Preparation Of Microparticles Research Articles

Effect of oral zoledronate administration on bone turnover in older women.

The aim of this work is to assess the safety and efficacy of two oral zoledronate preparations by determining their effects on bone resorption in healthy postmenopausal women. The preparations studied were zoledronic acid in enteric-coated capsules or a microparticle preparation of zoledronic acid in these capsules. Bone resorption was measured as β-C-telopeptideof type I collagen (CTX) in fasting serum. Separate cohorts, each of five women, were recruited and allocated in sequence to single doses of 20 mg, 40 mg, or 60 mg of oral zoledronate. Zoledronate 20 mg enteric capsules were well tolerated, reduced serum CTX by a median 51% at 1 week, but by only 17% at 1 month. Doses of 40 or 60 mg of this preparation produced APR and/or gastrointestinal symptoms in more than half of participants. With these doses, median CTX reduction at 1 week was >80%, ~70% at 1 month, but only ~30% at 6 months. Enteric capsules containing microparticles of zoledronate 20 mg reduced CTX by a median 53% at 1 week, with offset over 3 months. Two or three of these capsules dosed weekly reduced CTX by ~50% at 1 month, and by ~30% at 3 and 6 months. Oral zoledronate 20 mg circumvents the problem of APR symptoms but, even with multiple doses, the anti-resorptive effect is smaller and less sustained than with intravenous zoledronate. Probably a viable oral regimen of zoledronate dosing at intervals of weeks to months could be developed, but the advantage of infrequent dosing would be lost.

Preparation and Characterization of PLG Microparticles by the Multiple Emulsion Method for the Sustained Release of Proteins.

Rapid release and diminished stability are two of the limitations associated with the growth factors that are essentially used in dental applications. These growth factors are employed to enhance the quality and quantity of tissue or bone matter during regeneration. Therefore, drug delivery devices and systems have been developed to address these limitations. In this study, bovine serum albumin (BSA), as a representative growth factor, was successfully sustained by encapsulation with the medium-absorbable copolymer, poly(L-lactide-co-glycolide) (PLG) 70:30% mol, via the multiple emulsion method. Different PLG, PVA, and BSA concentrations were used to investigate their effects on the BSA encapsulation efficiency. The suitable ratios leading to a better characterization of microparticles and a higher encapsulation efficiency in producing encapsulated PLG microparticles were 8% (w/v) of PLG, 0.25% (w/v) of PVA, and 8% (w/v) of BSA. Furthermore, an in vitro release study revealed a bursting release of BSA from the encapsulated PLG microsphere in the early phase of development. Subsequently, a gradual release was observed over a period of eight weeks. Furthermore, to encapsulate LL-37, different proteins were used in conjunction with PLG under identical conditions with regard to the loading efficiency and morphology, thereby indicating high variations and poor reproducibility. In conclusion, the encapsulated PLG microparticles could effectively protect the protein during encapsulation and could facilitate sustainable protein release over a period of 60 days. Importantly, an optimal method must be employed in order to achieve a high degree of encapsulation efficiency for all of the protein or growth factors. Accordingly, the outcomes of this study will be useful in the manufacture of drug delivery devices that require medium-sustained release growth factors, particularly in dental treatments.

PREPARATION AND IN VITRO CHARACTERIZATION OF SOLID LIPID MICROPARTICLES FOR PROTEIN DELIVERY

Objective: The aim of this research was to assess the effect of the process and formulation parameters during the preparation of solid lipid microparticles. Solid lipid microparticles (SLMs) have evident advantages such as biocompatibility, simplicity of production and characterization, prolonged release, and especially high protein loading capacity, despite being less investigated than lipid nanoparticles.Material and Method: SLMs were prepared via emulsion solvent diffusion technique using glyceryl tridecanoate (GTD) as a biocompatible and biodegradable lipid. The optimum formulation conditions for producing homogenous spherical microparticles were found and represented by a triangle phase diagram area. After optimizing the particle size and encapsulation efficiency by changing the formulation parameters, the microparticles were characterized by in vitro release, morphological analysis, thermal analysis and electrophoretic analysis on the selected formulations.Result and Discussion: The maximum drug loading efficiency was achieved by combining 100 mg of lipid, 60% triacetin and 3% emulsifier. The average microparticle size was observed as 8.9 μm. The in vitro drug release were analyzed in pH 7.4 phosphate buffer and were mainly completed at 8th hour.

