Korsmeyer-Peppas Kinetic Model Research Articles

Antibacterial and Osteogenic Doxycycline Imprinted Bioglass Microspheres to Combat Bone Infection.

Currently, postoperative infection is a significant challenge in bone and dental surgical procedures, demanding the exploration of innovative approaches due to the prevalence of antibiotic-resistant bacteria. This study aims to develop a strategy for controlled and smart antibiotic release while accelerating osteogenesis to expedite bone healing. In this regard, temperature-responsive doxycycline (DOX) imprinted bioglass microspheres (BGMs) were synthesized. Following the formation of chitosan-modified BGMs, poly N-isopropylacrylamide (pNIPAm) was used for surface imprinting of DOX. The temperature-responsive molecularly imprinted polymers (MIPs) exhibited pH and temperature dual-responsive adsorption and controlled-release properties for DOX. The temperature-responsive MIP was optimized by investigating the molar ratio of N,N'-methylene bis(acrylamide) (MBA, the cross-linker) to NIPAm. Our results demonstrated that the MIPs showed superior adsorption capacity (96.85 mg/g at 35 °C, pH = 7) than nonimprinted polymers (NIPs) and manifested a favorable selectivity toward DOX. The adsorption behavior of DOX on the MIPs fit well with the Langmuir model and the pseudo-second-order kinetic model. Drug release studies demonstrated a controlled release of DOX due to imprinted cavities, which were fitted with the Korsmeyer-Peppas kinetic model. DOX-imprinted BGMs also revealed comparable antibacterial effects against Staphylococcus aureus and Escherichia coli to the DOX (control). In addition, MIPs promoted viability and osteogenic differentiation of MG63 osteoblast-like cells. Overall, the findings demonstrate the significant potential of DOX-imprinted BGMs for use in bone defects. Nonetheless, further in vitro investigations and subsequent in vivo experiments are warranted to advance this research.

Optimization, characterization and evaluation of sodium alginate nanoparticles for Ganoderic acid DM encapsulation: Inhibitory activity on tyrosinase activity and melanin formation

The efficacy of nanoencapsulation as a technology for enhancing the solubility of active substances has been demonstrated. In this particular investigation, Ganoderic acid DM (GA-DM) was encapsulated within sodium alginate nanoparticles (NPs) using the ionic crosslinking method. The confirmation of the successful loading of GA-DM was ascertained through the analysis of Fourier transform infrared spectrum (FTIR). Empirical evidence derived from the examination of scanning electron microscope (SEM) images, transmission electron microscope (TEM) images, atomic force microscope (AFM) images, and dynamic light scattering (DLS) demonstrated a regular distribution and spherical morphology, with an average particle size of approximately 133 nm. The investigation yielded an encapsulation efficiency of 95.27 ± 0.11 % and a drug loading efficiency of 21.17 ± 0.02 % for the prepared sample. The release kinetics of SGPN was fitted with the Korsmeyer-Peppas kinetic model corresponding to diffusion-controlled release. The incorporation of GA-DM into sodium alginate nanocarriers exhibited a mitigating effect on the cytotoxicity of HaCat and B16, while also demonstrating inhibitory properties against tyrosinase activity and melanin formation.

Designing of tragacanth gum-poly(2-(methacryloyloxy) ethyl] dimethyl-(3-sulfopropyl) ammonium hydroxide) and poly(acrylamide) based hydrogels for drug delivery and wound dressing applications

