Double Emulsion Solvent Evaporation Technique Research Articles

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.

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.

Targeted polymeric primaquine nanoparticles: optimization, evaluation, and in-vivo liver uptake for improved malaria treatment

Primaquine (PQ) is a widely used antimalarial drug, but its high dosage requirements can lead to significant tissue damage and adverse gastrointestinal and hematological effects. Recent studies have shown that nanoformulations can enhance the bioavailability of pharmaceuticals, thereby increasing efficacy, reducing dosing frequency, and minimizing toxicity. In this study, PQ-loaded PLGA nanoparticles (PQ-NPs) were prepared using a modified double emulsion solvent evaporation technique (w/o/w). The PQ-NPs exhibited a mean particle size of 228 ± 2.6 nm, a zeta potential of +27.4 mV, and an encapsulation efficiency of 81.3 ± 3.5%. Scanning electron microscopy (SEM) confirmed their spherical morphology, and the in vitro release profile demonstrated continuous drug release over 72 h. Differential scanning calorimetry (DSC) thermograms indicated that the drug was present in the nanoparticles, with improved physical stability. Fourier-transform infrared spectroscopy (FTIR) analysis showed no interactions between the various substances in the NPs. In vivo studies in Swiss albino mice infected with Plasmodium berghei revealed that the nanoformulated PQ was 20% more effective than the standard oral dose. Biodistribution studies indicated that 80% of the NPs accumulated in the liver, highlighting their potential for targeted drug delivery. This research demonstrates the successful development of a nanomedicine delivery system for antimalarial drugs, offering a promising strategy to enhance treatment efficacy while reducing adverse effects.

IN VITRO EVALUATION OF THE ANTIBACTERIAL EFFECT OF CHITOSAN COATED TEICOPLANIN-LOADED LIPID NANOPARTICLES AGAINST STAPHYLOCOCCUS AUREUS

Objective: The aim of this research is to formulate teicoplanin-loaded solid lipid nanoparticles (SLN) coated with chitosan to sustain teicoplanin release for effective antibacterial therapy. Material and Method: “Double emulsion-solvent evaporation technique was used for the production of SLNs. The nanoparticles were characterised in terms of morphology, size, encapsulation efficacy, in-vitro drug release and antibacterial activity studies after optimization of process and formulation parameters. Result and Discussion: Transmission electron microscopy images confirmed the formation of spherical SLNs. With chitosan coating, the size increased (from 80 nm to 106 nm) and the negative value of zeta potential (- 11.29) changed to positive (+34.41). The in-vitro release data showed prolonged release of teicoplanin from optimized SLN and chitosan-coated SLN (c-SLN) formulations over 1 week. The antibacterial activity study (S. aureus and Methicillin-resistant S. aureus) showed the activity of the teicoplanin loaded SLN formulations. In conclusion, this study demonstrated the potential of c-SLN for effective delivery of teicoplanin.

Construction of recombinant Omp25 or EipB protein loaded PLGA nanovaccines for Brucellosis protection

Safe and effective vaccine candidates are needed to address the limitations of existing vaccines against Brucellosis, a disease responsible for substantial economic losses in livestock. The present study aimed to encapsulate recombinant Omp25 and EipB proteins, knowledged antigen properties, into PLGA nanoparticles, characterize synthesized nanoparticles with different methods, and assessed their in vitro/in vivo immunostimulatory activities to develop new vaccine candidates. The recombinant Omp25 and EipB proteins produced with recombinant DNA technology were encapsulated into PLGA nanoparticles by double emulsion solvent evaporation technique. The nanoparticles were characterized using FE-SEM, Zeta-sizer, and FT-IR instruments to determine size, morphology, zeta potentials, and polydispersity index values, as well as to analyze functional groups chemically. Additionally, the release profiles and encapsulation efficiencies were assessed using UV–Vis spectroscopy. After loading with recombinant proteins, O-NPs reached sizes of 221.2 ± 5.21 nm, while E-NPs reached sizes of 274.4 ± 9.51 nm. The cumulative release rates of the antigens, monitored until the end of day 14, were determined to be 90.39% for O-NPs and 56.1% for E-NPs. Following the assessment of the in vitro cytotoxicity and immunostimulatory effects of both proteins and nanoparticles on the J774 murine macrophage cells, in vivo immunization experiments were conducted using concentrations of 16 µg ml−1 for each protein. Both free antigens and antigen-containing nanoparticles excessively induced humoral immunity by increasing produced Brucella-specific IgG antibody levels for 3 times in contrast to control. Furthermore, it was also demonstrated that vaccine candidates stimulated Th1-mediated cellular immunity as well since they significantly raised IFN-gamma and IL-12 cytokine levels in murine splenocytes rather than IL-4 following to immunization. Additionally, the vaccine candidates conferred higher than 90% protection from the infection according to challenge results. Our findings reveal that PLGA nanoparticles constructed with the encapsulation of recombinant Omp25 or EipB proteins possess great potential to trigger Brucella-specific humoral and cellular immune response.

