Hausner Ratio Research Articles

Microscopic, Micromeritic and Phytochemical Analysis of the Leaves of Pseuderanthemum maculatum (G. Lodd.) I. M. Turner, A Plant with Potential Pharmacognistic Uses

Background: Pseuderanthemum maculatum, Pseuderanthemum maculatum (G.Lodd.) I.M.Turner [previously Pseuderanthemum carruthersii (Seem.) Guillaumin var. carruthersii] is an ornamental plant with potential pharmacognostic uses in the management of hypertension and cancers. There hadn’t been much work done on this plant previously hence making the current research work very much significant. Methods: The leaves were collected, identified, air dried, pulverized, weighed and subjected to evaluation parameters using standard procedures. GC-MS analysis was also carried out on the dichloromethane extract of the leaf. Results: The results showed that the stomatal distribution was hypostomatic with diacytic stomatal type. Stomatal index was 23.12% and the stomatal number was 60 (69.9 ± 2.65)86. Flow rate of the leaf was poor with the bulk volume of 32.30 ± 1.04, tapped volume of 21.8 ± 0.76, bulk density of 0.32 ± 0.02, tapped density of 0.46 ± 0.02, angle of repose 42.65°, Carr's index of 31.06% and Hausner's ratio of 1.45 ± 0.03. The chemomicroscopy and fluorescence analyses revealed characteristic features for the drug. The water-soluble, methanol-soluble, ethanol-soluble extractive values were 20.67 %w/w, 11.67 %w/w and 11.33 %w/w respectively. The moisture content of the leaf powder was 9.84%w/w. The total ash, acid-insoluble and water-soluble ash values were 6.72%w/w, 1.34%w/w and 16.17%w/w respectively. The GC-MS analysis revealed the presence of 11 chemical constituents with phytochemicals such as hexanoic acid, benzoic acid, undecenoic acid, heptanoic acid and Eicosane which are of useful pharmaceutical importance. Conclusion: These data obtained from the pharmacognostic studies provides information about the identity, purity and quality of Pseuderanthemum maculatum.

Rheological, Thermal and Physicochemical Properties of Bioprocessed Flour From Cowpea, Sorghum and Orange Fleshed Sweet Potato

ABSTRACTThis study investigated the rheological, physicochemical, and thermal properties of fermented and germinated whole reddish‐brown cowpea, white sorghum and orange‐fleshed sweet potato. Germination substantially reduced the pasting and rheological attributes of flour suspensions compared to the fermentation process. This study observed notable increases in the hot paste, setback, and final viscosities after the fermentation of cowpea and sorghum, indicating an improvement in the ease of cooking and greater retrogradation tendency of starch molecules. Among the fermented flours, sorghum had the highest hot paste viscosity (848 mPa s) and final viscosity (1451 mPa s). The mechanical fingerprint revealed a viscoelastic solid character, with G′ > G″ over the frequency range of 0–10 rad/s for all samples. Temperature sweep data showed a sharp increase in G′ at about 80°C, corresponding to the onset of starch gelatinization. Shear‐thinning behavior was observed, except in germinated and raw sorghum flours, where molecular rearrangement resulted in an initial viscosity rise at a low share rate (< 20 s−1). Differential scanning calorimetric analysis revealed a marginal variation in the peak transition temperature of gelatinization (98°C–104°C for all flours except raw sorghum flour, 83.87°C). The fermented sweet potato flour indicated good flour particle flowability expressed as Carr's compressibility index (30.99) and the Hausner ratio (1.45); however, the available reducing sugars could have influenced its high percentage solubility (49.83%), thus impacting low pasting viscosities. The contrasting technological features suggest an avenue to intensify efforts in exploring composite bioprocessed flours for applications in novel foods.

Influence of stearate dry coating on ibuprofen powder: What about the combustibility?

