Particle Entrapment Research Articles

Enhanced bioavailability of Quercetin-loaded niosomal in situ gel for the management of Parkinson’s disease

BackgroundParkinson’s disease (PD) is the second most prevalent neurological disorder, characterized by motor symptoms such as tremor and rigidity due to the degeneration of dopaminergic neurons in the substantia nigra. This study investigates the formulation of quercetin, a natural bioflavonoid with potent antioxidant and anti-inflammatory properties, as niosomes for intranasal delivery to enhance its bioavailability and therapeutic potential for PD.MethodsThe niosomal formulation was optimized for critical parameters including particle size, entrapment efficiency, and zeta potential. Male Wistar rats were utilized to assess the effects of quercetin-loaded niosomes on motor function, dopaminergic neuron protection, and oxidative stress alleviation.ResultsThe optimized niosomal formulation exhibited a particle size of 195 nm, a polydispersity index (PDI) of 0.29, a zeta potential (ZP) of −30.63 mV, and an entrapment efficiency (EE) of 82.77%. In vivo evaluations conducted using the haloperidol-induced PD model revealed significant enhancements in behavioural, biochemical, and histopathological outcomes when compared to both disease controls and the standard treatment group. Additionally, short-term stability tests confirmed the robustness of the formulation.ConclusionThe findings suggest that the quercetin-loaded niosomal formulation offers improved drug delivery and efficacy, indicating its potential as a superior treatment option for PD compared to conventional dosage forms. This approach may pave the way for enhanced therapeutic strategies targeting the neurodegenerative processes underlying Parkinson’s disease.

Development and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis.

The current project was designed to develop piperine-loaded solid lipid microparticles (SLMs) to assess the anti-arthritic potential of piperine (PIP). Variable proportions of carnauba wax, beeswax, and tween 80 were employed for preparing SLMs by using the solvent evaporation technique. The developed formulations were subjected to particle size measurements, entrapment efficiency (EE), and zeta potential (ZP) determination. Microparticles were also investigated for piperine-lipid compatibility, thermal analysis, surface morphology, piperine (PIP) release trend, and anti-rheumatic activity in rats. The network's grafting was confirmed by FTIR and XRD results. The thermal stability of the constructed network was confirmed by the DSC and TGA results. SEM findings confirm porous surface morphology. The dissolution experiments on SLMs confirmed the sustained release profile, delivering 87.82% to 94.92% of piperine at 7.4 pH for 24h. All developed formulations followed a zero-order kinetic model and the Korsmeyer-Peppas model. Furthermore, the anti-rheumatic potentials of piperine from SLMs were also investigated and compared with diclofenac sodium (the standard treatment) in a rat model. The analysis revealed that PIP significantly reduced the severity of arthritis, as confirmed by the findings of multiple arthritic assessment parameters.

Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design.

Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients. However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability. In addition, the absorption of ICZ from commercial oral dosage forms is highly affected by food intake and pH. The current study aimed to develop, optimize, and characterize ICZ-loaded solid lipid nanoparticles (ICZ-SLNs) using a Central Composite Design for improved solubility and extendedrelease profile. ICZ-SLNs were optimized based on physicochemical characteristics. ICZ-SLNs were also evaluated for differential scanning calorimetry (DSC), in-vitro release, lyophilization, transmission electron microscopy (TEM), and physicochemical stability at refrigerated and room temperatures for three months. The optimized ICZ-SLNs formulation showed particle size, polydispersity index, zeta potential, drug content, and entrapment efficiency of 335.6±8.0 nm, 0.25±0.02, -23.8±0.5 mV, 98.3±2.5%, and 99.5±1.5%, respectively. ICZ-SLN dispersions showed extended-release profiles for ICZ compared to the control solution over 24 h. The absence of the endothermic melting drug peak of the lyophilized formulation indicated that the drug was converted to its amorphous form inside the solid matrix. In addition, TEM studies showed spherical shape nanoparticles. Moreover, the optimized ICZ-SLN formulation was stable at both tested storage conditions. The current ICZ formulation could exhibit improved oral bioavailability with better therapeutic outcomes during the treatment of systemic fungal infections.

