Residue-Free Orally Administered Drug Carrier Based on a Porous Aromatic Framework for Efficient Multisite Treatment.

Nowadays, oral medications are the primary method of treating disease due to their convenience, low cost, and safety, without the need for complex medical procedures. To maximize treatment effectiveness, almost all oral medications utilize drug carriers, such as capsules, liposomes, and sugar coatings. However, these carriers rely on dissolution or fragmentation to achieve drug release, which leads to drugs and carriers coabsorption in the body, causing unnecessary adverse drug reactions, such as nausea, vomiting, abdominal pain, and even death caused by allergy. Therefore, the ideal oral drug carrier should avoid degradation and absorption and be totally excreted after drug release at the desired location. Herein, a gastrointestinally stable oral drug carrier based on porous aromatic framework-1 (PAF-1) is constructed, and it is modified with famotidine (a well-known gastric drug) and mesalazine (a well-known ulcerative colitis drug) to verify the excellent potential of PAF-1. The results demonstrate that PAF-1 can accurately release famotidine in stomach, mesalazine in the intestine, and finally be completely excreted from the body without any residue after 12 h. The use of PAF materials for the construction of oral drug carriers with no residue in the gastrointestinal tract provides a new approach for efficient disease treatment.

Application of nanoparticles in breast cancer treatment: a systematic review.

It is estimated that cancer is the second leading cause of death worldwide. The primary or secondary cause of cancer-related mortality for women is breast cancer. The main treatment method for different types of cancer is chemotherapy with drugs. Because of less water solubility of chemotherapy drugs or their inability to pass through membranes, their body absorbs them inadequately, which lowers the treatment's effectiveness. Drug specificity and pharmacokinetics can be changed by nanotechnology using nanoparticles. Instead, targeted drug delivery allows medications to be delivered to the targeted sites. In this review, we focused on nanoparticles as carriers in targeted drug delivery, their characteristics, structure, and the previous studies related to breast cancer. It was shown that nanoparticles could reduce the negative effects of chemotherapy drugs while increasing their effectiveness. Lipid-based nanocarriers demonstrated notable results in this instance, and some products that are undergoing various stages of clinical trials are among the examples. Nanoparticles based on metal or polymers demonstrated a comparable level of efficacy. With the number of cancer cases rising globally, many researchers are now looking into novel treatment approaches, particularly the use of nanotechnology and nanoparticles in the treatment of cancer. In order to help clinicians, this article aimed to gather more information about various areas of nanoparticle application in breast cancer therapy, such as modifying their synthesis and physicochemical characterization. It also sought to gain a deeper understanding of the mechanisms underlying the interactions between nanoparticles and biologically normal or infected tissues.

Synthesis and characterization of ion-induced sodium alginate/soy protein isolate microgels for the controlled release.

In this study, sodium alginate/ soy protein isolate (SPI) microgels cross-linked by various divalent cations including Cu2+, Ba2+, Ca2+, and Zn2+ were fabricated. Cryo-scanning electron microscopy observations revealed distinctive structural variations among the microgels. In the context of gastric pH conditions, the degree of shrinkage of the microgels followed the sequence of Ca2+ > Ba2+ > Cu2+ > Zn2+. Meanwhile, under intestinal pH conditions, the degree of swelling was ranked as Zn2+ > Ca2+ > Ba2+ > Cu2+. The impact of these variations was investigated through in vitro digestion studies, revealing that all microgels successfully delayed the release of ß-carotene within the stomach. Within the simulated intestinal fluid, the microgel cross-linked with Zn2+ exhibited an initial burst release, while those cross-linked with Cu2+, Ba2+, or Ca2+ displayed a sustained release pattern. This research underscores the potential of sodium alginate/SPI microgels cross-linked with different divalent cations as efficient controlled-release delivery systems.

Low-Density Polyethylene-Based Novel Active Packaging Film for Food Shelf-Life Extension via Thyme-Oil Control Release from SBA-15 Nanocarrier.