Optimisation of microencapsulation efficiency of propolis phenolic compounds by double emulsion method using response surface methodology

AbstractThe aim of this study was to optimise the microencapsulation efficiency of propolis phenolic compounds by double emulsion solvent evaporation technique (W1/O/W2). The solvent/sample ratio and the polymer and surfactant concentration parameters were optimised using response surface methodology (RSM) through Box–Behnken Design (BBD). For each parameter studied, total phenolic content encapsulation efficiency (TPCEE), free radical scavenging activity (DPPH), and ferric reducing antioxidant power (FRAP) were evaluated. The results showed that the optimal parameters were: 31.60 mg mL−1 for sample/solvent ratio, 606.28 mg mL−1 for poly(ε-caprolactone) (PCL) concentrations, and 2.05 g mL−1 for poly(vinyl alcohol) (PVA) concentration. The optimum values obtained were: 84.62% for encapsulation efficiency of phenolic content, 51.89% for DPPH, and 48,733 mg Trolox Equivalent/100 g dry weight for FRAP. The experimental checking of results revealed the validity of elaborated models and their suitability for the prediction of both responses. The developed mathematical models have expressed a high level of significance through RSM optimisation processes for phenolic antioxidants of propolis.

Synthesis and characterization of tenofovir disoproxil fumarate loaded nanoparticles for HIV‐1 treatment

AbstractThe remarkable ability of the human immunodeficiency virus (HIV) to evade the host's immune system and conventional antiretroviral therapy, has posed significant challenges in achieving complete eradication of the virus in people living with HIV (PLWHIV). However, nanotechnology has emerged as promising avenue for addressing some of the obstacles associated with the use of antiretroviral drugs by modifying drug molecules in nanoscale dimensions. Hence, the present study explores the utilization of poly(epsilon‐caprolactone) (PCL) as a carrier for encapsulating tenofovir disoproxil fumarate (TDF), offering an alternative treatment approach for HIV infection. TDF‐loaded polymeric nanoparticles were successfully prepared using double emulsion solvent evaporation technique and characterized. The characterization of TDF‐loaded polymeric nanoparticles at varied drug to polymer ratios showed that TDF was loaded in PCL with an encapsulation efficiency and drug loading capacity in the range of 23–46% and 4.8–19.9%, respectively. Of note, the neutralization efficacy of TDF‐loaded polymeric nanoparticles was more improved compared to free TDF. Encapsulation of TDF with PCL did not hinder the antiviral activity of TDF against HIV‐1 infection but rather enhanced its potency.

Aerosolizable Pyrazinamide-Loaded Biodegradable Nanoparticles for the Management of Pulmonary Tuberculosis.

Background: Pyrazinamide is a Biopharmaceutical Classification System class III antibiotic indicated for active tuberculosis. Methods: In the present work, pyrazinamide-loaded biodegradable polymeric nanoparticles (PNPs) based dry powder inhaler were developed using the double emulsion solvent evaporation technique and optimized using design of experiments to provide direct pulmonary administration with minimal side effects. Batches were characterized for various physicochemical and aerosol performance properties. Results: Optimized batch exhibited particle size of 284.5 nm, % entrapment efficiency of 71.82%, polydispersibility index of 0.487, zeta potential of -17.23 mV, and in vitro drug release at 4 hours of 79.01%. Spray-dried PNPs were evaluated for drug content, in vitro drug release, and kinetics. The particle mass median aerodynamic diameter was within the alveolar region's range (2.910 μm). In the trachea and lung, there was a 2.5- and 1.2-fold increase in in vivo deposition with respect to pure drug deposition, respectively. In vitro drug uptake findings showed that alveolar macrophages with pyrazinamide PNPs had a considerably higher drug concentration. Furthermore, accelerated stability studies were carried out for the optimized batch. Results indicated no significant change in the evaluation parameters, which showed stability of the formulation for at least a 6-month period. Conclusion: PNPs prepared using biodegradable polymers exhibited efficient pulmonary drug delivery with decent stability.

