Carrier Formulation Research Articles

Formulation, development and in vivo characterization of selegiline hydrochloride nanostructured lipid nanocarrier loaded microneedle array patch for depression.

Depression is a common mental condition causing depressed mood and loss of pleasure. The primary treatment approach for the management of depression consists of the use of selegiline (MAO-B) inhibitor compound. The present work aimed to develop and optimize selegiline-loaded nanostructured lipid carriers for transdermal application, utilizing a 23 full factorial design approach. The optimized nanostructured lipid carriers formulation (Batch B7) demonstrated a particle size of 158.71±0.56nm, a narrow size distribution (0.266±0.006), high entrapment efficiency (59.60±0.34%), and a zeta potential of -23.2±2.21mV. Furthermore, x-ray diffraction and differential scanning calorimetry studies revealed the amorphous transformation of selegiline within the nanostructured lipid carrier. Transmission Electron Microscopy study has shown that nanostructured lipid carrier particles had a spherical shape with a smooth surface. These optimized nanostructured lipid carriers were then incorporated into a microneedle array patch for transdermal delivery. The selegiline-loaded nanostructured lipid carrier microneedle array patch exhibited no skin irritation in a rabbit model. It enhanced drug diffusion ex vivo (1.13-fold compared to pure selegiline-loaded microneedle array patch) with 90% drug release in 12h. The pharmacokinetic study demonstrated a steady and controlled release profile with a half-life of 29.9±0.14h and AUC0-t (26.57±0.51 μg/ml*h) of selegiline loaded nanostructured lipid carrier microneedle array patch. On the contrary, a pure selegiline-loaded microneedle array patch showed a short half-life of 6.5±0.26h and AUC0-t (20.90±0.31μg/ml*h). The sustained release profile and prolonged half-life in plasma and the brain suggest improved therapeutic efficacy. Histopathology analysis revealed no significant toxicity to vital organs. Thus, a selegiline nanostructured lipid carrier-loaded microneedle array patch can increase brain bioavailability compared to a pure selegiline-loaded microneedle array patch for managing depression.

Optimization and Characterization of a Nanostructured Lipid Carrier Containing α-Tocopherol/Tocotrienol Prepared using Rice Bran Oil and Palm Kernel Stearin

Background: α-tocopherol and tocotrienol are known for their antioxidant properties and cannot be produced directly in the human body. However, their use remains limited because of their low solubility, instability, and susceptibility to oxidation and high temperatures. Objective: This study aims to identify the optimal formulation of a carrier of phytonutrient α- tocopherol/tocotrienol prepared via ultrasonication with rice bran oil (RBO), palm kernel stearin (PKS), and Tween 80 and determine the characteristics of the optimal formulation during storage. Methods: The box-behnken design (three factors and levels) was used to determine the formulation of a nanostructured lipid carrier -tocopherol/tocotrienol (NLC-TT) based on the solid: liquid lipid ratio, total lipid: surfactant ratio, and sonication time. Results: The optimal NLC-TT formulation prepared with a solid: liquid lipid ratio of 7.5:2.5, total lipid: surfactant ratio of 1:3.9, and sonication time of 12 min and 6 s yielded a particle size of 126.7 nm, a polydispersity index of 0.339, a zeta potential of -31.7 and an encapsulation efficiency (EE) of 96.4%. During storage, NLC-TT and NLC-free particles exhibited particle sizes of 123.6-144.2 nm, polydispersity indices of 0.245-0.339, zeta potentials of -31.7--39.6 mV, EEs of 96.4%-89.6%, stabilities of 2.02-1.63, peroxide values of 0.05-0.25 mEqO2/kg, anisidine values of 0.07-1.60 and free fatty acid contents of 0.04%-0.08%. Conclusion: RBO and PKS are potential lipid-based carrier systems for tocopherol/ tocotrienol and exhibit good stability during storage.

