Carriers For Drug Delivery Applications Research Articles

Pseudoternary Phase Diagram and Antibacterial Activity of Microemulsion-Based Citronella Oil

Citronella oil (CTO) is extracted from citronella leaves by maceration or steam distillation process, which has antibacterial and insect-repellent activities. However, the use of CTO is limited and requires modification in other formulations, such as microemulsion (ME), to increase its bioactivities. ME consists of oil, water, surfactant and/or cosurfactant and is commonly applied in food and beverages, cosmetics, and carrier for drug delivery applications. CTO was used as the oil phase for ME with nonionic surfactant and ethanol as a cosurfactant for lowering interfacial tension between oil and water phase. Subsequent observations regarding stability and antibacterial tests were carried out on ME formulations with surfactant/cosurfactant mixture of 2 due to its largest ME area. A hydrodynamic diameter analysis was also carried out to see the stability of the ME within a period of 50 d. ME with 10% CTO, 30% surfactant mixture, and 60% water showed the best formulation observed from the consistent hydrodynamic diameter measurement. In addition, ME with different formulations could inhibit the growth of Escherichia coli and Staphylococcus aureus by more than 90%. From this research, CTO-based ME potentially improve and develop drug carrier applications, especially via topical route.

Investigation of Levan-Derived Nanoparticles of Dolutegravir: A Promising Approach for the Delivery of Anti-HIV Drug as Milk Admixture

Nanoparticles composed of Levan and Dolutegravir (DTG) have been successfully synthesized using a spray drying procedure specifically designed for milk/food admixture applications. Levan, obtained from the microorganism Bacillus subtilis, was thoroughly characterized using MALDI-TOF and solid-state NMR technique to confirm its properties. In the present study, this isolated Levan was utilized as a carrier for drug delivery applications. The optimized spray-dried nanoparticles exhibited a smooth surface morphology with particle sizes ranging from 195 to 329 nm. In the in-vitro drug release experiments conducted in water media, the spray-dried nanoparticles showed 100 % release, whereas the unprocessed drug exhibited only 50 % release at the end of 24 h. Notably, the drug release in milk was comparable to that in plain media, indicating the compatibility. The improved dissolution rate observed for the nanoparticles could be attributed to the solid-state conversion (confirmed by XRD analysis) of DTG from its crystalline to amorphous state. The stability of the drug was verified using Fourier Transform Infra-Red Spectroscopy and Thermogravimetry-Differential Scanning Calorimetry analysis. To evaluate the in-vitro cellular toxicity, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was conducted, which revealed the CC50 value of 88.88 ± 5.10 µg/mL for unprocessed DTG and 101.08 ± 37.37 µg/mL for DTG nanoparticles. These results indicated that the toxicity of the nanoparticles was comparable to the unprocessed drug. Furthermore, the anti-HIV activity of the nanoparticles in human cell lines was found to be similar to that of the pure drug, emphasizing the therapeutic efficacy of DTG in combating HIV.

Chemical Modification of Aluminum Nitride Nanotubes (AlNNT) using-OH, C=O, R-SH functional groups: First Principle's study

Based on the First Principle's density functional theory, we have investigated the structural and electronic properties of pristine aluminum nitride nanotube (AlNNT), which is chemically modified with various biologically available functional groups such as hydroxyl (-OH), thiol (R-SH) and carbonyl (C=O). The structural stability is examined through minimum total energy difference and binding energy by repeated random perturbation. Structural analysis shows that functional groups were found to induce sp3 transition in AlNNT as reflected in the p character. Our finding shows that, (5, 5) AlNNT possesses a wide band gap semiconducting behavior with an energy bandgap of 3.27 eV. Chemical functionalization reduces the band gap of armchair AlNNT (5, 5). The chemical potential of the pristine AlNNT is found to be -3.94 eV. Chemical potential analysis shows a blue shift for the bio complex system with respect to the pristine system. The ionic character and Gibbs free energy of solvation determine the structure's solubility in aqueous media. Chemical tuning of AlNNT with functional groups induces polar covalent characteristics which makes them to be used as possible carriers for drug delivery applications.

