Emulsification-diffusion Method Research Articles

A Preliminary Report Regarding the Morphological Changes of Nano-Enabled Pharmaceutical Formulation on Human Lung Carcinoma Monolayer and 3D Bronchial Microtissue.

Background and Objectives: Nowadays, the development of enabled pharmaceutical nanoparticles of solid lipid type is continuously growing, because they have the potential to be used for targeted drug release leading to an increased effect of chemotherapy, being used in lung cancer nano-diagnosis and nano-therapy. The current study reports the preliminary results obtained regarding the biological effect of a new nano-enabled pharmaceutical formulation in terms of its cytotoxic and biosafety profile. Materials and Methods: The pharmaceutical formulations consist of solid lipid nanoparticles (SLN) obtained via the emulsification-diffusion method by loading green iron oxide nanoparticles (green-IONPs) with a pentacyclic triterpene (oleanolic acid-OA). Further, a complex biological assessment was performed, employing three-dimensional (3D) bronchial microtissues (EpiAirwayTM) to determine the biosafety profile of the SLN samples. The cytotoxic potential of the samples was evaluated on human lung carcinoma, using an in vitro model (A549 human lung carcinoma monolayer). Results: The data revealed that the A549 cell line was strongly affected after treatment with SLN samples, especially those that contained OA-loaded green-IONPs obtained with Ocimum basilicum extract (under 30% viability rates). The biosafety profile investigation of the 3D normal in vitro bronchial model showed that all the SLN samples negatively affected the viability of the bronchial microtissues (below 50%). As regards the morphological changes, all the samples induce major changes such as loss of the surface epithelium integrity, loss of epithelial junctions, loss of cilia, hyperkeratosis, and cell death caused by apoptosis. Conclusions: In summary, the culprit for the negative impact on viability and morphology of 3D normal bronchial microtissues could be the too-high dose (500 µg/mL) of the SLN sample used. Nevertheless, further adjustments in the SLN synthesis process and another complex in vitro evaluation will be considered for future research.

In-vitro and In-silico Examinations on Baicalein-loaded Solid Lipid Nanoparticles for Neurodegeneration

Background:: In the current scenario, most of the population affected by neurogenera-tive disorders like Alzheimer's, Parkinson's, Huntington's, etc., exist among the 10% population 65 years of age group. Neurodegenerative diseases are characterised as chronic and progressive disorders that occur due to the degeneration of neurons. Baicalein is a flavonoid glycoside derived from the roots of Scutellaria baicalensis. Earlier research suggested that it could be used to treat neurodegenerative illnesses. Baicalein, which was selected for the current study, was designed in-to a solid lipid nanoparticle (SLN) formulation. The SLNs have low permeability across BBB and are delivered by the non-invasive route, i.e., through nasal delivery. The In-silico docking studies were performed to examine and compare the binding affinity of Baicalein to already established drugs on the two most viable targets of Alzheimer's disease, i.e., Beta- secretase and Acetylcho-linesterase. Objective:: The current work is to formulate and evaluate the Baicalein-loaded SLN for neuro-degenerative disorders via a non-invasive route. Methods:: Baicalein loaded SLN was developed by solvent emulsification diffusion method, and formulation is characterised by using different parameters such as particle size analysis, zeta po-tential, scanning electron microscope, transverse electron microscope, X-ray diffraction, Differen-tial scanning calorimetric, Fourier transforms -infrared radiations, drug entrapment, in-vitro drug release and in-silico docking studies. Results:: The particle size of Baicalein-loaded SLN was 755.2 ± 0.48 nm, the Polydispersity index was 0.06, and the zeta potential was -32.5 ± 0.36 mV. The drug entrapment and loading efficien-cy of the optimised formulation were found to be 94% ± 0.653 and 18.2% ± 0.553, respectively. Optimised formulation shows 84.6% ± 0.3% of drug release within 30 minutes, which demon-strates the sustained release of the drug. Conclusion:: Baicalein-loaded SLN is formulated and evaluated for the treatment of neurodegen-erative disorders. SLN is an approach to overcome the challenge of bypassing the BBB by admin-istering the drug via an intranasal route. Hence, when analysed together with the results of Bai-calein-loaded SLN and in-silico studies, it was correlated that Baicalein proved to have a targeted moiety for neurodegeneration.