Formulation, Optimization, In-Vitro and In-Vivo Evaluation of Nateglinide-Loaded Nanostructured Lipid Carriers for Enhanced Bioavailability

Formulation, Optimization, In-Vitro and In-Vivo Evaluation of Nateglinide-Loaded Nanostructured Lipid Carriers for Enhanced Bioavailability

Comparative Assessments of New Hair-Straightening Cosmetic Formulations on Wavy Type 2 Hair

Hair straighteners are among the most technically complex products to be safely and effectively developed, and this challenge has increased even more with the higher incidence of resistant hair among consumers. This underscores the importance of studying new active ingredients, combinations and carrier formulations to improve performance without compromising safety. In this research, we compared eight hair-straightening formulations with different active ingredients and/or concentrations to develop new, safer and more effective texture modifiers. Eight formulations were developed and compared with each other and to controls (virgin and bleached hair) regarding mechanical and thermal resistance, cuticle morphology, hair shine and fiber diameter. Results showed that all formulations were safe and effective at straightening hair. Specifically, 13.3% and 9.4% ammonium thioglycolate (G03 and G04) were more suitable for wavy and curly hair, 12.5% and 7.9% amino methyl propanol thioglycolate (G05 and G06) for finer or chemically processed hair, 5% and 4% sodium cysteamine (G07 and G08) for curly and tight curly hair to control volume, and 2% and 1% of a combination of ammonium thioglycolate with sodium thioglycolate (G09 and G10) for more resistant wavy and curly hair.

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.

Formulation and Characterization of Resveratrol-Loaded Nanostructured Lipid Carriers (NLC) with Mesua ferrea Seed Oil as Liquid Lipid

Nanostructured Lipid Carriers (NLCs) are colloidal drug delivery systems composed of both solid and liquid lipids. They enhance drug loading capacity, regulate the release of poorly water-soluble drugs, and are suitable for targeted delivery. Resveratrol, a polyphenol with promising anticancer properties, faces challenges due to its low water solubility, poor bioavailability, and chemical instability, resulting in rapid metabolism and excretion. Therefore, it is crucial to develop a delivery system that safeguards resveratrol during its transit through the body. This study aimed to develop and characterize resveratrol-loaded NLCs using the nano-precipitation method followed by ultrasonication, incorporating Mesua ferrea seed oil as the liquid lipid. The NLCs were evaluated for particle size, morphology (TEM), zeta potential, drug entrapment efficiency, drug loading, and in vitro drug release. The resulting NLCs demonstrated stability and homogeneity, with a particle size of 181.6 ± 12.4 nm, a polydispersity index (PDI) of 0.135 ± 0.09, drug entrapment efficiency of 82.76 ± 12.2%, and drug loading capacity of 42.94 ± 7.5%. They exhibited sustained drug release, achieving 84.56% release within 24 h. These findings suggest that the developed NLCs can effectively enhance the incorporation and controlled release of poorly water-soluble drugs like resveratrol, offering potential advantages over conventional delivery systems.

Preparation and Characterization of Nanostructured Lipid Carriers (NLCs) Containing Glycyrrhiza glabra Extract for the Treatment of Skin Hyperpigmentation.

This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation. Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using Dynamic Light Scattering (DLS). The best formulation was chosen for further surface characterization, including Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), and Fouriertransform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation. Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic. The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.

Design Formulation of Nanospanlastic Novel Carriers as a Promising Approach to Enhanced Bioavailability in Intranasal Drug Delivery for Sinusitis: Statistical Optimization and In vitro and In vivo Characterization

Background: Most new biologically active chemicals require better water solubility and slower dissolution rates. Cefdinir (CFD) has a very low bioavailability in its crystalline form and is poorly soluble in water. Objective: By preparing cefdinir's spanlastic nanovesicles (SNVs) using the ethanol injection method, the current study has attempted to enhance the drug's solubility and bioavailability using a statistical design approach. Methods: Independent variables, including the nonionic surfactant concentration, edge activator (EA), sonication time, SNVs entrapment efficiency, particle size, zeta potential, PDI, and in vitro release, have been evaluated. The best CFD-SNVs were positioned within in situ gel with muco-adhesive properties made of hydroxypropyl methylcellulose and deacetylated gellan gum. By contrasting intranasal injection of the produced gel with an IV solution, animal models have been used to investigate CFD's systemic and cerebral dynamics. Results: Statistical analysis has suggested an ideal SNVs formulation with nonionic surfactant (65 mg), EA (15 mg), and sonication (3 min). The sol-gel temperature for forming the mucoad-hesive in situ gel containing SNVs has been found to be 34.03°C, and 18.36 minutes has been the extended mucociliary transit time. Following intranasal injection, compared to SNV dispersion, the gelling system has exhibited higher brain bioavailability (2251.9 ± 75 vs. 5281.6 ± 51%, re-spectively). The gel has also demonstrated effective drug targeting of the brain with higher direct transport percentage indices. Conclusion: Mucoadhesive in situ gel with CFD-loaded SNVs can be administered via the in-tranasal route. To enhance bioavailability in the brain and drug targeting from the nose to the brain, nasal in situ gel loaded with CFD-SNVs could be a new carrier to be employed in sinusitis.

