Biocompatible Delivery Research Articles

Targeting CD44-positive ovarian cancers via engineered paclitaxel prodrug nanoparticles for enhanced chemotherapeutic efficacy

Ovarian cancer (OvCa) is currently the fifth most lethal malignancy affecting women health owing to the lack of early diagnosis and treatment choices available before the disease has progressed to a later stage. Paclitaxel (PTX) has shown substantial antineoplastic action against a variety of human cancers, including OvCa, for multiple decades. Despite this, the therapeutic use of this drug is not yet adequate owing to surfactant-related toxicities and off-target effects. In response to these constraints, nanoparticle carriers have evolved as delivery tools for the biocompatible and target delivery of PTX. In this work, a novel polymeric PTX formulation was developed for targeted therapy of OvCa cells, which was achieved by prodrug engineering and HA decoration strategies. Further studies indicated that HA-coated nanodrugs (HA-PLA-PTX NPs) could preferentially accumulate in the CD44-expressing SKOV3 cells, which induced elevated cytotoxicity, reduced cell proliferation, and increased cell apoptosis. In vivo study also demonstrated that equivalent doses of HA-PLA-PTX NPs surpassed the clinical PTX formulation Taxol in a SKOV3 xenograft tumor model. In conclusion, HA-PLA-PTX NPs might be a potentially feasible delivery system for effective OvCa treatment.

NIR-Active Porphyrin-Decorated Lipid Microbubbles for Enhanced Therapeutic Activity Enabled by Photodynamic Effect and Ultrasound in 3D Tumor Models of Breast Cancer Cell Line and Zebrafish Larvae.

Porphyrin is known to enable the photodynamic effect during cancer drug delivery and molecular imaging. However, its hydrophobicity and tendency to aggregate in an aqueous medium create a significant hurdle for its use as an anticancer drug. Loading porphyrin onto biocompatible delivery vehicles can enhance its efficacy. This can be achieved by using gas-filled microbubbles that can be administered intravenously. This study aimed at developing near-infrared (NIR)-active porphyrin-loaded lipid microbubbles with anticancer activity enhanced by sonodynamic and photodynamic effects. The porphyrin-loaded microbubbles were studied for their cell toxicity, cellular uptake of porphyrin, and effect on cellular three-dimensional (3D) invasion of breast cancer cells (MDA-MB-231) in cellulo. Toxicity studies in zebrafish larvae (Danio rerio) in the presence and absence of photodynamic and sonodynamic therapy were also conducted. The results suggest that with a higher concentration of porphyrin loaded on microbubbles, the porphyrin-loaded microbubbles display a higher therapeutic effect facilitated by photodynamic and sonodynamic therapy, which results in enhanced cellular uptake and cellular toxicity. A lower concentration of loaded porphyrin microbubbles exhibits high cellular viability and good fluorescence intensity in the NIR region, which can be exploited for bioimaging applications.

Synergetic treatment of oxygen microcapsules and lenvatinib for enhanced therapy of HCC by alleviating hypoxia condition and activating anti-tumor immunity

Hypoxia is a typical characteristic of hepatocellular carcinoma (HCC), which causes tremendous obstacles to tumor treatments. Current first-line treatment may further deteriorate tumor hypoxia. For example, Lenvatinib, a receptor tyrosine kinase inhibitor (RTKI), suppresses tumor growth via blocking vascular endothelial growth factor (VEGF) signaling, and can also inhibit angiogenesis, thus limiting oxygen supply to tumor sites. Therefore, alleviating tumor microenvironment (TME) hypoxia holds great potential for enhancing the therapeutic effect of RTKI. Here, nanoparticle-stabilized oxygen microcapsules, a stable and biocompatible oxygen-loaded delivery system, are successfully prepared through interfacial polymerization of polydopamine nanoparticles. The microcapsules with a large loading capacity of oxygen in the core show excellent bioavailability and dispersity, which could effectively improve the hypoxic TME when they serve as oxygen delivery vehicles. Synergetic treatments of Lenvatinib and oxygen microcapsules could induce the transition of “cold tumor” in an immune-suppressed state to “hot tumor” in an immune-activated state by improving tumor hypoxic TME and reducing angiogenesis in HCC. It is revealed that combined treatments of oxygen microcapsules and Lenvatinib could polarize tumor-associated macrophages (TAMs) to anti-tumor M1 cells and activate T cell-mediated anti-tumor immune responses. The results suggest that synergetic therapy using oxygen microcapsules and Lenvatinib could alleviate the hypoxic TME and enhance the therapeutic performance of RTKI, demonstrating a promising anti-tumor strategy for enhanced therapy of HCC.

