Carrier System Research Articles

Functionalized and Theranostic Lipidic and Tocosomal Drug Delivery Systems: Potentials and Limitations in Cancer Photodynamic Therapy.

Photodynamic therapy (PDT) is a multidisciplinary area, which involves photophysics and photochemical sciences and plays an important role in cancer diagnosis and treatment. PDT involves a photo-activable drug called photosensitizer (PS), a specific wavelength of light and cellular compounds to produce toxic oxygen species in a much-localized way to destroy malignant tumors. Despite the various benefits of PDT, some PS-related limitations hinder its use as an ideal treatment option for cancer. To address these limitations (e.g., poor bioavailability, weak permeability, hydrophobicity, and aggregation), lipid-based and vesicular drug delivery systems have been employed. These carrier systems possess the ability to enhance the bioavailability, permeability, and solubility of the drug. Furthermore, they tend to load hydrophobic and lipophilic compounds and can be employed for an efficient and targeted drug delivery. The purpose of this review is to highlight the precise idea of PDT, the limitations of PDT related to PS, and the application of lipidic and tocosomal carriers in PDT for the treatment of various types of cancers. Liposomes, nanoliposomes, solid lipid nanoparticles, vesicular phospholipid gels, exosomes, transferosomes, and tocosomes are presented as commonly-employed vesicular drug carriers. Moreover, the amalgamation of cell-based drug delivery systems (CBDDS) with PDT holds considerable potential as an encouraging avenue in cancer treatment, especially in the context of immunotherapy.

Structurally Dynamic Monocyte-Liposome Hybrid Vesicles as an Anticancer Drug Delivery Vehicle: A Crucial Correlation of Microscopic Elasticity and Ultrafast Dynamics.

A biomimetic cell-based carrier system based on monocyte membranes and liposomes has been designed to create a hybrid "Monocyte-LP" which inherits the surface antigens of the monocytes along with the drug encapsulation property of the liposome. Förster resonance energy transfer (FRET) and polarization gated anisotropy measurements show the stiffness of the vesicles obtained from monocyte membranes (Mons), phosphatidylcholine membranes (LP), and Monocyte-LP to follow an increasing order of Mons > Monocyte-LP > LP. The dynamics of interface bound water molecules plays a key role in the elasticity of the vesicles, which in turn imparts higher delivery efficacy to the hybrid Monocyte-LP for a model anticancer drug doxorubicin than the other two vesicles, indicating a critical balance between flexibility and rigidity for an efficient cellular uptake. The present work provides insight on the influence of elasticity of delivery vehicles for enhanced drug delivery.

Nebulization and In Vitro Upper Airway Deposition of Liposomal Carrier Systems.

Liposomal carrier systems have emerged as a promising technology for pulmonary drug delivery. This study focuses on two selected liposomal systems, namely, dipalmitoylphosphatidylcholine stabilized by phosphatidic acid and cholesterol (DPPC-PA-Chol) and dipalmitoylphosphatidylcholine stabilized by polyethylene glycol and cholesterol (DPPC-PEG-Chol). First, the research investigates the stability of these liposomal systems during the atomization process using different kinds of nebulizers (air-jet, vibrating mesh, and ultrasonic). The study further explores the aerodynamic particle size distribution of the aerosol generated by the nebulizers. The nebulizer that demonstrated optimal stability and particle size was selected for more detailed investigation, including Andersen cascade impactor measurements, an assessment of the influence of flow rate and breathing profiles on aerosol particle size, and an in vitro deposition study on a realistic replica of the upper airways. The most suitable combination of a nebulizer and liposomal system was DPPC-PA-Chol nebulized by a Pari LC Sprint Star in terms of stability and particle size. The influence of the inspiration flow rate on the particle size was not very strong but was not negligible either (decrease of Dv50 by 1.34 μm with the flow rate increase from 8 to 60 L/min). A similar effect was observed for realistic transient inhalation. According to the in vitro deposition measurement, approximately 90% and 70% of the aerosol penetrated downstream of the trachea using the stationary flow rate and the realistic breathing profile, respectively. These data provide an image of the potential applicability of liposomal carrier systems for nebulizer therapy. Regional lung drug deposition is patient-specific; therefore, deposition results might vary for different airway geometries. However, deposition measurement with realistic boundary conditions (airway geometry, breathing profile) brings a more realistic image of the drug delivery by the selected technology. Our results show how much data from cascade impactor testing or estimates from the fine fraction concept differ from those of a more realistic case.