Nanostructured lipid carrier formulation for delivering poorly water-soluble ITF3756 HDAC inhibitor

Histone deacetylases (HDACs) are enzymes that play crucial roles in cellular processes by hydrolyzing acetyl-L-lysine side chains in core histones, thereby regulating gene expression and maintaining homeostasis. Histone deacetylase inhibitors (HDACi) have emerged as promising agents, particularly in cancer treatment, due to their ability to induce cytotoxic and pro-apoptotic effects. Selective HDAC6 inhibitors, such as ITF3756, have shown low off-target toxicity and promising pharmacological activities, but their poor water solubility limits their application in nanoparticulate drug delivery systems. Here, we optimized a nanostructured lipid carrier (NLC) formulation for delivering ITF3756 using the design of experiments (DOE) and response surface methodology (RSM). An interaction between the factor surfactant and formulation volume was observed, thus demonstrating that the surfactant concentration impacts the NLC size. It can be speculated that the higher the amount of the drug in the formulation, the lower the polydispersion index (PDI), thus resulting in more stable nanostructures. The optimized ITF3756-NLC demonstrated a size of 51.1 ± 0.3 nm, 8.85 ± 4.71 mV charge, and high entrapment efficiency (EE%), maintaining stability for 60 days. Moreover, ITF3756-NLC enhanced α-tubulin acetylation in melanoma, lung, and brain cancer cell lines, indicating retained or improved bioactivity. The ITF3756-NLC formulation offers a viable approach for enhancing the bioavailability and therapeutic efficacy of HDAC6 inhibitors, demonstrating potential for clinical applications in cancer immunotherapy.

Cutaneous Lupus Erythematosus Treatment Revolution: Exploring the Latest Nano Lipid Drug Delivery Innovations

: This review article aims to explore recent advancements in the treatment of Cutaneous Lupus Erythematosus (CLE) by focusing on the innovative use of Nano Lipid Carrier formulations. It assesses the efficacy, safety, and potential therapeutic benefits of these novel formulations in managing CLE symptoms. A comprehensive search was conducted across various scientific databases, including PubMed, MEDLINE, and Google Scholar, to identify relevant studies, clinical trials, and reviews pertaining to CLE treatment, particularly those involving various NLC formulations. Studies were selected based on their relevance to CLE treatment, with a specific emphasis on recent innovations. Data extraction involved gathering information on study design, intervention methods, outcomes, and conclusions related to the efficacy and safety of novel formulations in managing CLE symptoms. The synthesized data reveal promising outcomes associated with the use of NLC in treating CLE. These formulations offer enhanced drug delivery, improved skin penetration, and targeted therapy, resulting in better symptom management and reduced adverse effects compared to conventional treatments. Various studies demonstrate the efficacy of NLC embedded in reducing inflammation, controlling disease activity, and improving the quality of life for CLE patients. The latest advancements in CLE treatment, using novel methods, present a significant revolution in managing this chronic autoimmune skin condition. The reviewed literature highlights the potential of Nano lipid carrier embedded hydrogel as a promising therapeutic approach for CLE, offering improved efficacy, safety, and patient compliance. Further research and clinical trials are warranted to validate these findings and establish NLC as a standard treatment modality for CLE.

Using kraft lignin nanoparticles for the stabilization of nano/micro wax carriers

Due to its amphiphilic structure, lignin has the potential to stabilize emulsions via adsorption at the oil/water interface. By converting lignin into nanoparticles, we can significantly enhance its emulsion-stabilizing capabilities through a Pickering-type stabilization mechanism. Two essential elements may be modified to fine-tune emulsion stability: the size of the lignin nanoparticles (LNPs) and the physicochemical nature of the lipid phase. In this context, we highlight the behavior and utility of unmodified LNPs in the preparation of Pickering emulsions made up of water and a complex bio-based pharmaceutical-grade wax that can be used for the formulation of lipid carriers. As a proof-of-concept, we employ the developed Pickering emulsions to encapsulate indocyanine green (ICG), an FDA-approved dye commonly used in medical imaging applications. We demonstrate that ultra-small LNPs are well-suited for the colloidal stabilization of pharmaceutical wax ester micro beads. This stabilization does not require any lignin modification. Additionally, we present evidence that our new lipid/lignin hybrid carrier has potential as a new drug delivery system.