Formulation and Evaluation of Biopolymer Incorporated Nanogel of Nabumetone

ABSTRACT: The objective of this research was to improve the solubilization, dissolution rate, and thereby anti-inflammatory activity of the BCS class II drug Nabumetone (NSAID). A solid dispersion (SD) approach with Gelucire 50/13 was used to enhance the solubility. Microwave-induced fusion method was used for the development of SD, as it demonstrated a remarkable increase in the solubility and dissolution rate of pure drugs when compared to traditional solid dispersions. A number of parameters of the SD were evaluated in vitro, including solubility, dissolution, and Fourier Transformed Infrared Spectra obtained (FT-IR). The rate of dissolution was inclined to betterment with the drug: polymer ratio 1:0.5 showing drug release 99.60 ± 29. The objective of the work was to evolve a Nanogel for topical delivery of Nabumetone. The emulsification-diffusion method was used to create nanogel using the polymers Carbopol-940, Gelucire-50/13, and triethanolamine as gelling agents. Chitosan was added to the formulation as a biopolymer. Menthol was employed as a penetration enhancer. Using the spontaneous emulsification-diffusion method, six distinct formulations of Nabumetone-loaded Nanogel were successfully created and evaluated for particle size, zeta potential, thermodynamic stability, and rheology study. Using a cellophane membrane, the gels were examined for diffusion study further, and drug content, viscosity, spreadability, pH, and clarity were accessed. The formulation F4 batch had the best in-vitro drug release profile, with a 96.04% release rate over 270 minutes. Optimized gel F4 underwent a skin irritation study on Wistar rats and passed the test. The topical application of Nabumetone as Nanogel proved to be an effective approach to drug delivery.

Nanocapsules novel drug delivery system: A review

Nanocapsules have been various sub micrometer poorly water–soluble drug delivery systems comprised of the oil–based predicated or even a solubilized fundamental enveloped besides synthetic polymer cell wall. Nanocapsules have indeed been vesicular processes where the narcotic seems to be restricted to the pore largely made up of pore water fundamental encapsulated by the polymeric. Nanocapsules are used as only two types after all synthetic polymers. Natural polymers a Synthetic polymers. Nanocapsules have indeed been prepared by different methods some of these have been the Nanoprecipitation method, Emulsion diffusion method, Double emulsification method, Emulsion coacervation method, Polymer coating method, and Layer –by-Layer. Different characterization along with evaluation methods have been performed full nanocapsules dispersed polyethylene nanocapsules is used even though sub-micron narcotic wants to pick up to get a slow release together with efficient drug looking to attack. Microparticles, residing all through relatively small size, range once 10 nanometers to 1000 nanometers they include a fluid/ strong core wherein the drug has been placed into a pore, which would be enveloped by a special and distinct thermoplastic polymer constituted after all synthetic as well as bioplastic they’ve attracted super great awareness, so because barrier methods coting, which really have been usually pyrophoric and easily metabolizable along with slow this very same discharges chemical ingredients.

Cellulose-Silk Fibroin Composite Particles for Hydrophilic Drug-Controlled Release System: Preparation and Characterization

The objective of this study was to investigate the dissolution of cellulose (C) powder as a potential material for particle formation when combined with a silk fibroin (SF) solution. Each polymer solution as well as a mixture of cellulose and silk fibroin in different ratios were prepared into particles using the solvent emulsion-diffusion method. The particle morphology was characterized by scanning electron microscopy (SEM) and by attenuated reflection Fourier-transformed infrared spectroscopy (ATR-FTIR) and thermogravimetric analyzer (TGA) for the C-SF molecular interaction and thermal properties, respectively. The results showed that the cellulose particles appeared as separate fibers and loosely bound together, while silk fibroin particles were spherical in shape with dense texture and smooth surface. The C/SF mixed particles with different ratios could be formed into spherical particles and a ratio of 1:3 has the most spherical and solid. The ATR-FTIR results indicated the absorption spectra of the main functional groups both cellulose and silk fibroin. Blue dextran helped to enhance the temperature of the maximum decomposition rate (Td,max) of the particles via hydrogen bond interaction between the blue dextran and polymers. A burst release of blue dextran was observed in the first 12 h due to the swelling of particle surfaces and the slowest release found in the silk fibroin particles. The C/SF composite showed different blue dextran- eleased profiles and the particle with a high content of silk fibroin-released blue dextran in slowly rate. The results of this work can be used as a basis for applying C/SF composite particles in a hydrophilic drug release-controlled system.