The use of natural raw substances for food preservation could provide a great contribution to food waste reduction, circular economy enhancement, and green process application widening. Recent studies indicated that the use of porous materials as adsorbents for natural essential oils provided nanohybrids with excellent antioxidant and antimicrobial properties. Following this trend in this work, a thymol oil (TEO) rich SBA-15 nanohybrid was prepared and characterized physiochemically with various techniques. This TEO@SBA-15 nanohybrid, along with the pure SBA-15, was extruded with low-density polyethylene (LDPE) to develop novel active packaging films. Results indicated that TEO loading was higher than other porous materials reported recently, and the addition of both pure SBA-15 and TEO@SBA-15 to the LDPE increased the water/oxygen barrier. The film with the higher thyme-oil@SBA-15 nanohybrid content exhibited a slower release kinetic. The antioxidant activity of the final films ignited after 48 h, was in the range of 60-70%, and was almost constant for 7 days. Finally, all tests indicated a sufficient improvement by the addition of thyme-oil@SBA-15 nanohybrids in the pure LDPE matrix and the concentration of wt. 10% of such nanocarriers provided the optimum final LDPE/10TEO@SBE-15 active packaging film. This material could be a potential future product for active packaging applications.

Performance effectiveness of nano-lignin in production of gel with nano-chitosan for controlling release of salicylic acid.

This work deals with assessing the performance of lignin nanoparticles (LNPs) in solving the problem of using salicylic acid as an agrochemical compound, via controlling its release. LNPs, obtained from black liquor, have been used to develop new delivery systems. Gels from chelating of LNPs with chitosan or chitosan nanoparticles (Cs-NPs) in presence or absence of cationic starch are investigated to achieve this essential aim. The nanoparticles are examined by TEM, ATR-FTIR, and XRD techniques. Based on measurements of swelling, encapsulation, release profile, release kinetic modeling of salicylic acid (SA), infrared spectroscopy, thermo-gravimetric analysis and scanning electron microscope the behavior of the investigated nanocomposite gels is assessed. The results show that the SA release profile of Cs-NPs and its nanocomposite with LNPs in phosphate-buffered saline (PBS) (7.4) (51.5-69.4 %) is higher than that of the mixture of water and ethanol (34.9-50.4 %). The release profile in PBS (7.4) demonstrates a trend of prolonged SA release over a 48-hour period. Best control of the SA-release can be achieved by CsNPs-LNPs nanocomposite. Comparing the results with previous literature demonstrates the promising characteristics of these examined gel nanocomposites. The release of SA from nanocomposites is regulated by a diffusion mechanism and follows the Ritger-Peppas and Higuchi models for kinetic release.

Silica Microparticles from Sugarcane By-Products as an Encapsulation System for Retinoids Aimed at Topical Sustained Release.

The encapsulation of retinol within silica microparticles has emerged as a promising opportunity in the realm of cosmetic and pharmaceutical formulations, driven by the need to reinforce the photoprotection and oxidation stability of retinol. This work examines the process of encapsulating retinol into silica microparticles. The association efficiency, microparticle size, molecular structure, morphology, oxidation, and release profile, as well as biocompatibility and skin sensitization, were evaluated. Results showed that 0.03% of retinol and 9% of emulsifier leads to an association efficiency higher than 99% and a particle size with an average of 5.2 µm. FTIR results indicate that there is an association of retinol with the silica microparticles, and some may be on the surface. Microscopy indicates that when association happens, there is less aggregation of the particles. Oxidation occurs in two different phases, the first related to the retinol on the surface and the second to the associated retinol. In addition, a burst release of up to 3 h (30% free retinol, 17% associated retinol) was observed, as well as a sustained release of 44% of retinol up to 24 h. Encapsulation allowed an increase in the minimal skin cytotoxic concentrations of retinol from 0.04 µg/mL to 1.25 mg/mL without skin sensitization. Overall, retinol is protected when associated with silica microparticles, being safe to use in cosmetics and dermatology.

Comparison of Emulsion Stabilizers: Application for the Enhancement of the Bioactivity of Lemongrass Essential Oil.