Optimization of spray drying process conditions for producing insulin-loaded alginate/chitosan polyelectrolyte complexes

The aim of this study was to optimize the formulation parameters for spray-dried insulin-loaded alginate/chitosan polyelectrolyte complexes (PECs) intended for oral insulin delivery, utilizing response surface methodology. A 3-factor, 3-level Box-Behnken experimental design was used to assess the effects of three independent factors: alginate concentration, liquid feed rate, and inlet temperature, on three dependent responses: particle size, production yield, and entrapment efficiency. The structural properties and cytotoxic effects of insulin in the optimized spray-dried PECs were also investigated. The final optimized formulation achieved a particle size of 407.7 nm, a production yield of 58.88%, and an entrapment efficiency of 67.9%. In vitro release studies demonstrated that Alg/CS PECs exhibited pH-sensitive drug release behavior, following Makoid-Banakar kinetics. Structural analysis revealed that the spray-drying process maintained the native conformation and stability of the insulin. Moreover, the optimized formulations showed no cytotoxicity.

Multifunctional Dual Enzyme-Responsive Nanostructured Lipid Carriers for Targeting and Enhancing the Treatment of Bacterial Infections.

Bacterial infections pose an increasingly worrisome threat to the health of humankind, with antibiotic resistance contributing significantly to this burden. With current conventional antibiotics perpetuating the problem, and a paucity in developing antibiotics, drug delivery systems incorporating nanotechnology appear promising. As such, a dual enzyme-responsive multifunctional nanostructured lipid carrier (NLC) incorporating farnesol (FAN) and triglycerol monostearate (TGMS), was conceptualized for the codelivery of vancomycin (VCM) and antimicrobial peptide (AMP) to enhance the antibacterial activity of VCM. In silico studies and Microscale Thermophoresis demonstrated the strong binding relationships between the NLC constituents and two enzymes that exist in higher concentrations during host infection, namely lipase and a matrix metalloproteinase (MMP). The formulated nanosystem, VCM-AMP-TF-NLCs, had a particle size, polydispersity index, zeta potential, and entrapment efficiency of 149.00 ± 2.97 nm, 0.07 ± 0.01, -5.51 ± 1.21 mV, and 86.20% ± 1.47%, respectively. The NLCs, which showed stability, and biocompatibility, also demonstrated lipase- and MMP-responsiveness. The in vitro antibacterial studies revealed 2-fold and 8-fold reductions in the minimum inhibitory concentration for the NLCs compared to bare VCM, against methicillin-resistant Staphylococcal aureus (MRSA) and Escherichia coli, respectively. Furthermore, in vivo studies revealed that tissues treated with the VCM-AMP-TF-NLCs displayed significantly reduced bacterial burdens (up to 8.73-fold) and less histopathological cellular injury, edema, and necrosis compared to the tissues treated with bare VCM alone. The results support the superiority of the VCM-AMP-TF-NLCs as a multifunctional dual enzyme-responsive NLC compared to bare VCM.

Impact of Formulation Variables on Meloxicam spanlastics Preparation

Spanlastic is a modern drug delivery that combines vesicular and nanoparticulate characteristics with numerous advantages over topical applied conventional vesicular systems in terms of stablility, penetration flexibility, and targeting. Meloxicam (MX) is a potent non-steroid anti-inflammatory drug that is frequently utilized for the short- and long-term treatment of chronic pain and inflammatory diseases including rheumatoid arthritis. However, the oral administration of MX often includes several adverse effects, including gastrointestinal disturbances and ulceration. Thus, the aim is a preparation of proper formula for MX-loaded spanlastics via studying the formulation variables that may affect their properties using the ethanol injection method. Variables include; span®60: edge activator ratio, the type of edge activators, the amount of MX, and the type of organic phase solvent were studied for their impact on particle size, polydispersity index, and entrapment efficiency. The formula that was selected showed sustained release for six hours, entrapment efficiency of 70.66±1.15%, zeta potential (-4.51), and particles that were 495±9.9 nm in size. Overall, the results indicated that spanlastics had the potential carrier for medicine delivery systems.