Dust explosion is one common type of process safety incident within the pharmaceutical industry. During powder processing, surface modification is widely used to increase dust flowability by alleviating inter-particle cohesion. However, it is currently unclear whether the addition of guest particles affects the combustibility of pharmaceutical powders. To investigate the explosion hazard of stearate-coated ibuprofen powder, this paper studied the ignition sensitivity and explosion severity of pure and coated ibuprofen by determining a series of explosion parameters in accordance with ASTM standards. The results indicated that the addition of stearate significantly reduced the minimum ignition energy of the mixture. Other parameters including the minimum ignition temperature, the minimum explosible concentration, the maximum explosion pressure, and the maximum rate of pressure rise were found to have less correlation with the improvement in dust flowability. Powder characterization through methods such as the Hausner ratio, scanning electron microscope, thermo-gravimetric analysis, and X-ray diffraction were employed to investigate chemical phase changes between coated mixtures and pure pharmaceuticals. The effects of improved dust flowability and dust dispersibility on the combustibility of ibuprofen dust were discussed to improve explosion-proof awareness in the pharmaceutical industry.

Encapsulation of ɣ-Aminobutyric Acid Compounds Extracted from Germinated Brown Rice by Freeze-Drying Technique

Gamma-aminobutyric acid (GABA) from plants has several bioactivities, such as neurotransmission, anti-cancer cell proliferation, and blood pressure control. Its bioactivities vary when exposed to pH, heat, and ultraviolet. This study analyzed the protective effect of the GABA encapsulation technique using gum arabic (GA) and maltodextrin (MD) and the freeze-drying method. The impact of different ratios of the wall material GA and MD on morphology, GABA content, antioxidant activity, encapsulation efficiency, process yield, and physical properties were analyzed. Results showed that the structure of encapsulated GABA powder was similar to broken glass pieces of various sizes and irregular shapes. The highest GABA content and encapsulation efficiency were, respectively, 90.77 mg/g and 84.36% when using the wall material GA:MD ratio of 2:2. The encapsulated powder’s antioxidant activity was 1.09–1.80 g of encapsulation powder for each formula, which showed no significant difference. GA and MD as the wall material in a 2:2 (w/w) ratio showed the lowest bulk density. The high amount of MD showed the highest Hausner ratio (HR), and Carr’s index (CI) showed high encapsulation efficiency and process yield. The stability of encapsulated GABA powder can be kept in clear glass with a screw cap at 35 °C for 42 days compared to the non-encapsulated one, which can be preserved for only 18 days under the same condition. In conclusion, this study demonstrated that the freeze-drying process for GABA encapsulation preserved GABA component extracts from brown rice while increasing its potential beneficial properties. Using a wall material GA:MD ratio of 2:2 resulted in the maximum GABA content, solubility, and encapsulation efficiency while having the lowest bulk density.

Development and Characterization of Fast-Dissolving Tablets to Enhance Bioavailability of BCS Class II Drugs by Solid Dispersion Method

Background: Rapid tablet or capsule dissolution requires the tablet to disintegrate and dissolve at a higher rate, enhancing drug dissolution and bioavailability. Suitable disintegrants have shown an appreciable rate of disintegration or dissolution. Using factorial design for formulation to improve bioavailability is a key focus in pharmaceutical research to enhance dissolution Methods: Azelnidipine (Azp) tablets were formulated with Hydroxypropyl β-cyclodextrin (HβCD), β-cyclodextrin (βCD), and Kolliphor HS15 (HS15) to enhance solubility. A 23 factorial design optimized the formulation, focusing on disintegration time (DT) and time for 90% dissolution (T90). Eight formulations (F1-F8) were prepared using the kneading method. Tablets were evaluated for physical properties, drug content, friability, dissolution, and drugexcipient interactions (FTIR and DSC). The optimal formulation (F9) was determined via desirability analysis. Results: Tablets showed acceptable Carr's index (CI), Hausner ratio (HR), and Angle of Repose (AR). Increasing βCD concentration decreased DT, enhancing water absorption and faster dissolution. βCD tablets had the lowest DT among the formulations, with F4 showing the best disintegration. Higher HS15 concentration also reduced DT, with F8 achieving the highest drug release (T90%) within 60 minutes. R² values ranged from 0.922 to 0.994, indicating high predictability. The optimal formulation had a desirability of 1.0, consisting of 3.523 mg HS15, 28.4 mg βCD, and 1.49 mg βCD, with a DT of 102 ± 1.13 seconds and 98% dissolution. FTIR and DSC confirmed no drug–excipient interactions. Conclusion: Optimized super disintegrant concentrations and wet granulation techniques resulted in tablets with strong mechanical properties, rapid disintegration, and consistent drug content. Future research and in vivo studies should explore additional excipient combinations.