Preservation of Fresh-Cut 'Maradol' Papaya with Polymeric Nanocapsules of Lemon Essential Oil or Curcumin.

Papaya is one of the most consumed fruits in the world; however, tissue damage caused by cuts quickly leads to its decay. Therefore, this study aimed to prepare and characterize lemon oil and curcumin nanocapsules to evaluate their capacity for preserving fresh-cut papaya. Lemon essential oil and curcumin nanocapsules were prepared using ethyl cellulose (EC) and poly-(ε-caprolactone) (PCL) by the emulsification-diffusion method coupled with ultrasound. The particles had sizes smaller than 120 nm, with polydispersity indices below 0.25 and zeta potentials exceeding -12 mV, as confirmed by scanning electron microscopy. The nanoparticles remained stable for 27 days, with sedimentation being the instability mechanism observed. These nanoparticles were employed to coat fresh-cut papaya, which was stored for 17 days. The results demonstrated their remarkable efficacy in reducing the respiration rate. Furthermore, nanocapsules maintained the pH and acidity levels of the papayas for an extended period. The lemon oil/EC nanocapsule treatment retained the color better. Additionally, all systems exhibited the ability to minimize texture loss associated with reduced pectin methylesterase activity. Finally, the nanocapsules showed a notable reduction in polyphenol oxidase activity correlating with preserving total phenolic compounds in the fruit. Therefore, the lemon oil and curcumin nanoparticles formed using EC and PCL demonstrated their effectiveness in preserving fresh-cut 'Maradol' papaya.

Photoactive Parietin-loaded nanocarriers as an efficient therapeutic platform against triple-negative breast cancer

The application of photodynamic therapy has become more and more important in combating cancer. However, the high lipophilic nature of most photosensitizers limits their parenteral administration and leads to aggregation in the biological environment. To resolve this problem and deliver a photoactive form, the natural photosensitizer parietin (PTN) was encapsulated in poly(lactic-co-glycolic acid) nanoparticles (PTN NPs) by emulsification diffusion method. PTN NPs displayed a size of 193.70 nm and 157.31 nm, characterized by dynamic light scattering and atomic force microscopy, respectively. As the photoactivity of parietin is essential for therapy, the quantum yield of PTN NPs and the in vitro release were assessed. The antiproliferative activity, the intracellular generation of reactive oxygen species, mitochondrial potential depolarization, and lysosomal membrane permeabilization were evaluated in triple-negative breast cancer cells (MDA-MB-231 cells). At the same time, confocal laser scanning microscopy (CLSM) and flow cytometry were used to investigate the cellular uptake profile. In addition, the chorioallantoic membrane (CAM) was employed to evaluate the antiangiogenic effect microscopically. The spherical monomodal PTN NPs show a quantum yield of 0.4. The biological assessment on MDA-MB-231 cells revealed that free PTN and PTN NPs inhibited cell proliferation with IC50 of 0.95 µM and 1.9 µM at 6 J/cm2, respectively, and this can be attributed to the intracellular uptake profile as proved by flow cytometry. Eventually, the CAM study illustrated that PTN NPs could reduce the number of angiogenic blood vessels and disrupt the vitality of xenografted tumors. In conclusion, PTN NPs are a promising anticancer strategy in vitro and might be a tool for fighting cancer in vivo.