PLGA-Encapsulated Haemonchus contortus Antigen ES-15 Augments Immune Responses in a Murine Model.

Haemonchus contortus is a gastrointestinal parasite that adversely impacts small ruminants, resulting in a notable reduction in animal productivity. In the current investigation, we developed a nanovaccine by encapsulating the recombinant protein rHcES-15, sourced from the excretory/secretory products of H. contortus, within biodegradable poly (D, L-lactide-co-glycolide) (PLGA) nanoparticles (NPs). The development of this nanovaccine involved the formulation of PLGA NPs using a modified double emulsion solvent evaporation technique. Scanning electron microscopy (SEM)verified the successful encapsulation of rHcES-15 within PLGA NPs, exhibiting a size range of 350-400 nm. The encapsulation efficiency (EE) of the antigen in the nanovaccine was determined to be 72%. A total of forty experimental mice were allocated into five groups, with the nanovaccine administered on day 0 and the mice euthanized at the end of the 14-day trial. The stimulation index (SI) from the mice subjected to the nanovaccine indicated heightened lymphocyte proliferation (*** p < 0.001) and a noteworthy increase in anti-inflammatory cytokines (IL-4, IL-10, and IL-17). Additionally, the percentages of T-cells (CD4+, CD8+) and dendritic cell phenotypes (CD83+, CD86+) were significantly elevated (** p < 0.01, *** p < 0.001) in mice inoculated with the nanovaccine compared to control groups and the rHcES-15 group. Correspondingly, higher levels of antigen-specific serum immunoglobulins (IgG1, IgG2a, IgM) were observed in response to the nanovaccine in comparison to both the antigenic (rHcES-15) and control groups (* p < 0.05, ** p < 0.01). In conclusion, the data strongly supports the proposal that the encapsulation of rHcES-15 within PLGA NPs effectively triggers immune cells in vivo, ultimately enhancing the antigen-specific adaptive immune responses against H. contortus. This finding underscores the promising potential of the nanovaccine, justifying further investigations to definitively ascertain its efficacy.

Microfluidic-assisted preparation of PLGA nanoparticles loaded with insulin: a comparison with double emulsion solvent evaporation method

Poly lactic-co-glycolic acid (PLGA) is an ideal polymer for the delivery of small and macromolecule drugs. Conventional preparation methods of PLGA nanoparticles (NPs) result in poor control over NPs properties. In this research, a microfluidic mixer was designed to produce insulin-loaded PLGA NPs with tuned properties. Importantly; aggregation of the NPs through the mixer was diminished due to the coaxial mixing of the precursors. The micromixer allowed for the production of NPs with small size and narrow size distribution compared to the double emulsion solvent evaporation (DESE) method. Furthermore, encapsulation efficiency and loading capacity indicated a significant increase in optimized NPs produced through the microfluidic method in comparison to DESE method. NPs prepared by the microfluidic method were able to achieve a more reduction of trans-epithelial electrical resistance values in the Caco-2 cells compared to those developed by the DESE technique that leads to greater paracellular permeation. Compatibility and interaction between components were evaluated by differential scanning calorimetry and fourier transform infrared analysis. Also, the effect of NPs on cell toxicity was investigated using MTT test. Numerical simulations were conducted to analyze the effect of mixing patterns on the properties of the NPs. It was revealed that by decreasing flow rate ratio, i.e. flow rate of the organic phase to the flow rate of the aqueous phase, mixing of the two streams increases. As an alternative to the DESE method, high flexibility in modulating hydrodynamic conditions of the microfluidic mixer allowed for nanoassembly of NPs with superior insulin encapsulation at smaller particle sizes.