Application of SAP to Improve the Handling Properties of Iron Ore Tailings of High Cohesiveness: Could a Reagent Help the Decommissioning Process of a Dam?

This work aims to evaluate the use of a superabsorbent polymer (SAP) to provide improvements in the handling properties of iron ore tailings (IOT). The material studied came from the magnetic separation reprocessing of the material discarded at the Gelado Dam, located in Serra dos Carajás in the state of Pará, Brazil. While the concentrate presents reasonable handling conditions, the tailings, with 61.5% iron, 15% moisture, and 39% of the mass, have high cohesiveness and adhesiveness due to their fine nature and the climatic conditions of the Amazon rainforest. However, the tailings can still be considered a product as long as the handling and transportation logistics are feasible. Thus, studies with an SAP and IOT were carried out in a bench rotating drum to promote mixing between them, and the main variables studied were the SAP dosage and the required contact time. The improvement in the physical properties of the IOT were evaluated considering the Hausner ratio, Carr index, Jenike’s flow function index, Atterberg limits, and chute angle. The superabsorbent polymer promoted a significant improvement in the state of consistency of the material, and the best performance was obtained with a dosage of 1000 g t−1. As long as a suitable contact condition was promoted, a contact time of 1 min was enough to achieve the expected benefits. After dosing with the superabsorbent polymer, the material’s handling classification changed from ‘cohesive’ to ‘easy flow’, and the chute angle was reduced from 90° to levels below 60°. It was concluded that the application of the superabsorbent polymer has the potential to improve the fluidity of the material discarded in the magnetic concentration operation, allowing it to be handled throughout the production and transportation chain. The SAP appears to be an important additive for the full use of the material present in the dam (100% recovery), with both economic and socio-environmental benefits.

Formulation and Evaluation of Glipizide-loaded Mucoadhesive Microparticle Using Salvia hispanica Seeds Mucilage as Co-polymer

Aims: Chia seed (Salvia hispanica L.) gum is a mucoadhesive, biodegradable polymer with sustained release properties. Objective: The objective of this study was to compare different formulations of glipizide-loaded microparticles using chia seed mucilage and sodium alginate, focusing on sustained release and mucoadhesive properties. Background: The present study aimed to comparatively evaluate various eco-friendly formulations of glipizide-loaded microparticles prepared using chia seed mucilage and sodium alginate. Materials and Methods: Gum was extracted from chia seeds and lyophilized, and preformulation studies were performed according to established protocols. Microparticles were formulated using the ionic gelation method, with sodium alginate as a copolymer and zinc chloride as a cross-linking agent. The prepared microparticles were evaluated using scanning electron microscopy (SEM) for size and particle aggregation, and Fourier Transform infrared spectroscopy (FTIR) for drug-polymer interaction, entrapment efficiency, swelling index, and in vitro drug release. Results: The % yield of chia seed mucilage was 27.35%. The pH of the mucilaginous suspension was 4.67 ± 0.50. The moisture content value was 14.56 % ± 0.50. The values of Carr's index and Hausner's ratio were 22.58 ± 1.89 and 1.38 ± 0.05, respectively. FTIR spectra showed no interaction between pure glipizide and chia seed mucilage, confirming no possible change in glipizide's pharmacology. SEM studies have confirmed the shape of the microparticles to be spherical, with average sizes ranging from 1235.18 ± 8.7 to 1423.25 ± 9.5 µm, and the drug entrapment efficiency ranged from 64.25 ± 2.52 to 81.82 ± 7.56%. The release of glipizide from the microparticles was sustained, and the Higuchi and Korsmeyer-Peppas models were found to be the best-fit kinetic models. Conclusion: The promising copolymer blend of chia seed mucilage and sodium alginate was used for the development of sustained-release dosage forms. A copolymer blend with a ratio of 1:1 produced glipizide-loaded microparticles with sustained release profiles and good mucoadhesive ability, along with a high percentage of drug entrapment efficiency.

