system, we distinguished the differential protein bands between CA-biotin and biotin. This quantitative proteomic analysis revealed, for the first time, that the biotin-containing enzyme methylcrotonoyl-CoA carboxylase 1 (MCCC1) directly binds to CA. The interaction between H26 and MCCC1 was examined in vitro. The research on the mechanisms by which CA and H26 address Type 2 diabetes mellitus (T2DM) focused on the insulin resistance signaling pathway, specifically targeting MCCC1. The results indicated that H26 shows significant promise as a potential hypoglycemic agent, while MCCC1 may serve as a valuable target for addressing insulin resistance. This presents a promising opportunity for developing new medications aimed at improving the health of patients with type 2 diabetes mellitus (T2DM) or hyperglycemia.

Stability and in vitro digestion behavior of astaxanthin-loaded Pickering emulsions stabilized by OSA-modified starch: Influence of oil phase content.

Astaxanthin, a lipid-soluble carotenoid, is widely recognized for its health-promoting properties. However, its use in functional foods is limited due to its low water solubility, chemical instability, and poor bioavailability. This study evaluated the potential of esterified starch-stabilized emulsions as astaxanthin carriers. The effects of the oil phase content on the emulsion properties, stability, and in vitro digestion behavior of the emulsions were investigated. All emulsions exhibited adequate encapsulation efficiency (>80%) for astaxanthin. Moreover, the particle size and viscosity of the emulsions increased with an increasing oil phase content. The emulsion with a 10% oil phase content (E-10%) showed high retention of astaxanthin (>40%) under the temperature, pH, and ionic strength conditions tested and long-term stability (42days). On the other hand, the release of free fatty acids and bioaccessibility of astaxanthin were negatively correlated with the oil phase content. And the bioaccessibility of astaxanthin was increased to 11.66% (for E-10%). Under a constant emulsifier concentration, E-10% and E-20% exhibited a thicker interfacial layer at the oil/water interface. Based on this, a smaller particle size may favor oil droplet dispersion and inhibit droplet floatation and aggregation, improving emulsion stability. Therefore, this study provides useful information on the effect of the oil phase content in esterified starch-stabilized Pickering emulsion delivery systems.

Recent advances in modifications, biotechnology, and biomedical applications of chitosan-based materials: A review.

Chitosan, a natural polysaccharide with recognized biocompatibility, non-toxicity, and cost-effectiveness, is primarily sourced from crustacean exoskeletons. Its inherent limitations such as poor water solubility, low thermal stability, and inadequate mechanical strength have hindered its widespread application. However, through modifications, chitosan can exhibit enhanced properties such as water solubility, antibacterial and antioxidant activities, adsorption capacity, and film-forming ability, opening up avenues for diverse applications. Despite these advancements, realizing the full potential of modified chitosan remains a challenge across various fields. The purpose of this review article is to conduct a comprehensive evaluation of the chemical modification techniques of chitosan and their applications in biotechnology and biomedical fields. It aims to overcome the inherent limitations of chitosan, such as low water solubility, poor thermal stability, and inadequate mechanical strength, thereby expanding its application potential across various domains. This review is structured into two main sections. The first part delves into the latest chemical modification techniques for chitosan derivatives, encompassing quaternization, Schiff base formation, acylation, carboxylation, and alkylation reactions. The second part provides an overview of the applications of chitosan and its derivatives in biotechnology and biomedicine, spanning areas such as wastewater treatment, the textile and food industries, agriculture, antibacterial and antiviral activities, drug delivery systems, wound dressings, dental materials, and tissue engineering. Additionally, the review discusses the challenges associated with these modifications and offers insights into potential future developments in chitosan-based materials. This review is anticipated to offer theoretical insights and practical guidance to scientists engaged in biotechnology and biomedical research.

Unfolding bovine serum albumin decorated selenium nanoparticles crosslinking with chitosan: Achieve stabilization of Pickering emulsions gel and enhance resveratrol bioaccessibility.