The strategy of cell extract based metal organic frameworks (CE-MOF) for improved enzyme characteristics

A convenient cell extract based metal organic frameworks (CE-MOF) strategy was used to produce self-assembled hybrid microparticles of enzymes with improved characteristics. It was shown that many metal ions and enzymes could be used to construct catalytically active CE-MOF microparticles. As a proof-of-principle study, the β-xylosidase BH3683 was used to prepare FeSO4-CE-MOF-BH3683 microparticles to explore the factors influencing preparation of the microparticles. As a result, DNA, RNA, polysaccharides and proteins were found to play important roles in the formation of the microparticles and affected enzyme activities through interaction with enzyme molecules. Compared with the free BH3683, the optimum temperature of FeSO4-CE-MOF-BH3683 increased 5 °C, and the relative activity at 70 °C increased two times. Moreover, FeSO4-CE-MOF-BH3683 have stronger tolerance to different concentrations of various organic solvents and high-concentration xylose than the free BH3683, and the CE-MOF microparticles prepared by BH3683 and xylanase XynII could catalyze high-concentration xylan more efficiently than their free counterparts. In addition, FeSO4-CE-MOF-BH3683 exhibited about 40 % of its initial activity after reused for 10 times, showing satisfactory reusability. To sum up, this strategy might have wide application potential in the fields of biocatalysis, biofuel production, fertilizer industry, etc.

Preparation and Characteristics of Alginate Microparticles for Food, Pharmaceutical and Cosmetic Applications.

Alginates are the most widely used natural polymers in the pharmaceutical, food and cosmetic industries. Usually, they are applied as a thickening, gel-forming and stabilizing agent. Moreover, the alginate-based formulations such as matrices, membranes, nanospheres or microcapsules are often used as delivery systems. Alginate microparticles (AMP) are biocompatible, biodegradable and nontoxic carriers, applied to encapsulate hydrophilic active substances, including probiotics. Here, we report the methods most frequently used for AMP production and encapsulation of different actives. The technological parameters important in the process of AMP preparation, such as alginate concentration, the type and concentration of other reagents (cross-linking agents, oils, emulsifiers and pH regulators), agitation speed or cross-linking time, are reviewed. Furthermore, the advantages and disadvantages of alginate microparticles as delivery systems are discussed, and an overview of the active ingredients enclosed in the alginate carriers are presented.

Polymer type effect on PLGA-based microparticles preparation by solvent evaporation method with single emulsion system using focussed beam reflectance measurement

Aim This study aimed to investigate the effect of polymer type on solidification rate of PLGA polymeric microparticles and particle size/distribution of the emulsion droplets/hardened PLGA polymeric microparticles during solvent evaporation process using FBRM (Focussed Beam Reflectance Measurement). Methods PLGA polymeric microparticles were prepared by an O/W solvent evaporation method using various PLGA polymers, including PLGA Resomer® RG503H, RG502H and RG752H. The particle size mean, chord length distribution (CLD), and chord count of the emulsion droplets/hardened microparticles were monitored by FBRM. The morphology of polymeric microparticles were characterised by optical microscopy and scanning electron microscopy (SEM). Results The transformation of the emulsion droplets into solid microparticles occurred within the first 30 (± 1.04), 34 (± 1.15) and 37 (± 0.82) min and square weighted mean chord lengths are 64.08 (± 3.18), 52.36 (± 5.27) and 42.18 (± 4.61) µm when PLGA Resomer® RG503H, RG502H and RG752H were used respectively. Larger square weighted mean chord length of PLGA polymeric microparticles gave lower chord counts. PLGA RG752H microparticles gave smallest square weighted mean chord length and the chord counts was the highest. The CLDs measured by FBRM showed that a larger particle size mean gave longer CLD and a lower peak of particle number. SEM data revealed that the morphology of microparticles was influenced by type and physical properties of polymer. Conclusions FBRM can be employed for online monitoring of the shift in the microparticle CLD and detect transformation of the emulsion droplets into solid microparticles during the solvent evaporation process. The microparticle CLD and transformation process were strongly influenced by polymer type.