Theoretical Analysis of Riboflavin Adsorption on Hexagonal Boron Nitride for Drug Delivery Applications: Unveiling the Influence of Point Defects.

This research delves into the intriguing realm of investigating the stability of vitamin B2 (riboflavin, Rf) on hexagonal boron nitride (h-BN), both in its pristine state and in the presence of vacancy defects, with the aim of harnessing their potential as carriers for drug delivery applications. Employing the density functional theory (DFT), we perform binding energy calculations and analyze the electronic structure of the BN@Rf system to unravel the nature of their interactions. Our comprehensive DFT calculations unequivocally demonstrate the spontaneous physical sorption of the drug onto the h-BN surface, facilitated by the formation of π-π stacking interactions. The adsorption energy spans a range from -1.15 to -4.00 eV per system, emphasizing the robust nature of the BN@Rf bonding. The results show that the HOMO and LUMO of riboflavin are located exactly in the region of the iso-alloxazine rings of riboflavin. This arrangement fosters the formation of π-π stacking between riboflavin and boron nitride, effectively facilitating the transfer of electron density within the BN@Rf system. Furthermore, our investigations reveal the significant impact of vacancy defects within the boron nitride lattice. These vacancies alter the behavior of the structure, prompting riboflavin to metamorphose from an electron donor to an electron acceptor, expanding our understanding of the interplay between boron nitride defects and riboflavin sorption. Therefore, it is imperative to exert meticulous oversight of the structural integrity of h-BN, given that the existence of vacancies may lead to a noticeable change in its adsorption properties. The obtained data could amplify our capacity to conceive and refine drug delivery h-BN-based systems.

Zeolitic Imidazolate Framework-8-Loaded Hydrogels as a Highly Biocompatible Carrier for Drug Delivery Applications

Zeolitic imidazolate frameworks-8 (ZIF-8), a type of metal-organic frameworks (MOFs), displays high porosity, large surface areas, and tunable functionality in nanocomposites, promising carrier for drug delivery applications. In this work, ZIF-8 nanomaterials were synthesized via precipitation under three different conditions and subsequently loaded onto chitosan/pluronic F-127 (CS/PL) hydrogels. The ZIF-8 materials prepared in NH4OH solution (ZIF-8-NH4OH) showed a regular cubic shape with a large particle size of approximately 963 nm due to the acceleration of crystal growth in a basic medium. Meanwhile, the ZIF-8 species prepared in H2O and MeOH (ZIF-8-H2O and ZIF-8-MeOH, respectively) displayed crystal sizes of approximately 152 and 240 nm, respectively. The overall toxicity of the ZIF-8 nanomaterials was determined with an XTT assay against the L929 mouse fibroblast cell line. The morphology of the cells was altered at a concentration of over 30 µg/mL due to cell membrane deformations. This result correlated with the lactate dehydrogenase (LDH) release study by detection of LDH release at a concentration of over 25 µg/mL (50% LDH release). To reduce the toxicity of the ZIF-8 materials, CS/PL hydrogels were appropriately prepared and used to encapsulate the ZIF-8 at 0.095% w/w. Cytotoxicity results of the ZIF-8-loaded CS/PL hydrogels indicated over 75% cell viability of the L929 cells. These results presented significant implications for future applications of the ZIF-8 particles in the delivery of drugs or other compounds.

Chitosan-Based Particulate Carriers: Structure, Production and Corresponding Controlled Release.

The state of the art in the use of chitosan (CS) for preparing particulate carriers for drug delivery applications is reviewed. After evidencing the scientific and commercial potentials of CS, the links between targeted controlled activity, the preparation process and the kinetics of release are detailed, focusing on two types of particulate carriers: matrix particles and capsules. More precisely, the relationship between the size/structure of CS-based particles as multifunctional delivery systems and drug release kinetics (models) is emphasized. The preparation method and conditions greatly influence particle structure and size, which affect release properties. Various techniques available for characterizing particle structural properties and size distribution are reviewed. CS particulate carriers with different structures can achieve various release patterns, including zero-order, multi-pulsed, and pulse-triggered. Mathematical models have an unavoidable role in understanding release mechanisms and their interrelationships. Moreover, models help identify the key structural characteristics, thus saving experimental time. Furthermore, by investigating the close relation between preparation process parameters and particulate structural characteristics as well as their effect on release properties, a novel "on-demand" strategy for the design of drug delivery devices may be developed. This reverse strategy involves designing the production process and the related particles' structure based on the targeted release pattern.