Design, Development and Characterization of Econazole loaded Nanoparticles for Topical Application

Background and Objectives: Econazole nitrate (ECN) loaded nanoparticles with topical administration were the focus of the current study, which aimed to improve the topical efficacy of the medicine in treating fungal infections while also mitigating the drug’s gastrointestinal (GI) side effects. Further colloidal carrier methodology was employed as a method for the topical administration of medications with precision. Method: The emulsification-diffusion (E-D) method is an alternate approach for preparing nanogels that avoids the toxicitysolvent issues associated with the emulsification-evaporation technique. Its ease of use, enhanced stability, and adaptability have all been verified by a variety of research groups. ECN loaded with dichloromethane in stabilizer solution, formulated by high-speed homogenization at elevated pressure. The addition of aqueous phase with repeated homogenization cycles causes drug diffusion into nanogels. Further addition of mannitol as cryoprotectant and Carbapol 940 as gelling agent stabiles the formulation. Results: The typical size of the particles, polydispersity index (PDI), and zeta potential were all measured with the use of the Malvern zetasizer. Of the five NFs, the lyophilized batch of NF3 exhibited the lowest zeta potential (-11.6 mV) and the PDI (0.208), indicating that the composition was stable. DSC and XRD analysis revealed an amorphous transformation of ECN. The scanning electron micrograph demonstrated discrete, roundish particles. The existence, viscosity, and spreading ability of a gelled dispersion of the selected NLCs were evaluated. Total od 77% of the medication was released in-vitro from a chosen formulation of ECN-loaded nanogels. As a result, it is reasonable to assume that ECN-loaded nanogels are an effective drug delivery system for treating fungal infections since they prolong the duration of drug release. Conclusion: Under degraded conditions, there are not any peaks that conflict with one another. As a result, a technique was developed that is highly applicable due to its sensitivity, strength, accuracy, and demonstration of stability.

Karakterisasi Nanokapsul Ekstrak Daun Serunai (Chromolaena odorata L.) dengan Variasi Kitosan-Alginat Menggunakan Metode Emulsi-Difusi

Serunai (Chromolaena odorata L.) is a plant that has been widely used in medicine, one of which is as an antidiabetic. But treatment using plant extracts has drawbacks to the solubility of the active substance and its bioavailability in the body. Nanocapsules are one of the systems in particle technology that can solve this problem by utilizing a polymer that will encapsulate the active substance and release it slowly at the intended target. To achieve this, the manufacture of nanocapsules must meet several characteristic requirements such as particle size, potential zeta, absorption efficiency, and emulsion stability. This study was conducted to identify the nanocapsules characteristics of Serunai leaf extract (Chromolaena odorata L.) with chitosan-alginate variations and identify the influence of chitosan-alginate variations on the characteristics of nanocapsules. This study is a laboratory experimental study with a one-group posttest-only design. The manufacture of Serunai leaf extract nanocapsules using the emulsion-diffusion method, which is then characterized including particle size determination, potential zeta determination, absorption efficiency test (%EE), and emulsion stability test. The results obtained from the determination of the particle size of Formula I 196.4 nm, Formula II 264.2 nm, and Formula III 207.4 nm, potential zeta Formula I -36.1 mV, Formula II -40.1 mV, and Formula III -36.5 mV, the formula I %EE values 99.7%, Formula II 99.8%, and Formula III 99.7%, as well as all formulas indicating the emulsion type m/a. Three formulas have met the requirements of nanocapsules characteristics. The formula is best obtained in Formula II with a chitosan concentration of 0.3% and alginate of 0.6%, so chitosan-alginate variations influence the characteristic results.

Fabrication of Nanogel for Topical Drug Delivery of Montelukast

A novel nanocrystal system of montelukast (MTK) was designed to improve the transdermal delivery, while ensuring chemical stability of the labile compound. MTK nanocrystal Nanogel was fabricated using using nano dispersion method (Modified emulsification diffusion method). In the pre-formulation study, there was not any physicochemical interaction between drug and polymer had been evaluated by FTIR. The melting point was found to be 134- 137 0C. It is freely soluble in Cyclohexane & butanol ratio and water. The standard curve of ondansetron had been prepared by Cycloheaxxane & butanol (7:3). Montelukast nanogel were prepared by nanodispersion method. Formulations of different drug ratio were optimized with selected parameters like particle size, PDI, Zeta potential, entrapment efficiency, clarity test. pH test of gel, viscosity and gelation temperature. Drug release studies were performed by dialysis bag diffusion technique at a temperature (37°C). The study was continued for 24 hours till. The maximum amount of drug montelukast release 87% within 24 hr. The study was monitored at 37°C. Preparation, characterization and drug release study of montelukast loaded nanogel. This approach of montelukast loaded nanogel with chitosan as the polymer is quite successfully developed.
 