Bioweathering in monogenetic volcanoes: the case of Xitle in Mexico City

This contribution describes biological weathering features produced by microbial communities growing on rock surfaces denominated biological rock crusts. We provide arguments related to the importance of recognizing rocks as an ecological niche and a review of main recognized bio-weathering processes in basaltic bedrock. We particularly address the features found in the lava flow of the monogenetic volcano Xitle, which is located in the volcanic field of the Sierra del Chichinautzin in the south of Mexico City. We found that the diversity and distribution of organisms within the rock crusts varies depending on the superficial texture and porosity of the lavas. Mosses have a preference for vesicles and crevices, while lichens can establish in smoother and more exposed areas. The predominant biological weathering features we have found associated with these crusts are incrustation, penetration, vesicle infilling, endolithic colonization, fractures, and particle entrapment. It is worth noting that bioweathering features are related to specific biological groups: lichens exert all of the features found, while mosses are mostly associated with particle entrapment and vesicle infilling, and biofilms are related to penetration and endolithic colonization. Therefore, this article discusses the importance of geoheritage conservation in relation to the biodiversity these lavas harbor.

Ameliorated delivery of Amphotericin B to Macrophages using Chondroitin Sulfate Surface-Modified Liposome Nanoparticles

Background The neglected tropical disease leishmaniasis has significant adverse effects from current treatments and limited therapeutic options are currently available. Objective The aim of this study was to develop a surface-modified nano-liposomal drug delivery system, anchored with chondroitin sulfate (CS), to effectively transport Amphotericin B (AmB) to macrophages. Methods Conventional liposome formulations (CL-F) and CS-coated surface-modified liposome formulations (CS-SML-F) were formulated by the thin film hydration method and characterized for particle size, polydispersity index (PDI), zeta potential and entrapment efficiency with long-term stability. In-vitro drug release using simulation medium, deformability index (DI) by using a polycarbonate membrane, and cell uptake studies among murine macrophages via flow cytometry were analyzed. Scanning and transmission electron microscopy were used to study the surface morphology and shape of the particles. Results Optimized conventional liposome CL-F6, CL-F9 and surface-modified liposomes CS-SML-F6 and CS-SML-F9 exhibited particle size diameters around 280 nm with a PDI of approximately 0.3 over six months of storage at 5 °C, maintaining stable surface charge (circa -30 mV). Sustained drug release peaked between 4 and 12 hours and surface morphology showed a uniform distribution of spherical liposome particles. Cell uptake measured by flow cytometry showed the highest rate of macrophage targeting by the CS-SML-Fs. Conclusion These findings have demonstrated that CS surface-modification has enhanced nanoparticle targeting to macrophage binding sites, particularly the cysteine-rich domain, potentially advancing macrophage-targeted drug delivery systems.

Development and Characterization of Novel Combinations and Compositions of Nanostructured Lipid Carrier Formulations Loaded with Trans-Resveratrol for Pulmonary Drug Delivery.

This study aimed to fabricate, optimize, and characterize nanostructured lipid carriers (NLCs) loaded with trans-resveratrol (TRES) as an anti-cancer drug for pulmonary drug delivery using medical nebulizers. Novel TRES-NLC formulations (F1-F24) were prepared via hot, high-pressure homogenization. One solid lipid (Dynasan 116) was combined with four liquid lipids (Capryol 90, Lauroglycol 90, Miglyol 810, and Tributyrin) in three different ratios (10:90, 50:50, and 90:10 w/w), with a surfactant (Tween 80) in two different concentrations (0.5 and 1.5%), and a co-surfactant, soya phosphatidylcholine (SPC S-75; 50 mg). Amongst the analyzed 24 TR-NLC formulations, F8, F14, and F22 were selected based on their physicochemical stability when freshly prepared and following storage (4 weeks 25 °C), as well as in terms of particle size (<145 nm), polydispersity index (PDI; <0.21) and entrapment efficiency (>96%). Furthermore, F14 showed greater stability at 4 and 25 °C for six months and exhibited enhanced aerosolization performance, demonstrating the greater deposition of TRES in the later stages of the next-generation impactor (NGI) when using an air-jet nebulizer than when using an ultrasonic nebulizer. The F14 formulation exhibited greater stability and release in acetate buffer (pH 5.4), with a cumulative release of 95%. Overall, formulation F14 in combination with an air-jet nebulizer was identified as a superior combination, demonstrating higher emitted dose (ED; 80%), fine particle dose (FPD; 1150 µg), fine particle fraction (FPF; 24%), and respirable fraction (RF; 94%). These findings are promising in the optimization and development of NLC formulations, highlighting their versatility and targeting the pulmonary system via nebulization.