DEVELOPMENT AND CHARACTERIZATION OF PH-RESPONSIVE POLYMERIC MICROBEADS INTERCALATED WITH MONTMORILLONITE FOR CONTROLLED RELEASE OF DOXORUBICIN

Objective: The aim of the present study is to develop pH-responsive polymeric microbeads for controlled release of doxorubicin. Methods: Doxorubicin-encapsulated polymeric microbeads were developed by a simple ionotropic gelation method using sodium alginate, gum ghatti, and montmorillonite (MMT). In this work, we investigate the positive benefits of MMT mineral as a drug carrier for the controlled release of DOX. X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, and scanning electron microscopy (SEM) were used to characterize the generated microbeads. The influence of hetero-ionic concentration on drug encapsulation efficiency and drug release from microbeads was examined. In vitro release and swelling studies were performed at pH 2.0 and 7.4 at 37 °C. The cytotoxicity of the developed microbeads was studied using in vitro cultures of the human breast cancer cell line (MCF-7). Results: FTIR confirms the generation of microbeads and also the interaction between the polymer matrix, DOX and MMT clay. XRD analysis reveals the molecular dispersion of DOX and the presence of MMT in the polymeric matrix. SEM studies reveal the developed microbeads are spherical in shape with rough surfaces. Swelling and in vitro release studies are dependent on the pH of the test medium, which may be favorable for intestinal drug delivery. MTT results reveal that the developed microbeads showed good in vitro toxicity against MCF-7 cells. The drug release kinetics of the generated microbeads are followed by both the higuchi and korsmeyer-peppas models. Conclusion: The findings suggest that the DOX-encapsulated microbeads are promising carriers for drug delivery applications. The fabricated microbeads further needs warrant for drug delivery applications.

LipoParticles: a lipid membrane coating onto polymer particles to enhance the internalization in osteoblast cells.

LipoParticles, core-shell assemblies consisting of a polymer core coated by a lipid membrane, are promising carriers for drug delivery applications with intracellular targets. This is of great interest since it is actually challenging to treat infections involving intracellular bacteria such as bone and joint infections where the bacteria are hidden in osteoblast cells. The present work reports for the first time to the best of our knowledge the proof of enhanced internalization of particles in osteoblast cells thanks to a lipid coating of particles (= LipoParticles). The ca. 300 nm-sized assemblies were elaborated by reorganization of liposomes (composed of DPPC/DPTAP 10/90 mol/mol) onto the surface of poly(lactic-co-glycolic acid) (PLGA) particles, and were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), and zetametry. Optimization of these assemblies was also performed by adding poly(ethylene glycol) (PEG) chains on their surface (corresponding to a final formulation of DPPC/DPTAP/DPPE-PEG5000 8/90/2 mol/mol/mol). Interestingly, this provided them colloidal stability after their 20-fold dilution in PBS or cell culture medium, and made possible their freeze-drying without forming aggregates after their re-hydration. Their non-cytotoxicity towards a human osteoblast cell line (MG63) was also demonstrated. The enhanced internalization of LipoParticles in this MG63 cell line, in comparison with PLGA particles, was proven by observations with a confocal laser scanning microscope, as well as by flow cytometry assays. Finally, this efficient internalization of LipoParticles in MG63 cells was confirmed by TEM on ultrathin sections, which also revealed localization close to intracellular Staphylococcus aureus.

