Emulsion Solvent Evaporation Research Articles

A baculoviral gene and drug-eluting (GDES) stent to promote re-endothelialization and prevent restenosis caused by atherosclerosis

Abstract Background Coronary artery disease (CAD) is a prevalent condition affecting approximately one in every 20 individuals over the age of 20, resulting in significant health and economic burdens worldwide. Atherosclerosis, characterized by plaque buildup in the arteries, is a leading cause of CAD, involving endothelial dysfunction, inflammation, and smooth muscle cell hyperproliferation. The standard interventions for CAD, namely bare-metal stents (BMS) or drug-eluting stents (DES), often lead to complications such as blood clotting, inflammation, and arterial re-narrowing, necessitating further interventions and potentially leading to severe outcomes like heart failure, stroke, or death. Additionally, the TGFβ1 gene regulates SMC proliferation and ECM secretion, promoting endothelial cell proliferation, inhibiting smooth muscle cell hyperproliferation, reducing reactive oxygen species production. Purpose This innovative stent aims to mitigate complications associated with conventional stents by promoting endothelial health and preventing inflammation and hyperproliferation downstream. The purpose of this study is to design a new gene and drug eluting stent and evaluate their preclinical efficacy and safety in addressing some of the key limitations of currently available coronary stents. Methods The TGFβ1 expressing baculoviruses loaded PLGA nanoparticles are prepared by double emulsion solvent evaporation method. The formulated nanoparticles were characterized by their surface morphology, particle size, zeta potential, and in vitro release. Moreover, the designed nanoparticles undergo a further investigation for their therapeutic efficiency using cell lines. The GDES is synthesized by dip-coating a BMS into a solution containing Everolimus and genipin carrying baculoviruses expressing TGFβ1 in nanoparticles. The stent elutes the gene and drug over specific durations pertaining to a sustained release profile. The study assesses the functionality and safety of the GDES through in vitro and in vivo experiments, including cell culture studies and animal models. Results The PLGA nanoparticles at 115.3±1.4 nm with a polydipersity (pdi) index of 0.152 have a sustained release profile for the TGFβ1 expressing baculovirus. The findings demonstrate that the GDES effectively promotes endothelial health and prevents inflammation and hyperproliferation downstream. The expression of TGFβ1 facilitates the formation of a fully reconstituted endothelial lining, reducing the risk of complications. Additionally, the prolonged release of Everolimus prevents inflammation and the progression of neointimal hyperplasia. The stent coating and system exhibit non-cytotoxicity and hemocompatibility, ensuring safety during expansion and degradation over time. Overall, the combined action of gene and drug elution in the GDES shows promising results in addressing current complications associated with cardiovascular stents.

RABV antigenic peptide loaded polymeric nanoparticle production, characterization, and preliminary investigation of its biological activity

Nanoparticle-based antigen carrier systems have become a significant area of research with the advancement of nanotechnology. Biodegradable polymers have emerged as particularly promising carrier vehicles due to their ability to address the limitations of existing vaccine systems. In this study, we successfully encapsulated the G5-24 linear peptide, located between amino acids 253 and 275 in the primary sequence of the rabies virus G protein, into biodegradable and biocompatible PLGA copolymer using the double emulsion solvent evaporation method. The resulting nanoparticles had a size of approximately 230.9 ± 0.9074 nm, with a PDI value of 0.168 ± 0.017 and a zeta potential value of -9.86 ± 0.132 mV. SEM images confirmed that the synthesized nanoparticles were uniform in size and distribution. Additionally, FTIR spectra indicated successful peptide loading into the nanoparticles. The encapsulation efficiency of the peptide-loaded nanoparticles was 73.3%, with a peptide loading capacity of 48.2% and a reaction yield of 30.4%. Peptide release studies demonstrated that 65.55% of the peptide was released in a controlled manner over 28 d, following a 'biphasic burst release' profile consistent with the degradation profile of PLGA. This controlled release is particularly beneficial for vaccine studies. Cytotoxicity tests revealed that the R-NP formulation did not induce cytotoxicity in fibroblast cells and enhanced NO production in macrophages, indicating its potential for vaccine development.