Resveratrol (Res) is a natural polyphenol exhibiting anti-oxidant and anti-inflammatory activity. However, the applications of Res have been limited due to its low stability and water solubility. To enhance the bioaccessibility of Res, unfolding bovine serum albumin-modified selenium nanoparticles (UBSA@SeNPs) encapsulated within chitosan (CS)-coated Pickering emulsions (CS-UBSA@SeNPs-PE) were used to load Res. The results showed that Res-loaded CS(0.06%)-UBSA@SeNPs-PE has small droplet size (16.13μm), high gel properties and excellent antioxidant properties. During the simulated digestion process, CS reduced the release rate of Res from Res-loaded CS(0.06%)-UBSA@SeNPs-PE (42.27%) to reach a slow release effect. Importantly, Res could quickly release from CS-UBSA@SeNPs-PE within intestinal fluid or in the presence of chitosanase. In simulated absorption experiments, the intestinal permeability of Res in Res-loaded CS(0.06%)-UBSA@SeNPs-PE were enhanced by 292.31% compare to Res-loaded CS(0%)-UBSA@SeNPs-PE. In pharmacokinetic studies, Res-loaded CS(0.06%)-UBSA@SeNPs-PE had an area under the curve (AUC) up to 3467.99±127.43ng*h/mL. Furthermore, CS also improved the mucoadhesive nature of UBSA@SeNPs-PE, resulting in a gut-retention time of Res-loaded CS(0.06%)-UBSA@SeNPs-PE that reached up to 60h. In conclusion, CS-UBSA@SeNPs-PE can serve as an effective oral delivery system for improving the bioaccessibility of Res.

Co-assembled supramolecular hydrogel of asiaticoside and Panax notoginseng saponins for enhanced wound healing.

Self-assembling natural drug hydrogels have emerged as promising biomaterials for scalable and customizable drug delivery systems attributed to their inherent biocompatibility and biodegradability. Asiaticoside (AS), a bioactive compound derived from Centella asiatica (L.) Urb., is known for its antioxidant, antifibrotic, and anti-inflammatory properties, primarily accelerating wound healing through the promotion of collagen synthesis. However, its low water solubility leads to poor transdermal absorption and reduced bioavailability when applied topically. Panax notoginseng saponins (PNS), active compounds derived from the stems of Panax notoginseng (Burk.) F.H. Chen, exhibit amphiphilic and surfactant properties, rendering them effective stabilizers. Our research has demonstrated that the co-assembly of AS and PNS forms a hydrogel, termed AS&PNS hydrogel, which significantly enhances wound healing by reducing interleukin-6 (IL-6) levels and promoting the production of vascular endothelial growth factor (VEGF). Treatment with AS&PNS hydrogel also tended to normalize epidermal thickness and improve collagen fiber organization at the wound site. This novel hydrogel material presents a straightforward and effective approach to managing skin wounds.

Investigation of the antibacterial activity, cytotoxicity, and effects on enamel and composite resin of mouthwash formulations prepared with three different Boron compounds.

This study investigated the use of oral rinse solutions formulated with boron-containing compounds, known for their antibacterial activity, as an alternative to chlorhexidine (CHX). Boron nitride (BN), boric acid (BA) and sodium borate (SB) were used in the study. BN was used in nanosuspension (BN-NS) due to its low solubility in water. BA and SB were also prepared and used in solution form (BA-S, SB-S). Antibacterial activity against cariogenic bacteria was evaluated using agar well diffusion and microdilution techniques, and antibiofilm activity was evaluated using the crystal violet method. Cytotoxicity in human gingival cell lines (HGF-1) was evaluated using MTT and LDH assays. Surface hardness was measured with Vicker's Microhardness tester and surface roughness was measured with a profilometer. CHX was used as the control group. BN-NS, BA-S, and SB-S showed antibacterial and antibiofilm activity against all cariogenic bacteria. BN-NS and SB-S demonstrated much lower cytotoxicity compared to CHX, while BA-S exhibited similar cytotoxicity. SB-S caused an increase in enamel surface hardness (p = 0.017), whereas no significant changes were observed in surface roughness or hardness in the other groups (p > 0.05). BN-NS and SB-S showed antibacterial effects and antibiofilm activity on all tested cariogenic bacteria. BN-NS and SB-S showed lower cytotoxicity than CHX, and their effects on enamel and composite resin surfaces were similar to the control group. Further studies are needed to support the use of BN-NS and SB-S as alternatives to CHX. BN-NS and SB-S are promising alternatives to the antibacterial agent CHX, which is known to be cytotoxic.

