Biocompatibility Studies Research Articles

Sonochemical synthesis characterization and biocompatibility studies of polymeric composites for biomedical applications

In this work the in situ synthesis of mixtures of Polymethylmethacrylate (PMMA), High Density Polyethylene (HDPE) and Polypropylene (PP) with biocompatible ceramics was carried out, using high frequency ultrasound as an energy source. Starting from calcium hydroxide and ammonium hydrogen phosphate, two different crystalline phases were obtained: hydroxyapatite (HA) and calcite (CaCO3). FTIR and XRD studies showed that for the materials prepared with HDPE, only CaCO3 was formed during the synthesis process. When Polypropylene used, mixtures of HA with CaCO3 were obtained, while for the materials synthesized with Polymethylmethacrylate, only pure HA was obtained. DSC analyses did not reveal any significant changes in the melting temperatures of HDPE and PP, nor in the glass transition temperature of PMMA with the incorporation of HA and CaCO3, in the polymeric matrices. TGA, showed that the decomposition temperatures of these materials increased with respect to those of the polymers alone, indicating a significant thermal stability. Biocompatibility tests with osteoblastic cells and Scanning Electron Microscopy (SEM) studies showed that the composites of PMMA with HA, PP with HA/CaCO3 and HDPE with CaCO3, are capable of promoting cell adhesion and proliferation mechanisms, revealing potential applications as biomaterials for bone replacement.

In Situ Gelling Eye Drops of Tacrolimus with Improved Ocular Delivery and Therapeutic Efficacy.

In situ gelling eye drops of tacrolimus (FK506 Gel) were developed to address the formulation challenge of tacrolimus for anterior ocular inflammatory diseases. Both in silico and in vitro investigations were conducted to screen a suitable cyclodextrin species to increase the drug solubility. Guanosine was employed as the gelator and combined with inclusion complexes of tacrolimus in the presence of borate anions to obtain FK506 Gel, which gelated when came into contact with cations in tear fluid and led to the formation of a nanofibrous hydrogel. The versatility of our design to improve the solubility and ocular retention of the hydrophobic drug was demonstrated in vivo with coumarin 6 as a model drug. A mouse dry eye model was used to evaluate the therapeutic effects of FK506 Gel, which, in combination with the biocompatibility study, suggested that FK506 Gel served as a superior treatment for anterior ocular inflammatory diseases.

Microfluidic-assisted synthesis of mesoporous silica nanoparticles as drug carriers: characterization and biocompatibility studies

Microfluidic-assisted synthesis of mesoporous silica nanoparticles as drug carriers: characterization and biocompatibility studies

Fabrication and evaluation of four combinations of pullulan-based biopolymeric, microporous scaffolds impregnated with peppermint oil for management of partial thickness burn wounds and accelerated tissue regeneration

Burn injuries are common in both civilian and military settings and cause severe morbidity and mortality. The present study aimed to develop microporous bioactive scaffolds from the natural polysaccharide, pullulan, combined individually with Gelatin (Gel)/ Alginate (Alg)/ Chitosan (Ch)/ Carboxy-methyl cellulose (CMC), and crosslinked with glutaraldehyde to form a polymeric network. The objective was to evaluate and compare their efficacy in healing second degree partial-thickness burn wounds. The scaffolds were also impregnated with peppermint oil (PEO) to provide potential analgesic and cooling effects. Scaffolds were characterized using FTIR, TGA and SEM analysis to understand the intra-and intermolecular interactions and morphological characteristics. In vitro parameters like fluid uptake ability, biodegradation and hemolytic index were also assessed. Biocompatibility studies, including cell adhesion, migration and proliferation, were conducted using L929 mouse fibroblast cell lines. The in vivo efficacy was evaluated in Sprague Dawley rats inflicted with second degree burns to assess and compare wound retraction across different experimental groups. Histology, immunohistochemistry along with gram and picrosirius staining studies were also performed. The average pore size of all biopolymeric scaffold combinations ranged between 25.6-298μm. All four test combinations were non-hemolytic, with hemolytic indices between 0.3-2.9. Wound retraction studies in rats clearly indicated that among the four test combinations studied, Pu/Gel/PEO scaffold not only reduced local inflammation faster but also accelerated dermal regeneration in comparison to positive control as well as other test combinations (viz., Pu/Alg/PEO, Pu/Ch/PEO, and Pu/CMC/PEO). Immunohistochemistry results corroborated animal efficacy findings and demonstrated enhanced expression level of epidermal growth factor and fibroblast growth factor-2 in Pu/Gel/PEO scaffold treated group. Picrosirius staining also revealed enhanced collagen deposition in Pu/Gel/PEO scaffold treated group. The study findings suggest that biopolymeric scaffolds made from pullulan combined with gelatin and PEO (Pu/Gel/PEO) could serve as a promising substrate for skin regeneration template for second degree burns.