Salmon-IgM Functionalized-PLGA Nanosystem for Florfenicol Delivery as an Antimicrobial Strategy against Piscirickettsia salmonis.

Salmonid rickettsial septicemia (SRS), caused by Piscirickettsia salmonis, has been the most severe health concern for the Chilean salmon industry. The efforts to control P. salmonis infections have focused on using antibiotics and vaccines. However, infected salmonids exhibit limited responses to the treatments. Here, we developed a poly (D, L-lactide-glycolic acid) (PLGA)-nanosystem functionalized with Atlantic salmon IgM (PLGA-IgM) to specifically deliver florfenicol into infected cells. Polymeric nanoparticles (NPs) were prepared via the double emulsion solvent-evaporation method in the presence of florfenicol. Later, the PLGA-NPs were functionalized with Atlantic salmon IgM through carbodiimide chemistry. The nanosystem showed an average size of ~380-410 nm and a negative surface charge. Further, florfenicol encapsulation efficiency was close to 10%. We evaluated the internalization of the nanosystem and its impact on bacterial load in SHK-1 cells by using confocal microscopy and qPCR. The results suggest that stimulation with the nanosystem elicits a decrease in the bacterial load of P. salmonis when it infects Atlantic salmon macrophages. Overall, the IgM-functionalized PLGA-based nanosystem represents an alternative to the administration of antibiotics in salmon farming, complementing the delivery of antibiotics with the stimulation of the immune response of infected macrophages.

Mannose targeting of poly(lactic-co-glycolic acid): a promising approach for improving sublingual allergen-specific immunotherapy

Objective One of the most effective treatments for allergic respiratory diseases is allergen-specific sublingual immunotherapy (SLIT). While, mannose targeting has been applied in various immunostimulatory approaches, but it has not been investigated in sublingual allergen-specific immunosuppressive treatment. This study assesses mannose targeting for the ovalbumin (Ova) loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles(NPs). Methods The emulsion-solvent evaporation method was employed for the synthesis of PLGA NPs containing Ova, and subsequently they attached to D-mannose. Ova-sensitized mice underwent treatment in different ways: subcutaneous administration of 10 µg Ova, sublingual administration of 5 and 10 µg Ova loaded in PLGA NPs, 5 and 10 µg Ova loaded in mannose-targeted PLGA NPs, 10 µg Ova, and 10 µg Ova loaded in dendritic cell-specific aptamer-attached PLGA NPs. Serum Ova-specific IgE and IgG2a levels, as well as IFN-γ, IL-4, IL-10, and IL-17a levels in the supernatant of Ova-stimulated splenocytes were measured. Splenocyte proliferation was assessed using an MTT assay, and also lung histological examinations, and nasal lavage fluid cell counting were performed. Results Ova-specific IgE, IL-4, IL-17a levels, eosinophil cell count, and splenocyte proliferation were remarkably reduced in the mice treated with mannose or aptamer targeted NPs compared to other groups. Also, IL-10 and IFN-γ levels were remarkably increased in the targeted NPs groups. Conclusion Our findings indicated that mannose targeting of PLGA NPs could decrease allergen dose and improve immunomodulatory effects of SLIT. However, this approach suggests an effective formulation for SLIT in the mice model, further studies with common allergens are needed for application in humans.