Bioactive tragacanth gum (TG) was functionalized by covalent crosslinking of poly[2-(methacryloyloxy) ethyl] dimethyl-(3-sulfopropyl) ammonium hydroxide (PMEDSAH) to design network structure in form of hydrogel wound dressings (HWD). These copolymers were encapsulated with antibiotic drug vancomycin to enhance wound healing potential of the dressings. The copolymers were characterized by SEM, AFM, FTIR, 13C NMR, XRD, and TGA-DSC analysis. SEM demonstrated uneven heterogeneous morphology and AFM revealed rough surface of copolymer. Inclusion of synthetic component into HD was confirmed by FTIR and 13C NMR. Hydrogel dressings absorbed 8.49 ​± ​1.03 ​g/g simulated wound fluid and exhibited non-hemolytic (3.7 ​± ​0.02 % hemolytic potential) and antioxidant (37.42 ​± ​1.54 ​% free radical scavenging in DPPH assay) properties. Polymers required 35.0 ​± ​5.0 ​mN detachment force to get it detach from the mucosal surface during mucoadhesive test. Tensile strength was found to be 1.88 ​± ​0.13 ​N/mm2 during mechanical stability test. Hydrogel dressings were permeable to O2/H2O and impermeable to microbes. Release of drug vancomycin occurred through non-Fickian diffusion mechanism and release profile was best described by Korsmeyer-Peppas kinetic model. Overall, these results revealed that these hydrogels could be explored as materials for hydrogel wound dressings.

Kinetic analysis of aroma compound release from Citrus aurantium essential oil-casein-phospholipid-nanocomposites

In this study, Citrus aurantium essential oil encapsulated in casein-phospholipid nanocomposites (CAEO–CS–PL-NCs) was prepared and evaluated for controlled-release capacity of aroma compounds. The particle size of the nanocomposites was strongly influenced by the phospholipid concentration in the nanocomposites. The Avrami and Korsmeyer-Peppas kinetic models were used to analyze the aroma release kinetics of freeze-dried CAEO–CS–PL-NCs (FD-CAEO–CS–PL-NCs) at different temperatures and relative humidities. FD-CAEO–CS–PL-NCs were stored for various times with tea leaves to evaluate their potential for making scented teas. The Avrami kinetic analysis indicated that the release of aroma compounds from FD-CAEO–CS–PL-NCs conformed to diffusion-limited, or first-order kinetics, depending on the temperature and relative humidity. The Korsmeyer-Peppas kinetic analysis indicated that the release of aroma compounds from FD-CAEO–CS–PL-NCs involved three release mechanisms, Fickian diffusion, non-Fickian diffusion and the erosive mechanism. The release mechanism involved varied depending on different conditions and different aroma compounds, and at low temperature and relative humidity effective controlled release of aroma compounds was achieved, resulting from intermolecular interactions with the casein micelles. FD-CAEO–CS–PL-NCs showed significantly sensory scores increasing effect of scented tea. The findings will facilitate future developments in the formulation of scented teas, by incorporating aromatic essential oils from fruits and flowers, in the form of essential oil-casein-phospholipid nanocomposites.

Polydimethylsiloxane Organic-Inorganic Composite Drug Reservoir with Gliclazide.

A novel organic-inorganic gliclazide-loaded composite bead was developed by an ionic gelation process using acidified CaCl2, chitosan and tetraethylorthosilicate (TEOS) as a crosslinker. The beads were manufactured by crosslinking an inorganic silicone elastomer (-OH terminated polydimethylsiloxane, PDMS) with TEOS at different ratios before grafting onto an organic backbone (Na-alginate) using a 32 factorial experimental design. Gliclazide's encapsulation efficiency (EE%) and drug release over 8 h (% DR 8 h) were set as dependent responses for the optimisation of a pharmaceutical formula (herein referred to as 'G op') by response surface methodology. EE % and %DR 8 h of G op were 93.48% ± 0.19 and 70.29% ± 0.18, respectively. G op exhibited a controlled release of gliclazide that follows the Korsmeyer-Peppas kinetic model (R2 = 0.95) with super case II transport and pH-dependent swelling behaviour. In vitro testing of G op showed 92.17% ± 1.18 cell viability upon testing on C2C12 myoblasts, indicating the compatibility of this novel biomaterial platform with skeletal muscle drug delivery.