Microfluidic preparation of antimicrobial microparticles composed of l-lactide/1,3-dioxolane (co)polymers loaded with quercetin

The resistance of microorganisms against commonly used antibiotics is becoming an increasingly important problem in the food and pharmaceutical industries. Therefore, the development of novel bactericidal agents, as well as the design of drug delivery systems based on materials composed of biocompatible and biodegradable building blocks, has attracted increasing attention. To address this challenge, microparticles composed of l-lactide homopolymer and l-lactide/1,3-dioxolane (co)polymers loaded with quercetin (Q) were fabricated by using a microfluidic technique. This method enables the preparation of homogeneous particles with sizes ranging from 60 to 80 µm, composed of degradable semicrystalline or amorphous (co)polyesters. The microencapsulation of Q in a (co)polymeric matrix enables prolonged release of the antimicrobial agent. The antibacterial properties of the obtained biocompatible microparticles are confirmed by the agar diffusion plate method for various bacterial strains. Therefore, Q-loaded microparticles can have important applications in food preservation as a novel antimicrobial system.

Hollow Silica Microparticles Based on Amphiphilic Polyphosphazenes.

Hollow microparticles are important materials, offering a larger surface area and lower density than their solid counterparts. Furthermore, their inner void space can be exploited for the encapsulation and release of guest species in a variety of applications. Herein, we present phosphazene-based silica hollow microparticles prepared via a surfactant-free sol-gel process through self-assembly of the alkoxysilyl-containing polymer in water–ethanol solution. Solely, a silane-derived polyphosphazene was used as the precursor for the microparticle formation, without additional classical silica sources. These novel hollow silica-based microparticles were prepared without surfactant, using a designed amphiphilic polyphosphazene for the particle formation made by two components, a hydrophilic unit consisting of 3-mercaptopropyl(trimethoxysilane), and a hydrophobic unit (dodecanethiol) attached to the double bonds from the poly(allylamine)phosphazene backbone via a thiol-ene photoreaction. Due to these two functionalities, a “vesicle”-like self-assembled structure was formed in the reaction medium, which could be then utilized for the microparticle preparation. The influence of NaOH during the synthesis was shown to affect the size and the wall thickness of the microparticles. This effect may enhance the possibilities to tailor such microparticles for drug delivery purposes or for future controlled release of other substances, such as drugs, fragrances, or anticorrosive pigments.

Fabrication of apigenin nanoparticles using antisolvent crystallization technology: A comparison of supercritical antisolvent, ultrasonic-assisted liquid antisolvent, and high-pressure homogenization technologies

Flavonoids have many positive pharmacological properties, such as antioxidant, antitumor, and anti-inflammatory activities. However, factors such as low water solubility and low dissolution rate limit their use. To overcome their poor solubility, carrier-free apigenin (API) microparticles and nanoparticles were prepared using three types of antisolvent precipitation technologies: supercritical antisolvent (SCF) technology, ultrasonic-assisted liquid antisolvent (UAL) technology, and high-pressure homogenization (HPH) technology. All three technologies can produce uniform tiny particles. However, the API particles obtained using these different techniques show subtle differences in terms of physical and chemical properties and biological activity. The preparation, characterization, and potential use of API microparticles and nanoparticles to improve in vitro release were studied. The resulting API particles were investigated and compared using Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy. We determined the optimum conditions for SCF, UAL, and HPH technologies to produce API microparticles and nanoparticles. The antioxidant and antitumor properties of the API particles were also investigated. The results demonstrated that the reduced particle size of the APIs prepared via SCF, UAL, and HPH technologies contributed to the enhanced dissolution rate, which in turn enhanced API bioactivity.

Antimicrobial Properties of TiO2 Microparticles Coated with Ca- and Cu-Based Composite Layers.