A Review on Nanoparticles : The Building Blocks of Tomorrows Technology

Nanoparticles, defined as particles with dimensions in the nanometer range, exhibit unique properties that differ from their bulk counterparts, making them invaluable across various fields such as medicine, electronics, and environmental protection. Their small size and specific characteristics enable advanced applications, including targeted drug delivery, enhanced imaging, and improved sensors. Notable types of nanoparticles include silver, gold, magnetic, iron oxide, and platinum, each with distinct uses: silver for antimicrobial applications, gold for protein detection and drug delivery, magnetic for drug delivery and bio sensing, iron oxide for diagnostics and therapy, and platinum for catalysis. Nanoparticles are synthesized through top-down methods like milling and laser ablation, and bottom-up approaches such as sol-gel and hydrothermal processes. Their preparation involves techniques like emulsion-solvent evaporation and polymerization. Effective characterization, including analysis of size, shape, zeta potential, and drug entrapment efficiency, is essential for optimizing their performance in various applications. The review's current focus is on the synthesis, types, characterization, and most advanced applications of nanotechnology.

Se-incorporated polycaprolactone spherical polyhedron enhanced vitamin B2 loading and prolonged release for potential application in proliferative skin disorders

Development of novel drug vehicles for vitamin B2 (VitB2) delivery is very important for designing controllable release system to improve epidermal growth and bone metabolism. In this work, selenium (Se)-incorporated polycaprolactone (PCL) spherical polyhedrons are successfully synthesized via a single emulsion solvent evaporation method which is utilized to load VitB2 to fabricate cell-responsive Se-PCL@VitB2 delivery systems. Their physicochemical properties are characterized by DLS, SEM, XRD, FTIR, and TGA-DSC. The release kinetics of VitB2 or Se from the samples are investigated in PBS solution (pH = 2.0, 5.0, 7.4, 8.0 and 12.0). The cytocompatibilities are also evaluated with normal BMSC and epidermal HaCat cells. Results exhibit that Se-PCL@VitB2 particles presents spherical polyhedral morphology (approximately (3.25 ± 0.46) μm), negative surface charge (-(54.03 ± 2.94) mV), reduced crystallinity and good degradability. Stability experiments imply that both VitB2 and Se might be uniformly dispersed in PCL matrix. And the incorporation of Se facilely promotes the loading of VitB2. The encapsulation efficiency and loading capacity are (98.42 ± 1.06)% and (76.25 ± 1.27) for Se-PCL@VitB2 sample. Importantly, it exhibits more prolonged release of both VitB2 and Se in neutral PBS solution (pH = 7.4) than other pH conditions. Presumably, the electrostatic interaction between Se, VitB2 and PCL contribute to its release mode. Cell experiments show that Se-PCL@VitB2 presents strong cytotoxicity to HaCat cells mainly due to the cytotoxic effect of Se anions and PCL degradation products. However, it exhibits weak inhibitory effect on BMSC cells. These note that the synthesized Se-PCL@VitB2 particles can be promising drug vehicles for potential application in epidermal proliferative disorders.

Basil seed mucilage as a bioadhesive polymer: Development of naproxen sodium microspheres and suppositories with in-vitro and ex-vivo studies

Background and purpose: The study explores basil seed mucilage as a bioadhesive carrier for naproxen sodium, demonstrating its ability to enhance solubility when administered rectally. The mucilage, derived from Ocimum basilicum seeds, showed bioadhesive properties and thermal stability, as confirmed by FTIR spectroscopy and X-ray diffraction analysis. Experimental approach: Microspheres were prepared using a double emulsion solvent evaporation technique, varying polymer ratios to optimize drug delivery. Key results: Particle size analysis revealed a range of 456±0.51 to 712±0.21 µm, with larger microspheres formed at higher mucilage concentrations due to increased viscosity. Encapsulation efficiency ranged from 45.01±0.25 % to 79.4±0.93 %, improving with higher basil/alginate ratios. The superior batch, OBM5, showed excellent mucoadhesive qualities in ex-vivo assays, attributed to the increased polymer content, facilitating interaction with rectal mucosa. SEM analysis of OBM5 indicated a spherical, monolithic structure conducive to free flow. Drug release was efficient, with OBM5 achieving 88.7±1.3 % after 7 hours, indicating a control­led release profile. Conclusion: Incorporated into polyethylene glycol (PEG) 4000 suppositories, suppose­tories were completely disintegrated in buffer solution within 25 minutes. The bioadhesive force of basil seed mucilage on rectal mucosa was significantly enhanced, reaching 6.44±0.58 g, correlating with mucilage concentration. These findings underscore the efficacy of basil seed mucilage as a bioadhesive biopolymer for rectal drug delivery systems.