PH-responsive release of ciprofloxacin hydrochloride from micro-, nano-, and functionalized nanocellulose

This research evaluated pH-responsive release characteristics for the drug (ciprofloxacin hydrochloride) from micro-, nano-, and functionalized cellulose forms. Nanocrystalline cellulose (NCC) was prepared from microcrystalline cellulose (MCC) by sulfuric acid hydrolysis. The aldehyde (–CHO) groups were introduced at the carbon-2 (C-2) and carbon-3 (C-3) positions of glucose moiety of the cellulose network by selective oxidation to form di-aldehyde nanocellulose (DANC). The conversion was validated by chemical, spectroscopic, morphological, and crystallographic analysis. Drug binding capacity (mg/g) of DANC was higher (200.8 mg/g) compared to NCC (138.3 mg/g) and MCC (120.2 mg/g), respectively. The increase in pH from 2.5 to 8.5 enhanced drug release for all the excipients. At pH 2.5, slow release of the drugs was observed. In 6 h, DANC released 44.7 % of the loaded drug at pH 2.5. However, drug release reached equilibrium (84.8 % of loaded drug) within 10 min at pH 8.5. The release kinetics at acidic pH were validated using zero-order, first-order, Higuchi, and Korsmeyer-Peppas kinetics models. Higuchi and Korsmeyer–Peppas' kinetic models interpreted drug release phenomena with a good fit. This implies that diffusion, dissolution, swelling, and slight erosion contribute to drug release. The results suggest that selective functionalization can be applied to cellulose for its potential applications in pH-responsive drug delivery, and therefore, the functionalized cellulose deserves immediate attention.

Evaluating physiochemical characteristics of tragacanth gum-gelatin network hydrogels designed through graft copolymerization technique

The present work deals with the evaluation of the physiochemical and biomedical properties of hydrogels derived from copolymerization of tragacanth gum (TG) and gelatin for use in drug delivery (DD) applications. Copolymers were characterized by field emission-scanning electron micrographs (FE-SEM), electron dispersion X-ray analysis (EDAX), Fourier transform infrared spectroscopy (FTIR), 13C-nuclear magnetic resonance (NMR), thermo-gravimetric analysis (TGA), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. FE-SEM revealed heterogeneous morphology and XRD analysis demonstrated an amorphous nature with short range pattern of polymer chains within the copolymers. The release of the drug ofloxacin occurred through a non-Fickian diffusion mechanism and the release profile was best described by the Korsmeyer-Peppas kinetic model. The hydrogels exhibited blood compatibility and demonstrated a thrombogenicity value of 75.63 ± 1.98 % during polymer-blood interactions. Polymers revealed mucoadhesive character during polymer-mucous membrane interactions and required 119 ± 8.54 mN detachment forces to detach from the biological membrane. The copolymers illustrated the antioxidant properties as evidenced by 2, 2′-diphenylpicrylhydrazyl (DPPH) assay which demonstrated a 65.71 ± 3.68 % free radical inhibition. Swelling properties analysis demonstrated that by change in monomer and cross linker content during the reaction increased the crosslinking of the network. These results suggest that the pore size of network hydrogels could be controlled as per the requirement of DD systems. The copolymers were prepared at optimized reaction conditions using 14.54 × 10−1 molL−1 of acrylic acid monomer and 25.0 × 10−3 molL−1 of crosslinker NNMBA. The optimized hydrogels exhibited a crosslink density of 2.227 × 10−4 molcm−3 and a mesh size of 7.966 nm. Additionally, the molecular weight between two neighboring crosslinks in the hydrogels was determined to be 5332.209 gmol−1.The results indicated that the combination of protein-polysaccharide has led to the development of hydrogels suitable for potential applications in sustained drug delivery.

NIR-triggered drug delivery system based on tungsten disulfide nanosheets coated pH/temperature responsive polymer for controlled delivery of palbociclib: Release kinetics models