Active film made from Psidium guajava peel and starch for use in food packaging

The disposal of plastic film is a global problem that generates much pollution. The full use of waste from the food industry brings numerous benefits, including sustainable practices. Using films made with natural antioxidants derived from agro-industrial waste is considered an alternative to minimize these impacts. Given this context, this study aimed to develop and characterize films based on guava (Psidium guajava) peel flour for active food packaging. The films presented low thickness and solubility in water, proving to be a barrier to water vapor and suitable for maintaining the integrity of foods added to them. Moreover, their elasticity and resistance proved to be moderate and their moisture content is high due to the presence of large amounts of phenolic compounds from guava peel flour (320.58 ± 81.1 mg gallic acid/100 g sample), resulting in clear, slightly greenish-yellow films, which present their best effect as active antioxidant packaging to be applied in alcoholic foods (36 μmol Trolox/g), followed by use in acidic foods (17.2 μmol Trolox/g). This study demonstrated the potential for applying guava residue as a raw material for producing biodegradable films, proposing a purpose for the peel of this fruit.

Drug Delivery Systems Utilizing Essential Oils and Their Compounds—A Promising Approach to Fight Pathogens

Essential oils (EOs) and their compounds are becoming a growing interest in medical sciences. Despite their potential as antimicrobial, anxiolytic, cytotoxic, and immunosuppressive drugs, their chemical characteristics make them difficult to use in direct treatment. This article intends to summarize the current body of knowledge regarding drug delivery systems that can overcome obstacles, such as low water solubility, volatility, oxidation potential, photodegradation, and thermal instability of EO compounds. Various materials like zeolites, alginate, chitosan, cellulose nanomaterials, zein, poly (D,L-lactic-co-glycolic) acid, liposomes, nanoemulsions, and their modifications can help to mitigate these problems, but their utilization in medical settings is still lacking. The biggest issue in the utilization of natural compounds seems to be the very low number of clinical trials, which seriously impedes their usage despite favorable outcomes in/of in vitro experiments.

Bioconjugation of Podophyllotoxin and Nanosystems: Approaches for Boosting Its Biopharmaceutical and Antitumoral Profile

Podophyllotoxin is a natural compound belonging to the lignan family and is well-known for its great antitumor activity. However, it shows several limitations, such as severe side effects and some pharmacokinetics problems, including low water solubility, which hinders its application as an anticancer agent. Over the past few years, antitumor research has been focused on developing nanotechnology-based medicines or nanomedicines which allow researchers to improve the pharmacokinetic properties of anticancer compounds. Following this trend, podophyllotoxin nanoconjugates have been obtained to overcome its biopharmaceutical drawbacks and to enhance its antitumor properties. The objective of this review is to highlight the advances made over the past few years (2017–2023) regarding the inclusion of podophyllotoxin in different nanosystems. Among the huge variety of nanoconjugates of diverse nature, drug delivery systems bearing podophyllotoxin as cytotoxic payload are organic nanoparticles mainly based on polymer carriers, micelles, and liposomes. Along with the description of their pharmacological properties as antitumorals and the advantages compared to the free drug in terms of biocompatibility, solubility, and selectivity, we also provide insight into the synthetic procedures developed to obtain those podophyllotoxin-nanocarriers. Typical procedures in this regard are self-assembly techniques, nanoprecipitations, or ionic gelation methods among others. This comprehensive perspective aims to enlighten the medicinal chemistry community about the tendencies followed in the design of new podophyllotoxin-based drug delivery systems, their features and applications.