Chitosan Oligosaccharide Modified Bovine Serum Albumin Nanoparticles for Improving Oral Bioavailability of Naringenin.

With the rapid development of nanotechnology, the research and development of nano-drugs have become one of the development directions of drug innovation. The encapsulation of the nanoparticles can change the biological distribution of the drug in vivo and improve the bioavailability of the drug in vivo. Naringenin is poorly soluble in water and has a low bioavailability, thus limiting its clinical application. The main purpose of this study was to develop a nano-sized preparation that could improve the oral bioavailability of naringenin. Chitosan oligosaccharide modified naringenin-loaded bovine serum albumin nanoparticles (BSA-COS@Nar NPs) were prepared by emulsification solvent evaporation and electrostatic interaction. The nanoparticles were characterized by HPLC, laser particle size analyzer, transmission electron microscope and X-ray diffraction analysis. The release in vitro was investigated, and the behavior of nanoparticles in rats was also studied. The caco-2 cell model was established in vitro to investigate the cytotoxicity and cellular uptake of nanoparticles. BSA-COS@Nar NPs were successfully prepared, and the first-order release model was confirmed in vitro release. In vivo pharmacokinetic results indicated that the area under the drug concentration- time curve (AUC) of BSA-COS@Nar NPs was 2.37 times more than free naringenin. Cytotoxicity and cellular uptake results showed that BSA-COS@Nar NPs had no significant cytotoxic effect on Caco- 2 cells and promoted cellular uptake of the drug. BSA-COS@Nar NPs could improve the in vivo bioavailability of naringenin.

Nanospheres as the delivery vehicle: novel application of Toxoplasma gondii ribosomal protein S2 in PLGA and chitosan nanospheres against acute toxoplasmosis.

Toxoplasma gondii (T. gondii) is a zoonotic disease that poses great harm to humans and animals. So far, no effective T. gondii vaccine has been developed to provide fully protection against such parasites. Recently, numerous researches have focused on the use of poly-lactic-co-glycolic acid (PLGA) and chitosan (CS) for the vaccines against T. gondii infections. In this study, we employed PLGA and CS as the vehicles for T. gondii ribosome protein (TgRPS2) delivery. TgRPS2-PLGA and TgRPS2-CS nanospheres were synthesized by double emulsion solvent evaporation and ionic gelation technique as the nano vaccines. Before immunization in animals, the release efficacy and toxicity of the synthesized nanospheres were evaluated in vitro. Then, ICR mice were immunized intramuscularly, and immune protections of the synthesized nanospheres were assessed. The results showed that TgRPS2-PLGA and TgRPS2-CS nanospheres could induce higher levels of IgG and cytokines, activate dendritic cells, and promote the expression of histocompatibility complexes. The splenic lymphocyte proliferation and the enhancement in the proportion of CD4+ and CD8+ T lymphocytes were also observed in immunized animals. In addition, two types of nanospheres could significantly inhabit the replications of T. gondii in cardiac muscles and spleen tissues. All these obtained results in this study demonstrated that the TgRPS2 protein delivered by PLGA or CS nanospheres provided satisfactory immunoprotective effects in resisting T. gondii, and such formulations illustrated potential as prospective preventive agents for toxoplasmosis.

Preparation, Characterization and Evaluation of Monosaccharide Tagged Nanostructured Lipid Carriers for Targeting of Etravirine to Macrophagic AIDS Viral Reservoirs.