Recent Advances in Reversible Liquid Organic Hydrogen Carrier Systems: From Hydrogen Carriers to Catalysts.

Liquid organic hydrogen carriers (LOHCs) have gained significant attention for large-scale hydrogen storage due to their remarkable gravimetric hydrogen storage capacity (HSC) and compatibility with existing oil and gas transportation networks for long-distance transport. However, the practical application of reversible LOHC systems has been constrained by the intrinsic thermodynamic properties of hydrogen carriers and the performances of associated catalysts in the (de)hydrogenation cycles. To overcome these challenges, thermodynamically favored carriers, high-performance catalysts, and catalytic procedures need to be developed. Here, significant advances in recent years have been summarized, primarily centered on regular LOHC systems catalyzed by homogeneous and heterogeneous catalysts, including dehydrogenative aromatization of cycloalkanes to arenes and N-heterocyclics to N-heteroarenes, as well as reverse hydrogenation processes. Furthermore, with the development of metal complexes for dehydrogenative coupling, a new family of reversible LOHC systems based on alcohols is described that can release H2 under relatively mild conditions. Finally, views on the next steps and challenges in the field of LOHC technology are provided, emphasizing new resources for low-cost hydrogen carriers, high-performance catalysts, catalytic technologies, and application scenarios.

Self-enhanced nanohydrogel electrochemiluminescence biosensor based on CRISPR/Cas12a and gold platinum nanoparticles modification for high-sensitivity detection of Burkholderia pseudomallei

The simple, rapid, and accurate detection of highly lethal melioidosis is crucial for early clinical diagnosis and improving cure rates. Currently, due to time consumption, low sensitivity and detection rate the existing clinical detection methods cannot satisfy the needs of clinical diagnosis. Herein, a novel self-enhanced porous hydrogel material (Au@PEI-ABEI@Pt) for ultrasensitive ECL strategy of detection B. pseudomallei was report. The novel porous hydrogel material composed of PEI-ABEI porous hydrogel, gold nanoparticles (AuNP) and platinum nanoparticles (PtNP) have large specific surface area and porous structure, which not only fix more ABEI to realize self-enhanced ECL signal amplification, but also facilitate ion diffusion and efficient utilization of catalytic materials, realizing rapid electron transfer and zero-distance catalysis, significantly improving the initial signal of ECL sensor. Moreover, the most attractive aspect is that Au@PEI-ABEI@Pt hydrogels with good biocompatibility can achieve widespread application of CRISPR/Cas12a in solid-phase carriers without affecting the sensitivity, specificity and shearing activity of CRISPR/Cas12a. After coupling with the ECL system and CRISPR/Cas12a signal amplification strategy, the Au@PEI-ABEI@Pt can achieve an ultrasensitive ECL assay of B. pseudomallei with the LOD of 5 CFU mL−1 in complex samples, with high specificity and stability to effectively classify B. pseudomallei and other Gram-negative bacteria. This study shows that the developed porous hydrogel materials not only serve as an excellent ECL signal reporter to significantly improve the detection sensitivity of ECL biosensors, but also provide a new approach for the wide application of CRISPR/Cas systems in solid-phase carriers.

PNIPAm-Based pH and Thermoresponsive Copolymer Hydrogel for Hydrophobic and Hydrophilic Drug Delivery.