Recent focus on cellulose nanomaterials, particularly biodegradable and biocompatible cellulose nanocrystals (CNCs), has prompted their use as emulsion stabilizers. CNCs, when combined with salt, demonstrate enhanced emulsion stabilization. This study explored three emulsion stabilizers: Tween 80, soybean CNCs with salt (salted CNCs), and a combination of salted CNCs with Tween 80. Soybean CNCs, derived from soybean stover, were characterized by Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). Antifungal testing against Aspergillus flavus revealed increased bioactivity in all lemongrass essential oil (EO)-loaded emulsions compared to pure essential oil. In addition, all three emulsions exhibited a slight reduction in antifungal activity after 30 days of room temperature storage. The release experiment revealed that the EO-loaded nanoemulsion exhibited a slow-release profile. The nanoemulsion stabilized by salted CNCs and Tween 80 exhibited significantly lower release rates when compared to the nanoemulsion stabilized solely by Tween 80, attributed to the gel network formed by salted CNCs. The findings of this study highlight the efficacy of cellulose nanocrystals procured from soybean byproducts in conjunction with synthetic surfactants to create nanoencapsulated essential oils, resulting in improved antimicrobial efficacy and the achievement of sustained release properties.

Fabrication of controlled-release polymeric microneedles containing progesterone-loaded self-microemulsions for transdermal delivery.

Progesterone (PG) has been approved for hormone replacement therapy to mitigate the risk of endometrial carcinoma. However, there has been a lack of success in oral PG due to its rapid degradation. Transdermal PG has advantages but lacks efficacy due to its poor solubility (Log p = 3.9). Therefore, this study aimed to evaluate how combining self-microemulsifying drug delivery systems (SMEDDS) and polymeric microneedles (MNs) could improve the transdermal delivery of PG in a controlled-release manner. Among PG-SMEDDS, PG-SME5 was selected for its desirable properties and stability. The two-layer polymeric MNs formulation incorporating PG-SME5 (PG-SMEDDS-tMNs) was formulated from aqueous blends of polymers as a first layer and 20% PCL as a second layer. It successfully penetrated neonatal porcine skin with the dissolution of the first layer observed within 15 min after application. In vitro skin permeation revealed that the percentage of PG which permeated the skin over 82 h using PG-SMEDDS-tMNs was higher than a PG-suspension and PG-SMEDDS. The Higuchi kinetic showed controlled release over 15 days of PG from PG-SMEDDS-tMNs. These studies suggested that incorporating PG-SMEDDS into controlled-release two-layer polymeric MNs could be a promising approach for improving the transdermal delivery of PG.

Delivery Systems for Plasma-reactive Species and their Applications in the Field of Biomedicine.

Cold atmospheric plasma (CAP) is an ionized matter with potential applications in various medical fields, ranging from wound healing and disinfection to cancer treatment. CAP's clinical usefulness stems from its ability to act as an adjustable source of reactive oxygen and nitrogen species (RONS), which are known to function as pleiotropic signaling agents within cells. Plasma-activated species, such as RONS, have the potential to be consistently and precisely released by carriers, enabling their utilization in a wide array of biomedical applications. Furthermore, understanding the behavior of CAP in different environments, including water, salt solutions, culture medium, hydrogels, and nanoparticles, may lead to new opportunities for maximizing its therapeutic potential. This review article sought to provide a comprehensive and critical analysis of current biomaterial approaches for the targeted delivery of plasma-activated species in the hope to boost therapeutic response and clinical applicability.

Recent advances of polymeric nanoplatforms for cancer treatment: smart delivery systems (SDS), nanotheranostics and multidrug resistance (MDR) inhibition.