Purpose of the study: The present study aimed to develop and examine monosaccharide-decorated nanoparticles specifically designed for macrophage targeting of etravirine. Methods: Nanostructured lipid carriers (NLC) were prepared with stearylamine as such or after tagging with mannose and galactose as one of the lipid components of NLC. Prior to synthesis, a docking study was used to analyze the potential for interaction of the stearylamine- sugar conjugates with respective lectin receptors. Mannose and galactose-conjugated stearylamine were separately synthesized. Fourier-transform infrared spectroscopy (FTIR), mass spectrometry (MS) and nuclear magnetic resonance (NMR) studies were used to assess successful reactions. Etravirine-loaded non-targeted nanostructured lipid carriers (NLCs) were synthesized with the emulsification solvent evaporation method and characterized for parameters such as zeta potential, in-vitro release, entrapment efficiency and particle size. To create targeted nanoparticles, stearylamine was replaced with either of the conjugated lipids in the formulation. For stability, all NLC dispersions were lyophilized. In-vitro investigations included cellular uptake and cytotoxicity assessments in the RAW 264.7 macrophage cell line. Following intravenous administration of the NLCs in Wistar rats, in-vivo biodistribution was evaluated. Results: The docking studies showed good binding potential of both conjugated lipids for respective receptors. Evaluation of synthesized products showed successful conjugation of sugars to stearylamine. The synthesized nanoparticles demonstrated impressive etravirine loading capabilities and exhibited a circular shape with a mean size of approximately 260 nm. Drug release from all NLC formulations persisted for over 24 hours and remained stable after lyophilization. In-vitro evaluations in the RAW 264.7 macrophage cell line revealed that mannosylated nanoparticles had enhanced uptake when compared to non-targeted and galactosylated counterparts. In-vivo plasma and tissue distribution studies corroborated the in-vitro findings, as the mannosylated NLCs displayed a higher distribution into organs with a rich presence of macrophages. Conclusion: The studies indicate that while sugar tagging of nanoparticles can prove to be an effective strategy for targeting drugs to macrophagic tissue for tackling latent AIDS virus, the choice of sugar is critical.

Design, Devlopment and Evaluation of Gastroretentive Floating Microspheres of Glibenclamide: In-vitro In-vivo Studies .

The current research study was designed to characterize the ethyl cellulose act as a carrier mediator used to prepare a floating microsphere of glibenclamide for developed gastroretentive sustain release floating drug delivery. Different microspheres of glibenclamide were formulated by the emulsion solvent evaporation technique of glibenclamide with EC in different ratios by using two solvent systems (ethanol and chloroform). After evaluating the micropolitics properties, %of yield value, drug loading efficiency, entrapment efficiency, diameter and surface morphology of the microsphere by using DLS and SEM, in-vitro drug release in gastric content, in-vitro buoyancy, and in-vivo floatation using animal model, compatibility study by FTIR, DSC and any other analytical study to demonstrate all formulation (especially GM2) was showing excellent results. So this work shows great gastro etentive floating drug delivery system for prolonged periods of time which is very useful in future for further study.

Neutrophil membrane-coated multifunctional biomimetic nanoparticles for spinal cord injuries

Spinal cord injury (SCI) is one of the most complex diseases. After SCI, severe secondary injuries can cause intense inflammatory storms and oxidative stress responses, leading to extensive neuronal apoptosis. Effective regulation of inflammation and oxidative stress after SCI remains an unresolved challenge. In this study, resveratrol-loaded nanoparticles coated with neutrophil membranes (NMR) were prepared using the emulsion-solvent evaporation method and membrane encapsulation technology. Multifunctional biomimetic nanoparticles retain neutrophil membrane-related receptors and possess a strong adsorption capacity for inflammatory factors. As a drug carrier, NMR can sustainably release resveratrol for >72 h. Moreover, co-culture studies in vitro show that the NMR help regulate macrophage polarization to relieve inflammatory response, reduce intracellular reactive oxygen species by approximately 50%, and improve mitochondrial membrane potential to alleviate oxidative stress. After injecting NMR into the injury site, it reduces early apoptosis, inhibit scar formation, and promote neural network recovery to improve motor function. This study demonstrates the anti-inflammatory, antioxidant, and neuroprotective effects of NMR, thus providing a novel therapeutic strategy for SCI.