Effects of Different Dehulling Methods on Physical and Chemical Properties of Tartary Buckwheat Flour

AbstractDehulling is a necessary step in the processing of Tartary buckwheat products. In this study, the effects of three different dehulling methods on the starch structure and physical and chemical properties of Tartary buckwheat are systematically analyzed. The results show that, first, explosion‐puffing dehulling treatment (EPT) destroys many of the starch granules, increases the average granular size by 261.7%, and decreases the ∆H by 66.5%; steam dehulling treatment (ST) and dry heat dehulling treatment (DHT) have no significant destructive effect on starch granules. Second, EPT increases the brightness and whiteness and decreases the Hausner ratio and Carr index of Tartary buckwheat flour, which gives Tartary buckwheat flour better fluidity and sensory quality. Third, EPT results in lower packed bulk density and smaller solubility changes with varying temperatures (50–90 °C), indicating that EPT is more applicable to the production of buckwheat tea. Fourth, ST achieves lower adhesiveness, higher hardness, and higher springiness, indicating that ST is more suitable for the production of buckwheat gel products. Fifth, DHT maximizes the retention of resistant starch (RS). ST maximizes rutin retention in buckwheat rice. These results can be used as a reference for selecting different dehulling methods for different buckwheat products.

High nitrogen steels produced by laser powder bed fusion – Processability of an additivated austenitic steel powder

The additivation of conventional metal powders allows the expansion of the range of materials and alloys suitable for powder bed fusion additive manufacturing of metals. The combination of material properties, the improvement of currently used powder properties, and their processability are the focus of this technique. This work investigates the influence of the additivation of Si3N4 particles to X2CrNi18–9 austenitic stainless-steel powder on the resulting powder properties and processability by PBF-LB/M. The aim is to process a composite material consisting of a steel matrix in which retained Si3N4 particles are embedded. A subsequent heat treatment by hot isostatic pressing should allow dissociation of Si3N4 and the associated nitrogen diffusion into the austenitic matrix to produce a high nitrogen steel (HNS). Despite some degradation in powder properties, as indicated by a decrease in the Hausner ratio from 1.24 to 1.15, PBF-LB/M successfully produced samples in a process window of 30–36 J/mm3.

Synthesis of agro-industrial wastes/sodium alginate/bovine gelatin-based polysaccharide hydrogel beads: Characterization and application as controlled-release microencapsulated fertilizers

Synthesis of novel agro-industrial wastes/sodium alginate/bovine gelatin-based polysaccharide hydrogel beads, micromeritic/morphometric characteristics of the prepared formulations, greenhouse trials using controlled-release microencapsulated fertilizers, and acute fish toxicity testing were conducted simultaneously for the first time within the scope of an integrated research. In the present analysis, for the first time, 16 different morphometric features, and 32 disinct plant growth traits of the prepared composite beads were explored in detail within the framework of a comprehensive digital image analysis. The hydrogel beads composed of 19 different agro-industrial wastes/materials were successfully synthesized using the ionotropic external gelation technique and CaCl2 as cross-linker. According to micromeritic characteristics, the ionotropically cross-linked beads exhibited 77.86 ± 3.55 % yield percentage and 2.679 ± 0.397 mm average particle size. The dried microbeads showed a good swelling ratio (270.02 ± 80.53 %) and had acceptable flow properties according to Hausner's ratio (1.136 ± 0.028), Carr's index (11.94 ± 2.17 %), and angle of repose (25.03° ± 5.33°) values. The settling process of the prepared microbeads was observed in the intermediate flow regime, as indicated by the average particle Reynolds numbers (169.17 ± 82.81). Experimental findings and non-parametric statistical tests reveal that dried fertilizer matrices demonstrated noteworthy performance on the cultivation of red hot chili pepper plant (Capsicum annuum var. fasciculatum) according to the results of greenhouse trials. Surface morphologies of the best-performing fertilizer matrices were also characterized by Scanning Electron Microscopy. Moreover, the static fish bioassay experiment confirmed that no abnormalities and acute toxic reactions occurred in shortfin molly fish (Poecilia sphenops) fed with dried leaves of red hot chili pepper plants grown with formulated fertilizers. This study showcased a pioneering investigation into the synthesis of microcapsules using synthesized hydrogel beads along with digital image processing for bio-waste management and sustainable agro-application.