Nanotheranostics is a promising field that combines the benefits of diagnostic and treatment into a single nano-platform that not only administers treatment but also allows for real-time monitoring of therapeutic response, decreasing the possibility of under/over-drug dosing. Furthermore, developing smart delivery systems (SDSs) for cancer theranostics that can take advantage of various tumour microenvironment (TME) conditions (such as deformed tumour vasculature, various over-expressed receptor proteins, reduced pH, oxidative stress, and resulting elevated glutathione levels) can aid in achieving improved pharmacokinetics, higher tumour accumulation, enhanced antitumour efficacy, and/or decreased side effects and multidrug resistance (MDR) inhibition. Polymeric nanoparticles (PNPs) are being widely investigated in this regard due to their unique features such as small size, passive/active targeting possibility, better pharmaceutical kinetics and biological distribution, decreased adverse reactions of the established drugs, inherent inhibitory properties to MDR efflux pump proteins, as well as the feasibility of delivering numerous therapeutic substances in just one design. Hence in this review, we have primarily discussed PNPs based targeted and/or controlled SDSs in which we have elaborated upon different TME mediated nanotheranostic platforms (NTPs) including active/passive/magnetic targeting platforms along with pH/ROS/redox-responsive platforms. Besides, we have elucidated different imaging guided cancer therapeutic platforms based on four major cancer imaging techniques i.e., fluorescence/photo-acoustic/radionuclide/magnetic resonance imaging, Furthermore, we have deliberated some of the most recently developed PNPs based multimodal NTPs (by combining two or more imaging or therapy techniques on a single nanoplatform) in cancer theranostics. Moreover, we have provided a brief update on PNPs based NTP which are recently developed to overcome MDR for effective cancer treatment. Additionally, we have briefly discussed about the tissue biodistribution/tumour targeting efficiency of these nanoplatforms along with recent preclinical/clinical studies. Finally, we have elaborated on various limitations associated with PNPs based nanoplatforms.

Wheat bran arabinoxylan-soybean protein isolate emulsion-filled gels as a ß-carotene delivery carrier: Effect of polysaccharide content on textural and rheological properties.

This study aimed to investigate the effects of different wheat bran arabinoxylan (WBAX) concentrations (1, 2, 3, and 4 wt%) on the structural and physicochemical properties of WBAX-soybean protein isolate (SPI) emulsion-filled gels (EFGs) prepared using laccase and heat treatment. The properties of the various gels as well as their microstructure, rheology, and in vitro digestion behaviors were investigated. Results showed that WBAX-SPI EFGs with a 3 wt% WBAX concentration had a smooth and uniform appearance, high water holding capacity (98.5 ± 0.2 %), and enhanced mechanical properties. Rheological experiments suggested that a stronger and closer gel network was formed at 3 wt% WBAX concentration. Fourier transform infrared spectroscopy showed that laccase and heat treatment not only catalyzed the intramolecular crosslinking of WBAX and SPI, respectively, but also promoted the interaction between WBAX and SPI. Confocal laser scanning microscopy revealed that the WBAX gel network was interspersed within the SPI network. The interactions contributing to the gelation analysis revealed that chemical (disulfide bond) and physical (hydrogen bond and hydrophobic) interactions promoted the formation of denser EFGs. Furthermore, the WBAX-SPI EFGs provided a ß-carotene bioaccessibility of 21.8 ± 0.6 %. Therefore, our study suggests that WBAX-SPI EFGs hold promising potential for industrial applications in the delivery of ß-carotene.

Preparation of polysaccharide-based nanoparticles by chitosan and flaxseed gum polyelectrolyte complexation as carriers for bighead carp (Aristichthys nobilis) peptide delivery.

Polysaccharide-based nanoparticles formed by the polyelectrolyte complexation between chitosan (CS) and flaxseed gum (FG) was developed in this work, and it was further used as a carrier for bighead carp peptide (BCP) delivery. The CS molecular weight (MW) of 50 kDa and CS/FG mass ratio of 1:2 at pH 3.5 were optimal conditions for the NP preparation, with the minimum particle size (∼155.1 nm) and the maximum BCP encapsulation efficiency (60.3 %). The BCP-loaded CS/FG NPs exhibited the smallest particle size (175.8 nm). Both CS/FG NPs and CS/FG-BCP NPs exhibited roughly uniform spherical shape. FT-IR spectra confirmed the existence of hydrogen bonds and electrostatic interactions in the nanoparticles. The BCP-loaded NPs displayed a higher thermal stability than BCP. Moreover, the release of BCP was controllable and dose-dependent, following a first-order kinetics model. These findings suggested that our CS/FG NPs are a promising carrier for bioactive peptide delivery.

Thymol@activated Carbon Nanohybrid for Low-Density Polyethylene-Based Active Packaging Films for Pork Fillets' Shelf-Life Extension.