Empowering Arthritis Patients: Optimized Drug Delivery through Piroxicam Microcapsule-Embedded Scaffold Implants via Box-Behnken Experimental Design.

The necessity for extended drug discharge to alleviate pain without adverse effects underscores the importance of innovative drug delivery systems. Achieving sustained pain relief without compromising patient safety is a critical objective in healthcare. By extending the duration of drug action while suppressing side effects, such systems offer enhanced therapeutic outcomes and improved patient quality of life. This study endeavors to develop and appraise an innovative implantable drug delivery system by integrating NSAID-loaded gelatin microcapsules into a gelatin scaffold designed to augment drug delivery efficiency and sustain drug release. Piroxicam-loaded microcapsules with a 1:1 ratio of poly lactic acid and poly lacto glycolic acid showed smaller particle size, good yield, entrapment efficiency, and discharge. They were selected to make gelatin scaffolds with Box Behnken Design using Design Expert software for optimization. The better scaffolds were made in the form of rod-shaped sub-dermal implants. The primary focus of the investigation was the evaluation of critical parameters, specifically entrapment efficiency and drug discharge properties as dependent variables. Microcapsules with a 1:1 ratio of PLA and PLGA showed smaller particle sizes, good yield, entrapment efficiency, and discharge. Notably, the Design Expert-driven optimization yields highly favorable results. Furthermore, the scaffolds loaded with microcapsules exhibited favorable physicochemical assets, including drug discharge, for an extended period, underscoring their versatility for drug delivery. By employing Design Expert software for optimization, the study demonstrates promising results, particularly in sustained pain management for arthritis, potentially improving therapeutic outcomes and patient quality of life. The study concludes that the prepared implants (holding scaffolds impregnated with piroxicam-loaded microcapsules) can be promising for relieving arthritis all day.

Network Pharmacology and Optimization of β-Sitosterol-Loaded Solid Lipid Nanoparticles Using Box-Behnken Design for Enhanced Solubility and Sustained Drug Release in Diabetes.

The pharmaceutical industry has paid a lot of attention to solid lipid nanoparticles (SLN) because they show promising drug delivery vehicles. This work aimed to design and optimize the SLN of β-sitosterol, a hydrophobic drug, to improve solubility and sustained action. An ultrasonication technique after melting was used to design SLN using a randomized response surface Box-Behnken design (BBD). Network pharmacology analysis was performed to explore the interactions between genes. According to the findings, Compritol ATO 888 was the most soluble at a drug: lipid ratio of 1:3. Particle size, PDI, zeta, and entrapment efficiency (EE) were observed as 168.83nm, 0.231 -28.9 Mv, and 68.29%, respectively. The optimized formulation did not undergo any chemical changes, as depicted through DSC. The in vitro drug release investigation showed that the SLN released the drug continuously for 28 hours. Scanning Electron Microscopy (SEM) revealed homogenous, spherical particles. The antidiabetic potential of the formulation was assessed through the potential of glucose uptake by yeast, and the α-amylase inhibitory assay revealed its significant antidiabetic potential when compared with that of the standard drug metformin. The network pharmacology of β-sitosterol demonstrated gene interaction with hexokinase, phosphoglucomutases, glucose-6-phosphate dehydrogenase, hexose-6-phosphate dehydrogenase, and glutathione disulfide reductase. The β-sitosterol-loaded SLN generated by BBD was found to be a potential method for improving drug solubility with sustained drug release and was found to be long-term storage stable.