Reviewing the Potential Use of Curcumin Extract for Topical Therapy Supporting Burn Wound Healing

Introduction: Wound dressing is a fundamental aspect of modern healthcare, encompassing a diverse range of materials and techniques aimed at optimizing the healing process while safeguarding against infection and further injury. By understanding the specific benefits of different types of wound dressings, healthcare professionals can optimize the healing process and improve patient outcomes Methods: This literature review was compiled using information from numerous open access web databases. Data were compiled and analyzed. Results and Discussions: Curcumin has the ability to improve burn wound healing. Curcumin can reduce inflammation by inhibiting proinflammatory cytokines. It also helps cell proliferation, and has an antimicrobial effect, therefore it speeds up burn wound healing and prevents keloid formation. Conclusion: Curcumin has potential activity in speeding up burn wound healing, thanks to its anti-inflammation, antioxidant, and antimicrobial activity. However, due to low solubility in water of curcumin and its instability, further research must be done to find out better form for curcumin

Harnessing Nanotechnology to Enhance Essential Oil Applications

Essential oils (EOs) are versatile natural compounds with significant antimicrobial, antioxidant, antifungal, and therapeutic properties, making them valuable in industries such as food preservation, agriculture, and healthcare. However, their inherent volatility, low water solubility, and susceptibility to environmental degradation limit their direct applications. Nanotechnology offers transformative solutions to these challenges, enhancing the stability, bioavailability, and efficacy of EOs through innovative nano systems such as nano emulsions, encapsulations, and nanocomposites. This study explores the integration of nanotechnology with essential oils, emphasizing advanced preparation techniques, physicochemical properties, and diverse applications. It highlights sustainable approaches, including eco-friendly synthesis and biodegradable carriers, which align with global trends toward green chemistry. By addressing key challenges and proposing future directions, this research underscores the potential of EO nano systems to deliver multifunctional and environmentally conscious solutions for global challenges such as food security, antimicrobial resistance, and sustainable agriculture.

Optimization of the poloxamer 407-conjugated gelatin to synthesize pH-sensitive nanocarriers for controlled paclitaxel delivery

Chemotherapy is one of the most prevalent and efficacious treatments for a wide variety of cancers; however, chemotherapeutic agents have clinically limited applications due to their low water solubility and risk of side effects. Nanomedicine can help to easily deliver hydrophobic and hydrophilic agents for cancer treatment. Here, we describe a nanocarrier system that enables the sustainable and controllable release of hydrophobic anticancer drugs, Paclitaxel, based on poloxamer 407-conjugated gelatin (GeP) copolymers. The particle size, zeta potential, morphology, and thermal stability of the nanogels were characterized. The successful synthesis of nanogels was confirmed by analyzing their chemical components. Among the GePs at different amounts of poloxamer 407, a ratio of gelatin and poloxamer (Ge:P) at 1:15 for preparation resulted in the nanogels being positive in charge, spherical in shape, and 97.84 ± 2.94 nm in hydrodynamic diameter (Dh), with optimal drug-carrying efficacy. The in vitro drug release from nanogels was accelerated in the tumor microenvironment at pH 5.5 in comparison to pH 7.4, and the drug release kinetics from nanogels were due to Fickian diffusion. Finally, the cytotoxicity assays indicated that GePs were biocompatible nanocarriers without toxicity on both normal (VERO) and breast cancer cell (MCF-7) lines, which could improve the pharmacokinetics and pharmacodynamics of paclitaxel. Overall, these results revealed an optimal ratio (1:15) of Ge:P for the synthesis of pH-responsive hybrid nanogels for sufficient paclitaxel releasement to kill MCF-7 for effective cancer treatment.

Enhanced Corneal Repair with Hyaluronic Acid/Proanthocyanidins Nanoparticles.