The ability of TiO2 to generate reactive oxygen species under UV radiation makes it an efficient candidate in antimicrobial studies. In this context, the preparation of TiO2 microparticles coated with Ca- and Cu-based composite layers over which Cu(II), Cu(I), and Cu(0) species were identified is presented here. The obtained materials were characterized by a wide range of analytical methods, such as X-ray diffraction, electron microscopy (TEM, SEM), X-ray photoelectron (XPS), and UV-VIS spectroscopy. The antimicrobial efficiency was evaluated using qualitative and quantitative standard methods and standard clinical microbial strains. A significant aspect of this composite is that the antimicrobial properties were evidenced both in the presence and absence of the light, as result of competition between photo and electrical effects. However, the antibacterial effect was similar in darkness and light for all samples. Because no photocatalytic properties were found in the absence of copper, the results sustain the antibacterial effect of the electric field (generated by the electrostatic potential of the composite layer) both under the dark and in light conditions. In this way, the composite layers supported on the TiO2 microparticles’ surface can offer continuous antibacterial protection and do not require the presence of a permanent light source for activation. However, the antimicrobial effect in the dark is more significant and is considered to be the result of the electric field effect generated on the composite layer.

Preparation of Poly(vinyl Alcohol) Microparticles for Freeze Protection of Sensitive Fruit Crops.

Poly(vinyl alcohol) (PVA) displays ice recrystallization inhibition (IRI) properties as many antifreeze proteins found in cold tolerant organisms. The molecular architecture and composition (molecular weight and distribution of pendant OH and acetate groups) have been studied to improve the antifreezing properties of PVA, suggesting that the molecular architecture of PVA plays an important role in IRI activity. The present work deals with the preparation of PVA microparticles using an alkaline treatment. The effect of PVA molecular weight on the morphology and antifreezeing properties of PVA microparticles was investigated. The antifreezeing property of PVA microparticles on the susceptibility of flower bud tissues to freeze damage was also evaluated. The alkaline treatment of an aqueous PVA solution produced stable polymer chain aggregates with spherical shapes. The average size of the PVA microparticles increased significantly with the increasing molecular weight of the PVA macromolecule precursor. The PVA microparticles inhibited the growth of ice crystals and blocked ice growth at concentrations as low as 0.01 % w/v. The effect of impeding ice crystal growth by preventing the joining of adjacent ice crystals is attributed to the larger size of the PVA particles adsorbed on the ice surface compared to the aggregated PVA macromolecules in saline solution. The thermal hysteresis activity of PVA macromolecules and microparticles was not detected by differential scanning calorimetry analysis. The PVA microparticles reduced the incidence of freeze injuries in flower bud tissues by 55% and their application, considering the low toxicity of PVA, has a high potential for freeze protection in fruit crops.

Flow Dispersion for Obtaining Ivermectin Encapsulated in Polycaprolactone Microparticles

Introduction. Ivermectin is an antiparasitic drug that has been widely used in veterinary medicine. Parasitic diseases of farm animals cause great economic damage and pose the risk of human infection. Prolonged dosage forms of ivermectin are effective against them. The first step in the creation of such a drug was the preparation and study of polymeric microparticles of polycaprolactone with encapsulated ivermectin. Aim. Obtaining polymeric microparticles of polycaprolactone with encapsulated ivermectin using a continuous flow-through unit. Materials and methods. The object of the study was microparticles of polycaprolactone with encapsulated ivermectin obtained on a continuous flow-through unit. Determination of the average particle size and size distribution was carried out by the method of laser diffraction. Microscopy was used to visually assess the shape and size of the microparticles. UV – spectrophotometry was use to quantitative determination of ivermectin. Results and discussion. Polymeric microparticles of polycaprolactone with encapsulated ivermectin was obtained and had an average size of 126.63 ± 42.67 μm and contained 32,73–62,00 % of ivermectin. Suspensions prepared from the obtained microparticles were passed through a 20G injection needle without noticeable resistance, which indicates the possibility of their use as the basis of an injectable preparation. Conclusion. Obtained results confirm the possibility of using flow-through dispersion using a device developed by us for obtaining polycaprolactone microparticles with encapsulated ivermectin, which are suitable for injection. Thus, the results obtained make it possible to continue studies of microparticles and create a drug based on them.