The regulated and targeted administration of hydrophobic and hydrophilic drugs is both promising and challenging in the field of drug delivery. Developing a hydrogel which is responsive to dual stimuli is considered a promising and exciting research area of study. In this work, melamine functionalized poly-N-isopropyl acrylamide-co-glycidyl methacrylate copolymer has been developed by copolymerizing glycidyl methacrylate (GMA) monomer with N-isopropyl acrylamide (NIPAm) and further functionalized with melamine units (pNIPAm-co-pGMA-Mela). The prepared pNIPAm-co-pGMA-Mela copolymer hydrogel was characterized using various characterization techniques, including 1H NMR, FTIR, SEM, zeta potential, and particle size analysis. A hydrophobic drug (ibuprofen, Ibu) and hydrophilic drug (5-fluorouracil, 5-Fu) were selected as model drugs. Dual pH and temperature stimuli-responsive drug release behavior of the pNIPAm-co-pGMA-Mela hydrogel was evaluated under different pH (pH 7.4 and 4.0) and temperature (25 °C, 37 °C, and 45 °C) conditions. Furthermore, the in vitro biocompatibility of the developed pNIPAm-co-pGMA-Mela copolymer hydrogel was determined on MDA-MB-231 cells. The pH and temperature-responsive drug delivery study results reveal that the pNIPAm-co-pGMA-Mela hydrogel system is responsive to both pH and temperature stimuli and exhibits about ~100% of Ibu and 5-Fu, respectively, released at pH 4.0/45 °C. Moreover, the MTT assay and hemocompatibility analysis results proved that the pNIPAm-co-pGMA-Mela hydrogel system is biocompatible and hemocompatible, suggesting that that it could be used for drug delivery applications. The experimental results suggest that the proposed pNIPAm-co-pGMA-Mela hydrogel system is responsive to dual pH and temperature stimuli, and could be a promising drug carrier system for both hydrophilic and hydrophobic drug delivery applications.

Romanian Wild-Growing Chelidonium majus-An Emerging Approach to a Potential Antimicrobial Engineering Carrier System Based on AuNPs: In Vitro Investigation and Evaluation.

Novel nanotechnology based on herbal products aspires to be a high-performing therapeutic platform. This study reports the development of an original engineering carrier system that jointly combines the pharmacological action of Chelidonium majus and AuNPs, with unique properties that ensure that the limitations imposed by low stability, toxicity, absorption, and targeted and prolonged release can be overcome. The metabolite profile of Romanian wild-grown Chelidonium majus contains a total of seventy-four phytochemicals belonging to eight secondary metabolite categories, including alkaloids, amino acids, phenolic acids, flavonoids, carotenoids, fatty acids, sterols, and miscellaneous others. In this study, various techniques (XRD, FTIR, SEM, DLS, and TG/DTG) were employed to investigate his new carrier system's morpho-structural and thermal properties. In vitro assays were conducted to evaluate the antioxidant potential and release profile. The results indicate 99.9% and 94.4% dissolution at different pH values for the CG-AuNPs carrier system and 93.5% and 85.26% for greater celandine at pH 4 and pH 7, respectively. Additionally, three in vitro antioxidant assays indicated an increase in antioxidant potential (flavonoid content 3.8%; FRAP assay 24.6%; and DPPH 24.4%) of the CG-AuNPs carrier system compared to the herb sample. The collective results reflect the system's promising perspective as a new efficient antimicrobial and anti-inflammatory candidate with versatile applications, ranging from target delivery systems, oral inflammation (periodontitis), and anti-age cosmetics to extending the shelf lives of products in the food industry.

GalNAc- or Mannose-PEG-Functionalized Polyplexes Enable Effective Lectin-Mediated DNA Delivery.

A cationic, dendrimer-like oligo(aminoamide) carrier with four-arm topology based on succinoyl tetraethylene pentamine and histidines, cysteines, and N-terminal azido-lysines was screened for plasmid DNA delivery on various cell lines. The incorporated azides allow modification with various shielding agents of different polyethylene glycol (PEG) lengths and/or different ligands by copper-free click reaction, either before or after polyplex formation. Prefunctionalization was found to be advantageous over postfunctionalization in terms of nanoparticle formation, stability, and efficacy. A length of 24 ethylene oxide repetition units and prefunctionalization of ≥50% of azides per carrier promoted optimal polyplex shielding. PEG shielding resulted in drastically reduced DNA transfer, which could be successfully restored by active lectin targeting via novel GalNAc or mannose ligands, enabling enhanced receptor-mediated endocytosis of the carrier system. The involvement of the asialoglycoprotein receptor (ASGPR) in the uptake of GalNAc-functionalized polyplexes was confirmed in the ASGPR-positive hepatocarcinoma cell lines HepG2 and Huh7. Mannose-modified polyplexes showed superior cellular uptake and transfection efficacy compared to unmodified and shielded polyplexes in mannose-receptor-expressing dendritic cell-like DC2.4 cells.