In vitro biocompatibility, electrical, mechanical, and structural study of lead-free HAp/BNBK composites for bio-implantation

In vitro biocompatibility, electrical, mechanical, and structural study of lead-free HAp/BNBK composites for bio-implantation

Polyvinyl alcohol and alginate bio-composite film containing titanium dioxide nanotubes for skin injury repair

This study explores the potential of polyvinyl alcohol (PVA) and alginate (SA) blend polymer films with embedded titanium dioxide nanotubes (TiO2NT) for wound healing applications. The nanocomposite film (PVA+SA@TiO2NT) was fabricated via a simple solvent casting process. The synergistic interaction between PVA and alginate significantly enhanced the film's stability in aqueous environments without compromising its weight. After 24 hours of immersion, the film exhibited a substantial swelling capacity (836±6%) and good WVTR ((282±4%). Scanning electron microscopy (SEM) revealed the formation of a smooth and random pore structure within the film. Fourier-transform infrared spectroscopy (FTIR) confirmed the successful formation of hydrogen bonds between PVA and alginate, along with the presence of Ti-O bonds, indicating successful incorporation of TiO2NT into the PVA+SA matrix. X-ray diffraction (XRD) analysis further corroborated the presence of TiO2NT. In vitro biocompatibility studies demonstrated the non-cytotoxic nature of the PVA+SA@TiO2NT bio-composite film. Additionally, in vitro wound healing studies suggest its potential as a promising biomaterial for wound dressing applications. These findings warrant further investigation to elucidate the complete mechanisms of action and optimize the nanocomposite's properties for clinical translation.

Biopharmaceutical modulatory effects of newly engineered bile acid-Tyloxapol nanogels for attenuation of cytotoxicity in auditory cells

This study presents novel thermoresponsive nanogels composed of chenodeoxycholic acid and Tyloxapol for potential inner ear drug delivery. The nanogels exhibit non-Newtonian, shear-thinning fluid behaviour and rapid gelation at body temperature. Biocompatibility studies were conducted on auditory and macrophage cell lines. Nanogels had a minimal impact on cellular viability, glycolysis, and mitochondrial respiration of auditory cells after 24 h of exposure. However, mitochondrial function analysis in macrophages revealed a significant decrease in oxidative phosphorylation and coupling efficiency after nanogel exposure, accompanied by increased proton leakage. Despite these metabolic disruptions, glycolysis remained unaffected. The Poloxamer matrix appears to be responsible for these effects, independent of the presence of bile acids or Tyloxapol. This study highlights the potential of bile acid-enriched nanogels in drug delivery, particularly their biocompatibility and injectability while acknowledging challenges related to mitochondrial dysfunction in immune cells. These findings suggest that thermoresponsive bile acid and Tyloxapol nanogels have the potential to be safe and effective drug delivery vehicles for inner ear applications.