Retraction note to: Treatment of methicillin resistant Staphylococcus aureus wound infection using vancomycin-loaded nanoparticles: An in vitro and in vivo study.

Due to the rise of bacteria that are resistant to multiple drugs, treating infections in burn wounds has become a worldwide problem. It is important to find new ways to treat these infections. Lipid-based drug delivery systems have emerged as a promising type of carrier for antibiotics as well as antibacterial agents, such as antimicrobial peptides and nucleic acids, for wound infections. To this end, the current study assessed the antibacterial effects and wound healing properties of vancomycin-loaded solid lipid nanoparticles (SLN) against methicillin-resistant Staphylococcus aureus (MRSA) surgical wound infections. vancomycin-SLN was synthesized by double emulsion solvent evaporation techniques, and then in vitro antibacterial activity was evaluated by well diffusion and broth microdilution methods. A surgical wound was inflicted on 36 male rats; the infection was caused by MRSA, and free vancomycin and vancomycin-SLN were topically applied. Particle size, PDI, zeta potential, drug loading, and encapsulation efficiency of the optimum vancomycin-SLN were 350 ± 24 nm, 0.402 ± 0.014, -16.3 ± 2.5 mV, 13.9 ± 1.4%, and 92.14 ± 3.1%, respectively. In vitro antibacterial assays showed lower MICs for free vancomycin and killed bacteria more efficiently than vancomycin-SLN. However, the synthesized nanoparticles indicated long-term antibacterial activity against MRSA. Animals that were treated with vancomycin-SLN showed the best wound healing procedure. Treatment of rats with vancomycin-SLN increased re-epithelialization and decreased granulation tissue development, as seen by histological analysis. Antibiotic-loaded SLN could not only manage wound infection but also enhance wound healing. Therefore, this kind of treatment should be considered by scientists as an applicable treatment for wounds.

In vitro performance of composition-equivalent PLGA microspheres encapsulating exenatide acetate by solvent evaporation

The once-weekly Bydureon® (Bdn) PLGA microsphere formulation encapsulating the GLP-1 receptor agonist, exenatide acetate, is an important complex injectable product prepared by coacervation for the treatment of type 2 diabetic patients. Encapsulation by coacervation is useful to minimize an undesirable initial burst of exenatide, but it suffers from manufacturing difficulties such as process scale-up and batch-to-batch variations. Herein we prepared exenatide acetate-PLGA formulations of similar compositions using the desirable alternative double emulsion-solvent evaporation technique. After screening several process variables, we varied the PLGA concentration, the hardening temperature, and the collected particle size range, and determined the resulting drug and sucrose loading, initial burst release, in vitro retention kinetics, and peptide degradation profiles using Bdn as a positive control. All formulations exhibited a triphasic release profile with a burst, lag, and rapid release phase, although the burst release was greatly decreased to <5% for some. Marked differences were observed in the peptide degradation profiles, particularly the oxidized and acylated fractions, when the polymer concentration was varied. For one optimal formulation, the release and peptide degradation profiles were similar to Bdn microspheres, albeit with an induction time shift of one week, likely due to the slightly higher Mw of PLGA in Bdn. These results highlight the effects of key manufacturing variables on drug release and stability in composition-equivalent microspheres encapsulating exenatide acetate and indicate the potential of manufacturing the microsphere component of Bdn by solvent evaporation.

Controlled release of inactivated influenza virus and α-galactosylceramide from PLGA microparticles results in long-term protection against influenza infection