Impact of variety and drying methods on the physicochemical, functional, and thermal properties of Ethiopian potato (Plectranthus edulis) tuber flour

This study aimed to analyse the physicochemical, structural, functional, and thermal properties of flour from two indigenous Ethiopian Potato (Plectranthus edulis) varieties, Chanqua and Loffo, and to compare with wheat flour (WF). The study also investigated how oven and sun drying methods affected the physicochemical properties of the flours. The results demonstrated a significant distinction (p ≤ 0.05) between the flour samples and WF, attributable to variations in both the varieties and the drying methods except that no significant difference in pH was observed due to the varieties, and the fibre and ash content did not vary significantly with the drying methods. The moisture content (MC) of the flours ranged from 5.72 % in oven-dried Chanqua Ethiopian potato flour (OD-CEPF) to 7.53 % in sun-dried Loffo Ethiopian potato flour (SD-LEPF), both of which were lower compared to WF. The protein content varied from 4.47 % (SD-CEPF) to 5.93 % (OD-LEPF). FTIR tests revealed a significant impact on the structural changes, leading to variations in the location and intensity of infrared absorption peaks, particularly in sensitive regions. Whereas, the XRD patterns showed characteristic B-type diffraction, with a relative crystallinity (RC) of 31.97 % in CEPF and 30.53 % in LEPF having a significant difference (p ≤ 0.05) between them. LEPF had better flow properties than CEPF, with lower Hausner ratio (HR) (1.16 vs. 1.25), Carr's index (CI) (14.51 % vs. 20.26 %), and angle of repose (31.00° vs. 34.67°). It also showed significantly higher (p ≤ 0.05) water absorption capacity (WAC), oil absorption capacity (OAC) and swelling power (SP) properties than CEPF. The study also indicated notable distinctions in the thermal and paring properties of flours. The oven drying method was found to be superior in enhancing the physicochemical properties, with LEPF showing better physicochemical, functional, structural, and thermal properties than CEPF.

Correlation analysis of feedstock flowability and temperature for laser-based powder bed fusion of polymers

Purpose For additive manufacturing (AM) through laser-based powder bed fusion of polymers (PBF-LB/P), accurate characterization of powder flowability is vital for achieving high-quality parts. However, accurately characterizing feedstock flowability presents challenges because of a lack of consensus on which tests to perform and the diverse forces and mechanisms involved. This study aims to undertake a thorough investigation into the flowability of eight feedstock materials for PBF-LB/P at different temperatures using various techniques. Design/methodology/approach For ambient temperature assessments, established metrics such as avalanche angle and Hausner ratio, along with the approximated flow function coefficient (FFCapp), are used. The study then focuses on the influence of elevated temperatures representative of in-process conditions. FFCapp and differential scanning calorimetry (DSC) are performed and analyzed, followed by a correlation analysis as a holistic approach to identify key aspects for flowability. Furthermore, two feedstock materials are compared with a previous study to connect the present findings to PBF-LB/P processing. Findings The study revealed intrinsic material properties such as mechanical softening near the melting point to become significant. This partially explains why certain powders with poor ambient temperature flowability are consistently demonstrated to produce high-quality parts. FFCapp and thermal characterization through DSC are identified as critical metrics for optimizing feedstock material characteristics across temperature ranges. Originality/value Previous studies emphasized specific characterizations of feedstock material at ambient temperature, presented a limited materials selection or focused on metrics such as shape factors. In contrast, this study addresses a partially understood aspect by examining the critical role of temperature in governing feedstock material flowability. It advocates for the inclusion of temperature variables in flowability analyses to closely resemble the PBF-LB/P process, which can be applied to material design, selection and process optimization.