Self-fluorescence property of octa-arginine functionalized hydroxyapatite nanoparticles aids in studying their intracellular fate in R1 ESCs

Deciphering the endocytosis mechanisms of nanoparticle entry in cells is crucial to understand the fate of nanoparticles and the biological activity of the transported cargo. Such studies require the use of reporter agents such as fluorescent markers. Previously, we have reported the synthesis of self-fluorescent HAp nanoparticles as efficient nucleic acid delivery agents in prokaryotic and eukaryotic cells. Here, we show the application of biocompatible self-fluorescent nano delivery vehicle based on HAp and CPP- octa-arginine as an efficient system to study the mechanisms of intracellular fate of a gene delivery agent. The pathway of octa-arginine functionalized HAp NP (R8HNP) and HAp NP uptake in R1 ESCs was elucidated using confocal microscopy with the help of endocytic inhibitors. The NPs mainly enter R1 ESCs by clathrin mediated and macropinocytosis pathways. It was established that the NPs escape endosomal degradation by proton sponge effect owing to their ability to buffer the pH and trigger osmotic rupture. The functionalization of CPP, effectively enhanced the internalization and endosomal escape in R1 ESCs. The detailed results of these studies are outlined in this manuscript.

Biobased Chicken Eggshell Powder for Efficient Delivery of Low-Dose Silver Nanoparticles (AgNPs) to Enhance Their Antimicrobial Activities against Foodborne Pathogens and Biofilms.

Despite the current sanitation practices to decontaminate food-contact surfaces, persistent biofilms still pose significant threats to human health by inducing cross-contamination. This study aims to enhance the antimicrobial activity of low-dose silver nanoparticles (AgNPs) against foodborne pathogens and their biofilms through the development of a biobased delivery carrier for metallic nanoparticles. In this study, chicken eggshell powder (EP) was used as a biocompatible delivery carrier, and it possesses a strong ability to encapsulate green-synthesized AgNPs with an encapsulation efficiency of 80.18%. The EP carriers stabilized AgNPs in an organic-rich environment and prevented the aggregation of nanoparticles. The results of antimicrobial test demonstrate that EP significantly enhanced the antimicrobial efficacy of low-dose AgNPs (2 μg/mL), enabling 5-log reductions of planktonic Escherichia coli and Listeria innocua within 25 min and 60 min treatments, respectively, even in the presence of high organic content (chemical oxygen demand, COD = 1000 mg/L). Due to the high affinity of EP to bind biofilms, the encapsulated low-dose AgNPs can inactivate approximately 2-log CFU/cm2 of biofilms within a 2-h treatment. The proposed AgNPs@EP composite with a low silver concentration (2 μg/mL) can effectively inactivate and remove biofilms from food-contact surfaces in which such a low concentration of AgNPs is unlikely to induce negative impacts on human health and environment. Therefore, this antimicrobial AgNPs@EP composite can potentially be used as a biobased sanitizer for food-contact surfaces in a food manufacturing plant.

Liquid crystalline lipid nanoparticle promotes the photodynamic activity of gallium protoporphyrin against S. aureus biofilms.