Programmable Drug Release from a Dual-Stimuli Responsive Magnetic Metal–Organic Framework

Along with the increasing incidence of cancer and drawbacks of traditional drug delivery systems (DDSs), developing novel nanocarriers for sustained targeted-drug release has become urgent. In this regard, metal–organic frameworks (MOFs) have emerged as potential candidates due to their structural flexibility, defined porosity, lower toxicity, and biodegradability. Herein, a FeMn-based ferromagnetic MOF was synthesized from a preassembled Fe2Mn(μ3-O) cluster. The introduction of the Mn provided the ferromagnetic character to FeMn-MIL-88B. 5-Fluoruracil (5-FU) was encapsulated as a model drug in the MOFs, and its pH and H2S dual-stimuli responsive controlled release was realized. FeMn-MIL-88B presented a higher 5-FU loading capacity of 43.8 wt % and rapid drug release behavior in a tumor microenvironment (TME) simulated medium. The carriers can rapidly release loaded drug of 70% and 26% in PBS solution (pH = 5.4) and NaHS solution (500 μM) within 24 h. The application of mathematical release models indicated 5-FU release from carriers can be precisely fitted to the first-order, second-order, and Higuchi models of release. Moreover, the cytotoxicity profile of the carrier against human embryonic kidney cells (HEK293T) suggests no adverse effects up to 100 μg/mL. The lesser toxic effect on cell viability can be attributed to the low toxicity values [LD50 (Fe) = 30 g·kg–1, (Mn) = 1.5 g·kg–1, and (terephthalic acid) = 5 g·kg–1] of the MOFs structural components. Together with dual-stimuli responsiveness, ferromagnetic nature, and low toxicity, FeMn-MIL-88B MOFs can emerge as promising carriers for drug delivery applications.

Protein Binding of Benzofuran Derivatives: A CD Spectroscopic and In Silico Comparative Study of the Effects of 4-Nitrophenyl Functionalized Benzofurans and Benzodifurans on BSA Protein Structure.

Benzofuran derivatives are synthetic compounds that are finding an increasing interest in the scientific community not only as building blocks for the realization of new materials, but also as potential drugs thanks to their ability to interact with nucleic acids, interfere with the amyloid peptide aggregation and cancer cell cycle. However, their ability to interact with proteins is a theme still in need of investigation for the therapeutic importance that benzofurans could have in the modulation of protein-driven processes and for the possibility of making use of serum albumins as benzofurans delivery systems. To this scope, we investigated the protein binding ability of two 4-nitrophenyl-functionalized benzofurans previously synthesized in our laboratory and herein indicated as BF1 and BDF1, which differed for the number of furan rings (a single moiety in BF1, two in BDF1), using bovine serum albumin (BSA) as a model protein. By circular dichroism (CD) spectroscopy we demonstrated the ability of the two heteroaromatic compounds to alter the secondary structure of the serum albumin leading to different consequences in terms of BSA thermal stability with respect to the unbound protein (ΔTm > 3 °C for BF1, −0.8 °C for BDF1 with respect to unbound BSA, in PBS buffer, pH 7.5) as revealed in our CD melting studies. Moreover, a molecular docking study allowed us to compare the possible ligand binding modes of the mono and difuranic derivatives showing that while BF1 is preferentially housed in the interior of protein structure, BDF1 is predicted to bind the albumin surface with a lower affinity than BF1. Interestingly, the different affinity for the protein target predicted computationally was confirmed also experimentally by fluorescence spectroscopy (kD = 142.4 ± 64.6 nM for BDF1 vs. 28.4 ± 10.1 nM for BF1). Overall, the above findings suggest the ability of benzofurans to bind serum albumins that could act as their carriers in drug delivery applications.

Lipid Cubic Mesophases Combined with Superparamagnetic Iron Oxide Nanoparticles: A Hybrid Multifunctional Platform with Tunable Magnetic Properties for Nanomedical Applications.