Biodegradability and formulation of triclosan-degrading and plant-growth-promoting Pseudomonas sp. MS45

Abstract. Sipahutar MK. 2024. Biodegradability and formulation of triclosan-degrading and plant-growth-promoting Pseudomonas sp. MS45. Biodiversitas 25: 2980-2992. This study presents the isolation of Pseudomonas sp. MS45, a microorganism that can consume triclosan (TCS) as its only carbon and energy source, leading to its detoxification. The rarity of a toxicity study of TCS before and after biodegradation treatment is addressed in this study. Allium cepa's genotoxicity exposed TCS's cytotoxicity, generating multiple damaged chromosomes, in contrast to the insignificant consequences of its broken-down metabolites. The study also optimized the different kinetic parameters for TCS-specific biodegradation and Pseudomonas sp. MS45-specific growth. The biodegradation pattern followed the Michaelis-Menten model with a maximum specific biodegradation rate (Vmax) of 0.01 µmole h-1 mg cell protein-1 and a half saturation constant (Ks) of 21.98 µM. The growth pattern followed the Haldane model with a maximum specific growth rate (µmax) of 0.03 h-1, half saturation constant (Ks) of 4.56 µM, and TCS inhibition constant (Ki) of 32.81 µM. In addition to its TCS-degrading ability, Pseudomonas sp. MS45 also possesses various plant growth promotion traits, and it was incorporated into two solid carrier formulations: vermiculite and rice bran. The study found that vermiculite, especially with PEG, was the most consistent formulation for Pseudomonas sp. MS45, in terms of maintaining bacterial survival and TCS-degrading ability. This study marks the initial report on the biodegradation and formulation of TCS-destroying and Plant-Growth-Promoting (PGP) Pseudomonas sp. MS45, offering promising implications for environmental and agricultural applications.

Enhanced assembly stability for amine-based cationic glycolipid

Glycolipids incorporating positive charges, mediated by an imidazolium cation, have shown potential for effective formulation of vesicular drug carriers, reflecting repulsive electrostatic forces, promoting the formation of nanosized assemblies and preventing unwanted Oswald ripening (Goh et al. (2019), ACS Omega 4, 17,039). Our continuous development of an assembly-based drug delivery system prompted us to investigate a pH-sensitive analogue, leading to the synthesis of a 6-amino-Guerbet glycoside. However, in contrast to the imidazolium counterpart, the amine-mediated charge increased the intermolecular cohesions, furnishing bigger assemblies instead, which further increased upon introduction of acid. Moreover, assemblies exhibited a significantly reduced positive charge density. It is concluded that strong proton-initiated hydrogen bonding between amino groups provide cohesive head group interactions overcompensating possible repulsive charge interactions. While this behavior invalidates the application of the amino-glucoside as dispersing agent for the formulation of small vesicles, it potentially paves a route towards enhanced vesicle stability.

Formulation of Metoclopramide Hydrochloride-Loaded Lipid Carriers by QbD Approach for Combating Nausea: Safety and Bioavailability Evaluation in New Zealand Rabbit.