Antimicrobial photodynamic therapy (aPDT) has emerged as an innovative strategy to combat antibiotic resistant microbes; yet aPDT efficacies against biofilms are sub-optimal due to inability of photosenstizers to reach microbes embedded in biofilm matrix. To overcome this challenge, liquid crystal lipid nanoparticles (LCNP) were employed in this study as a smart, biocompatible and triggerable delivery system for the new photosensitizer gallium protoporphyrin (GaPP), due to their capabilities in promoting efficient antimicrobial delivery to biofilms. The relationship between GaPP loading of LCNP, reactive oxygen species (ROS) production and the in vitro antibacterial activity against two antibiotic resistant Staphylococcus aureus strains was established. LCNP substantially improved the antibacterial activity of GaPP, completely eradicating S. aureus and MRSA planktonic cultures, using a GaPP concentration of 0.8μM and light dose 1.9J/cm2. At the same concentration and light dose, unformulated GaPP triggered only a 4 log10 and 2 log10 reduction in respective planktonic cultures. Most importantly, the activity of GaPP against biofilms was enhanced by 2-fold compared to unformulated GaPP, reducing the viability of S. aureus and MRSA biofilms by 8 log10 and 5 log10, respectively. The biosafety of photoactivated GaPP-LCNP was evaluated against human fibroblasts, which indicated a high safety profile of the treatment. Therefore, these findings encourage further investigations of GaPP-LCNP as a potential treatment for localized chronic infections.

Molecular Descriptors as a Facile Tool toward Designing Surface-Functionalized Nanoparticles for Drug Delivery.

Modulating the surface chemistry of nanoparticles, often by grafting hydrophilic polymer brushes (e.g., polyethylene glycol) to prepare nanoformulations that can resist opsonization in a hematic environment and negotiate with the mucus barrier, is a popular strategy toward developing biocompatible and effective nano-drug delivery systems. However, there is a need for tools that can screen multiple surface ligands and cluster them based on both structural similarity and physicochemical attributes. Molecular descriptors offer numerical readouts based on molecular properties and provide a fertile ground for developing quick screening platforms. Thus, a study was conducted with 14 monomers/repeating blocks of polymeric chains, namely, oxazoline, acrylamide, vinylpyrrolidone, glycerol, acryloyl morpholine, dimethyl acrylamide, hydroxypropyl methacrylamide, hydroxyethyl methacrylamide, sialic acid, carboxybetaine acrylamide, carboxybetaine methacrylate, sulfobetaine methacrylate, methacryloyloxyethyl phosphorylcholine, and vinyl-pyridinio propanesulfonate, capable of imparting hydrophilicity to a surface when assembled as polymeric brushes. Employing free, Web-based, and user-friendly platforms, such as SwissADME and ChemMine tools, a series of molecular descriptors and Tanimoto coefficient of molecular pairs were determined, followed by hierarchical clustering analyses. Molecular pairs of oxazoline/dimethyl acrylamide, hydroxypropyl methacrylamide/hydroxyethyl methacrylamide, acrylamide/glycerol, carboxybetaine acrylamide/vinyl-pyridinio propanesulfonate, and sulfobetaine methacrylate/methacryloyloxyethyl phosphorylcholine were clustered together. Similarly, the molecular pair of hydroxypropyl methacrylamide/hydroxyethyl methacrylamide demonstrated a high Tanimoto coefficient of >0.9, whereas the pairs oxazoline/vinylpyrrolidone, acrylamide/dimethyl acrylamide, acryloyl morpholine/dimethyl acrylamide, acryloyl morpholine/hydroxypropyl methacrylamide, acryloyl morpholine/hydroxyethyl methacrylamide, carboxybetaine methacrylate/sulfobetaine methacrylate, and glycerol/hydroxypropyl methacrylamide had a Tanimoto coefficient of >0.8. The analyzed data not only demonstrated the ability of such in silico tools as a facile technique in clustering molecules of interest based on their structure and physicochemical characteristics but also provided vital information on their behavior within biological systems, including the ability to engage an array of possible molecular targets when the monomers are self-assembled on nanoparticulate surfaces.

Fiber-laser platform for precision brain surgery.