Formulation and evaluation of herbal microsphere gel

Formulation and evaluation of herbal microsphere gel involves designing a gel-based delivery system for herbal active ingredients encapsulated within microspheres. The process typically includes selecting suitable herbal extracts, encapsulating them into microspheres using techniques like solvent evaporation or emulsion-solvent evaporation, and then incorporating these microspheres into a gel base. Evaluation criteria may include physical characteristics (particle size, morphology), drug release kinetics, rheological properties, stability, and efficacy of the herbal ingredients. This approach aims to enhance the stability, controlled release, and therapeutic efficacy of herbal compounds, offering potential applications in various fields including pharmaceuticals, cosmetics, and personal care products. This present study demonstrated the effectiveness of carbopol based herbal gel containing extracts of tamarind possessing antibacterial activity. Thus, the formulated herbal gel incorporated with tamarind extracts show great promises in the management of antibacterial activity. Gel loaded with microspheres of tamarind was prepared with aim to deliver the drug which passes through transdermal route as it provides quick onset of action when compared to oral route. This gel loaded with microspheres of tamarind was successfully prepared using solvent evaporation method.

Preparation and In Vitro Characterization of Carbamazepine-Loaded Chitosan-Coated/Uncoated PLGA and Zein Nanoparticles

The aim of this study is to prepare CBZ-loaded chitosan (Ch)- coated/uncoated poly(lactic-co-glycolic acid) (PLGA) and Zein (using 20 mg or 40 mg Zein) nanoparticles (CBZ-PLGA-Zein-NPs or CBZ-PLGA-Zein-Ch-NPs) and to characterize (Particle size, PDI, zeta potential, percent encapsulation efficiency (EE%), FT-IR, DSC and XRD analyzes, and in vitro release study) them in vitro. These nanoparticles were prepared using a modified emulsification-solvent evaporation method. The particle sizes of CBZ-PLGA-Zein(20)-NPs, CBZ-PLGA-Zein(40)-NPs and CBZ-PLGA-Zein(20)-Ch-NPs were found to be about 222 nm, 245 nm and 221 nm, respectively. The PDI value of all NP formulations was below 0.3. This indicates a narrow particle size distribution. The EE% values of CBZ-PLGA-Zein(20)-NPs, CBZ-PLGA-Zein(40)-NPs and CBZ-PLGA-Zein(20)-Ch-NPs were determined as about 64%, 56% and 62%, respectively. The coating of the optimum formulation (containing 20 mg Zein) with chitosan did not lead to a significant difference in the particle size and EE% value of this formulation (P>0.05). A sustained release of CBZ from all prepared NPs formulations was achieved until 48th h. In conclusion, CBZ-PLGA-Zein(20 mg or 40 mg)-NPs and CBZ-PLGA-Zein(20 mg)-Ch-NPs were successfully prepared and characterized in vitro.

Optimization and evaluation of a chitosan-coated PLGA nanocarrier for mucosal delivery of Porphyromonas gingivalis antigens