Optimization of nano-structured lipid carriers for enhanced salbutamol delivery via buccal mucoadhesive film

Salbutamol sulphate (SS) is a widely prescribed β2 agonist for different respiratory disorders. However, its short plasma half-life and poor oral bioavailability strongly limit its compliance. This study targeted formulating SS in nanostructured lipid carriers (SS-NLCs) embedded in a buccal mucoadhesive film to enhance bioavailability and sustain release through an easy route of administration aiming to improve patient compliance and reduce dose-related side effects. SS-NLCs were prepared using glycerol monostearate (GMS), Labrasol® oil, and poloxamer 407 utilizing a full 23 factorial design. Eight SS-loaded NLCs formulations were evaluated for particle size distribution, zeta potential, and entrapment efficiency. The optimum formula selected according to design expert® statistical analysis, was subsequently incorporated in a polymeric buccal mucoadhesive film and subjected to in vitro and in vivo characterization. The optimum SS-NLCs showed a mean particle size of 119.1 ± 1.28 nm, polydispersity index of 0.248 ± 0.023, zeta potential of - 40.9 ± 0.47 mV, and entrapment efficiency of 68.20 ± 2.05 % with apparent controlled release. Casting SS-NLCs in a mucoadhesive polymeric mixture resulted in a smooth strong film with a prolonged in vitro drug release duration reaching 10 h. In vivo, buccal application of the formulated film showed significantly higher Cmax (107.53 ± 5.20 ng/ml) and delayed Tmax to 4 h with improving the bioavailability of SS by 4.10 folds compared to oral SS solution. Consequently, the buccal polymeric mucoadhesive film of SS-NLCs holds promise as an alternative route for sustained release, enhancing bioavailability, and improving therapeutic efficacy in treating respiratory disorders.

Stabilization of caffeine-loaded nanoliposomes via chitosan coating and spray drying for application in food products

In this study, caffeine (CAF) was loaded into nanoliposomes (n-LPs) and chitosan-coated n-LPs, so called nanochitosomes (n-CTs). Among different CAF concentrations (1–5 mg/mL) and various chitosan coatings (0.1–1.0 mg/mL), n-LPs loaded with 4 mg/mL CAF (n-LPs-4) and coated with 0.4 mg/mL chitosan (n-CTs-0.4) exhibited the best physical properties, encapsulation efficiency (EE), and antioxidant activity. Under different storage conditions (4 °C, 25 °C, 70 °C, and freeze-thaw), freeze-thaw stress had the most detrimental effect on structural stability and unintended CAF release. However, chitosan coating layer increased its resistance to stress and controlled release in gastrointestinal conditions. To evaluate release mechanisms and kinetics, release data were fitted to zero-order, Kopcha, Korsmeyer-Peppas, and Higuchi models. CAF release kinetics in both simulated gastric and intestine conditions followed a Fickian diffusion mechanism. The release data fitted well with Kopcha and Korsmeyer-Peppas models, with R2 > 0.92. The differential scanning calorimetry of CAF showed an endothermic peak at 237.85 °C. This peak was not observed after incorporation into n-LPs and n-CTs, indicating successful CAF encapsulation in these structures. Spray-drying of n-LPs-4 and n-CTs-0.4 resulted in particles with good production yield, physicochemical properties, moisture content, water activity, solubility, and color indices. FTIR analysis confirmed successful CAF loading inside n-LPs, chitosan placement on their membrane surface, and entrapment of particles within maltodextrin carriers. Morphological features revealed spherical particles in both n-LPs and n-CTs, along with instability, aggregation, and size-varied wrinkled structures (in powders) after spray drying. Finally, texture analysis and sensory evaluation of enriched Gaz (one of the traditional and conventional sweets in Iran) with CAF-loaded n-LPs-4 and n-CTs-0.4 powders indicated the production of a high quality and functional product with acceptable characteristics.