Minimally invasive neurological surgeries are increasingly being sought after for treatment in neurological pathologies and oncology. A critical limitation in these minimally invasive procedures is lack of specialized tools that allow for space-time controlled delivery of sufficient energy for coagulation and cutting of tissue. Advent of fiber-lasers provide high average power with improved beam quality (lower M2), biocompatible silica fiber delivery, reduced cost of manufacturing, and radiant output stability over long operating periods. Despite these advancements, no fiber-laser based surgical tools are currently available for tissue resection in vivo. Here we demonstrate a first to our knowledge, fiber-laser platform for performing precise brain surgery in a murine brain model. In this study, our primary aims were to first demonstrate efficacy of fiber-lasers in performing precise blood-less surgery in a murine brain with limited non-specific thermal damage. Second, fiber-lasers' ability to deliver radiant energy through biocompatible silica fibers was explored in a murine brain model for blood less resection. A bench-top optical coherence tomography (OCT) guided fiber-laser platform was constructed with a stereotactic stage for performing precision brain surgery. A pulsed quasi-continuous wave ytterbium (Yb) fiber-laser (1.07 µm) was used to perform vascular specific coagulation while a pulsed nanosecond thulium fiber-laser (1.94 µm) was used to conduct bloodless cutting, all under the guidance of a swept-source OCT system centered at 1310 +/- 70 nm. Specialty linear and circular cuts were made in an in vivo murine brain for bloodless brain tissue resection. The two fiber-lasers were combined into a single biocompatible silica fiber to conduct brain surgery resection under the bench-top OCT system's imaging microscope. Vascular specific coagulation was demonstrated in all five mice studied. Bloodless linear cuts and point cuts were demonstrated in vivo. Histologically, thermal injury was measured to be less than 100 µm while a removal rate of close to 5 mm3/s was achieved with an average Tm fiber-laser power of 15 W. To the authors' knowledge, this is the first demonstration of a fiber-laser platform for conducting in vivo bloodless brain tissue resection with a pulsed thulium (Tm) fiber-laser and a quasi-continuous wave (QCW) Yb fiber-laser. The demonstrated fiber-laser platform, if successfully configured for use in the operating room (OR), can provide surgeons a tool for rapid removal of tissue while making surgical resections of brain regions more precise, and can be basis for a flexible cutting tool capable of reaching hard-to-operate regions.

Fabrication of polysaccharide-stabilized zein nanoparticles by flash nanoprecipitation for doxorubicin sustained release

The effective fabrication of biocompatible and robust delivery carriers is an ongoing challenge in the nanomedicine for cancer treatments. Zein has proven Generally Recognized as Safe (GRAS) for clinical uses. However, its poor solubility and stability in aqueous media limits the broad applications of zein-based nanoparticles (NPs). In this study, a novel flash nanoprecipitation (FNP) was utilized to fabricate polysaccharide-stabilized zein NPs (polysaccharide/zein NPs) with small size and good stability over two weeks. The physicochemical properties of NPs were determined by the concentration and polysaccharides/zein weight ratio. FNP preparation at lower concentration (0.5 mg/mL) of polysaccharides and zein as well as the weight ratio of 1:1 led to the formation of smaller NPs with lower polydispersity. Alginate-stabilized zein NPs (AlgZ) exhibited excellent drug encapsulation efficiency (∼77.9%) and loading capacity up to ∼ 16.3% when they were used as carriers for doxorubicin (DOX). Specifically, DOX-loaded AlgZ showed sustained release of DOX, which enables the significantly prolonged cancer cell-killing and inhibits the burst release of DOX, thus exhibited great potential in the sustainable delivery of hydrophobic drugs.

High density lipoprotein nanoparticle as delivery system for radio-sensitising miRNA: An investigation in 2D/3D head and neck cancer models

Radiotherapy is one of the main treatment options for head and neck cancer patients. However, its clinical efficacy is hindered by both radiation induced side effects and radio-resistance. Radio-sensitising approaches with acceptable toxicity are being actively investigated. Among these, RNA therapeutics have great potentials as radio-sensitisers owing to their ability to target pathways specific to radio-resistance. However, their clinical translation is challenging due to delivery issues. Herein, we report the application of high-density lipoprotein nanoparticle (HDL NPs) as a biocompatible delivery system for a well-established radio-sensitising RNA, miR-34a. A simple/fast microfluidic based technique was used to prepare miR-34a-HDL NPs. Profiling of the radiation response in the UM-SCC-1 head and neck cancer cell line confirmed reduced metabolic activity and increased radiation induced apoptosis upon treatment with miR-34a-HDL NPs. The radio-sensitising properties of miR-34a-HDL NPs were further confirmed in a more biologically relevant co-culture spheroid model of head and neck cancer. Increased apoptotic activity and disrupted cell cycle were induced by miR-34a delivered by HDL NPs. The enhanced radio-biologic effects observed in both 2D and 3D models confirmed the utility of HDL NPs as an efficient delivery system for radio-sensitising RNA.