This study investigates the therapeutic potential of hyaluronic acid/proanthocyanidin (HA/PAC) nanoparticles in treating alkali-induced corneal burns. Alkali burns are common ocular emergencies that can lead to severe vision impairment if not promptly and properly treated. The low water solubility of proanthocyanidins (PACs), which are potent antioxidant and anti-inflammatory agents, limits their bioavailability and therapeutic efficacy. To overcome this, hyaluronic acid (HA) was utilized as a carrier to form HA/PAC nanoparticles, enhancing PAC's solubility and bioavailability. The HA/PAC nanoparticles were characterized for morphology, granulometric distribution, hemolysis, and cytotoxicity, demonstrating high blood compatibility and noncytotoxicity. The in vitro antioxidant and anti-inflammatory capacities of HA/PAC were evaluated, showing enhanced activity compared to PAC alone. In vivo studies on C57 mice confirmed the accelerated healing of corneal injuries and reduced corneal opacity with HA/PAC treatment. Histopathological analysis and cytokine quantification further supported the anti-inflammatory and proregenerative effects of HA/PAC, suggesting its potential as an effective treatment for corneal alkali burns.

Cellulose-based delivery systems for bioactive ingredients: A review.

Considering the outstanding advantages including abundant resources, structure-performance designability, impressive mechanical strength, and 3D network structure-forming ability, cellulose is an ideal material for encapsulating bioactive ingredients. Due to its low solubility in water, large-scaled morphology and poor flexibility, cellulose is unsuitable for the construction of carriers. Consequently, the majority of cellulose is employed following physical or chemical modification. Cellulose and its derivatives are extensively employed in the food industry, including fat replacement, food packaging composites, food additives, 3D-printed food and delivery systems. Their benefits in food delivery systems are particularly pronounced. Therefore, the distinguishing features, preparation methods, recent developments and effectiveness of different cellulose-based delivery systems for bioactive ingredients are discussed. Cellulose-based delivery systems offer unique advantages in terms of environmental impact reduction, modification facilitation, stimuli-responsive release as well as tailored design, and their application has gained widespread recognition. However, they are facing challenges in the application process comprising modification methods for cellulose-based materials, new methods for commercial preparation on a wide scale, cellulose-based multifunctional conveyance systems and systematic evaluation using in vivo experiments. In conclusion, this review provides theoretical references for the development of novel delivery carriers as well as the efficient application and popularization of cellulose-based delivery systems.

Curcumin Solubility and Bioactivity Enhancement Through Amorphization with Tryptophan via Supercritical Fluid Technology.

Curcumin, a compound known for its antioxidant and neuroprotective properties, faces challenges due to its low water solubility, which can limit its effectiveness. One effective method to address this issue is through amorphization. Incorporating curcumin into a polymeric matrix to form amorphous solid dispersions is a common approach. Another strategy involves co-amorphous systems, where low-molecular-weight components act as co-formers. A recent innovative approach combines these strategies. This study used tryptophan as a co-former and prepared systems using supercritical fluid technology. The amorphous nature of two systems was confirmed through X-ray powder diffraction: one with 10% curcumin and a polymer, and another with 10% curcumin, a polymer, and tryptophan. Fourier-transform infrared analysis demonstrated molecular interactions among all components in the systems. Scanning electron microscopy revealed that the amorphization process significantly modified the morphology of the powder particles. The ternary system with tryptophan notably increased curcumin solubility by over 300-fold. The amorphous form of curcumin in both systems exhibited significantly higher dissolution rates compared to its crystalline form. The system with tryptophan showed more than a threefold improvement in permeability according to the PAMPA test. The enhanced solubility led to over a sixfold increase in antioxidant activity and a 25-fold improvement in the inhibition of the enzyme butyrylcholinesterase.