Recent advances in understanding Alzheimer's disease (AD) suggest the possibility of an infectious etiology, with Porphyromonas gingivalis emerging as a prime suspect in contributing to AD. P. gingivalis may invade systemic circulation via weakened oral/intestinal barriers and then cross the blood-brain barrier (BBB), reaching the brain and precipitating AD pathology. Based on the proposed links between P. gingivalis and AD, a prospective approach is the development of an oral nanovaccine containing P. gingivalis antigens for mucosal delivery. Targeting the gut-associated lymphoid tissue (GALT), the nanovaccine may elicit both mucosal and systemic immunity, thereby hampering P. gingivalis ability to breach the oral/intestinal barriers and the BBB, respectively.The present study describes the optimization, characterization, and in vitro evaluation of a candidate chitosan-coated poly(lactic-co-glycolic acid) (PLGA-CS) nanovaccine containing a P. gingivalis antigen extract. The nanocarrier was prepared using the double emulsion solvent evaporation method and optimized for selected experimental factors, e.g. PLGA amount, surfactant concentration, w1/o phase ratio, applying a d-optimal statistical design to target the desired physicochemical criteria for its intended application. After nanocarrier optimization, the nanovaccine was characterized in terms of particle size, polydispersity index (PdI), ζ-potential, encapsulation efficiency (EE), drug loading (DL), morphology, and in vitro release profile, as well as for mucoadhesivity, stability under simulated gastrointestinal conditions, antigen integrity, in vitro cytotoxicity and uptake using THP-1 macrophages.The candidate PLGA-CS nanovaccine demonstrated appropriate physicochemical, mucoadhesive, and antigen release properties for oral delivery, along with acceptable levels of EE (55.3 ± 3.5 %) and DL (1.84 ± 0.12 %). The integrity of the encapsulated antigens remained uncompromised throughout NPs production and simulated gastrointestinal exposure, as confirmed by SDS-PAGE and Western blotting analyses. Furthermore, the nanovaccine showed effective in vitro uptake, while exhibiting low cytotoxicity. Taken together, these findings underscore the potential of PLGA-CS NPs as carriers for adequate antigen mucosal delivery, paving the way for further investigations into their applicability as vaccine candidates against P. gingivalis.

Two-step emulsification for the fabrication of homogeneous PCL microspheres encapsulating geniposidic acid with antioxidant properties

The mortality rate of neurological disorders is increasing globally, and natural antioxidant geniposidic acid (GPA) holds great potential in the treatment of neuronal oxidative damage. Nevertheless, its inherent instability constrains its pragmatic utilization. Herein, we introduced a drug delivery system capable of protecting unstable natural active compounds from degradation. Among the various methods for preparing drug-loaded microspheres, the emulsification-solvent evaporation technique is one of the most commonly employed due to its efficiency and simplicity. Nevertheless, this method results in microspheres with heterogeneous particle sizes. To address this limitation, we developed a two-step emulsification method involving stirring and homogenization. Using the biocompatible, synthetic, biodegradable polymer polycaprolactone (PCL) as the drug delivery carrier, we prepared GPA-loaded PCL microspheres via the two-step emulsification method. The results demonstrated that the microspheres possessed uniform particle size (polydispersity index = 0.12), excellent drug loading capacity (∼4.86%), sustained drug release profiles (∼68.55% in 264 h), and biocompatibility (cell viability >85%). The in vitro tests showed that the microspheres exerted antioxidant effects by scavenging reactive oxygen species (ROS) induced by oxidative stress, thereby protecting neuronal cells from oxidative damage. This work presents a promising new approach for the treatment of neuronal oxidative damage.

Magnetically targeted lidocaine sustained-release microspheres: optimization, pharmacokinetics, and pharmacodynamic radius of effect

ObjectiveThis study aimed to optimize the formulation of magnetically targeted lidocaine microspheres, reduce the microsphere particle size, and increase the drug loading and encapsulation rate of lidocaine. The optimized microspheres...

Development and characterization of palbociclib-loaded PLGA nanobubbles for targeted cancer therapy