The focus of the research was to overcome the limitations of metoclopramide (MTC) when administered intranasally. The aim was to improve its bioavailability, increase patient compliance, and prolong its residence time in the nasal cavity. MTC-loaded liposomes were prepared by applying the film hydration method. A study was conducted to determine how formulation variables affected encapsulation efficiency (EE %), mean particle size (MPS), and zeta potential (ZP). The MTC-liposomes were further loaded into the in situ gel (gellan gum) for longer residence times following intranasal administration. pH, gelling time, and in vitro release tests were conducted on the formulations produced. In vivo performance of the MTC-loaded in situ gels was appraised based on disparate parameters such as plasma peak concentration, plasma peak time, and elimination coefficient compared to intravenous administration. When the optimal liposome formulation contained 1.98% of SPC, 0.081% of cholesterol, 97.84% of chloroform, and 0.1% of MTC, the EE of MTC was 83.21%, PS was 107.3 nm. After 5 h, more than 80% of the drug was released from MTC-loaded liposome incorporated into gellan gum in situ gel formulation (Lip-GG), which exhibited improved absorption and higher bioavailability compared to MTC loaded into gellan gum in situ gel (MTC-GG). Acceptable cell viability was also achieved. It was found out that MTC-loaded liposomal in situ gel formulations administered through the nasal route could be a better choice than other options due to its ease of administration, accurate dosing, and higher bioavailability in comparison with MTC-GG.

Formulation and evaluation of piperine-loaded ultra-small unilamellar carrier

Background: Piperine is an alkaloid that has a stimulatory effect on the proliferation and dentricity of melanocytes. Therefore, it is a potential drug for vitiligo. Objectives: To formulate an Emulgel containing piperine-loaded Ultra-Small Unilamellar Carrier (USUC) with virgin coconut oil, soy lecithin and tween 80, and to evaluate the physicochemical properties. Method: Piperine-loaded USUC was formulated using a spontaneous water phase titration method at a stirring speed of 1500 rpm for 15 minutes with a base composition of 2.3% oil phase, 1% surfactant and 2.3% co-surfactant. Emulgel preparations were made by mixing USUC piperine into a 5% carbopol base. Result: Piperine-loaded USUC was obtained in the form of spherical globules with a Z-average size of 15.0 nm, a zeta potential of -39.5 mV and a polydispersion index of 0.312. The emulgel preparation has a pH of (6.5 ± 0.1), and a viscosity (of 44.800 ± 0.367) cP and is physically stable. Permeation of piperine from USUC emulgel follows zero-order kinetics (y = 0.130x-2.027; R2 = 0.9998) with a flux value of (3.408 ± 1.110) µg/cm2/hour, which is significantly different from permeation of non-USUC piperine gel (0.000 ± 0) µg/cm2/hour)(p &lt;0.05). Conclusion: Piperine-loaded USUC in emulgel formulation produced nanosized spherical globules, indicating a significantly different amount of permeated piperine compared to conventional piperine gel.

An Updated Comprehensive Review on Novel Drug Delivery Systems (NDDS) In the Pharmaceuticals

The field of pharmaceutical sciences has witnessed a paradigm shift with the advent of Novel Drug Delivery Systems (NDDS), which aim to enhance therapeutic efficacy, reduce side effects, and improve patient compliance. This comprehensive review explores the latest advancements and innovations in NDDS, encompassing a diverse range of delivery platforms and strategies.(NDDs are transforming the landscape of pharmaceutical treatment, offering unparalleled potential for enhanced therapeutic efficacy, improved bioavailability, controlled release, targeted delivery, and enhanced stability. This comprehensive review explores the diverse landscape of NDDS, highlighting recent advancements and addressing key challenges. Prominent NDDS include liposomes, nanoparticles, micelles, polymeric drug conjugates, monoclonal antibodies, implants, and patches. Each system possesses unique properties and applications, tailored to specific drugs and therapeutic needs. Recent breakthroughs in targeted nanocarriers, gene therapy vectors, and 3D-printed personalized dosage forms are pushing the boundaries of innovation. The main highlights of the present review firstly the basics on NDDs, the several approaches of nano drug carriers for the drug delivery with their preparation methods and example. The middle version of review discuss the recent advancements techniques in the preparation of NDDs carriers and lastly the marketed formulation of particular drug carrier.

Development of a Versatile Lipid Core for Nanostructured Lipid Carriers (NLCs) Using Design of Experiments (DoE) and Raman Mapping.