The field experiments results on remote determination of soil moisture portraits

The introduction of precision farming technologies into the practice of agricultural production is an urgent task, the solution of which would ensure the sustainable development of crop production, cost reduction and saving of water and other resources. The purpose of the work is to obtain and demonstrate the results of field experiments on remote determination of soil moisture portraits, temperature maps of the soil surface and relief maps conducted in the fields of the vegetable complex of CJSC «Gorodishche» in the Stupinsky district of the Moscow region using a complex of a new bipolarization microwave radiometer and a precision navigation receiver placed on a tractor. Field experiments on remote determination of portraits of soil moisture and surface temperature were carried out, as well as the microrelief parameter was determined and the features of the mutual correlation characteristics of various thematic maps were studied. Maps of portraits of humidity and temperature and surface topography of the soil were obtained. The electromagnetic compatibility of the microwave radiometer with «John Deere» tractor systems has been verified. Data have been prepared for entering into the database of radiometric measurements of soils. The work carried out will make it possible to clarify some parameters of the microwave radiometric system and its compatibility with the navigation receiver, radio modem and carrier systems. The analysis of the data obtained will make it possible to develop recommendations for optimizing technological processes and reclamation measures. The accumulation of a database of radiometric measurements will allow the further use of artificial intelligence technologies to refine the brightness-humidity conversion algorithms and the introduction of the developed equipment and algorithms into the technological processes of growing crops ensures the sustainable development of crop production technologies, increasing yields and obtaining additional profit by the agro-industrial complex.

Nano Lipid Carriers as a Promising Drug Delivery Carrier for Neurodegenerative Disorders - An Overview of Recent Advances.

The last few decades have seen a rise in the number of deaths caused by neurological disorders. The blood-brain barrier (BBB), which is very complex and has multiple mechanisms, makes drug delivery to the brain challenging for many scientists. Lipid nanoparticles (LNPs) such as nanoemulsions, solid-lipid nanoparticles, liposomes, and nano lipid carriers (NLCs) exhibit enhanced bioavailability and flexibility among these nanocarriers. NLCs are found to be very effective. In the last few decades, they have been a center of attraction for controlled drug delivery. According to the current global status of specific neurological disorders, out of all LNPs, NLC significantly reduces the cross-permeability of drugs through the BBB due to their peculiar properties. They offer a host of advantages over other carriers because of their biocompatibility, safety, non-toxicity, non-irritating behavior, stability, high encapsulation efficiency, high drug loading, high drug targeting, control of drug release, and ease in manufacturing. The biocompatible lipid matrix is ideally suited as a drug carrier system due to the nano-size range. For certain neurological conditions such as Parkinsonism, Alzheimer's, Epilepsy, Multiple sclerosis, and Brain cancer, we examined recent advances in NLCs to improve brain targeting of bioactive with special attention to formulation aspects and pharmacokinetic characteristics. This article also provides a brief overview of a critical approach for brain targeting, i.e., direct nose-to-brain drug delivery and some recent patents published on NLC".

Green Synthesis, Characterization, Encapsulation, and Measurement of the Release Potential of Novel Alkali Lignin Micro-/Submicron Particles.

The applicability of biopolymer micro-/nano- technology in human, veterinary medicine, pharmaceutical, and food technology is rapidly growing due to the great potential of biopolymer-based particles as effective carrier systems. The use of lignin as a basic heteropolymer biomatrix for the design of innovative micro-/submicron formulations allows the achievement of increased biocompatibility and offers various active functional groups presenting opportunities for customization of the physicochemical properties and bioactivities of the formulations for diverse applications. The aim of the present study was to develop a simple and ecofriendly methodology for the synthesis of lignin particles with micro- and submicron size; to evaluate their physicochemical, spectral, and structural characteristics; and to examine their capacity for encapsulation of biologically active molecules and potential for in vitro release of bioflavonoids in simulated gastrointestinal media. The presented methodologies apply cheap and green solvents; easy, straightforward, quick, and sensitive processes requiring little equipment, non-toxic substances, and simple methods for their characterization, the determination of encapsulation capacity towards the poorly water-soluble bioactive compounds morin and quercetin, and the in vitro release potential of the lignin matrices.