BackgroundPolymers that respond to changes in ambient conditions, such as physiological pH and temperature, have garnered increasing interest in the realm of drug delivery systems. In this study, a novel pH and temperature dual-responsive carrier was prepared for palbociclib delivery. MethodsThe tungsten disulfide nanosheets were functionalized with allyl glycidyl ether, allyl alcohol, and N-vinylcaprolactam, and then grafted with 2, 3-diaminopyridine. The in-vitro drug release was studied in simulated cancer (pH=5.6) and blood (pH=7.4) fluids at different temperatures. Significant FindingsThe in-vitro drug release test showed better release behavior at high temperatures in simulated cancer fluid compared to lower temperatures in simulated blood fluid, releasing about 87.53% of the entrapped drug within 6 h at 45 °C in simulated cancer fluid. The drug release shown the best fitting with the Korsmeyer-Peppas kinetic model. When the near-infrared laser irradiation was applied for 15 min, the drug release from the nanocarrier was three times higher than that without the laser irradiation. The maximum sorption capacity of the drug was achieved at approximately 79.04 mg g−1 at pH=8 for 45 min at 25 °C. The sorption procedure was found to follow the Langmuir isotherm and a pseudo-2nd-order kinetic model quite well.

3D-Printed Chitosan-Based Scaffolds with Scutellariae baicalensis Extract for Dental Applications.

The plant material Scutellariae baicalensis radix, which is rich in flavones (baicalin), possesses antibacterial, antifungal, antioxidant, and anti-inflammatory properties. This work aimed to develop a 3D-printed chitosan-based hydrogel rich in Scutellariae baicalensis extract as an innovative approach for the personalized treatment of periodontal diseases. Chitosan-based hydrogels were prepared, and the printability of the prepared hydrogels was determined. The hydrogel with 2.5% w/v of high molecular-weight chitosan (CS), 2% w/v gelatin (Gel), and 10% w/w of extract (Ex) presented the best printability, producing smooth and uniform scaffolds. It was proved that the CS/Gel/Ex hydrogel was stabilized by hydrogen bonds and remained in amorphous dispersion in the 3D-printed structures (confirmed by ATR-FTIR and XRPD). Due to the amorphization of the active substance, a significant increase in the release of baicalin in vitro was observed. It was demonstrated that there was an initial burst release and a continuous release profile (n = 3). Higuchi kinetic was the most likely baicalin release kinetic. The second fit, the Korsmeyer-Peppas kinetics model, showed coupled diffusion of the active ingredient in the hydrated matrix and polymer relaxation regulated release, with n values ranging from 0.45 to 0.89. The anti-inflammatory properties of 3D-printed scaffolds were assessed as the ability to inhibit the activity of the hyaluronidase enzyme. Activity was assessed as IC50 = 63.57 ± 4.98 mg hydrogel/mL (n = 6). Cytotoxicity tests demonstrated the biocompatibility of the material. After 24 h of exposure to the 2.5CS/2Gel/10Ex scaffold, fibroblasts migrated toward the scratch, closed the "wound" by 97.1%, and significantly accelerated the wound healing process. The results render the 3D-printed CS/Gel/extract scaffolds as potential candidates for treating periodontal diseases.

Effect of cross-linking agents on sodium alginate-based quercetin beads: physicochemical properties and controlled release kinetics

Alginates have a variety of biological, physical, and chemical properties that can be modified to meet a specific purpose. Ionic crosslinking is an easy method of alginate modification. This study examined the ionic crosslinking agents (Ca2+, Ba2+, Mg2+) on swelling ratio, water solubility, and % sol-gel fraction of modified alginate. The performance of the modified alginate used to encapsulate quercetin, such as % encapsulation efficiency (% EE), % release of quercetin, and quercetin release kinetics were examined. The variables used in this study were the concentration of alginate and ionic crosslinking agents. At 3% alginate concentration and 0.3 M, ionic crosslinking agent concentration positively correlated with swelling ratio and water solubility. In contrast, the ionic crosslinking agent that positively correlates to the % sol-gel fraction is Ca2+. Encapsulation of quercetin using a crosslinking agent with ion Ca2+ and 2.5 ppm of quercetin concentration showed the highest % EE of 87%. Modified alginate induced quercetin release from beads at pH 1.4 and 7. The release of quercetin from modified alginate followed the Korsmeyer-Peppas kinetic model (R2 >0.99). The results of the FTIR analysis confirmed that a new peak at 1271 cm-1 was C-O-C characteristic of quercetin, indicating quercetin loaded on encapsulated beads. The morphological analysis showed that the surface of modified alginate (Ca-Ag/Ba-Ag/Mg-Ag) was rough and porous. This study established that modified alginate using different ionic crosslinking agents can be a suitable matrix for encapsulating quercetin.