Development of Topical Nanogel as a Promising Delivery of NSAID’s Tenoxicam using Natural Permeation Enhancer Essential Oil (Euckolyptus)

Tenoxicam (TNX) is an effective non-steroidal anti-inflammatory drug (NSAIDs) used to treat rheumatoid arthritis. Like other NSAIDs, tenoxicam has the disadvantage of being linked to gastrointestinal side effects. Furthermore, this drug is having weak transdermal penetration, preventing transdermal administration. The goal of this study was to develop a TNX nanogel with a smaller particle size to improve the anti-inflammatory drug's bioavailability and assess its potential in rheumatoid arthritis. The modified emulsification-diffusion method is used to develop nanosized dispersion of TNX using noveon polycarbophil AA-1 as a gelling agent. Moreover, essential oils increase skin penetration by interacting with the stratum corneum (SC). They were found to be successful in increasing skin penetration of both lipophilic and hydrophilic drugs. The rheology, particle size, drug content, % drug release, and in-vitro diffusion study of prepared TNX nanogel were performed. Based on the rheological features of the formulations it was found to be substantial, with the particle size of 125.05nm and zeta potential -8.47mV, drug content of 97.05%, % drug release 97.40% drug diffusion of 97.42%, and pH of 6.2. Tenoxicam nanogel was prepared by using noveon polycarbophil AA-1 and eucalyptus oil as a permeation enhancer was proven to be suitable as a typical topical gel formulation for the treatment of edema and rheumatoid arthritis.

Fabrication, In Vitro, and In Vivo Assessment of Eucalyptol-Loaded Nanoemulgel as a Novel Paradigm for Wound Healing.

Wounds are the most common causes of mortality all over the world. Topical drug delivery systems are more efficient in treating wounds as compared to oral delivery systems because they bypass the disadvantages of the oral route. The aim of the present study was to formulate and evaluate in vitro in vivo nanoemulgels loaded with eucalyptol for wound healing. Nanoemulsions were prepared using the solvent emulsification diffusion method by mixing an aqueous phase and an oil phase, and a nanoemulgel was then fabricated by mixing nanoemulsions with a gelling agent (Carbopol 940) in a 1:1 ratio. The nanoemulgels were evaluated regarding stability, homogeneity, pH, viscosity, Fourier-transform infrared spectroscopy (FTIR), droplet size, zeta potential, polydispersity index (PDI), spreadability, drug content, in vitro drug release, and in vivo study. The optimized formulation, F5, exhibited pH values between 5 and 6, with no significant variations at different temperatures, and acceptable homogeneity and spreadability. F5 had a droplet size of 139 ± 5.8 nm, with a low polydispersity index. FTIR studies showed the compatibility of the drug with the excipients. The drug content of F5 was 94.81%. The percentage of wound contraction of the experimental, standard, and control groups were 100% ± 0.015, 98.170% ± 0.749, and 70.846% ± 0.830, respectively. Statistically, the experimental group showed a significant difference (p < 0.03) from the other two groups. The results suggest that the formulated optimized dosage showed optimum stability, and it can be considered an effective wound healing alternative.

PREPARATION AND CHARACTERIZATION OF ALGINATE CHITOSAN CROSSLINKED NANOPARTICLES BEARING DRUG FOR THE EFFECTIVE MANAGEMENT OF ULCERATIVE COLITIS