Front Cover: Overcoming STING Agonists Barriers: Peptide, Protein, and Biomembrane‐based Biocompatible Delivery Strategies (Chem. Asian J. 6/2022)

By virtue of being a central mediator of type I interferon (IFN), the stimulator of interferon genes (STING) pathway has emerged as an exciting target for antiviral and antitumor immunity. Along with the development of the STING pathway, more and more agonists have been adopted by Novartis, Bristol-Myers Squibb, Merck and so on for the treatment of advanced or metastatic tumors in clinical trials. Up to now, the number of STING agonists-based clinical trials has reached 15 and is growing. However, STING agonists cyclic dinucleotides (CDNs) displayed almost zero efficacy in clinical trials, likely due to poor cellular permeability and rapid diffusion despite intratumoral injection. This triggered urgent demands for highly effective delivery strategies to improve the cellular permeability, tissue targetability and retention of STING agonists. Here, the recent progress of STING agonist applications against viruses and tumors is summarized, and delivery strategies with a focus on biocompatible platforms are highlighted. More information can be found in the Review by Yong-Fang Zheng and Jun-Jun Wu.

Targeted delivery of cancer drug paclitaxel to chordomas tumor cells via an RNA nanoparticle harboring an EGFR aptamer

Paclitaxel has been extensively used in clinics for cancer treatment. However, its limited solubility in aqueous solution and high occurrence of side effects have also been widely reported. In this study, we constructed a biocompatible RNA nanoparticle delivery system (3WJ-EGFRapt) that includes 3WJ (3-way junction) nanoparticle with a size of 4.85 ± 0.59 nm as a backbone and an EGFR (epidermal growth factor receptor) aptamer for specific targeting to chordomas cells, which owns the encapsulation ability of drug paclitaxel (PTX) for cancer therapy. Confocal microscopy and flow cytometry results confirmed 3WJ-EGFRapt nanoparticle exhibited excellent specific targeting to chordomas cell U-CH2 which is an EGFR(+) cell line; while the 3WJ nanoparticle lose the targeted ability. Both of the two nanoparticles own no sensitivity to lung cancer cell H520 which is an EGFR(-) cell line. Moreover, the 3WJ-EGFRapt nanoparticle encapsulated drug PTX could enhance the inhibition efficiency of chordomas tumor cells U-CH2 as compared to free PTX alone. This work demonstrates that RNA-3WJ constructed with a targeting aptamer provides a compromising targeted drug delivery ability on chordomas cells for therapeutics.

The inhibitory role of si-UBB delivered by degradable dendrimers-based lipid nanoparticles in ovarian cancer

ObjectiveRNA interference holds tremendous potential in the treatment of malignant tumors. However, efficient and biocompatible delivery methods are needed for systemic delivery of small interfering RNA (siRNA). In this study, we explored the delivery efficiency and therapy effect of si-UBB-5A2SC8 in ovarian cancer.Methods and materialsSi-UBB-5A2SC8 nanoparticles were successfully prepared according to the established procedure and the characteristic of nanoparticles was determined by digital laser scanning. Flow cytometry and confocal analysis demonstrated si-UBB was efficiently transfected to cell by the delivery of 5A2SC8 complexes. The in vitro gene knockdown efficiency of ubiquitin B was demonstrated by RT-qPCR and Western blot analysis, which was further verified by the inhibition of proliferation and migration of ovarian cancer cells. Accumulative efficiency of si-UBB-5A2SC8 nanoparticles was investigated in BALB/c mice bearing SKOV3-GFP tumor xenograft. In vivo imaging was adopted to test the accurate location of the nanoparticle in the tumor. The feature of the tumor and pivotal organ was determined. TUNEL and caspase-3 expression was used to analyze the underling mechanism of the inhibition effect.ResultsThe average size and the zeta potential of the si-UBB-5A2SC8 was (150 ± 11) nm and − (20 ± 4) mV, respectively. Transmission electronic microscopy showed the nanoparticle was near-spherical with the mean size of (100 ± 15) nm. Flow cytometry and confocal microscopic images demonstrated 5A2SC8 complex could successfully deliver Cy5.5-siRNA to the cytoplasm of ovarian cancer cells. qRT-PCR and western blot demonstrated the mRNA and protein expression of ubiquitin B was decreased to 62.5% and 36.5% of the control group, which was accompanied with the decreased proliferation and migration ability in si-UBB-5A2SC8-transfected cells. Ex vivo fluorescence imaging demonstrated 5A2SC8 complex could successfully carry siRNA to the tumor lesion and exert the inhibition effect, which was verified by the decreased tumor weight and increased apoptosis and caspase-3 expression in mice treated with si-UBB-5A2SC8.Conclusions5A2SC8 complex was a safe and efficient gene delivery vehicle and ubiquitin B was a potential target for the ovarian cancer targeted therapy.