Surface Engineering of Ti6Al4V: Impact of Rhenium–Carbon Coatings with Molybdenum Anchors on Biocompatibility and Corrosion Behavior

Titanium alloys, particularly Ti6Al4V, are widely used in biomedical applications due to their excellent mechanical properties and inherent biocompatibility. However, enhancing their surface characteristics, such as biocompatibility and corrosion resistance, remains a key challenge for their long-term use in medical implants. In this study, we investigate the effects of rhenium–carbon coatings deposited on Ti6Al4V substrates via magnetron sputtering, incorporating a molybdenum anchoring layer. X-ray diffraction (XRD) and energy dispersive spectroscopy (EDS) analyses confirmed the formation of rhenium carbides, elemental rhenium, and rhenium oxides within the coatings. Despite these successful depositions, scanning electron microscopy (SEM) revealed significant delamination and poor adhesion of the coatings to the Ti6Al4V substrates. Corrosion resistance, evaluated through potentiodynamic polarization tests, showed an increase in corrosion current densities and more negative corrosion potentials, indicating a detrimental effect on the substrate’s corrosion resistance. Biocompatibility assessments using PK15 cells demonstrated a marked decrease in cell viability and metabolic activity, particularly in samples with higher surface roughness. These findings underscore the critical need for the optimization of surface preparation and deposition processes to improve both the adhesion and biocompatibility of rhenium–carbon coatings on Ti6Al4V substrates. Future research should aim to refine coating technique to enhance adhesion, explore the mechanisms of cytotoxicity related to surface roughness, and expand biocompatibility studies across different cell lines and biological environments.

Clarithromycin-tailored cubosome: A sustained release oral nano platform for evaluating antibacterial, anti-biofilm, anti-inflammatory, anti-liver cancer, biocompatibility, ex-vivo and in-vivo studies

The clinical implication of clarithromycin (CLT) is compromised owing to its poor solubility and, subsequently, bioavailability, unpalatable taste, rapid metabolism, short half-life, frequent dosing, and adverse effects. The present investigation provides an innovative sustained-release oral drug delivery strategy that tackles these challenges. Accordingly, CLT was loaded into a cubosome, a vesicular system with a bicontinuous cubic structure that promotes solubility and bioavailability, provides a sustained release system combating short half-life and adverse effects, masks unpleasant taste, and protects the drug from destruction in gastrointestinal tract (GIT). Nine various formulas were fabricated using the emulsification method. The resulting vesicles increased the encapsulation efficiency (EE %) from 57.64 ± 0.04 % to 96.80 ± 1.50 %, the particle size (PS) from 147.30 ± 21.77 nm to 216.61 ± 5.37 nm, and the polydispersity index (PDI) values ranged from 0.117 ± 0.024 to 0.278 ± 0.073. The zeta potential (ZP) changed from −20.65 ± 2.01 mV to −33.98 ± 2.60 mV. Further, the release profile exhibited a dual release pattern within 24 h., with the percentage of cumulative release (CR %) expanding from 30.06 ± 0.42 % to 98.49 ± 2.88 %, optimized formula was found to be CC9 with EE % = 96.80 ± 1.50 %, PS = 216.61 ± 5.37 nm, ZP = −33.98 ± 2.60 mV, PDI = 0.117 ± 0.024, CR % = 98.49 ± 2.88 % and IC50 of 0.74 ± 0.19 µg/mL against HepG-2 cells with scattered unilamellar cubic non-agglomerated vesicles. Additionally, it exhibited higher anti-MRSA biofilm, relative bioavailability (2.8 fold), and anti-inflammatory and antimicrobial capacity against Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis, and Staphylococcus aureus compared to free CLT. Our data demonstrate that cubosome is a powerful nanocarrier for oral delivery of CLT, boosting its biological impacts and pharmacokinetic profile.