The Fabrication, Drug Loading, and Release Behavior of Porous Mannitol.

Porous materials are widely used as an effective strategy for the solubilization of insoluble drugs. In order to improve the solubility and bioavailability of low water-solubility drugs, it is necessary to prepare porous materials. Mannitol is one of the most popular excipients in food and drug formulations. In this study, porous mannitol was investigated as a drug carrier for low water solubility drugs. Its fabrication, drug loading, and drug release mechanisms were investigated. Porous mannitol was fabricated using the co-spray-antisolvent process and utilizing polyvinylpyrrolidone K30 (PVP K30) as the template agent. Porous mannitol particles were prepared by changing the proportion of the template agent, spraying the particles with mannitol, and eluting with ethanol in order to regulate their pore structure. In subsequent studies, porous mannitol morphology and characteristics were determined systematically. Furthermore, curcumin and ibuprofen, two poorly water-soluble drugs, were loaded into porous mannitol, and their release profiles were analyzed. The results of the study indicated that porous mannitol can be prepared using PVP K30 as a template and that the amount of template agent can be adjusted in order to control the structure of the porous mannitol. When the template agent was added in amounts of 1%, 3%, and 5%, the mannitol pore size increased by 167.80%, 95.16%, and 163.98%, respectively, compared to raw mannitol. Molecular docking revealed that mannitol and drugs are adsorbents and adhere to each other by force interaction. The cumulative dissolution of curcumin and ibuprofen-loaded porous mannitol reached 69% and 70%, respectively. The release mechanism of curcumin and ibuprofen from drug-loaded mannitol was suitable for the Korsmeyer-Peppas kinetic model. In summary, the co-spray-antisolvent method proved effective in fabricating porous materials rapidly, and porous mannitol had a remarkable effect on drug solubilization. The results obtained are conducive to the development of porous materials.

Kaempferia parviflora Extracellular Vesicle Loaded with Clarithromycin for the Treatment of Helicobacter pylori Infection.

Kaempferia parviflora extracellular vesicles (KPEVs) have been reported as promising nanovesicles for drug delivery. This study aimed to load clarithromycin (CLA) into KPEVs (KPEVS-CLA) and determine the physical properties, drug-releasing efficiency, gastric cell uptake, anti-H. pylori activities, and anti-inflammatory responses in comparison with free CLA and KPEVs. The size and surface charge of KPEVs-CLA were evaluated using dynamic light scattering and visualized using a transmission electron microscope. The encapsulation efficiency (EE%), loading capacity (LC%), and drug release of KPEVs-CLA were examined using HPLC. Anti-H. pylori growth and anti-adhesion were evaluated. IL-8 gene expression, NF-κB signaling proteins, and anti-inflammatory profiles were examined using qRT-PCR, Western blotting, and Bio-Plex immunoassay, respectively. Anti-chemotaxis was then examined using a Transwell assay. KPEVs-CLA were intact and showed a negative surface charge similar to that of KPEVs. However, slightly enlarged KPEVs were observed. CLA was successfully loaded into KPEVs with EE of 93.45% ± 2.43%, LC of 9.3% ± 3.02%. CLA release in the PBS and gastric mimic buffer with Fickian diffusion (n ≤ 0.43) according to Korsmeyer-Peppas kinetic model (R2=0.98). KPEVs-CLA was localized in the gastric cells' cytoplasm and perinuclear region. Anti-H. pylori growth and anti-H. pylori adhesion of KPEVs-CLA were compared with those of free CLA with no cytotoxicity to adenocarcinoma gastric cells. KPEVs-CLA significantly reduced IL-8, G-CSF, MIP-1α, and MIP-1β levels. Moreover, KPEVs-CLA showed a superior effect over CLA in reducing G-CSF, MIP-1α, and NF-κB phosphorylation and monocyte chemotactic activities. KPEVs serve as potential carriers of CLA. They exhibited a higher efficiency in inhibiting gastric cell inflammation mediated by H. pylori infection than free CLA. The establishment of KPEVs-CLA as a nanodrug delivery model for H. pylori treatment could be applied to other plant extracellular vesicles or loaded with other cancer drugs for gastric cancer treatment.