Whey protein and maltodextrin conjugated foam-mat dried honey powder: Functional, physicochemical, structural, rheological and thermal characterization

Honey in its natural form possesses considerable challenges in mass production and transportation owing to its viscosity and stickiness, making it prone to crystallization over time. Dried honey powder makes it convenient for handling and processing. In this study, foam mat dried powder (FMDP) was obtained by foam mat drying technique in which whey protein isolate (WPI) and maltodextrin (MD) were used as foaming agent and foam stabilizer, respectively. The obtained FMDP was characterized in terms of physical, chemical, functional, phytochemical, rheological and structural properties to study the impact of foaming agents. WPI was found to improve the functionality, stability and glass transition temperature and on the other hand, MD was found to enhance the stability, crystallinity and the color of the FMDP. FTIR helped in understanding the changes in the functional groups attributed to the foaming agents. The crystallinity and the microstructural changes in the FMDP were observed from X-ray diffractograms and SEM micrographs, respectively. The rheological characterization confirmed the viscous nature of honey. The study confirmed the interaction between proteins and polysaccharides, which subsequently improved the heat stability, functional properties, solubility, emulsifying capacity, antioxidant properties, and solubility. The dried honey samples demonstrated minimal caking, low cohesiveness (Hausner ratio: 1.16 ± 0.027–1.29 ± 0.041), good and fair flowability (ranging between 14.25 ± 2.02–22.52 ± 2.25). Therefore, it can be concluded that during this study, protein and polysaccharide conjugate FMDP was obtained with better quality attributes, which can be further incorporated during various product development in food industries.

Analysis of physicochemical, functional, and antioxidant properties of four different Indian seaweed species

The present study aims to elucidate the nutritional, functional, flow, and antioxidant properties of Ulva fasciata, Ulva lactuca, Chaetomorpha linum, and Gracilaria edulis. The highest percentage of protein (24.26 %) in U. fasciata; fat (6.33 %) and total carbohydrates (46.39 %) in C. linum; crude fibre (8.67 %) in U. lactuca; ash (22.45 %) content in G. edulis was observed among the four-seaweed. The highest oil absorption capacity was found for C. linum (1.59 %), followed by G. edulis (1.21 %), U. lactuca (1.04 %), and U. fasciata (0.91 %). The water absorption capacity in U. fasciata (4.55 %) was observed to be the highest followed by C. linum (3.84 %), U. lactuca (3.78 %), and G. edulis (2.22 %). U. fasciata exhibited the highest solubility (35.83 ± 1.97 %) and emulsifying capacity (99.00 ± 0.00 %), while G. edulis showed the highest foaming capacity (75.00 ± 1.00 %). The angle of repose of G. edulis and C. linum powder showed excellent flowability than U. lactuca and U. fasciata. Carr's index and Hausner ratio showed that all seaweed samples were free-flowability, except for G. edulis and C. linum. The bulk density (0.71 g/cm3) and tapped density (0.85 g/cm3) of U. fasciata were observed to be the highest, whereas true density (1.11 g/cm3) was recorded highest in U. lactuca. The most increased antioxidant activity was found in G. edulis (65.90 %) followed by C. linum (53.01 %), U. lactuca (51.76 %), and U. fasciata (43.56 %). The total phenolic content (10.93 mg GAE/g) and flavonoid content (1.71 mg QE/g) were higher in U. fasciata. FTIR analysis detected the presence of amide, amino, hydroxyl, ester groups and it can conclude the presence of essential components such as proteins, amino acids, polysaccharides, and fat. Thus, the selected four marine seaweeds act as a good source of functional components and can be utilized for the development of functional food products such as bread, biscuits, cookies, tea, snacks, soups and beverages.

Inhaled Ivermectin-Loaded Lipid Polymer Hybrid Nanoparticles: Development and Characterization.