Hybrid materials composed of superparamagnetic iron oxide nanoparticles (SPIONs) and lipid self-assemblies possess considerable applicative potential in the biomedical field, specifically, for drug/nutrient delivery. Recently, we showed that SPIONs-doped lipid cubic liquid crystals undergo a cubic-to-hexagonal phase transition under the action of temperature or of an alternating magnetic field (AMF). This transition triggers the release of drugs embedded in the lipid scaffold or in the water channels. In this contribution, we address this phenomenon in depth, to fully elucidate the structural details and optimize the design of hybrid multifunctional carriers for drug delivery. Combining small-angle X-ray scattering (SAXS) with a magnetic characterization, we find that, in bulk lipid cubic phases, the cubic-to-hexagonal transition determines the magnetic response of SPIONs. We then extend the investigation from bulk liquid-crystalline phases to colloidal dispersions, i.e., to lipid/SPIONs nanoparticles with cubic internal structure (“magnetocubosomes”). Through Synchrotron SAXS, we monitor the structural response of magnetocubosomes while exposed to an AMF: the magnetic energy, converted into heat by SPIONs, activates the cubic-to-hexagonal transition, and can thus be used as a remote stimulus to spike drug release “on-demand”. In addition, we show that the AMF-induced phase transition in magnetocubosomes steers the realignment of SPIONs into linear string assemblies and connect this effect with the change in their magnetic properties, observed at the bulk level. Finally, we assess the internalization ability and cytotoxicity of magnetocubosomes in vitro on HT29 adenocarcinoma cancer cells, in order to test the applicability of these smart carriers in drug delivery applications.

Encapsulation of 5‐Fluorouracil Treated Reduced Graphene Oxide in Sodium Alginate Matrix for Controlled and pH‐Responsive Drug Delivery

AbstractThe present work encompasses the fabrication of sodium alginate microbeads embedded with 5‐fluorouracil (5‐FU)/reduced graphene oxide (rGO) for pH‐responsive drug delivery. Initially, 5‐FU is treated with rGO and then encapsulated with an alginate matrix by a simple ionotropic gelation technique with different cross‐linking agents for the controlled release of 5‐FU. The resultant beads were characterized by Fourier transform infrared spectroscopy (FTIR), X‐ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). Besides, swelling andin vitrodrug release studies were also carried out at pH 1.2, 5.4, and 6.8 at 37 °C. The presence of rGO in the alginate matrix could greatly enhance the 5‐FU loading and accomplish sustained release of 5‐FU. The presence of Mg2+ions in the alginate matrix could greatly affect the swelling and release rate. The anticancer activity of the alginate beads was assessed using an MTT assay against MCF‐7 cells. The results findings that the developed alginate beads are probably to be effective drug carriers for drug delivery applications.

Hyaluronate Functionalized Multi-Wall Carbon Nanotubes Loaded with Carboplatin Enhance Cytotoxicity on Human Cancer Cell Lines.

Cancer is a major global public health problem and conventional chemotherapy has several adverse effects and deficiencies. As a valuable option for chemotherapy, nanomedicine requires novel agents to increase the effects of antineoplastic drugs in multiple cancer models. Since its discovery, carbon nanotubes (CNTs) are intensively investigated for their use as carriers in drug delivery applications. This study shows the development of a nanovector generated with commercial carbon nanotubes (cCNTs) that were oxidized (oxCNTs) and chemically functionalized with hyaluronic acid (HA) and loaded with carboplatin (CPT). The nanovector, oxCNTs–HA–CPT, was used as a treatment against HeLa and MDA–MB-231 human tumor cell lines. The potential antineoplastic impact of the fabricated nanovector was evaluated in human cervical adenocarcinoma (HeLa) and mammary adenocarcinoma (MDA-MB-231). The oxCNTs–HA–CPT nanovector demonstrate to have a specific antitumor effect in vitro. The functionalization with HA allows that nanovector bio–directed towards tumor cells, while the toxicity effect is attributed mainly to CPT in a dose-dependent manner.

The Toxicity of Polystyrene-Based Nanoparticles in Saccharomyces cerevisiae Is Associated with Nanoparticle Charge and Uptake Mechanism.