Smart mucoadhesive 3-D network hydrogels for use in localized impregnated anticancer drug delivery

Recently, bioactive dietary fibers (DFs) have been explored for various benefits to human health because of their therapeutic activities. Role of DF psyllium (arabinoxylan (Ax)) has been established for curing colon cancer. Herein, methotrexate (MXT), an anti-neoplastic agent, was impregnated into network hydrogels developed from DF psyllium, through graft copolymerization reactions for its sustained colon-specific drug delivery (DD). Copolymers were characterized through SEM, AFM, FTIR, C13-NMR and TGA analysis. Smart hydrogels demonstrated antioxidant (39.40 ± 0.78% free radical scavenging in the DPPH assay), biocompatible (1.16 ± 0.22% hemolysis value in blood-polymer interactions), and mucoadhesive (7.0 ± 0.1 mN detachment force from the mucous membrane) properties. Sustained diffusion of MXT in colonic conditions occurred with a Fickian mechanism, and release profile obeyed the Korsmeyer-Peppas kinetic model. Overall, findings suggested the suitability of DF psyllium-based DD carriers for colon with enhanced potential.

GELLAN GUM- AND PECTIN-MAGNETIC GRAPHENE OXIDE NANOCARRIERS LOADED WITH CINNAMALDEHYDE FOR MOSQUITO LARVAE CONTROL

Magnetic nanoparticles have evolved over the last few decades as nanocarriers in drug delivery systems for hydrophobic drugs. Here, novel gellan gum magnetic graphene oxide (GG-GO-Fe3O4) and pectin magnetic graphene oxide (PEC-GO-Fe3O4) nanocomposites were prepared to carry cinnamaldehyde to control Aedes aegypti larvae. Fourier transform infrared (FTIR) spectroscopy, field emission scanning electron microscopy (FESEM) and scanning transmission electron microscopy (STEM) were employed to investigate the physicochemical characteristics of the nanocomposites. Entrapment efficiencies and loading capacities of nanocomposites on cinnamaldehyde were examined using ultraviolet-visible analysis. The successful cinnamaldehyde loading was confirmed by C-C and C-O stretches in the FTIR spectra. Results of in vitro release study showed the capabilities of GG-GO-Fe3O4 as a drug carrier system, extending the cinnamaldehyde release period for 36 h, and the release profiles for both nanocomposites fit the Korsmeyer-Peppas kinetic model with correlation coefficient (R2) values of over 0.9809. The cinnamaldehyde-loaded GG-GO-Fe3O4 nanocomposites induced 68% mortality after 72 h of exposure, with LC50 values ranging from 2.0488 and 15.9121 mg/L. The conjugation of GO-Fe3O4 with biopolymers improved the water solubility of cinnamaldehyde by 36.41 to 62.83 times vs. free cinnamaldehyde in water (1.42 mg/mL). Overall, these results are beneficial for researchers dealing with mosquito control and prevention.

Designing aloe vera-sterculia gum based copolymeric hydrogel dressings for drug delivery