Ivermectin (IVM), a drug originally used for treating parasitic infections, is being explored for its potential applications in cancer therapy. Despite the promising anti-cancer effects of IVM, its low water solubility limits its bioavailability and, consequently, its biological efficacy as an oral formulation. To overcome this challenge, our research focused on developing IVM-loaded lipid polymer hybrid nanoparticles (LPHNPs) designed for potential pulmonary administration. IVM-loaded LPHNPs were developed using the emulsion solvent evaporation method and characterized in terms of particle size, morphology, entrapment efficiency, and release pattern. Solid phase characterization was investigated by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). Using a Twin stage impinger (TSI) attached to a device, aerosolization properties of the developed LPHNPs were studied at a flow rate of 60 L/min, and IVM was determined by a validated HPLC method. IVM-loaded LPHNPs demonstrated spherical-shaped particles between 302 and 350 nm. Developed formulations showed an entrapment efficiency between 68 and 80% and a sustained 50 to 60% IVM release pattern within 96 h. Carr's index (CI), Hausner ratio (HR), and angle of repose (θ) indicated proper flowability of the fabricated LPHNPs. The in vitro aerosolization analysis revealed fine particle fractions (FPFs) ranging from 18.53% to 24.77%. This in vitro study demonstrates the potential of IVM-loaded LPHNPs as a delivery vehicle through the pulmonary route.

CRYSTALLO-CO-AGGLOMERATION OF SIMVASTATIN: IMPROVING DISSOLUTION AND MICROMERITIC PROPERTIES

Simvastatin (SMV), a poorly soluble drug, faces challenges in pharmaceutical formulation due to its limited solubility and poor flow properties. This study aimed to enhance the physicochemical properties of SMV by preparing spherical crystals using a crystallo-co-agglomeration. Spherical crystals of SMV were prepared by dissolving the drug in methanol and adding it to an aqueous solution containing PVP K-30 and PEG 6000 under constant stirring. The resulting agglomerates were filtered, dried, and characterized using Fourier Transform Infrared (FTIR) spectroscopy, Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), and dissolution testing. Micromeritic properties, including bulk density, Hausner ratio, compressibility index, angle of repose, and flowability, were also evaluated. FTIR confirmed the chemical integrity of SMV with minor shifts indicating interactions with stabilizers. PXRD and DSC analyses revealed reduced crystallinity and partial amorphization in the spherical crystals. SEM showed spherical morphology. Dissolution testing demonstrated a significantly enhanced dissolution rate for the spherical crystals compared to pure SMV. Improved micromeritic properties were also observed, indicating better flowability and packing density. Spherical crystallization significantly improved the solubility, dissolution rate, and flowability of SMV. This technique offers a promising strategy for enhancing the bioavailability and pharmaceutical performance of poorly soluble drugs.

Quantification of agglomerate size and interparticle forces with a modified Hausner ratio

A model is introduced in this study that establishes a relationship between bed voidage, agglomerate size, and the magnitude of interparticle forces (IPFs) with a focus on Geldart group C powders. A modified Hausner ratio (MHR), defined as the ratio of particle density to tapped bulk density for this specific group of powders, is a critical parameter of the model. The model leads to two fundamental equations. The first equation suggests that the ratio of agglomerate size to particle size is directly proportional to the square of the MHR. The second equation is a linear relationship between the ratio of IPFs and the weight of a particle with the fourth power of MHR. These equations were validated by comparing their outcomes for agglomerate size and magnitude of IPFs with the estimates of other experimental approaches. The results for Geldart group C powders showed that IPFs are at least an order of magnitude greater than the weight of a particle leading to the formation of agglomerates, which are at least three times greater than the primary particles. The proposed equations may not be applied to nanoparticles and powders with wide size distributions, necessitating further developments to achieve more accurate predictions for these cases.

Exploration of Nanomedicine-Based Dry Powder Inhalation Formulation Co-Loaded with Erlotinib and Curcumin for Treatment of Non-Small Cell Lung Cancer