Objective: Delivery of anticancer molecule to the liver remains a “holy grail” in molecular medicine and nanobiotechnology with conventional therapy, as conventional cancer chemotherapy does not prove effective as drug molecule does not reach to the target site at therapeutic concentration. Tumor vasculature differs from the vasculature of normal tissue both in morphology and biochemistry. Most of these differences appear too related to angiogenesis (formation of new blood vessels from pre-existing ones). For the present study nanoparticles (NPs) were chosen as a delivery system, because they have many advantages, e. g. they can pass through the smallest capillary vessels because of their ultra-tiny volume, can penetrate cells and tissue gap to arrive at, pH, ion and/or temperature sensitivity of materials, can improve the utility of drugs and reduce toxic side effects. Methods: PLGA (poly lactide co glycolic acid) was used for the preparation of NPs because of its biodegradability and biocompatibility. It degrades by hydrolysis of ester linkages in the presence of water in to two monomers lactic acid and glycolic acid. There are a number of ligands available for hepatic delivery, among them lactobionic acid (containing galactose moiety) was selected for present work. Preparation of plain nanoparticles was carried out using emulsification–diffusion method. Optimization of the polymer concentration is the first step during the study and it was performed by varying the polymer concentration where as keeping other variables constant. The prepared formulation was optimized on the basis of particle size and polydispersity index. Amount of drug was optimized on the basis of particle size and percentage entrapment efficiency. Results: Particle size and zeta potential of the nanoparticle were determined by zetasizer showed that particles are in nano range (blow 200 nm) and have acceptable range of zeta potential. Shape and surface morphology were determined by TEM and SEM analysis. The conjugation of lactobionic acid with PLGA polymer was proved by FTIR. The in vitro release profiles of entrapped drug from formulations were determined using dialysis membrane. For stability studies, the LDNPs (conjugated NPs) are stored at the temperatures 4±1 °C and room temperature. Human hepatoma cell line HepG2 by SRB assay was selected and it clearly suggests a dose dependent cytotoxicity response i.e. decrease in cell survival fraction with increasing concentration of drug. The in vivo study are important in evaluating the targeting efficacy of designed dosage form and also helps in establishing the correlation between the results obtained from in vitro experimentation to that from in vivo studies. The formulations were administered by tail vein to mice of four groups Group I: PBS 7.4 (control); Group II: 5-FU solution; Group III: DNPs; Group IV: LDNPs. Conclusion: The proposed targeting strategy is expected to enhance the therapeutic index of conventional anticancer drug as well as reduce its cytotoxic effects to normal cells.

Effects of Process and Formulation Parameters on Submicron Polymeric Particles Produced by a Rapid Emulsion-Diffusion Method

Emulsification-diffusion method is often used to produce polymeric nanoparticles. However, their numerous and/or lengthy steps make it difficult to use widely. Thus, a modified method using solvent blends (miscible/partially miscible in water, 25–100%) as the organic phases to overcome these disadvantages and its design space were investigated. To further simplify the process, no organic/aqueous phase saturation and no water addition after the emulsification step were performed. Biodegradable (PLGA) or pH-sensitive (Eudragit® E100) nanoparticles were robustly produced using low/medium shear stirring adding dropwise the organic phase into the aqueous phase or vice versa. Several behaviors were also obtained: lowering the partially water-miscible solvent ratio relative to the organic phase or the poloxamer-407 concentration; or increasing the organic phase polarity or the polyvinyl alcohol concentration produced smaller particle sizes/polydispersity. Nanoparticle zeta potential increased as the water-miscible solvent ratio increased. Poloxamer-407 showed better performance to decrease the particle size (~50 nm) at low concentrations (≤1%, w/v) compared with polyvinyl alcohol at 1–5% (w/v), but higher concentrations produced bigger particles/polydispersity (≥600 nm). Most important, an inverse linear correlation to predict the particle size by determining the solubility parameter was found. A rapid method to broadly prepare nanoparticles using straightforward equipment is provided.

The amount of dextran in PLGA nanocarriers modulates protein corona and promotes cell membrane damage.