Polystyrene latex (PSL) nanoparticles (NPs), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) liposomes, and hybrid NPs that have different concentrations, sizes, surface charges, and functional groups were used to determine their toxicity to Saccharomyces cerevisiae cells. The size, charge, and morphology of the nanoparticles were characterized by dynamic light scattering, electrophoretic light scattering, scanning transmission electron microscopy, and transmission electron microscopy analysis. The cell viabilities were determined by colony forming unit analysis and confocal laser scanning microscopy imaging. Uptake inhibition studies were performed to determine the internalization mechanism of PSL NPs. At 50 mg/L, both positively and negatively charged NPs were slightly toxic. With increasing concentration, however, full toxicities were observed with positively charged PSL NPs, while a marginal increase in toxicity was obtained with negatively charged PSL NPs. For negatively charged and carboxyl-functionalized NPs, an increase in size induced toxicity, whereas for positively charged and amine-functionalized NPs, smaller-sized NPs were more toxic to yeast cells. Negatively charged NPs were internalized by the yeast cells, but they showed toxicity when they entered the cell vacuole. Positively charged NPs, however, accumulated on the cell surface and caused toxicity. When coated with DOPC liposomes, positively charged NPs became significantly less toxic. We attribute this reduction to the larger-diameter and/or more-agglomerated NPs in the extracellular environment, which resulted in lower interactions with the cell. In addition to endocytosis, it is possible that the negatively charged NPs (30-C-n) were internalized by the cells, partly via direct permeation, which is preferred for high drug delivery efficiency. Negatively charged PSL NP exposure to the yeast cells at low-to-moderate concentrations resulted in low toxicities in the long term. Our results indicate that negatively charged PSL NPs provide safer alternatives as cargo carriers in drug delivery applications. Moreover, the variations in NP size, concentration, and exposure time, along with the use of hybrid systems, have significant roles in nanoparticle-based drug delivery applications in terms of their effects on living organisms.

A Review of Lignocellulosic-Derived Nanoparticles for Drug Delivery Applications: Lignin Nanoparticles, Xylan Nanoparticles, and Cellulose Nanocrystals.

Due to their biocompatibility, biodegradability, and non-toxicity, lignocellulosic-derived nanoparticles are very potential materials for drug carriers in drug delivery applications. There are three main lignocellulosic-derived nanoparticles discussed in this review. First, lignin nanoparticles (LNPs) are an amphiphilic nanoparticle which has versatile interactions toward hydrophilic or hydrophobic drugs. The synthesis methods of LNPs play an important role in this amphiphilic characteristic. Second, xylan nanoparticles (XNPs) are a hemicellulose-derived nanoparticle, where additional pretreatment is needed to obtain a high purity xylan before the synthesis of XNPs. This process is quite long and challenging, but XNPs have a lot of potential as a drug carrier due to their stronger interactions with various drugs. Third, cellulose nanocrystals (CNCs) are a widely exploited nanoparticle, especially in drug delivery applications. CNCs have low cytotoxicity, therefore they are suitable for use as a drug carrier. The research possibilities for these three nanoparticles are still wide and there is potential in drug delivery applications, especially for enhancing their characteristics with further surface modifications adjusted to the drugs.

Biodegradable Metal-Organic Framework-Based Microrobots (MOFBOTs).

Microrobots and metal-organic frameworks (MOFs) have been identified as promising carriers for drug delivery applications. While clinical applications of microrobots are limited by their low drug loading efficiencies and the poor degradability of the materials used for their fabrication, MOFs lack motility and targeted drug delivery capabilities. The combination of these two fields marks the beginning of a new era; MOF-based small-scale robots (MOFBOTs) for biomedical applications. Yet, biodegradability is a major hurdle in the field of micro- and nanoswimmers including small-scale robots. Here, a highly integrated MOFBOT that is able to realize magnetic locomotion, drug delivery, and selective degradation in cell cultures is reported for the first time. The MOF used in the investigations does not only allow a superior loading of chemotherapeutic drugs and their controlled release via a pH-responsive degradation but it also enables the controlled locomotion of enzymatically biodegradable gelatin-based helical microrobots under magnetic fields. The degradation of the integrated MOFBOT is observed after two weeks, when all its components fully degrade. Additionally, drug delivery studies performed in cancer cell cultures show reduced viability upon delivery of Doxorubicin within short time frames. This MOFBOT system opens new avenues for highly integrated fully biodegradable small-scale robots.