Alginate-based microencapsulation enhances antinociceptive and anti-inflammatory activities of Phyllanthus amarus and Phyllanthus muellerianus

Phyllantus amarus and P. muellerianus are herbs reported to possess anti-inflammatory activity. Antinociceptive and anti-inflammatory activities of alginate-based microsphere loaded with extracts of P. amarus and P. muellerianus was here reported. The extract-loaded microspheres were prepared using the ionotropic gelation method. The particle size, swelling index, entrapment efficiency, and FTIR spectroscopy were determined. Antinociceptive and anti-inflammatory activities of extract-loaded microspheres were evaluated in hotplate-induced nociception in mice and carrageenan-induced rat paw oedema, respectively. The physicohemical results showed rigid, free-flowing and spherical microspheres, with particle sizes ranging from 985.977±13.65 to 1232±12.99 µm and entrapment efficiencies of 20.9 ± 0.341 to 45.0 ± 0.002 %. Polymer-drug interaction revealed bands indicating aromatics, alcohols and alkenes. The extract-loaded microspheres showed improved antinociceptive and anti-inflammatory activities when compared to the extracts alone. The sodium alginate-based microspheres loaded with Phyllanthus amarus and Phyllanthus muellerianus extracts showed acceptable physicochemical properties and had improved antinociceptive and anti-inflammatory activity compared to the extracts alone.

DEVELOPMENT, CHARACTERIZATION, AND OPTIMIZATION OF REPAGLINIDE LOADED SPANLASTICS ALONG WITH INVESTIGATION OF DRUG SOLUBILITY IN VARIOUS MEDIA

Objective: This study seeks to explore the solubility of an antidiabetic drug with poor water solubility, Repaglinide (RPG), in various media, and develop and optimize RPG-loaded spanlastic formulations. Methods: A 72-hours solubility study was conducted for RPG in different media, followed by UV spectrum analysis. Spanlastics containing RPG were prepared through the thin-film hydration (TFH) method combined with ultrasonication, incorporating varying concentrations ofthe lipophilic, non-ionic surfactant agents, Span 60 and Tween 80. Characterization was performed To assess particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). Optimization was achieved by analysing characterization results and using a mixture design of Design Expert software which predicted the optimized formula. Results: RPG exhibited the highest solubility in phosphate buffer saline (PBS, pH 6.8) incorporating 0.5% Tween 20 (168.595 µg/mL), followed by PBS with 0.1% Tween 80 (80.355 µg/mL), PBS alone (56.163 µg/mL), and PBS with 0.1% sodium lauryl sulphate (SLS) (53.706 µg/mL). UV scanning in methanol revealed three characteristic absorption bands for RPG, with peak selection optimized for molar absorptivity in each medium. The RPG-loaded spanlastic formulations demonstrated nano-sized vesicles with uniform size distribution, high stability, and efficient drug encapsulation. Optimized spanlastics predicted a particle size 126.162 nm, PDI 0.416, ZP-43.258 mV, and EE% 77.753%. Conclusions: This research emphasizes the potential of optimized RPG-loaded spanlastics, developed through the thin-film hydration method, as a promising approach for improving the solubility and stability of poorly water-soluble drugs. RPG showed the highest solubility in PBS (pH 6.8) containing 0.5% Tween 20, and the formulation achieved desirable nanosize, uniformity, and high encapsulation efficiency. Peer Review History: Received 12 July 2024; Reviewed 16 September 2024; Accepted 23 October; Available online 15 November 2024 Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, asia_abdullah65@yahoo.com Average Peer review marks at initial stage: 6.0/10 Average Peer review marks at publication stage: 7.5/10 Reviewers: Antonio José de Jesus Evangelista, Federal University of Ceará, UFC, Brazil, tony_biomed@hotmail.com Asmaa Ahmed Mohamed Ahmed Khalifa, Pharos University, Alexandria, Egypt, asmaa.khalifa@pua.edu.eg

DEVELOPMENT, OPTIMIZATION AND ASSESSMENT OF NAPROXEN MICROSPONGES BY BOX-BEHNKEN DESIGN AS A TARGETTED AND CONTROLLED RELEASE DRUG DELIVERY