Τhe replacement of food packaging additives and preservatives with bio-based antioxidant/antibacterial compounds has been a common practice in recent years following the trend of bioeconomy and nanotechnology. Such bio-additives are often enclosed in nanocarriers for a controlled release process. Following this trend in this work, a thymol (TO)-rich activated carbon (AC) nanohybrid was prepared and characterized physicochemically with various techniques. This TO@AC nanohybrid, along with the pure activated carbon, was extruded with low-density polyethylene (LDPE) to develop novel active packaging films. The codenames used in this paper were LDPE/xTO@AC and LDPE/xAC for the nanohybrid and the pure activated carbon, respectively. X-ray diffractometry, Fourier-transform infrared spectroscopy, and scanning electron microscopy measurements showed high dispersity of both the TO@AC nanohybrid and the pure AC in the LDPE matrix, resulting in enhanced mechanical properties. The active film with 15 wt.% of the TO@AC nanohybrid (LDPE/15TO@AC) exhibited a 230% higher water/vapor barrier and 1928% lower oxygen permeability than the pure LDPE film. For this active film, the highest antioxidant activity referred to the DPPH assay (44.4%), the lowest thymol release rate (k2 ≈ 1.5 s-1), and the highest antibacterial activity were recorded, resulting in a 2-day extension of fresh pork fillets' shelf-life.

Controlled volatile release from ß-sitosterol-based oleogels based on different self-assembly mechanisms.

This study examined how the self-assembly mechanisms of ß-sitosterol-based oleogels influenced the release of volatile compounds. Microscopy, X-ray diffraction (XRD) and small-angle X-ray scattering (SAXS) measurements showed that the three ß-sitosterol-based oleogels (ß-sitosterol + Î³-oryzanol oleogels (SO), ß-sitosterol + lecithin oleogels (SL) and ß-sitosterol + monostearate oleogels (SM)) had significant differences in their microstructures, which were formed via different self-assembly mechanisms. SO exhibited the highest oil binding capacity (OBC), complex modulus (G*) and apparent viscosity. Dynamic and static headspace analyses suggested that network structure of ß-sitosterol-based oleogels affected the release of volatile components. SO showed the strongest retention effect, followed by SL and SM. The release of volatile compounds mainly related to structural strength and compositions of oleogels. These results indicated that ß-sitosterol-based oleogels formed with different self-assembly mechanisms have the potential to serve as effective delivery systems for controlling the release of volatile compounds.

Nanocapsules of ZnO Nanorods and Geraniol as a Novel Mean for the Effective Control of Botrytis cinerea in Tomato and Cucumber Plants.

Inorganic-based nanoparticle formulations of bioactive compounds are a promising nanoscale application that allow agrochemicals to be entrapped and/or encapsulated, enabling gradual and targeted delivery of their active ingredients. In this context, hydrophobic ZnO@OAm nanorods (NRs) were firstly synthesized and characterized via physicochemical techniques and then encapsulated within the biodegradable and biocompatible sodium dodecyl sulfate (SDS), either separately (ZnO NCs) or in combination with geraniol in the effective ratios of 1:1 (ZnOGer1 NCs), 1:2 (ZnOGer2 NCs), and 1:3 (ZnOGer2 NCs), respectively. The mean hydrodynamic size, polydispersity index (PDI), and ζ-potential of the nanocapsules were determined at different pH values. The efficiency of encapsulation (EE, %) and loading capacity (LC, %) of NCs were also determined. Pharmacokinetics of ZnOGer1 NCs and ZnOGer2 NCs showed a sustainable release profile of geraniol over 96 h and a higher stability at 25 ± 0.5 °C rather than at 35 ± 0.5 °C. ZnOGer1 NCs, ZnOGer2 NCs and ZnO NCs were evaluated in vitro against B. cinerea, and EC50 values were calculated at 176 µg/mL, 150 µg/mL, and > 500 µg/mL, respectively. Subsequently, ZnOGer1 NCs and ZnOGer2 NCs were tested by foliar application on B. cinerea-inoculated tomato and cucumber plants, showing a significant reduction of disease severity. The foliar application of both NCs resulted in more effective inhibition of the pathogen in the infected cucumber plants as compared to the treatment with the chemical fungicide Luna Sensation SC. In contrast, tomato plants treated with ZnOGer2 NCs demonstrated a better inhibition of the disease as compared to the treatment with ZnOGer1 NCs and Luna. None of the treatments caused phytotoxic effects. These results support the potential for the use of the specific NCs as plant protection agents against B. cinerea in agriculture as an effective alternative to synthetic fungicides.