Polymeric nanocarriers (NCs) are efficient vehicles to prevent drug unspecific biodistribution and increase the drug amounts delivered to tumor tissues. However, some toxicological aspects of NCs still lack a comprehensive assessment, such as their effects on cellular processes that lead to toxicity. We evaluate the interaction of poly(lactic-co-glycolic acid) (PLGA) NCs prepared using dextran (Dex) and Pluronic®-F127 as stabilizing agents with myocardial cells (H9C2), breast adenocarcinoma cells (MCF-7) and macrophages (RAW 264.7) to address the effect of Dex in PLGA NC formulations. By an emulsion diffusion method, doxorubicin-loaded NCs were prepared with no Dex (PLGA-DOX), 1% (w/v) Dex (Dex1/PLGA-DOX) and 5% (w/v) Dex (Dex5/PLGA-DOX). Uptake analyses revealed a significant reduction in Dex5/PLGA-DOX NC uptake by H9C2 and MCF-7, as in the case of Dex1/PLGA-DOX NCs in the absence of in vitro protein corona, revealing an effect of dextran concentration on the formation of protein corona. RAW 264.7 cells presented a greater uptake of Dex5/PLGA-DOX NCs than the other NCs likely because of receptor mediated endocytosis, since C-type lectins like SIGN-R1, mannose receptors and scavenger receptor type 1 that are expressed in RAW 264.7 can mediate Dex uptake. Despite the lower uptake, Dex5/PLGA-DOX NCs promote the generation of reactive oxygen species and oxidative membrane damage in MCF-7 and H9C2 even though cellular metabolic activity assessed by MTT was comparable among all the NCs. Our results highlight the importance of an in-depth investigation of the NC-cell interaction considering additional mechanisms of damage apart from metabolic variations, as nanoparticle-induced damage is not limited to imbalance in metabolic processes, but also associated with other mechanisms, e.g., membrane and DNA damage.

Metformin loaded injectable silk fibroin microsphere for the treatment of spinal cord injury

The repair of spinal cord injury is a great challenge in clinical. Improving the microenvironment of the injured site is the key strategy for accelerating axon regeneration and synaptic formation. Herein, a kind of silk fibroin microspheres functionalized by metformin through dopamine was developed using water-in-oil emulsification-diffusion method and surface modification technique, and the effect on cortical neuron was evaluated. The results showed that the microspheres showed a uniform size distribution with the diameter of around 60 μm and a concave structure. Moreover, the microspheres possessed good injectability and stability. In addition, the metformin could be successfully immobilized in the silk fibroin microspheres. The cell culture results displayed that the growth and morphology of cortical neurons on the microspheres with metformin concentration of 5 mg/mL and 10 mg/mL were obviously better than that on other samples. Notably, the spread area of single cortical cell on silk fibroin microspheres was increased with the ascending metformin concentration. Therefore, the results indicated that the metformin loaded silk fibroin microsphere could obviously improve the growth and spreading behavior of cortical neuron. The study may provide an important experimental basis for the development of drug loaded injectable biomaterials scaffolds for the treatment of spinal cord injury and have great potential for spinal cord regeneration.

PH‐receptive chlorhexidine‐loaded poly‐L‐glycolic acid platform delivery approach to stabilize adhesive‐orthodontic interface

AbstractThis study aimed to synthesize and characterize chlorhexidine (CHX)‐loaded poly‐L‐glycolic acid (PLGA) nanoparticles and to investigate the in vitro drug release in different pH conditions, antibacterial, cytotoxicity activity, and mechanical properties of CHX‐loaded PLGA‐modified Transbond XT adhesive at tooth‐bracket interface. PLGA nanoparticles with and without CHX were synthesized using emulsion diffusion method and characterized for morphology and chemical structure using transmission electron microscopy and Raman analysis. CHX‐loaded PLGA nanoparticles in Transbond XT orthodontic adhesive were prepared using two different concentrations of the nanoparticles (2.5 and 5 wt%) and characterized for degree of conversion (DC) using DC, antimicrobial MTT assay, and cytotoxicity testing. Bonded specimens were tested for shear bond strength (SBS) and adhesive remnant index (ARI) at the tooth‐bracket interface. The synthesized PLGA nanoparticles averaged between 60 and 80 nm in size. After loading CHX inside PLGA nanoparticles, the morphology of the PLGA nanoparticles was changed considerably into irregular shaped structures. Bracket samples treated with 5 wt% CHX‐loaded PLGA‐modified adhesive demonstrated the least mean DC scores. A 5 wt% CHX‐loaded PLGA‐modified adhesive specimens showed more profound antibacterial activity against Streptococcus mutans. The least mean SBS values were exhibited by 5 wt% CHX‐loaded PLGA‐modified adhesive samples, while a statistically significant difference was observed in the mean ARI values among all study groups at all‐time points (p = 0.018). A pH‐sensitive CHX release response was observed when loaded in PLGA nanoparticles. The formulated drug‐loaded nanocarrier exhibited remarkable physicochemical, spectral, and biological features.