Fabrication and Characterization of Thymol-Loaded Chitosan Nanogels: Improved Antibacterial and Anti-Biofilm Activities with Negligible Cytotoxicity.

Thymol is a monoterpene phenolic derivative extracted from the Thymus vulgaris which has antimicrobial effects. In the present study, thymol-loaded chitosan nanogels were prepared and their physicochemical properties were characterized. The encapsulation efficiency of thymol into chitosan and its stability were determined. The in vitro antimicrobial and anti-biofilm activities of thymol-loaded chitosan nanogel (Ty-CsNG), free thymol (Ty), and free chitosan nanogel (CsNG) were evaluated against both Gram-negative and Gram-positive multidrug-resistant (MDR) bacteria including Staphylococcus aureus, Acinetobacter baumanii, and Pseudomonas aeruginosa strains using the broth microdilution and crystal violet assay, respectively. After treatment of MDR strains with sub-minimum inhibitory concentration (Sub-MIC) of Ty-CsNG, free Ty and CsNG, biofilm gene expression analysis was studied. Moreover, cytotoxicity of Ty-CsNG, free Ty, and CsNG against HEK-293 normal cell line was determined using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The average size of Ty-CsNG was 82.71±9.6 nm, encapsulation efficiency was 76.54±0.62 % with stability up to 60 days at 4 °C. Antibacterial activity test revealed that Ty-CsNG reduced the MIC by 4-6 times in comparison to free thymol. In addition, the expression of biofilm-related genes including ompA, and pgaB were significantly down-regulated after treatment of strains with Ty-CsNG (P<0.05). In addition, free CsNG displayed negligible cytotoxicity against HEK-293 normal cell lines and presented a biocompatible nanoscale delivery system. Based on the results, it can be concluded that Ty-CsNG can be considered a promising candidate for enhancing antimicrobial and anti-biofilm activities.

Applications of Chitosan-Alginate-Based Nanoparticles-An Up-to-Date Review.

Chitosan and alginate are two of the most studied natural polymers that have attracted interest for multiple uses in their nano form. The biomedical field is one of the domains benefiting the most from the development of nanotechnology, as increasing research interest has been oriented to developing chitosan-alginate biocompatible delivery vehicles, antimicrobial agents, and vaccine adjuvants. Moreover, these nanomaterials of natural origin have also become appealing for environmental protection (e.g., water treatment, environmental-friendly fertilizers, herbicides, and pesticides) and the food industry. In this respect, the present paper aims to discuss some of the newest applications of chitosan-alginate-based nanomaterials and serve as an inception point for further research in the field.

Milk exosomes-mediated miR-31-5p delivery accelerates diabetic wound healing through promoting angiogenesis

The refractory diabetic wound has remained a worldwide challenge as one of the major health problems. The impaired angiogenesis phase during diabetic wound healing partly contributes to the pathological process. MicroRNA (miRNA) is an essential regulator of gene expression in crucial biological processes and is a promising nucleic acid drug in therapeutic fields of the diabetic wound. However, miRNA therapies have limitations due to lacking an effective delivery system. In the present study, we found a significant reduction of miR-31-5p expression in the full-thickness wounds of diabetic mice compared to normal mice. Further, miR-31-5p has been proven to promote the proliferation, migration, and angiogenesis of endothelial cells. Thus, we conceived the idea of exogenously supplementing miR-31-5p mimics to treat the diabetic wound. We used milk-derived exosomes as a novel system for miR-31-5p delivery and successfully encapsulated miR-31-5p mimics into milk exosomes through electroporation. Then, we proved that the miR-31-5p loaded in exosomes achieved higher cell uptake and was able to resist degradation. Moreover, our miRNA-exosomal formulation demonstrated dramatically improved endothelial cell functions in vitro, together with the promotion of angiogenesis and enhanced diabetic wound healing in vivo. Collectively, our data showed the feasibility of milk exosomes as a scalable, biocompatible, and cost-effective delivery system to enhance the bioavailability and efficacy of miRNAs.