Herein the present work, aloe vera (AV) and sterculia gum (SG) based polymer network hydrogels have been designed for use in wound dressing and drug delivery (DD) applications. The hydrogels were prepared by graft copolymerization reaction of poly(2-(methacryloyloxy) ethyl trimethylammonium chloride) [poly (METAC)] onto AV and SG. Polymers were characterized by FESEM, SEM, EDS, AFM, C13 NMR, FTIR, XRD and TGA-DTG analysis. Swelling, drug delivery and biomedical properties of dressings have been evaluated. Sustained diffusion of moxifloxacin drug from dressings exhibited a non-Fickian diffusion mechanism and the release profile was best fitted in the Korsmeyer-Peppas kinetic model. Various interactions of polymers with blood and goat membranes revealed the biocompatible and mucoadhesive nature of the dressings. Hydrogel dressings were found permeable to O2 and water vapour and impermeable to microbes. Overall, these properties revealed that these hydrogels could act as suitable materials for design of wound dressings. Furthermore, antioxidant properties of AV, wound healing characteristic of SG, antibacterial properties of poly(METAC) and encapsulated moxifloxacin drug in hydrogel dressings may enhance the wound healing potential of hydrogel wound dressings (HWD).

Synthesis of cationic gel-coated hydroxyapatite composites for pH- and thermo-responsive drug delivery in tumor microenvironments

Nanomedicine has gained a significant attention in biomedical science and engineering. It involves design and applications of engineered composites for targeted delivery, diagnostics, imaging, and therapeutic efficacy assessment. Herein, multi-stimuli responsive doxorubicin (DOX) loaded composites were prepared and used for controlled anticancer drug release for antitumor efficacy. In this study, we synthesized the HAp@PP composites by coating Pluronic® P123 and branched polyethylenimine (PP nanogel) on hydroxyapatite (HAp) particles. In-vitro cytotoxicity tests emphasized that HAp@PP composites presented a cell viability of more than 80 % before DOX loading. The fabricated HAp@PP–DOX composites indicated a pH-/thermo-reliant DOX release under tumor microenvironment conditions. Furthermore, the Korsmeyer-Peppas kinetic model yielded the best fit for the release of DOX under the conditions studied. The in-vitro assessment revealed that HAp@PP–DOX had a higher effect that free DOX, with a cell viability less than 25 % and 15 %, respectively, at a DOX concentration of 50 μg/mL. In the context of cancer treatment, the composites have the potential to be more effective than traditional chemotherapy by delivering drugs efficiently.

Preparation of PMMA-Based Temperature/pH Responsive Nanoparticles Encapsulating 5-Fluorouracil and Methotrexate In Situ by One-Pot Dispersion Photopolymerization.

In order to achieve long-term and controllable release of anti-tumor drugs at specific sites, temperature/pH responsive nanoparticles encapsulating 5-fluorouracil and methotrexate in situ are prepared through dispersion photopolymerization under green LED irradiation. The physicochemical properties of nanoparticles are characterized by scanning electron microscopy, Fourier transform infrared, dynamic light scattering, thermogravimetric/differential scanning calorimetry, and X-ray diffraction. In vitro drug release at different temperatures and pH values is examined to ascertain the release pattern of two drugs, which can be well described by Korsmeyer-Peppas kinetic model. The cytotoxicity evaluation illustrates that the tumor cells could be more effectively killed by the drug-loaded nanoparticles, and the improved therapeutic effect is attributed to the controllable and sustainable drug release as well as the enhanced cellular uptake. The blood safety and good biocompatibility of nanoparticles are further confirmed by hemolysis assay, indicating the prepared nanoparticles are potential candidates for effective tumor treatment.

A green approach for preparation of chitosan/hydroxyapatite/graphitic carbon nitride hydrogel nanocomposite for improved 5-FU delivery

Reducing the side effects of cancer treatment methods is an important issue. The loading efficiency and sustained release of 5-Fluorouracil (5-FU) have been significantly improved by creating a new method. A nanocarrier with pH sensitivity has been developed through the w/o/w emulsification method. It is loaded with 5-FU and comprises of chitosan (CS), hydroxyapatite (HAp), and graphitic carbon nitride (g-C3N4). g-C3N4 nanosheets were incorporated in CS/HAp hydrogel to improve the entrapment and loading efficiency. Drug loading efficiency and entrapment efficiency reached 48 % and 87 %, respectively, and the FTIR and XRD tests verified evidence of the formation of chemical bonds among the drug and nanocarrier. Structural analysis was done using FE-SEM. DLS and zeta potential were employed to obtain average size distribution and surface charge. The release profile of 5-FU in various conditions shows the nanoparticles' pH dependence, and the nanocomposite's controlled release is consistent with the Korsmeyer-Peppas kinetic model. Cell apoptosis and cytotoxicity were evaluated in vitro using flow cytometry and MTT analysis. The biocompatibility of CS/HAp/g-C3N4 against MCF-7 cells was shown by the MTT method and confirmed by flow cytometry. CS/HAp/g-C3N4@5-FU led to the highest apoptosis rate in MCF-7 cells, indicating the nanocarrier's efficiency in killing cancer cells. These data indicate that the designed CS/HAp/g-C3N4@5-FU can be a potential drug for treating cancer cells.