Abstract The objective of this study was to develop biodegradable microparticles with continuous release that can enhance and extend the long-term protection of single-dose vaccines. Several formulations of Poly (lactic-co-glycolic acid) (PLGA) microparticles were synthesized using a double emulsion solvent evaporation technique to encapsulate inactivated A/PR/8/34 (PR8) H1N1 influenza virus in combination with the invariant natural killer T (NKT) cell agonist α-galactosylceramide (α-GalCer). The most efficient controlled release particle formulations were injected into C57BL/6J mice. Additional control mice were injected with PBS alone, inactivated PR8 dissolved in PBS, or inactivated PR8 and α-GalCer dissolved in PBS. Thirty weeks after vaccination, mice were challenged with a lethal dose of live homologous virus. Mice immunized with the microparticle vaccine survived the infection and had reduced clinical disease and decreased weight loss compared to unvaccinated mice. After vaccination, mice injected microparticles presented a gradual increase production of PR8-specific IgGs that was dominated by IgG1 isotype that is usually produced by T helper (Th) 2 responses. In contrast, mice that received soluble vaccine presented a rapid antibody response that was dominated by antibodies of the Th1-associated IgG2a isotype. Collectively, these results demonstrate the potential of PLGA-based single-dose microparticle vaccines for providing long-term protection against influenza infection and potentially other pathogens. Supported by grants from USAMRAA (W81XWH-19-1-0005)

Box-Behnken Design of Experiments of Polycaprolactone Nanoparticles Loaded with Irinotecan Hydrochloride.

The Box-Behnken design of experiments (BBD) is a statistical modelling technique that allows the determination of the significant factors in developing nanoparticles (NPs) using a limited number of runs. It also allows the prediction of the best levels of variables to obtain the desired characteristics (size, charge, and encapsulation efficiency) of the NPs. The aim of this study was to examine the effect of the independent variables (amount of polymer and drug, and surfactant concentration) and their interaction on the characteristics of the irinotecan hydrochloride (IRH)-loaded polycaprolactone (PCL) NPs and to determine the most optimum conditions for producing the desired NPs. The development of the NPs was carried out by a double emulsion solvent evaporation technique with yield enhancement. The NPs data were fitted in Minitab software to obtain the best fit model. By using BBD, the most optimum conditions for producing the smallest size, highest magnitude of charge, and highest EE% of PCL NPs were predicted to be achieved by using 61.02 mg PCL, 9 mg IRH, and 4.82% PVA, which would yield 203.01 nm, -15.81 mV, and 82.35% EE. The analysis by BBD highlighted that the model was a good fit to the data, confirming the suitability of the design of the experiments.

Targeting CXCR4-expressing Cancer Cells with Avidin-poly (lactic-co-glycolic acid) Nanoparticle Surface Modified with Biotinylated DV1 Peptide.

Chemokine receptor CXCR4 is frequently present in cells of various cancers. Hence, targeted therapy using CXCR4 ligands, such as DV1 peptide, on drug-loaded nanoparticles, has the potential to enhance the efficiency of cancer treatment. The present study created a CXCR4-targeting drug delivery system using avidin-poly (lactic-co-glycolic acid) (PLGA) nanoparticle surface tagged with biotinylated DV1 peptide ligand. A double-emulsion solvent evaporation technique was employed to prepare avidin-PLGA nanoparticles and characterized by transmission electron microscopy (TEM) and dynamic light scattering. Uptake was studied by confocal microscopy after incorporating fluorescein isothiocyanate (FITC)-labeled albumin inside the nanoparticles during their synthesis. Peptide-biotin-avidin-PLGA nanoparticles were tested in vitro on CXCR4-expressing U87MG cells. Photomicroscopy was done by a Nikon A1 Confocal Microscope, and pictures were analyzed by Nikon NIS-Elements BR software. Experimental results confirmed the specificity of DV1 peptide-tagged avidin-PLGA nanoparticles for cells expressing CXCR4 receptors. The avidin-PLGA nanoparticles were successfully synthesized and the same was confirmed by tagging them with FITC-labeled biotin. Avidin-PLGA nanoparticle surface tagged with biotinylated DV1 peptide ligand has potential clinical application in the treatment of various cancers as targeted therapy for CXCR4-expressing cancer cells.