Green Synthesis and Characterization of Cobalt Nanoparticles Using Butea Monosperma Flower Extract and their Biocompatibility Studies

Green Synthesis and Characterization of Cobalt Nanoparticles Using Butea Monosperma Flower Extract and their Biocompatibility Studies

ROS-responsive nanomicelles encapsulating celastrol ameliorate pressure overload-induced cardiac hypertrophy by regulating the NF-κB signaling pathway

Celastrol (CEL) belongs to the group of non-steroidal immunosuppressants with the potential to improve cardiac hypertrophy (CH). However, the poor biocompatibility and low bioavailability of CEL limit its in vivo application. This study was aimed to develop a targeted drug delivery system that can efficiently and safely deliver CEL to target tissues, providing a research basis for the application of CEL in CH therapy. A novel ROS-sensitive drug-loaded nanomicelle, dodecanoic acid (DA)-phenylboronic acid pinacol ester-dextran polymer encapsulating CEL (DBD@CEL), was synthesized using chemical synthesis. Then, the morphology, particle size, drug-loaded content, and ROS-responsive release behavior of DBD@CEL were studied. Pharmacokinetics and biocompatibility were evaluated using healthy mice. Finally, the ability and mechanism of DBD@CEL in improving CH in vivo were investigated using a mouse CH model. DBD@CEL was successfully prepared with a drug loading of 18.9%. It exhibited excellent stability with an average particle size of 110.0 ± 1.7 nm. Within 48 h, DBD@CEL released only 19.4% in the absence of H2O2, while in the presence of 1 mM H2O2, the release rate increased to 71.5%. Biocompatibility studies indicated that DBD@CEL did not cause blood cell hemolysis, had no impact on normal organs, and did not result in abnormal blood biochemical indicators, demonstrating excellent biocompatibility. In vivo studies revealed that DBD@CEL regulated the activation of NF-κB signaling, inhibits pyroptosis and oxidative stress, and thereby ameliorates CH. The ROS-responsive DBD@CEL nanodrug delivery system enhances the therapeutic activity of CEL for CH, providing a promising drug delivery system for the clinical treatment of CH.

Antibacterial Biocomposite Based on Chitosan/Pluronic/Agarose Noncovalent Hydrogel: Controlled Drug Delivery by Alginate/Tetracycline Beads System.

Designing a wound dressing with controlled uptake, antibacterial, and proper biocompatibility is crucial for the appropriate wound healing process. In this study, alginate/tetracycline (Alg/TC) beads were produced and embedded into chitosan/pluronic/agarose semi-interpenetrating polymer network hydrogel, which serves as a potential biocompatible dressing for treating skin wounds. The effect of pluronic content on the porosity, swelling, mechanical characteristics, and degradation of the hydrogel was investigated. Furthermore, the impact of Alg beads on TC release was subsequently examined. In the absence of Alg beads, faster release was observed. However, after incorporating beads into the hydrogels, the release was sustained. Particularly, the hydrogel containing Alg beads exhibited a nearly linear release, reaching 74% after 2 days in acidic media. The antimicrobial activity and biocompatibility of the hydrogel were also evaluated to assess the capability of the TC-loaded hydrogels for wound dressing applications. The hydrogel demonstrated efficient antibacterial features against Gram-positive and Gram-negative bacteria. Additionally, the sample behavior was evaluated against exposure to yeast. Furthermore, based on biocompatibility studies using HFF2 cells, the TC-loaded hydrogel exhibited remarkable biocompatibility. Overall, this novel composite hydrogel shows remarkable biocompatibility and antibacterial activities which can be used as a great potential wound dressing to prevent wound infections due to its effective inhibition of bacterial growth.

Biocompatibility Study of Purified and Low-Temperature-Sterilized Injectable Collagen for Soft Tissue Repair: Intramuscular Implantation in Rats.