Ethosomes: Novel Vesicular Carriers for Effective Transdermal Delivery of Natural Therapeutics

Abstract: The topical delivery, being the most reliable route for drug administration, offers multiple advantages. The conventional topical dosage forms deliver a relatively higher amount of drug to achieve therapeutic action triggering hypersensitivity reactions accompanied by greasiness and staining issues. The advent of transdermal nanocarriers has waived off some of these limitations and assisted in achieving enhanced therapeutic efficacy with sustained release and minimal/no instances of systemic toxicity. The ethosome, one of the novel lipid carrier systems, has eased the administration of many hydrophilic and lipophilic drugs through the stratum corneum. It is a non-invasive drug carrier consisting of 45% ethanol, phospholipids, and non-ionic surfactants. The discovery of ethosomal technology has proved to be fruitful in delivering drugs with a wide range of polarity and other physicochemical parameters across skin. In this review, the ethosomal system has been explored for the delivery of complex phytoconstituents across the skin along with the key building material of ethosomes, associated mechanism of drug delivery, recent developments in ethosomes as a drug carrier, reported ethosomal formulations encapsulating various plant metabolites, conducted clinical trials and available ethosomal formulations for the delivery of phytocomponents across stratum corneum.

Recent advances in biopolymer based electrospun nanomaterials for drug delivery systems

AbstractDrug delivery systems, including liposomes, gels, prodrugs, and so forth, are used to enhance the tissue benefit of a pharmaceutical drug or conventional substance at a specific diseased site with little toxicological impact. Nanotechnology can be a rapidly developing multidisciplinary science that enables the production of polymers at the manometer scale for different medical applications. The use of biopolymers in drug delivery systems provides compatibility, biodegradability and low immunogenicity biologically. Large‐scale and smaller‐than‐expected medication particles can be delivered using biopolymers such as silk fibroins, collagen, gelatine, and others that are easily formed into suspensions. These drug carrier systems are functional at improving drug delivery and can be used in intranasal, transdermal, dental, and ocular delivery systems. This study discusses the latest developments in drug delivery methods based on nanomaterials, mainly using biopolymers like proteins and polysaccharides.

Adjuvant Novel Nanocarrier-Based Targeted Therapy for Lung Cancer.

Lung cancer has the lowest survival rate due to its late-stage diagnosis, poor prognosis, and intra-tumoral heterogeneity. These factors decrease the effectiveness of treatment. They release chemokines and cytokines from the tumor microenvironment (TME). To improve the effectiveness of treatment, researchers emphasize personalized adjuvant therapies along with conventional ones. Targeted chemotherapeutic drug delivery systems and specific pathway-blocking agents using nanocarriers are a few of them. This study explored the nanocarrier roles and strategies to improve the treatment profile's effectiveness by striving for TME. A biofunctionalized nanocarrier stimulates biosystem interaction, cellular uptake, immune system escape, and vascular changes for penetration into the TME. Inorganic metal compounds scavenge reactive oxygen species (ROS) through their photothermal effect. Stroma, hypoxia, pH, and immunity-modulating agents conjugated or modified nanocarriers co-administered with pathway-blocking or condition-modulating agents can regulate extracellular matrix (ECM), Cancer-associated fibroblasts (CAF),Tyro3, Axl, and Mertk receptors (TAM) regulation, regulatory T-cell (Treg) inhibition, and myeloid-derived suppressor cells (MDSC) inhibition. Again, biomimetic conjugation or the surface modification of nanocarriers using ligands can enhance active targeting efficacy by bypassing the TME. A carrier system with biofunctionalized inorganic metal compounds and organic compound complex-loaded drugs is convenient for NSCLC-targeted therapy.

Trends in the Incorporation of Antiseptics into Natural Polymer-Based Nanofibrous Mats.