Functional Peptide-Loaded Gelatin Nanoparticles as Eyedrops for Cornea Neovascularization Treatment.

Background: Corneal neovascularization (NV) is a process of abnormal vessel growth into the transparent cornea from the limbus and can disturb the light passing through the cornea, resulting in vision loss or even blindness. The use of nanomedicine as an effective therapeutic formulation in ophthalmology has led to higher drug bioavailability and a slow drug release rate. In this research, we designed and explored the feasibility of a new nanomedicine, gp91 ds-tat (gp91) peptide-encapsulated gelatin nanoparticles (GNP-gp91), for inhibiting corneal angiogenesis. Methods: GNP-gp91 were prepared by a two-step desolvation method. The characterization and cytocompatibility of GNP-gp91 were analyzed. The inhibition effect of GNP-gp91 on HUVEC cell migration and tube formation was observed by an inverted microscope. The drug retention test in mouse cornea was observed by in vivo imaging system, fluorescence microscope, and DAPI/TAMRA staining. Finally, the therapeutic efficacy and evaluation of neovascularization-related factors were conducted through the in vivo corneal NV mice model via topical delivery. Results: The prepared GNP-gp91 had a nano-scale diameter (550.6 nm) with positive charge (21.7 mV) slow-release behavior (25%, 240hr). In vitro test revealed that GNP-gp91 enhanced the inhibition of cell migration and tube formation capacity via higher internalization of HUVEC. Topical administration (eyedrops) of the GNP-gp91 significantly prolongs the retention time (46%, 20 min) in the mouse cornea. In chemically burned corneal neovascularization models, corneal vessel area with a significant reduction in GNP-gp91 group (7.89%) was revealed when compared with PBS (33.99%) and gp91 (19.67%) treated groups via every two days dosing. Moreover, GNP-gp91 significantly reduced the concentration of Nox2, VEGF and MMP9 in NV's cornea. Conclusion: The nanomedicine, GNP-gp91, was successfully synthesized for ophthalmological application. These data suggest that GNP-gp91 contained eyedrops that not only have a longer retention time on the cornea but also can treat mice corneal NV effectively delivered in a low dosing frequency, GNP-gp91 eyedrops provides an alternative strategy for clinical ocular disease treatment in the culture.

A hydrogel dressing with tunable critical temperature and photothermal modulating melittin release for multiply antibacterial treatment.

It is imperative to develop an antibiotic-free and long-term effective strategy for treating chronic wound infections due to the long-term utilization of antibiotics easily causing drug resistance. Herein, we fabricated a novel poly-N-isopropylacrylamide (PNIPAM)/polyacrylamide (PAM) coupling thermosensitive hydrogel integrating 1D lysozyme nanofiber doped with CuS nanoparticles (CuS/PP) and loading antibacterial peptide melittin (M) (CuS/PP-M) for combating chronic wound infection via photothermal modulating the release of melittin. For the CuS/PP-M hydrogel, the copolymerization of PNIPAM and PAM allows the lower critical solution temperature (LCST) higher than the body temperature, effectively hindering the spontaneous release of melittin when contacts the infected wound, while the integration of LNF/CuS nanofibers provides a stable photothermal treatment for triggering the release of melittin. As a result, the CuS/PP-M hydrogel exhibits synergistically enhanced effect on killing both Gram-positive and Gram-negative bacteria, which maintains more than 99 % bactericidal efficiency, even displays a long-term and multiply antibacterial performance by photothermal modulating melittin release. Moreover, the CuS/PP-M hydrogel presents both high antibacterial activity and excellent wound healing performance in the mouse wound model, thereby benefiting the chronic wound healing.