The clinical application of collagen-based biomaterials is expanding rapidly, especially in tissue engineering and cosmetics. While oral supplements and injectable skin boosters are popular for enhancing skin health, clinical evidence supporting their effectiveness remains limited. Injectable products show potential in revitalizing skin, but safety concerns persist due to challenges in sterilization and the risk of biological contamination. Traditional methods of sterilization (heat and irradiation) can denature collagen. This study addresses these issues by introducing a novel technique: the double filtration and low-temperature steam sterilization of a collagen gel. In vitro tests documented the sterility and confirmed that the collagen did not show cytotoxicity, degradation, integrity, and viscosity characteristics changes after the processing and sterilization. The collagen gel induced new collagen expression and the proliferation of human dermal fibroblasts when the cells were cultured with the collagen gel. An in vivo study found no adverse effects in rats or significant lesions at the implantation site over 13 weeks. These results suggest that this novel method to process collagen gels is a safe and effective skin booster. Advanced processing methods are likely to mitigate the safety risks associated with injectable collagen products, though further research is needed to validate their biological effectiveness and clinical benefits.

Enhancement of wound dressings through cerium canadate and hydroxyapatite-infused hyaluronic acide and PVA membranes: A comprehensive characterization and biocompatibility study

This study explores the emhancement of advanced wound dressings by enhancing traditional bandages with suitable biomedical materials. We utilized Hyaluronic Acid (HA) and Polyvinyl Alcohol (PVA) as a polymeric matrix to create a novel membrane. Employing a film casting technique, we incorporated varying ratios of biological nanoparticles—Hydroxyapatite (HAP) and Cerium Vanadate (Ce₃(VO₄)₄)—to improve the wound dressing's properties. Wettability assessments provided insights into the surface characteristics of the scaffolds, revealing a diverse range of contact angles that reflect varying hydrophilic properties. Notably, the pure PVA/HA sample exhibited a contact angle of approximately 31.2° ± 12.1°, indicating excellent hydrophilicity and a strong capacity for drug absorption. However, the doping of nanoparticles resulted in an raise in contact angles, suggesting a slight reduction in hydrophilicity. Specifically, the addition of HAP produced a contact angle of about 36.5° ± 6.7°, while the addition of Ce₃(VO₄)₄ resulted in a contact angle of approximately 38.6° ± 6.4°. A significant increase in contact angle to 42.23° ± 4.8° was observed when mixing the nanoparticles, though the introduction of Graphene Oxide (GO) reduced the angle to 37.4° ± 0.35°, enhancing the hydrophilic properties of the composite. Cell viability testing was conducted to confirm the biocompatibility and bioactivity of the fabricated scaffolds. The results confirmed the ability of the scaffolds to promote cell growth, with an increase of 88.4 % in cell growth ratio observed at a suitable drug concentration of approximately 0.68 μg/ml. These findings highlight the potential of the developed scaffolds to enhance the wound healing process.

Synthesis, evaluation, and biocompatibility study of magnetite nano particles in normal cells and cancer cells for health care application

Magnetic nanoparticles have been synthesized in a very simple and economical way by the co-precipitation method, where the effect of molar concentrations of ferric chloride anhydrous (FeCl3) and iron (II) sulphate heptahydrate (FeSO4.7 H20) on magnetite synthesis has been investigated. Also, a detailed study was conducted to study the effect of magnetite and hematite on both normal and cancerous cell lines. After this, the magnetic nanoparticles obtained were analyzed by x-ray Diffraction (XRD), scanning electron microscope (SEM) - energy dispersive x-ray (EDX), Fourier transform infrared spectroscopy (FTIR), zeta potential, vibrating sample magnetometer (VSM), atomic force microscopy (AFM), MTT test, and cell apoptotic assay. The XRD peaks for magnetite were easily discernible in the final formulation. SEM images showed round particles in nano ranges, and FTIR peaks showed the presence of magnetite. Zeta potential showed surface charges. VSM showed the magnetic property of magnetite, and AFM confirmed SEM images. It can be concluded that magnetic nanoparticles were synthesized by the co-precipitation method using an optimized molar concentration of reagents. Also, the necessity of coating uncoated magnetic nanoparticles can be seen from the MTT assay. Cell apoptotic assays have shown that synthesized magnetite nanoparticles have shown potential apoptotic activity on cancer cell lines.