Optimization of Citrus aurantifolia peel extract encapsulation in alginate-gelatin hydrogel microbeads for antibacterial wound dressing applications

The extract of Citrus aurantifolia peel has been encapsulated into alginate-gelatin-based microbeads using an external ionotropic gelation method to apply antibacterial wound dressings. Such variables, like the alginate-gelatin ratio, extract quantity, and CaCl2 cross-linkers, were optimized to produce a good yield, well-distributed size, and encapsulation efficiency. Antibacterial efficacy was tested against both S. aureus and E. coli. Optimal microbead characteristics were obtained at alginate:gelatin concentration ratio of 1.75 %:0.25 % (w/v), with 15 mg of extract and a 2 % CaCl2 cross-linker. These conditions resulted in the microbeads with 82.94 ± 1.056 % yield, particle sizes between 1.080–1.244 µm, and encapsulation efficiency of 79.127 ± 0.186 %. The microbeads exhibited an almost spherical morphology with a slightly rough surface. The extract release mechanism out of the microbeads was governed by both diffusion and erosion of the shells following the Korsmeyer-Peppas kinetic model (k = 1.014 ± 0.007/min). Upon immobilizing the microbeads on gauze, an add-on percentage of 73.98 % was observed. Moreover, the gauze-immobilized microbeads inhibited S. aureus and E. coli growth with inhibition zones of 11±1.48 and 12.56±4.89 mm, respectively. In conclusion, the antibacterial alginate-gelatin-based microbeads have demonstrated optimal characteristics and exhibited effective inhibition against S. aureus and E. coli, showcasing their potential as antibacterial wound dressings.

Formulation of Pharmaceutical Tablets Containing β-Cyclodextrin-4-Methyl-Umbelliferone (Hymecromone) Inclusion Complexes and Study of the Dissolution Kinetics

The present study focuses on the synthesis of the natural product 4-methyl-umbelliferone (4-MU, hymecromone), the preparation, characterization, and biological activity evaluation of 4-MU inclusion complexes with β-cyclodextrin (β-CD), as well as their incorporation into pharmaceutical tablets. The inclusion complexes (ICs) were characterized using DLS, SEM, TGA as well as FT-IR, UV-vis, and NMR spectroscopies. The release profile of 4-MU from the β-CD-4-MU ICs was studied in three different pH: 1.2 (aqueous hydrochloric acid), 7.4, and 6.8 (phosphate-buffered solutions), to simulate the stomach, physiological, and intestine pH, respectively. The ICs were incorporated in pharmaceutical tablets which were prepared by direct compression and were characterized for their mechanical properties. The optimal composition of 4-MU as the active pharmaceutical ingredient (API) and excipients was determined using design of experiment (DoE), and the dissolution studies were performed at pH 1.2 at 37 ± 0.5 °C. The sustained release profile of the pharmaceutical tablets showed a delayed burst release effect at 20 min (20% drug release) compared to that of the ICs at the same time interval (70%). The results indicated that the kinetic model describing the release profile of 4-MU from the ICs and tablets is the Higuchi model, while the release mechanism is swelling and diffusion, as was indicated by the Korsmeyer–Peppas kinetic model. The optimization analysis revealed that the optimum composition contains x1 = 150.95 mg of β-CD-4-MU ICs, x2 = 82.65 mg of microcrystalline cellulose, and x3 = 12.40 mg of calcium phosphate.