Conditionally designed luminescent DNA crystals doped by Ln3+(Eu3+/Tb3+) complexes or fluorescent proteins with smart drug sensing property.

In this work, a designed porous DNA crystal with high intrinsic biocompatibility was used as the scaffold material to load fluorescent guest molecules to detect anti-cancer drugs. It is shown here that the synthesized crystals have the characteristics consistent with the designed large solvent channels, and can therefore accommodate guest molecules such as fluorescent proteins that cannot be accommodated by less porous crystals. Eu(TTA)3phen and Tb(acac)3phen lanthanide complexes were individually noncovalently loaded into the porous crystals, resulting in hybrid luminescent DNA crystals. Emodin, an anti-cancer, anti-tumor, anti-inflammatory drug, was found to quench lanthanide complexes in solution or in crystals. Notably, emodin is the active ingredient of Lianhua Qingwen Capsule, an anti-COVID-19 drug candidate. Therefore, the porous DNA crystals reported here have potential applications as a biocompatible and theranostic delivery biomaterial for functional macromolecules.

Encapsulation of bioactive fermented wheat (Lisosan G) in Eudragit-liposomes

Liposomes are one of the most studied and most promising nanocarriers to date, representing a biocompatible, safe, and efficient delivery system for both hydrophilic and lipophilic compounds.This work aimed to evaluate the efficacy in encapsulating an aqueous extract of Lisosan G (LG), a Triticum aestivum whole grains fermented powder with strong antioxidant activity, into Eudragit-liposomes designed for oral delivery.The total phenolics and the antioxidant activity of LG extract and LG extract encapsulated in Eudragit-liposomes were evaluated by the Folin-Ciocalteu, DPPH, and FRAP colorimetric assays. Finally, the biological activity of both LG formulations was assessed as human erythrocytes protection from oxidative stress through the cellular antioxidant activity (CAA) assay.Our results demonstrate that the encapsulation into Eudragit-liposomes preserved the phenolics content of LG extract and retained its antioxidant properties both in vitro and ex vivo. Furthermore, LG Eudragit-liposomes exhibited increased ferric reducing capacity and protection of human erythrocytes from oxidative insult, probably due to the antioxidant properties of liposome constituents.Therefore, the encapsulation into Eudragit-liposomes represents an excellent strategy to prevent possible reduction and loss of activity of LG bioactive compounds, and to deliver them via oral administration.

Efficient Route to Synthesize Biocompatible Delivery System with its Morphological Changes Upon Solvent Variation

Efficient Route to Synthesize Biocompatible Delivery System with its Morphological Changes Upon Solvent Variation

Nanocellulose-based Delivery Systems and Cervical Cancer: Review of the Literature.

It has become clear that targeted therapy is one of the best options for decreasing the unpleasant side effects of existing common methods and reducing the number of deaths occurred due to many types of cancer. Biocompatible and non-toxic delivery systems are provided by nanomedicine for aiding targeted therapy in many diseases containing cancer. Cervical cancer (CC) is not only the most common gynecological cancer but also is ranked as the fourth common cancer between both men and women. Chemotherapy, radiotherapy, surgery, and immunotherapy are the approaches, which are being used for treating CC patients. However, more efficacy of these methods can be achieved with the help of nanomedicine and novel delivery systems. Nanocellulose is one of the agents used for designing these systems in order to deliver different drugs to a diversity of cancerous cells. In this review, we aim to investigate the competency of nanocellulose for establishing novel therapeutic methods for cervical cancer. We hope that our results help develop more drug delivery systems for targeted therapy to reduce the side effects and induce the efficacy of anti-cancer drugs.