Green synthesis of ZnO nanoparticles and biological applications as broad-spectrum bactericidal, antibiofilm effects and biocompatibility studies on Zebrafish embryo

This work generated zinc oxide nanoparticles (ZnO NPs) using Ocimum tenuiflorum in an inexpensive and environmentally friendly manner. The generated ZnO NPs were analysed using Ultra visible spectroscopy (UV–Vis), Fourier transformed infrared spectroscopy (FTIR), Scanning electron microscopy-Energy X-ray diffraction spectroscopy (SEM-EDX), Transmission electron microscopy (TEM), and X-ray diffraction (XRD). Bio-synthesized ZnO NPs showed UV–Visible absorbance maxima at 290 nm, indicating bio reduction and stability. The DRS spectra revealed a straight band gap value of 3.24 eV. Alcohols, alkanes, phenols, and amines in FTIR may contain reduced and capped zinc ions. Crystalline ZnO nanoparticles were verified by XRD. Biosynthesized ZnO NPs were exhibited in spherical and 5–35.49 nm in size by FESEM and TEM. EDX confirmed NPs zinc elemental signatures. Antibacterial properties showed that ZnO NPs effectively inhibited gram (+ve) and gram (−ve) pathogens, including E. coli (20.0 ± 0.8 mm), E. faecalis (20.0 ± 0.5 mm), S. aureus (18.01 ± 1.2 mm), and S. mutans (17.5 ± 1.0 mm). This study shows that biosynthesized ZnO NPs inhibit biofilm growth by 0.198–1.431 O.D values (Optical density). Antibiofilm inhibition was concentration-dependent. Nanoparticles proved effective against E. coli, S. mutans, S. aureus, and E. faecalis with MICs of 15 and 25 µg/mL. Time-dependent death kinetic studies indicated that 8–12 h ZnO NPs killed all bacteria. Also, ZnO NPs had low harmful effects on zebrafish eggs at doses upto 1 mg/mL. In summary, the production of green ZnO NPs offers a sustainable and biocompatible approach that is well-suited for various biological applications.

Unravelling the tissue regenerative nature of marine polysaccharide chitosan embedded halloysite reinforced poly (vinyl alcohol) nanocomposite films

The study focuses on developing the poly (vinyl alcohol) (PVA) nanocomposite films reinforced with Halloysite Nano-Tubes (HNT) which were surface functionalised with chitosan forming a Schiff base structure. The work was aimed to traverse its way in tissue engineering. Modification of halloysite with sea polysaccharide chitosan enhanced its ability to bind to the PVA matrix. The modification was assisted by FTIR, XRD, FESEM, TEM, AFM and DSC-TGA techniques. The films could withstand a higher temperature and exhibited high ranges of tensile strength and Young’s modulus. In addition, biocompatible studies such as in-vitro swelling, enzymatic degradation, water contact angle and hemolysis presented extremely well compatibilities proving it to be viable in physiological pH (in phosphate buffered saline). The cell adhesion and proliferation studies conducted on NIH3T3 mouse fibroblasts revealed the cell proliferation and tissue regeneration properties of the films. Both the tests performed for cell growth- Trypan blue dye exclusion and Acridine Orange Ethidium bromide assays showed a doubled rate of cell growth on the films which proves its biomedical nature.Graphical

Atranorin is a novel potential candidate drug for treating myelodysplastic syndrome

This work is devoted to the study of biocompatibility, cyto- and genotoxicity, mechanism of action and prospects for the use of atranorin, which is an AKT kinase inhibitor, for the treatment of myelodysplastic syndrome. Atranorin was isolated by preparative flash chromatography; identification was carried out by UV, IR, and NMR spectroscopy, mass spectrometry, and elemental analysis. Biocompatibility studies included studies of haemocompatibility, genotoxicity, antioxidant activity, cytotoxicity against ECV340 and HEK293 cell lines. Computer modelling of the interaction of atranorin with AKT kinase was carried out using docking followed by molecular dynamics of the resulting complexes; the ADMET properties of atranorin were also calculated. Flow cytometry included analysis of the expression level of PD-L1 and TIM-3 in the presence of atranorin on THP-1, Mono-Mac-1 and KG-1 cell lines, as well as human bone marrow cells.