Erlotinib is used as first-line chemotherapy for the treatment of non-small cell lung cancer (NSCLC), which accounts for approximately 85% of lung cancers. Curcumin has potential antitumor effects in different types of cancer including NSCLS with additional chemopreventive and radioprotective effects. The aim of the study was to develop erlotinib and curcumin co-loaded dry powder inhalation (EC-DPI) formulation using nanoprecipitation technique with a goal of achieving a stronger cytotoxic effect against A549 cancer cells. The optimized DPI formulation resulted in suitable particle size (313.28 ± 26.19 nm), polydispersity index (0.156 ± 0.016) and zeta potential (29.4 ± 1.22 mV). Carr’s index (6.62 ± 1.43) and Hausner ratio (1.058 ± 0.03) demonstrated excellent flowability of the powder. The fine particle fraction (64.7 ± 7.8%) and mass median aerodynamic diameter (2.98 ± 0.04 [Formula: see text]m) of the optimized formulation revealed good aerosol performance and its suitability for direct delivery to the lungs. In-vitro cytotoxic potential of EC-DPI was determined against A549 cancer cells and compared with curcumin-loaded DPI formulation (C-DPI) and erlotinib-loaded DPI formulation (E-DPI). The IC[Formula: see text] values for E-DPI and C-DPI were found to be 36.6 ± 2.4 [Formula: see text]M and 24.4 ± 2.7 [Formula: see text]M, respectively. The IC[Formula: see text] value for EC-DPI was 20.5 ± 2.1 [Formula: see text]M confirming the synergistic effect of both drugs against A549 cancer cells. The internalization of the drug inside A549 cells was detected by a cellular uptake study. The EC-DPI demonstrated the highest cellular uptake (0.07 ± 0.006 ng/[Formula: see text]g) followed by the formulation containing curcumin (0.05 ± 0.003 ng/[Formula: see text]g) and erlotinib (0.03 ± 0.004 ng/[Formula: see text]g) alone at the end of 6 h. Hence, the developed DPI formulation can be considered as a potential therapeutic approach for the direct delivery of erlotinib and curcumin to treat NSCLC.

Formulation and physicotechnical evaluation of a fixed dose combination of amlodipine, metformin and glibenclamide in the management of hypertension-diabetes mellitus comorbidity

The concept of fixed dose combination (FDC) dates as far back as the early 17th century and still finds relevance till today. Almost every disease condition has at least one approved FDC commercially available for its treatment. The prevalence of hypertension-diabetes mellitus (HTN-DM) comorbidity is high globally. However, there are no available FDC formulation approved to be used in managing patients with this comorbidity. This study was designed to fill this gap by formulating an FDC of Amlodipine (antihypertensive), Metformin (antidiabetic) and Glibenclamide (antidiabetic), which are already being used clinically as monotherapies in management of HTN-DM comorbid patients. The APIs were granulated using wet granulation method with the aid of the excipients, after which the granules properties were examined and subsequently compressed into tablets. The physicotechnical properties and in-vitro release profile were evaluated on the tablets. The results of granule properties such as angle of repose (22.8o), Hausner ratio (1.16) and Carr’s compressibility index (13) for the 8% binder batch show excellent flow properties and is indicative of forming tablets with good qualities. “8% binder” tablets batch has the following properties; hardness (kgF), friability (0.55%), disintegration time (220 secs), all within the acceptable official requirements. The release profile showed that the drugs were bioavailable from the tablets in good time. It can be concluded that the formulation of an FDC for HTN-DM comorbidity was a success and studies to confirm the compatibility of the APIs and excipients are recommended.

Effect of foaming and drying temperature on the physical, chemical, and functional properties of egg white powders produced using refractance window drying

This study investigated the effect of drying form (natural and foamed) and temperature (50–100 °C) on the physical, chemical, and functional properties of egg white powder produced using refractance window drying. The egg whites were dried in 4-55 min, depending on the drying conditions. On the one hand, the drying form was effective on the color properties, densities (bulk, tapped, or particle), Carr index, Hausner ratio, porosity, hygroscopicity, solubility, and foaming capacity of egg white powders. On the other hand, the drying temperature was effective for all analyzed properties except hygroscopicity, moisture content, and water activity of samples. The study demonstrated that foaming before refractance window drying enhances the color of the egg white powders and provides better solubility and foaming capacity. However, it has a detrimental effect on the flow properties of the powders evaluated according to the Carr index and Hausner ratio. Increasing the drying temperature until a certain extent (80 °C) generally provided better color, protein content, surface hydrophobicity, and functional properties. The study shows that egg powders suitable for different purposes (better foaming, low protein denaturation, better gelling, etc.) can be obtained if the drying form and temperature conditions are fine-tuned.