Oral PLGA-based DNA vaccines using interferons as adjuvants remarkably promote the immune protection of grass carp (Ctenopharyngodon idella) against GCRV infection

Grass carp hemorrhagic disease caused by grass carp reovirus (GCRV) results in significant economic losses to the global grass carp aquaculture industry. Oral vaccination is an ideal choice for disease precaution in aquaculture. However, oral vaccine can be degraded in the gut. Therefore, the selection of loading materials is essential. In this study, the S6 and S7 fragments (encoding the outer capsid protein VP4 and fibronectin VP56 of GCRV) and grass carp interferons (IFNs), including IFN1, IFN3, and IFNγ2 were used to create DNA vaccines and adjuvants based on pcDNA3.1, respectively. The oral DNA vaccine was encapsulated in poly(lactic-co-glycolic acid) (PLGA) and polyvinyl alcohol (PVA) with IFNs. The PLGA-PVA (PP) nano-microspheres were prepared by double emulsion-solvent evaporation technique. Using transmission electron microscopy and dynamic light scattering assays, it was determined the vaccines had a spherical structure with uniform particle size (643.5 ​± ​35.3 ​nm). The nano-microspheres possessed excellent encapsulation efficiency (81.6 ​± ​2.6%) and loading rate (0.54 ​± ​0.02%), and simultaneously exhibited negligible hemolytic activity and cell toxicity. The protection rate and tissue viral loads post-GCRV challenge in grass carp were assessed. The oral PP nano-microsphere with pVP4 ​+ ​pIFN1 (PP41) vaccine increased protection rate by 44% compared with the control group and was correlated with relatively low viral loads in the spleen, head kidney, and hindgut. Further, three crucial serum biochemical indexes, total superoxide dismutase (TSOD), complement C3 (C3), and lysozyme (LZM), were also dramatically increased. Furthermore, mRNA expressions of representative immune-related genes (IgM, IFN1, IFNγ2, MHC-Ⅰ, and CD8α) in the head kidney and spleen were significantly enhanced. In addition, mRNA expression of IgT was significantly boosted in the hindgut. The results indicate that DNA vaccine capsulated with PP is effective against GCRV infection. The present study provides insights into a prospective strategy for oral vaccine development in aquaculture.

Clindamycin phosphate and bone morphogenetic protein-7 loaded combined nanoparticle-graft and nanoparticle-film formulations for alveolar bone regeneration – An in vitro and in vivo evaluation

Commonly utilized techniques for healing alveolar bone destruction such as the use of growth factors, suffering from short half-life, application difficulties, and the ability to achieve bioactivity only in the presence of high doses of growth factor. The sustained release of growth factors through a scaffold-based delivery system offers a promising and innovative tool in dentistry. Furthermore, it is suggested to guide the host response by using antimicrobials together with growth factors to prevent recovery and achieve ideal regeneration. Herein, the aim was to prepare and an in vitro - in vivo evaluation of bone morphogenetic protein 7 (BMP-7) and clindamycin phosphate (CDP) loaded polymeric nanoparticles, and their loading into the alginate-chitosan polyelectrolyte complex film or alloplastic graft to accelerate hard tissue regeneration. PLGA nanoparticles containing CDP and BMP-7, separately or together, were prepared using the double emulsion solvent evaporation technique. Through in vitro assays, it was revealed that spherical particles were homogeneously distributed in the combination formulations, and sustained release could be achieved for >12 weeks with all formulations. Also, results from the micro-CT and histopathological analyses indicated that CDP and BMP-7 loaded nanoparticle-film formulations were more effective in treatment than the nanoparticle loaded grafts.

Harnessing Folate-Functionalized Nasal Delivery of Dox-Erlo-Loaded Biopolymeric Nanoparticles in Cancer Treatment: Development, Optimization, Characterization, and Biodistribution Analysis.