Objective: Due to weak physical, chemical stability and poor bioavailability of Naproxen conventional dosage form; the purpose of this work is to improve formulation stability, additionally to accomplish highest possible concentration of the drug in the blood by preparing Naproxen loaded microsponges. Methods: Naproxen Microsponge (NM) was created utilising the quasi emulsion technique. In this process Ethyl Cellulose (EC) acts as a polymer, Poly Vinyl Alcohol (PVA) acts as the emulsifier, and Dichloromethane acts as the solvent. To investigate how changes in different formulation and processing parameters affect important product qualities, a Box Behnken Design (BBD) was used. Particle Size, Percentage Yield, and Entrapment Efficiency (%EE) were selected as response factors, whereas independent variables including EC quantity (X1), PVA concentration (X2), and Stirring Speed (X3) were selected as independent variables. Results: The microsponges underwent thorough analysis using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), X-Ray Diffraction (XRD), and Particle Size analysis. The evaluation included studying the morphology, drug loading, and in vitro drug release. The compatibility studies showed no chemical interactions between the drug and the polymers used. It was observed that the ratio of drug to polymer had a significant impact on drug content, EE and particle size. The SEM results revealed that the microsponges were spherical with a porous surface and had a mean particle size of 15.15 µm. The in vitro drug release studies demonstrated that the optimized Naproxen Microsponge Formulation (NMF2) achieved over 80% extended drug release by the end of 8 h, following the Corsmeyer Peppas Model. Conclusion: The Naproxen loaded microspheres possessed a sustained release with improved bioavailability and better stability.

Development of paroxetine loaded nanotransferosomal gel for intranasal delivery with enhanced antidepressant activity in rats

The aim of this study was to develop paroxetine (PXT) loaded nanotransferosomal gel (PXT-NTFG) for intranasal brain delivery. The process involved fabricating PXT-NTFs (paroxetine-loaded nanotransferosomes) through a thin film hydration method and optimizing them based on parameters such as particle size (PS), zeta potential (ZP), polydispersity index (PDI), and entrapment efficiency (EE). The optimized PXT-NTFs exhibited uniform morphology with a PS of 158.30 ± 2.73 nm, low PDI (0.142 ± 0.072), high ZP (21.00 ± 0.75 mV), and excellent EE (88.09 ± 3.40 %). Characterization through various techniques confirmed the incorporation of PXT into the nanotransferosomes and its conversion to amorphous state. Moreover, PXT-NTFG was formulated with suitable viscosity and mucoadhesive properties. In vitro release studies demonstrated sustained drug release from PXT-NTFG at different pH levels as compared to PXT-NTFs and NTF dispersion. Similarly, ex vivo experiments showed 4 folds enhanced drug permeation from PXT-NTFG when compared with PXT conventional gel. Stability studies indicated that the optimized PXT-NTFs remained stable for four months at 4°C and 25°C. Additionally, improved behavioral outcomes, increased neuronal survival rates, and upregulated brain-derived neurotrophic factor (BDNF) expression was observed in lipopolysaccharide (LPS) induced depressed Sprague-Dawley rats after treatment with PXT-NTFG as compared to PXT-dispersion treated and untreated LPS-control groups. Notably, the formulation led to a significant reduction in brain and plasma TNF-α levels. In conclusion, intranasal PXT-NTFG is a promising formulation with sustained drug release, improved brain targeting and enhanced antidepressant activity.

Formulation and Optimization of Solid Lipid Nanoparticle-based Gel for Dermal Delivery of Linezolid Using Taguchi Design.