Formulation Development of Topical Preparation Containing Nanoparticles of Povidone-Iodine for Wound Healing.

Povidone-iodine (PVI) is an antiseptic drug that is used for wound healing or for repair of the damaged tissue. Studies on solid lipid nanoparticles (SLNs) indicate that this system could potentially be used as a delivery system with improved drug entrapment efficiency and controlled drug release for hydrophilic actives. This study focuses on developing a topical gel containing SLNs of PVI for wound healing. SLNs were prepared by using the solvent emulsification diffusion method. Lipids such as glycerol monostearate, palmitic acid, and stearic acid, and surfactants such as polysorbate 80, soyalecithin, and Pluronic F-68 were used for the preparation of SLN. These were screened out based on particle size and entrapment efficiency of SLN. Gel was prepared by using Carbopol 940 (1% w/w) and propylene glycol (10% w/w). Formulated SLNs were evaluated by various in vitro and in vivo techniques. Based on the results, the drug-to-lipid ratio (1:3) and 2% polysorbate 80 (surfactant) along with stirring rate (3,000 rpm) produced the desired particle size (285.4 nm) with good stability. 22.85% drug loading and 88.83% drug entrapment efficiency were found in the optimized formulation. In vitro drug release shows that it follows the Korsmeyer-Peppas model. The animal study shows that the period of epithelization produced by the test group was 17.14 ± 1.35 days, which was near to that of the standard group (16.25 ± 1.24 days). Clinical Trial Registration number: 1044/PO/Re/S/07/CPCSEA.

Implementation of the emulsification-diffusion method by solvent displacement for polystyrene nanoparticles prepared from recycled material.

From an integral perspective, nanotechnology can be used to care for the environment by improving current preparation methods and facilitating industrial scale-up. This article discusses the implementation of techniques for obtaining polystyrene nanoparticles (PSN), as an added value, using an emulsification and solvent displacement method (EDSD); the solvent displacement is a novel modification to the emulsion-diffusion methodology, where the diffusion is done directly on the emulsion, which allows concentrated dispersions that facilitate direct use to be obtained, eliminating the dilution with water and the recovery of water by additional processes. The solvent was recovered by reduced pressure, which is class 3, conforming to ICH, and making this method sustainable. The optimization of this process has not been reported elsewhere. This approach made it possible to obtain highly-concentrated nanoparticles while allowing the reuse of the solvent. A scaling proposal is presented that integrates the conditioning of the solid urban waste material called expanded polystyrene (EPS) foam that constitutes a serious environmental problem both nationally and globally. Hence, the article presents an alternative to the recycling of EPS, and a methodology in the context of green chemistry, because solvent is recovered to prepare other batches. The PSN obtained from this waste material had a minimum particle size of 225.8 nm, with a polydispersion index of 0.158. Process performance was 97.1%, and the solvent was recovered at a maximum rate of 85%. The morphology of the PSN was spherical and uniform, with a smooth surface.

Effect of nano-reduction on properties of β-glucan and its use as encapsulating agent for release of α-tocopherol

In this work, nanoreduction of β-glucan by emulsion diffusion method and its effect on structural, rheological and antioxidant properties were studied. Dynamic light scattering confirmed the formation of the β-glucan particles in the nanosize range with an average size of 78.5 nm. FTIR revealed a difference in the intensity of peaks between β-glucan nanoparticles and β-glucan. Rheological analysis of both gels showed Newtonian behaviour, however, nanoreduction of β-glucan decreased the viscosity of the gel. DPPH scavenging activity, reducing power and metal chelating activity were performed which displayed that antioxidant activity of β-glucan nanoparticles was significantly higher (P < 0.05) than β-glucan. Furthermore, β-glucan nanoparticles offered more protection to DNA against the oxidative damage caused by (-OH) radicals. Also, β-glucan nanoparticles and β-glucan were used as wall material for encapsulation of α-tocopherol and its in-vitro release behavior was studied during its transit in the GI tract. The release of α-tocopherol from β-glucan was observed higher in β-glucan nanoparticles than β-glucan.