Nanoparticles Based on Chondroitin Sulfate from Tuna Heads and Chitooligosaccharides for Enhanced Water Solubility and Sustained Release of Curcumin.

This study aimed to separate chondroitin sulfate (CS) from the heads of skipjack tuna (Katsuwonus pelamis) and yellowfin tuna (Thunnus albacares), by-products derived from canned tuna processing, via a biological process. The use of 1% w/w papain and an incubation time of 48 h resulted in a degree of hydrolysis of 93.75 ± 2.94% and a CS content of 59.53 ± 1.77 mg/100 g. The FTIR spectra of extracted CS products exhibited identical functional groups found in commercially available CS. The molecular weights of CS extracted from skipjack and yellowfin tuna heads were 11.0 kDa and 7.7 kDa, respectively. Subsequently, a CH:CS ratio of 3:2 for CS and chitooligosaccharides (CH) was chosen as the optimal ratio for the preparation of spherical nanoparticles, with %EE, mean particle size, PDI, and zeta potential values of 50.89 ± 0.66%, 128.90 ± 3.29 nm, 0.27 ± 0.04, and -12.47 ± 2.06, respectively. The CU content was enhanced to 127.21 ± 1.66 µg/mL. The release of CU from this particular nanosystem involved mainly a drug diffusion mechanism, with a burst release in the first 3 h followed by a sustained release of CU over 24 h. The DPPH and ABTS scavenging activity results confirmed the efficient encapsulation of CU into CHCS nanoparticles. This study will provide a theoretical basis for CS derived from tuna head cartilages to be used as a functional component with specific functional properties in food and biomedical applications.

Controlled Cascade-Release and High Selective Sterilization by Core-Shell Nanogels for Microenvironment Regulation of Aerobic Vaginitis.

Aerobic vaginitis (AV) is a gynecological disease associated with vaginal flora imbalance. The nonselective bactericidal nature of antibiotics and low customization rate of probiotic supplementation in existing treatments lead to AV recurrence. Here, a drug delivery strategy is proposed that works with the changing dynamics of the bacterial flora. In particular, a core-shell nanogel (CSNG) is designed to encapsulate prebiotic inulin and antimicrobial peptide Cath 30. The proposed strategy allows for the sequential release of both drugs using gelatinase produced by AV pathogenic bacteria, initially selectively killing pathogenic bacteria and subsequently promoting the proliferation of beneficial bacteria in the vagina. In a simulated infection environment in vitro, the outer layer of CSNGs, Cath 30 is rapidly degraded and potently killed the pathogenic bacterium Staphylococcus aureus at 2-6 h. CSNGs enhances proliferation of the beneficial bacterium Lactobacillus crispatus by more than 50% at 24 h. In a rat AV model, the drug delivery strategy precisely regulated the bacterial microenvironment while controlling the inflammatory response of the vaginal microenvironment. This new treatment approach, configured on demand and precisely controlled, offers a new strategy for the treatment of vaginal diseases.

Functional System Based on Glycyrrhizic Acid Supramolecular Hydrogel: Toward Polymorph Control, Stabilization, and Controlled Release.

Developments of a drug delivery system (DDS) based on a natural supramolecular hydrogel have been of wide interest due to its biocompatibility, efficacy, and adjustable performance. However, a simple and efficient design of functional hydrogel DDS based on the templated interplay of gelator and model drug is still a challenge. In this work, natural glycyrrhetinic acid (GA) gel was selected as a carrier to encapsulate the model drug pyrazinamide (PZA). It was found that the carboxyl-amide interaction at the interface of gel-drug achieved polymorph control, stabilization, and pH-responsive release. Powder X-ray diffraction confirmed that the metastable γ form of PZA was obtained from the GA gel. Spectral analysis and molecular dynamics simulation showed that the protonation at the amide-O promoted the discretization of PZA molecules in solution, resulting in the polymorphism. Furthermore, the gel-drug interplay increased the stability of the γ form significantly from 2 days to 3 months by in situ encapsulation in the GA gel. In vitro release study indicated that the GA gel achieved targeted control release of PZA due to the pH-responsiveness property of GA. This work provides a promising option for hydrogel-based DDS design combined with polymorph control and stabilization.