The objective of this study was to develop a versatile lipid core for the 'brick-dust type of drugs' (poorly water-soluble and poorly lipid-soluble drugs). In the first step, excipients of different polarities were classified according to their behavior in aqueous solutions. Subsequently, binary mixtures were prepared with cetyl palmitate (Crodamol™ CP pharma, Campinas, São Paulo, Brazil) as the solid lipid, and its miscibility with other excipients was evaluated using Raman mapping and classical least squares (CLS). Based on the results, the excipients Crodamol™ CP pharma (hydrophobic), Super Refined™ DMI (dimethyl isosorbide; hydrophilic, Mill Hall, PA, USA), and Super Refined™ Lauryl Lactate (lauryl lactate, medium polarity, Mill Hall, PA, USA) were chosen to compose the lipid core. The ideal proportion of these excipients was determined using a mixture design and the standard deviation (STD) of image histograms as the response variables. After statistical evaluation of the DoE results, the final composition was determined, and drugs with different logP (0 to 10) and physicochemical characteristics were evaluated in the optimized mixture. The drugs butamben (Sigma-Aldrich Co., Spruce Street, St. Louis, MO, USA), tacrolimus (NutriFarm, São Paulo, Brazil), atorvastatin calcium, and resveratrol (Botica da Terra, Campinas, Brazil) presented a homogeneous distribution in the optimized lipid core, indicating that this is a promising system to be used in nanostructured lipid carrier (NLC) formulations of such types of drugs.

Foliar application of cyanobacterial formulations stimulates plant growth and fruit quality in tomato under protected cultivation

ABSTRACT Cyanobacterial biofertilizers enhance plant and soil productivity across crops, through soil-seed application at the field level; however, their use as foliar treatment is less investigated. This study evaluated the role of foliar sprays, initiated 4 weeks after transplantation of nursery-raised seedlings in beds, and effected at weekly intervals for a period of eight weeks. towards enhancing plant growth, yield and quality of tomato grown in a climate-controlled polyhouse. Sprays were composed of aqueous formulations of carrier alone, and those amended with the formulations of plant-growth-promoting cyanobacterium Anabaena laxa (A. laxa) or biofilm Anabaena torulosa -Trichoderma viride (An-Tr) or suspension of 100 µM Fe EDTA. A. laxa brought about a significant increase in nitrate reductase and glutamine synthetase activity in leaves by 13%–17%, along with 3-fold stimulation in carbonic anhydrase activity. Cyanobacterium-amended foliar agents significantly enhanced soil dehydrogenase, urease activity, along with increments in organic carbon, Fe, Zn in soil and stimulated yield, fresh weight and quality of fruits. Both cyanobacterial formulations were promising in enhancing plant growth, fruit yield and quality, however, A. laxa also significantly improved microbiological activity and nutrient enrichment in soil. Future research is focused towards optimising the dose and storage life of such foliar agents for protected horticulture.

Administration sequence- and formation-dependent vaccination using acid-degradable polymeric nanoparticles with high antigen encapsulation capability.

Vaccines aim to efficiently and specifically activate the immune system via a cascade of antigen uptake, processing, and presentation by antigen-presenting cells (APCs) to CD4 and CD8 T cells, which in turn drive humoral and cellular immune responses. The specific formulation of vaccine carriers can not only shield the antigens from premature sequestering before reaching APCs but also favorably promote intracellular antigen presentation and processing. This study compares two different acid-degradable polymeric nanoparticles that are capable of encapsulating a moderately immunogenic antigen, GFP, at nearly full efficacy via electrostatic interactions or molecular affinity between His tag and Ni-NTA-conjugated monomners. This resulted in GFP-encapsulating NPs composed of ketal monomers and crosslinkers (KMX/GFP NPs) and NTA-conjugated ketal monomers and crosslinkers (NKMX/GFP NPs), respectively. Encapsulated GFP was found to be released more rapidly from NKMX/GFP NPs (electrostatic encapsulation) than from KMX/GFP NPs (affinity-driven encapsulation). In vivo vaccination studies demonstrated that while repeated injections of either NP formulation resulted in poorer generation of anti-GFP antibodies than injections of the GFP antigen itself, sequential injections of NPs and GFP as prime and booster vaccines, respectively, restored the humoral response. We proposed that NPs primarily assist APCs in antigen presentation by T cells, and B cells need to be further stimulated by free protein antigens to produce antibodies. The findings of this study suggest that the immune response can be modulated by varying the chemistry of vaccine carriers and the sequences of vaccination with free antigens and antigen-encapsulating NPs.

An LC-MS/MS method development for dapagliflozinloaded nanostructured lipid carrier formulation in rabbit plasma

An LC-MS/MS method development for dapagliflozinloaded nanostructured lipid carrier formulation in rabbit plasma