The objective of this study was to develop and optimize palbociclib-loaded nanobubbles for targeted breast cancer therapy. Biocompatible poly(DL-lactide-co-glycolide) was used to create nanobubbles loaded with palbociclib. The formulation process was meticulously crafted using a three-level Box-Behnken design and a double emulsion solvent evaporation method to precisely tailor the nanobubbles' properties. The Derringer's desirability method optimized variables by transforming responses into a desirability scale, resulting in a global desirability value. Optimal settings, A: 526.97 mg, B: 250 mg, C: 2.0% w/v, D: 6101 rpm, achieved a D value of 0.949. Palbociclib nanobubbles demonstrated a smaller particle size (31.78 ± 2.12) than plain nanobubbles (38.56 ± 3.56). PDI values indicated a uniform size distribution. The zeta potential remained consistent, with values of -31.34 ± 3.36 for plain and -31.56 ± 3.12 for drug-loaded nanobubbles. Encapsulation efficiency was 70.12%, highlighting effective drug encapsulation. Palbociclib release was significantly higher from nanobubbles in pH 7.4, especially with ultrasound, releasing almost 99.34% of the drug. Hemolytic activity assays confirmed safety for injection. Fluorescent intensity analysis revealed a two-fold increase in cellular uptake of palbociclib facilitated by ultrasound. The MTT assay demonstrated enhanced cytotoxicity of palbociclib-loaded nanobubbles, especially with ultrasound, emphasizing their potential for improved therapeutic efficacy. The IC50 values for palbociclib, without ultrasound, and with ultrasound were 98.3 μM, 72.34 μM, and 61.34 μM, respectively. The significant findings of this study emphasize the potential of palbociclib-loaded nanobubbles as a promising therapeutic system for improved breast cancer treatment.

Dexamethasone-loaded PLGA porous microspheres used as 3D-bioprinted bioink promote tissue-engineered cartilage regeneration

The current investigation focused on fabricating and thoroughly analyzing porous microspheres (MPs) comprising poly (lactic-co-glycolic acid, PLGA) encapsulating dexamethasone, by utilizing the water-in-oil-in-water (W/O/W) emulsion solvent evaporation technique. The meticulous characterization encompassed various parameters, including particle size distribution, morphology, and polymer integrity, all of which exhibited consistent attributes across the MPs populations. The analysis of drug content and release kinetics revealed a sustained and controlled liberation of dexamethasone, characterized by an initial burst release within the initial 3 days followed by a gradual, protracted release profile. Subsequent in vivo assessments further validated the potent anti-inflammatory effects of the dexamethasone-loaded PLGA MPs, as evidenced by notable reductions in CD86 immunohistochemical staining intensity, along with the change in membrane thickness. Additionally, the MPs demonstrated an impressive capability to support the maintenance of cartilage phenotype, as indicated by the augmented secretion of cartilage matrix components and elevated glycosaminoglycan content.  

A Comparative Study of Using Poly (D, L, Lactide-co-Glycolic Acid) and Chitosan Nanoparticle as Vaccine Delivery System for a Recombinant Fusion Protein of Newcastle Disease Virus

Introduction: The more effective method of preventing many infectious diseases is vaccination. Numerous infectious diseases that affect both humans and animals have significantly decreased as a result of routine immunization. Aim: The present study aimed to compare the efficacy of in-house built chitosan and Polylactide coglycolic acid (PLGA) nanoparticles coupled with Pichia pastoris expressed immunogenic fusion (F) protein of Newcastle disease (ND). Objectives: Synthesis of biodegradable nanoparticles such as PLGA and chitosan offers a promising opportunity as a vaccine delivery system. Methods: Chitosan nanoparticles and PLGA nanoparticles were synthesized by ionic gelation, and double emulsion solvent evaporation, respectively, and the size was 38.6± 0.84 nm and 320 ±1.5nm, respectively. They demonstrated good epitope integrity of recombinant fusion protein and in vitro release kinetics studies have proved consistent release profile of protein Results: In vivo pathogenicity assay of separately injected nanoparticles has proved no abnormal signs and mortality in chickens. Specific pathogen-free (SPF) chicks were vaccinated with chitosan and PLGA nanoparticles and a recombinant fusion protein of the ND virus. It was demonstrated that PLGA nanoparticles coupled with a fusion protein of Newcastle disease virus conferred a marginally better immune response than chitosan nanoparticles. Comparative study-based results showed that PLGA-based nanoparticles proved a better vaccine delivery vehicle and generated an effective immune response without needing further adjuvants. Conclusion: The present study is a scientific platform for developing the PLGA-based vaccine delivery vehicle to improve immune responses against many infectious diseases.