The aim of the present study is to develop Doxorubicin-Erlotinib nanoparticles (Dox-Erlo NPs) and folate-armored Dox-Erlo-NP conjugates for targeting glioma cancer. Glioma is one of the most common progressive cancerous growths originating from brain glial cells. However, the blood-brain barrier (BBB) is only semi-permeable and is highly selective as to which compounds are let through; designing compounds that overcome this constraint is therefore a major challenge in the development of pharmaceutical agents. We demonstrate that the NP conjugates studied in this paper may ameliorate the BBB penetration and enrich the drug concentration in the target bypassing the BBB. NPs were prepared using a biopolymer with a double-emulsion solvent evaporation technique and functionalized with folic acid for site-specific targeting. Dox-Erlo NPs and Dox-Erlo-NP conjugates were extensively characterized in vitro for various parameters. Dox-Erlo NPs and Dox-Erlo-NP conjugates incurred a z-average of 95.35 ± 10.25 nm and 110.12 ± 9.2 nm, respectively. The zeta potentials of the Dox-Erlo NPs and Dox-Erlo-NP conjugates were observed at -18.1 mV and -25.1 mV, respectively. A TEM image has shown that the NPs were well-dispersed, uniform, de-aggregated, and consistent. A hemolytic assay confirmed hemocompatibility with the developed formulation and that it can be safely administered. Dox-Erlo-NP conjugates significantly reduced the number of viable cells to 24.66 ± 2.08% and 32.33 ± 2.51% in U87 and C6 cells, respectively, and IC50 values of 3.064 µM and 3.350 µM in U87 and C6 cells were reported after 24 h, respectively. A biodistribution study revealed that a significant concentration of Dox and Erlo were estimated in the brain relative to drug suspension. Dox-Erlo-NP conjugates were also stable for three months. The findings suggest that the developed Dox-Erlo-NP conjugates may be a promising agent for administration in glioma therapy.

Enhanced Coating Protection of C-Steel Using Polystyrene Clay Nanocomposite Impregnated with Inhibitors.

Polymer-Clay Nanocomposite (PCN) coatings were prepared using the solution intercalation method. The raw Khulays clay was treated with NaCl to produce sodium clay (NaC). Thereafter, Cetyl Pyridinium Chloride (CPC) was used to convert NaC into the organic clay form (OC). PCN was prepared by adding polystyrene as the matrix to different weights of OC to prepare 1 wt.% and 3 wt.% PCN. To enhance the coating protection of C-steel in NaCl solution, PCN coatings were added to microcapsules loaded with some corrosion inhibitors PCN (MC). The microcapsules are prepared by the encapsulation of rare-earth metal Ce+3 ions and Isobutyl silanol into polystyrene via the Double Emulsion Solvent Evaporation (DESE) technique. Characterization techniques such as FTIR, X-Ray Diffraction (XRD), and Transmission Electron Microscopy (TEM) were employed. FTIR confirmed the success of the preparation, while XRD and TEM revealed an intercalated structure of 1 wt.% PCN while 3 wt.% PCN has a fully exfoliated structure. Electrochemical Impedance Spectroscopy (EIS), Electrochemical Frequency Modulation (EFM), and Potentiodynamic Polarization showed an enhanced protection efficiency of PCN (MC) coatings. The results demonstrated that the corrosion resistance (RCorr) of 3% PCN (MC) coating was higher than all the formulations. These PCN (MC) coatings may provide corrosion protection for C-steel pipes in many industrial applications.

Immobilization of the metagenomic lipase, LipG9, on porous pellets of poly-hydroxybutyrate produced by the double emulsion solvent evaporation technique.

This work aimed to produce porous poly-hydroxybutyrate (PHB) pellets in order to evaluate the pellets as a support for immobilization of the metagenomic lipase, LipG9. Four types of pelletized PHB particles with different morphological characteristics were obtained using the double emulsion and solvent evaporation technique (DESE). The micropores of these PHB pellets had similar average diameters (about 3nm), but the pellets had different specific surface areas: 11.7 m2 g-1 for the PHB powder, 8.4m2 g-1 for the control pellets (Ø<0.5mm, produced without the pore forming agent), 10.0m2 g-1 for the small pellets (Ø<0.5mm), 9.5m2 g-1 for the medium pellets (0.5 < Ø<0.8mm) and 8.4m2 g-1 for the large pellets (Ø>1.4mm). Purified LipG9 was immobilized by adsorption on these pellets, and the results were compared with those obtained with PHB powder. The highest immobilization yield (83%) was obtained for the medium PHB pellets, followed by large (76%) and small (55%) PHB pellets. The activity of LipG9 immobilized on the pellets, for the synthesis of ethyl oleate in n-hexane, was highest for the medium pellets (22Ug-1 ). The immobilization yield was high for PHB powder (99%) but the esterification activity was slightly lower (20Ug-1 ). These results show that pelletized PHBbeads can be used for the immobilization of lipases, with the advantage that pelletized PHB will perform better than PHB powder in large-scale enzyme bioreactors.