Linezolid (LNZ) is a synthetic oxazolidinone antibiotic approved for the treatment of uncomplicated and complicated skin and soft tissue infections caused by gram-positive bacteria. Typically, LNZ is administered orally or intravenously in most cases. However, prolonged therapy is associated with various side effects and life threatening complications. Cutaneous application of LNZ will assist in reducing the dose, hence minimizing the unwanted side/adverse effects associated with oral administration. Dermal delivery provides an alternative route of administration, facilitating a local and sustained concentration of the antimicrobial at the site of infection. The current research work aimed to formulate solid lipid nanoparticles (SLNs) based gel for dermal delivery of LNZ in the management of uncomplicated skin and soft tissue infections to maximise its benefits and minimise the side effects. SLNs were prepared by high-shear homogenisation and ultrasound method using Dynasan 114 as solid lipid and Pluronic F-68 as surfactant. The effect of surfactant concentration, drug-to-lipid ratio, and sonication time was investigated on particle size, zeta potential, and entrapment efficiency using the Taguchi design. The main effect plot of means and signal-to-noise ratio were generated to determine the optimized formulation. The optimized batch was formulated into a gel, and ex-vivo permeation study, in-vitro and in-vivo antibacterial activity were conducted. The optimised process parameters to achieve results were 2% surfactant concentration, a drug-to-lipid ratio of 1:2, and 360 s of sonication time. The optimized batch was 206.3± 0.17nm in size with a surface charge of -24.4± 4.67mV and entrapment efficiency of 80.90 ± 0.45%. SLN-based gel demonstrated anomalous transport with an 85.43% in vitro drug release. The gel showed a 5 cm zone of inhibition while evaluated for in vitro antibacterial activity against Staphylococcus aureus. Ex-vivo skin permeation studies demonstrated 20.308% drug permeation and 54.96% cutaneous deposition. In-vivo results showed a significant reduction in colony-forming units in the group treated with LNZ SLN-based gel. Ex-vivo studies ascertain the presence of the drug at the desired site and improve therapy. In-vivo results demonstrated the ability of SLN-based gel to significantly reduce the number of bacteria in the stripped infection model. The utilization of SLN as an LNZ carrier holds significant promise in dermal delivery.

Entrapment behavior of argon bubbles and non-metallic inclusions under combined magnetic fields in slab continuous casting

The entrapment of argon bubbles and non-metallic inclusions under combined applications of electromagnetic braking (EMBr) and electromagnetic stirring (EMS) is receiving increasing attention in slab continuous casting. A Eulerian-Lagrangian model, incorporating Archimedes electromagnetic force, was established to study the entrapment behavior of particles under multi-mode electromagnetic fields. Results showed that the novel EMBr device could enhance the mixing of liquid steel around the nozzle and significantly suppress inclusion entrapment. The optimal magnetic induction intensity ranged from 0.218 T to 0.272 T based on the number of entrapped particles beneath the slab surface. Furthermore, employing appropriate drag force coefficients and considering the Archimedes electromagnetic force were crucial for predicting the quantity and size of entrapment particles. Particles from the nozzle jet experienced a downward electromagnetic force induced by EMBr. EMS tended to drag particles toward the solidified shell, with a more pronounced effect on large-sized particles. More particles were entrapped by the solidified shell in numerical results. Further research should account for Archimedes electromagnetic force in quantitative examination of inclusion entrapment.

Comparative Study of Lycopene-Loaded Niosomes Prepared by Microfluidic and Thin-Film Hydration Techniques for UVB Protection and Anti-Hyperpigmentation Activity.

Niosomes are employed for their improved physical properties and stability and as a controlled delivery system. However, their large-scale production and different preparation methods affect their physical properties. The microfluidic method represents a novel approach to the preparation of niosomes that enables precise control and decreases the preparation time and steps compared to alternative methods. The UVB protection and anti-hyperpigmentation activities of lycopene-loaded niosomes prepared by microfluidic (MF) and novel conventional thin-film hydration (THF) methods were compared. Extract powders from tomatoes (T), carrots (C), and mixed red vegetables (MR) were utilized to prepare lycopene-rich extract-entrapped niosomes. The resulting niosome formulations were characterized by particle size, polydispersity index (PDI), zeta potential, FT-IR spectra, entrapment efficiency, lycopene-release profile, permeation, and stability. The lycopene extract-niosome formulations were evaluated for their potential to provide UVB protection to human keratinocytes (HaCaT) and for their anti-melanogenesis effects on B16F10 melanoma cells. The results indicated that niosomes prepared by the MF method exhibited high uniformity and homogeneity (reflected by a low PDI value) and maintained smaller sizes when processed through a chip utilizing a hydrodynamic flow-focusing (HFF) platform compared to THF niosomes. The release kinetics of all lycopene-niosome formulations followed the Korsmeyer-Peppas model. The FT-IR spectra indicated that lycopene was incorporated into the niosome bilaminar membrane. Moreover, niosomes obtained from MF demonstrated enhanced stability during heating-cooling cycles, along with high UVB protection and anti-melanogenesis effects. Therefore, these developed niosome preparation methods could be effectively applied to topical products.