Nanofibrous materials represent a very promising form of advanced carrier systems that can be used industrially, especially in regenerative medicine as highly functional bandages, or advanced wound dressings. By incorporation of antimicrobial additives directly into the structure of the nanofiber carrier, the functionality of the layer is upgraded, depending on the final requirement-bactericidal, bacteriostatic, antiseptic, or a generally antimicrobial effect. Such highly functional nanofibrous layers can be prepared mostly by electrospinning technology from both synthetic and natural polymers. The presence of a natural polymer in the composition is very advantageous. Especially in medical applications where, due to the presence of the material close to the human body, the healing process is more efficient and without the occurrence of an unwanted inflammatory response. However, converting natural polymers into nanofibrous form, with a homogeneously distributed and stable additive, is a great challenge. Thus, a combination of natural and synthetic materials is often used. This review clearly summarizes the issue of the incorporation and effectiveness of different types of antimicrobial substances, such as nanoparticles, antibiotics, common antiseptics, or substances of natural origin, into electrospun nanofibrous layers made of mostly natural polymer materials. A section describing the problematic aspects of antimicrobial polymers is also included.

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy.

The present study aims to develop a delivery system that can carry small interference RNA (siRNA) with small-molecule chemotherapeutic drugs, which can be used in cancer treatment. The drug delivery system combines the advantages of a therapeutic agent with two different mechanisms to ensure that it is used efficiently for cancer therapy. In this study, a nanostructured lipid carrier system was prepared, Docetaxel was loaded to these systems, and the Eph siRNA was adsorbed to the outer surface. In addition, DOTAP was added to the lipophilic phase to load a positive charge on the lipidic structure for interaction with the cells. Moreover, characterization, cytotoxicity, and transfection procedures were performed on the whole system. This candidate system was also compared to Taxotere, which is the first approved Docetaxel-containing drug on the market. Given the results, it was determined that the particle size of NLC-DTX was 165.3 ± 3.5 nm, the ζ potential value was 38.2 ± 1.7 mV, and the PDI was 0.187 ± 0.024. Entrapment efficacy of nanoparticles was found to be 92.89 ± 0.21%. It was determined that the lipidic system prepared in vitro release analyses were able to provide sustained release and exhibit cytotoxicity, even at doses lower than the dose used for Taxotere. The formulations prepared had a higher level of effect on cells when compared with pure DTX and Taxotere, but they also exhibited time-dependent cytotoxicity. It was also observed that the use of Eph siRNA together with the chemotherapeutic agent via formulation also contributed to this cell death. The results of the present study indicate that there is a promising carrier system in order to deliver hydrophilic nucleic acids, such as siRNA, together with lipophilic drugs in cancer treatment.

MaglevMotor: Design and optimisation of a novel hybrid linear actuator for 6 degrees of freedom rail‐passive Maglev carrier

AbstractA novel levitating hybrid linear actuator is proposed for magnetically levitated carrier systems. This hybrid linear actuator, “MaglevMotor”, is capable to levitate itself under the passive rail and thrusts itself in a single longitudinal direction. The proposed structure aims to reduce complexity by minimising the necessary number of components, resulting in simplified geometry, improved assembly convenience, and decreased manufacturing tolerances. The MaglevMotor is optimised in multi‐physics aspect. Optimisation objectives are maximising thrust force, minimising total mass and minimising mechanical deformation of yoke with constraints of a user defined magnetic flux density (B) in yoke and zero power condition for specific air gap value. The authors present pre‐optimisation studies, optimisation results and final MaglevMotor designs step by step. By utilising three of the MaglevMotors units, the carrier is able to achieve motion in six degrees of freedom. The carrier's performance targets, including a 0.2 G acceleration, a total mass of less than 10 kg, and a 5 mm levitation air gap, have been both attained and validated through corresponding experiments.

Bakuchiol nanoemulsion loaded electrospun nanofibers for the treatment of burn wounds.

The present work aims to develop and evaluate the wound healing potential of bakuchiol nanoemulsion loaded electrospun scaffolds. Since oxidative stress and microbial burden leads the burn wounds to become chronic and fatal to patients, a phytoconstituent, bakuchiol (BAK), was screened on the basis of antioxidant and antimicrobial potential which also defined its dose. Furthermore, BAK was incorporated into a nanoemulsion to enhance its therapeutic efficacy, reduce its dosage frequency, and maximize its stability. The present study is inclined towards the collaborative interaction of natural products and novel drug delivery systems to develop safe and therapeutically efficient systems for burn wound healing. The optimized nanoemulsion showed excellent antioxidant and antimicrobial potential against wound susceptible pathogens, i.e., Candida albicans and Methicillin-resistant Staphylococcus aureus which was further loaded into gelatin based hydrogel and nanofibrous scaffold system. The mesh structure of scaffolds was chosen as a suitable carrier system for wound healing process not only because it offers resemblance to skin's anatomy but is also capable of providing uniform distribution of wound biomarkers across the skin. The prepared nanofibers were assessed for their analgesic, anti-inflammatory, and wound healing potential which was observed to be significantly better than its gel formulation.