Extraction and characterization of biocompatible hydroxyapatite (Hap) from red big eye fish bone: Potential for biomedical applications and reducing biowastes

In this study, nanostructured hydroxyapatite (HAp) was successfully extracted from the bones of Priacanthus macracanthus (Red Big Eye), a species commonly processed in the fish industry, generating significant waste. The extraction process utilized an alkaline hydrolysis method optimized with 2 M sodium hydroxide at 250 °C for 5 h, producing high-purity HAp. Fourier transform infrared spectroscopy (FT-IR) confirmed the presence of characteristic phosphate peaks at 1044 cm⁻¹ and 963 cm⁻¹, and hydroxyl peaks at 632 cm⁻¹. Powder X-ray diffraction (XRD) analysis showed prominent peaks at 2θ values of 25.9°, 32.2°, 39.8°, and 46.7°, corresponding to the crystalline planes of HAp. Field-emission scanning electron microscopy (FESEM) revealed spherical HAp particles with sizes ranging from 50 to 80 nm. Biocompatibility was assessed using human osteoblast-like MG-63 cells, showing a proliferation rate of 92 % compared to the control. Cytotoxicity tests indicated no significant adverse effects, supporting the potential use of this HAp in biomedical applications. Importantly, this method offers a sustainable solution for managing fish bone waste, contributing to pollution control by reducing environmental burdens associated with discarded bone wastes. Future research will focus on in vivo biocompatibility studies and exploring applications in pollution mitigation and tissue engineering. This study highlights the dual benefits of utilizing biowaste for valuable HAp production and addressing environmental pollution challenges, making it a promising approach for sustainable material synthesis and environmental management. The cost-effective and environmentally friendly process further underscores the feasibility of scaling up this method for industrial applications, providing a greener alternative to conventional HAp synthesis.

The elasticity of silicone-stabilized liposomes has no impact on their in vivo behavior

BackgroundThe elastomechanical properties of nanocarriers have recently been discussed as important for the efficient delivery of various therapeutics. Some data indicate that optimal nanocarriers’ elasticity can modulate in vivo nanocarrier stability, interaction with phagocytes, and uptake by target cells. Here, we presented a study to extensively analyze the in vivo behavior of LIP-SS liposomes that were modified by forming the silicone network within the lipid bilayers to improve their elastomechanical properties. We verified liposome pharmacokinetic profiles and biodistribution, including retention in tumors on a mouse model of breast cancer, while biocompatibility was analyzed on healthy mice.ResultsWe showed that fluorescently labeled LIP-SS and control LIP-CAT liposomes had similar pharmacokinetic profiles, biodistribution, and retention in tumors, indicating that modified elasticity did not improve nanocarrier in vivo performance. Interestingly, biocompatibility studies revealed no changes in blood morphology, liver, spleen, and kidney function but indicated prolonged activation of immune response manifesting in increased concentration of proinflammatory cytokines in sera of animals exposed to all tested liposomes.ConclusionIncorporating the silicone layer into the liposome structure did not change nanocarriers’ characteristics in vivo. Further modification of the LIP-SS surface, including decoration with hydrophilic stealth polymers, should be performed to improve their pharmacokinetics and retention in tumors significantly. Activation of the immune response by LIP-SS and LIP-CAT, resulting in elevated inflammatory cytokine production, requires detailed studies to elucidate its mechanism.Graphical