Gelatin‐Coated Dual Cross‐Linked Sodium Alginate/Magnetite Nanoparticle Microbeads for Controlled Release of Doxorubicin

AbstractThe aim of the present work is fabrication of gelatin (GL) coated dual cross‐linked sodium alginate (SA)/magnetite nanoparticles (MNPs) microbeads as potential drug vehicle for extended release of doxorubicin (DOX). The microbeads were prepared using in situ ion‐exchange followed by simple ionotropic gelation technique. The developed beads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X‐ray diffraction (XRD) and scanning electron microscopy (SEM). Swelling studies and in vitro release studies were investigated in pH 1.2, 5.0 and 7.4 at 37 °C. Results suggested that both the swelling and in vitro release studies were influenced by the pH of test media, which might be suitable for intestinal drug delivery. The release mechanism was analyzed by fitting the release data into Korsmeyer‐Peppas equation. The results suggest that the fabricated DOX loaded compounds are good drug delivery carriers for drug delivery applications.

Synthesis of low toxicity metal-organic framework carrier for drug release

In this study, the [Zn(4,4′-bipy)(formic acid)2(NO3)2] (4,4′-bipy = 4,4′-bipyridine) metal-organic framework (MOF) (1) was synthesized using Zn(NO3)2·6H2O and 4,4′-bipyridine according to the solution solvothermal approach. In addition, thermogravimetric analysis (TGA), power X-ray diffraction (XRD), UV spectrophotometry, and Fourier transform infrared spectroscopy (FTIR) were carried out to determine the crystal phase and characterizations of 1. Thereafter, 1 was adopted to carry 5-fluorouracil (5-FU), which displayed a 5-FU loading of 37.9 wt%. Besides, the 5-FU-loaded 1 displayed pH-sensitive behavior with the release of 5-FU in acidic environment. Typically, the 5-FU release process was progressive and under efficient control, and 93% 5-FU was released in acidic environment at 72 h later, but only 58% 5-FU was released in the phosphate buffered saline (PBS, pH = 7.4). Furthermore, the toxicity of 1 was evaluated through cytotoxicity assays in HeLa and L02 cell lines, which showed significantly low toxicity of 1. Taken together, these results indicate that, the prepared 1 may potentially serve as a suitable carrier for drug delivery applications.

Nanoantioxidant-Based Silica Particles as Flavonoid Carrier for Drug Delivery Applications.

Nanosystems used in pharmaceutical formulations have shown promising results in enhancing the administration of drugs of difficult formulations. In particular, porous silica nanoparticles have demonstrated excellent properties for application in biological systems; however, there are still several challenges related to the development of more effective and biocompatible materials. An interesting approach to enhance these nanomaterials has been the development of nanoantioxidant carriers. In this work, a hybrid nanoantioxidant carrier based on porous silica nanoplatform with rosmarinic acid antioxidant immobilized on its surface were developed and characterized. Techniques such as dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), N2 adsorption–desorption measurements, differential scanning calorimetry (DSC), Fourier transform–infrared spectroscopy (FT-IR), and 2,2-diphenyl-1-picrylhydrazyl (DPPH●) assay were used to characterize and evaluate the antioxidant activity of nanocarriers. In addition, drug release profile was evaluated using two biorelevant media. The antioxidant activity of rosmarinic acid was maintained, suggesting the correct disposition of the moiety. Kinetic studies reveal that more morin is released in the simulated intestinal fluid than in the gastric one, while an anomalous non–Fickian release mechanism was observed. These results suggest a promising antioxidant nanocarrier suitable for future application in drug delivery.

Recent Advances in Silk Sericin/Calcium Phosphate Biomaterials

Calcium phosphates (CaPs) have been widely used in the field of biomedical engineering as bone graft substitutes or as carriers for drug delivery applications. Recent developments have focused on combining CaPs with proteins to obtain functional biomaterials that accommodate a broader spectrum of functional requirements. Silk sericin was considered an unutilized protein by-product from the textile industry, generating tons of residues every year. However, much effort has been dedicated to its recovery after being associated with numerous biological properties such as antioxidant, antibacterial, anti-coagulation and regenerative activities. Recently, sericin has also demonstrated to be suitable as a template for CaP mineralization. The present review focuses on the recent developments for the production of Sericin/CaP composites, exploring their potential applications in bioengineering and opening new avenues in other research fields such as in the cosmetic and food industries. In addition, this paper can also be useful as a guideline to design future research based on Sericin/CaP biomaterials.