Conception of pH-sensitive calcium alginate/poly vinyl alcohol hydrogel beads for controlled oral curcumin delivery systems. Antibacterial and antioxidant properties

Curcumin, a bioactive compound derived from the rhizome of Curcuma longa, has gained widespread attention for its potential therapeutic properties, including anti-inflammatory, antioxidant and anticancer effects. However, its poor aqueous solubility, instability and limited bioavailability have hindered its clinical applications.New beads formulations based on sodium alginate biopolymer (SA) and poly vinyl alcohol (PVA) were successfully prepared and evaluated as a potential drug vehicle for extended release of curcumin (Cur). Pristine and curcumin loaded calcium alginate/poly vinyl alcohol beads (CA/PVA and CA/PVA/Cur) at different compositions of SA and PVA were prepared by an ionotropic gelation method of SA followed by two freeze-thawing (FT) cycles for further crosslinking of PVA. Characterization techniques, such as scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), UV–Visible spectroscopy, thermogravimetric analysis (TGA) and x-ray diffraction (XRD) were used to confirm the successful microencapsulation of curcumin within the CA/PVA microcapsules. Furthermore, the swelling of pristine beads, pH-sensitive properties and in vitro release studies of curcumin loaded beads were investigated at 37 °C in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). The effect of the polymer blend ratio, the encapsulation efficiency (EE %) of curcumin, the loading capacity (LC μg/mg), the sphericity factor (SF), the antioxidant activity of the elaborated beads and their antimicrobial properties against bacteria and fungi were just as much evaluated.The obtained results indicate that the swelling and the behavior of the developed beads were influenced by the pH of the test medium and the PVA content. The introduction of PVA into the SA matrix greatly enhanced the physicochemical properties, the encapsulation efficiency and the loading capacity of the elaborated microparticles. Results also suggested that the antioxidant activity of the loaded beads (CA/PVA/Cur) showed a higher DPPH radical scavenging activity while the bacterial and fungal strains proved sensitive to the different formulations used in the assay. Moreover, the important drug encapsulation efficiency and the sustainable drug release of these materials make them promising for the development of new drug carrier systems for colon targeting.

Thermosensitive In Situ Gel of Nanosized Apremilast: Development and Assessment for Rheumatoid Arthritis Treatment

Rheumatoid arthritis, in short called as RA, is a severe auto-immune condition characterized by thickening of the synovium joints, inflammation and soreness of joints, which subsequently destroys the articular structures. The drug used to treat RA requires the delivery of a formulation in intact form to synovial joints and release of a whole amount of medicine into synovial fluids. Apremilast is an anti-inflammatory drug used to treat arthritis, but its oral drug delivery is limited because of its low bioavailability and side effects. The nanoparticle-based in situ gel helps in prolonged formulation retention, which enables drug release within specific tissues such as cartilage and synovium. The purpose of this research is to formulate and assess the efficacy of a thermosensitive in situ gel of nanosized apremilast for managing RA. A total of nine apremilast- loaded nanoparticles in situ gels designated as F1–F9 were prepared with different ratios of Eudragit RSPO and polyvinyl alcohol using 25% w/v poloxamer 407 and poloxamer 188 as gelling agents. Among the various formulations, F5 showed a particle size of 119 nm, 80.8% EE, 27.54% DL, 37.5 ± 1.7∘C gelation temperature, 55 ± 1.0 second gelation time and 866 ± 13 cps viscosity, with a better in vitro drug release profile of 75.54% for 24 h by non-Fickian diffusion mechanism; thus, it was chosen as the most productive formulation. In an in vivo study in rats, the optimized formulation reduced inflammation at the test site. The developed nanoparticles in situ gel will be a novel carrier system for drugs used to treat RA.