Characterisation of C‐β‐Cyclodextrin‐Thymol Inclusion Complexes as Delivery Systems for Antibacterial and Antioxidant Applications

ABSTRACTThymol (THY) is a natural antioxidant and antimicrobial; however, its biological activity and application in the food and pharmaceutical fields are limited due to its low water solubility and volatility. In this study, inclusion complexes of cationic‐β‐cyclodextrin‐THY (C‐β‐CD‐THY) were prepared by using the aqueous stirring method. Then UV–Vis spectra, FT‐IR, NMR, DSC, XRD and SEM data were collected to characterise the structure and morphology of the inclusion complexes. Phase solubility experiments showed a better solubilisation effect of C‐β‐CD‐THY than HP‐β‐CD‐THY. At a concentration of 0.64 mmol/L for THY, the DPPH scavenging rate was 60.99% and 61.31% for HP‐β‐CD‐THY and C‐β‐CD‐THY, respectively, whereas that of THY in 10% ethanol was only 43.47%. The bacteriostatic activity was verified using a circle of inhibition and the live/dead bacterial double stain. C‐β‐CD‐THY exhibited better antimicrobial activities against Escherichia coli and Staphylococcus aureus than HP‐β‐CD‐THY. In conclusion, the C‐β‐CD‐THY inclusion complexes have the potential to be applied as an effective bacteriostatic agent for food and pharmaceutical applications.

Synthesis and Biological Evaluation of New cis-Restricted Triazole Analogues of Combretastatin A-4.

The natural products combretastatins A-1 and A-4 are potent antimitotic and vascular-disrupting agents through their binding at the colchicine site in tubulin. However, these compounds suffer from a low water solubility and a tendency to isomerize to the inactive trans stilbenes. In this study, we have prepared a series of 18 cis-restricted triazole analogues of combretastatin A-4 (CA-4), maintaining, in all cases, the 3,4,5-trimethoxy phenyl ring A, with the aim of investigating the substitution pattern on the B-ring in a systematic way. To this end, cytotoxic activities of the cis-restricted analogues of CA-4 prepared were determined in two tumor cell lines, namely, HT-29 and A-549, as well as in the non-tumor cell line HEK-293, to pre-evaluate the selectivity profile of the compounds for the tumor cell lines. The main conclusion was the essential presence of methoxyl or ethoxyl groups at the para position of the B-ring in order to obtain good antitumor activities. Thus, the more active compounds in our study displayed IC50 values in the nanomolar range for the tumor cell lines but not for the normal cells. Consequently, these triazole analogues of CA-4 could serve as promising alternatives to the natural product, although further studies about their biological activity are essential in order to fully determine their viability as therapeutic agents in the treatment of cancer.

Curcumin-Based Nanoparticles: Advancements and Challenges in Tumor Therapy.

Curcumin, a bioactive compound derived from the rhizome of Curcuma longa L., has garnered significant attention for its potent anticancer properties. Despite its promising therapeutic potential, its poor bioavailability, rapid metabolism, and low water solubility hinder curcumin's clinical application. Nanotechnology offers a viable solution to these challenges by enabling the development of curcumin-based nanoparticles (CNPs) that enhance its bioavailability and therapeutic efficacy. This review provides a comprehensive overview of the recent advancements in the design and synthesis of CNPs for cancer therapy. We discuss various NP formulations, including polymeric, lipid-based, and inorganic nanoparticles, highlighting their role in improving curcumin's pharmacokinetic and pharmacodynamic profiles. The mechanisms by which CNPs exert anticancer effects, such as inducing apoptosis, inhibiting cell proliferation, and modulating signaling pathways, are explored in details. Furthermore, we examine the preclinical and clinical studies that have demonstrated the efficacy of CNPs in treating different types of tumors, including breast, colorectal, and pancreatic cancers. Finally, the review addresses the current challenges and future perspectives in the clinical translation of CNPs, emphasizing the need for further research to optimize their design for targeted delivery and to enhance their therapeutic outcomes. By synthesizing the latest research, this review underscores the potential of CNPs as a promising avenue for advancing cancer therapy.