Fabrication of mesoporous crystalline microparticles of poly(ether sulfone) via solvent-induced crystallization

Mesoporous polymer microparticles are promising for energy, environmental, and biomedical applications. A linear polymer microparticle is desirable from the perspective of polymer recycling. In this study, mesoporous crystalline microparticles of a commercially available high-performance polymer, poly(ether sulfone) (PES), were prepared. Solvent-induced crystallization of PES in nitrobenzene resulted in nearly spherical microparticles with an average size of 5 μm and narrow size distribution. The microstructure and mesoporosity of the microparticles were characterized with scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and nitrogen adsorption/desorption, which gave a pore size distribution peaking at 7 nm with a porosity of 0.44. Fourier-transform infrared spectroscopy, Raman spectroscopy, and thermogravimetric analysis confirmed the cocrystal of PES and nitrobenzene. The formation mechanism of the PES microparticles was elucidated based on the theory of polymer spherulite formation. This study gives an insight on solvent-induced crystallization of rigid high- T g polymers useful for the mesoporous polymer particle fabrication. • Solvent-induced crystallization of poly(ether sulfone) (PES) was investigated. • Nitrobenzene induces crystallization of PES and forms a polymer-solvent cocrystal. • The cocrystal spontaneously makes uniform microparticles with 5 μm diameter. • The microparticles gives large mesoporosity with specific surface area of 200 m 2 /g. • The method is promising as a facile preparation of polymer microparticles.

Preparation of Starch Phosphate Microparticle Derived from Cassava Starch

Starch is a vital ingredient that is frequently utilized in the culinary and pharmaceutical industries. However, native starch has drawbacks, namely low solubility and intolerance with extreme pH and temperature treatments. Therefore, the starch needs to be modified. Starch phosphate is one of chemical modification technique for starch that used a cross-linking agent such as sodium trimethaphosphate (STMP), sodium tripolyphosphate (STPP) or phosphate chloride (PCl3). This research aims to prepare the microparticles of modified starch from water in oil microemulsion to be applied as a drug delivery matrix. Starch phosphate was modified with a cross-linking method using sodium trimetaphosphate (STMP). The starch used was Cassava starch. Water in oil microemulsion was made with various surfactant compositions as emulsifiers according to Hydrophilic-Lipophilic Balance (HLB) variations values (4.5; 5.0; 5.5; 6.0) and sonication time 30 minutes. The solubility, swelling, and other physicochemical properties of phosphate starch were investigated. Additionally, the functional group analysis used Fourier Transform Infrared Spectroscopy (FTIR) and size particle analysis was performed using Particle Size Analysis (PSA). The result of the FTIR analysis confirmed that the presence of a phosphate groups in the modified starch has been found. The addition of cosurfactants and sonication treatment affected the characteristics of starch microparticles, the higher the HLB value and the addition of cosurfactants reduced the size of starch microparticles.

Mechanical characterization of soft microparticles prepared by droplet microfluidics

AbstractDroplet microfluidics is one of the most promising approaches that allows preparation of microparticles with tailored structure and composition. Various functional microparticles have been developed using microfluidics, where their controlled structure shows high potential for a wide range of applications. Among these, soft polymeric microparticles which exhibit low elastic modulus compared to ceramics and metals are extensively investigated in biomedical applications due to their biocompatibility, high surface‐to‐volume ratio, as well as soft and deformable nature. As the mechanical properties of soft microparticles play important role in determining how they function in each application, it is essential to adequately characterize them for the optimal design of functional microparticles. In this review, we mainly discuss the mechanical characterization methods of soft microparticles and their elastic property. A brief overview of the droplet microfluidics‐assisted fabrication of microparticles is also provided before discussing the mechanical characterization techniques. We then describe the general characterization methods and models employed to determine the elastic properties of microparticles. In addition, we discuss the relationship between the physical parameters (size, composition, and structure) and the elastic properties of the microparticles, followed by the role of elastic properties in various applications including microcarrier, bioink, and self‐healing to name a few.

Formulation and Evaluation of Interpenetrating Polymer Network Microparticles of Diclofenac Sodium

Diclofenac sodium, a model anti-inflammatory drug, has adverse effects like gastric irritation and hepatic toxicity. To overcome these problems Interpenetrating Polymer Network microparticles can be used as a controlled drug delivery system. Preparation of Interpenetrating Polymer Network microparticles using two or more polymer is a novel approach as the polymers produce synergistic effect which could increase the mechanical strength and resilience of the microparticles. The aim of the study was to prepare Interpenetrating Polymer Network microparticles of Diclofenac Sodium using chitosan and Ghatti gum which were used to deliver Diclofenac Sodium to the intestine. Microparticles prepared by emulsion-cross-linking method using gluteraldehyde as a cross-linker were characterized by Fourier Transform Infrared Spectroscopy, Differential scanning calorimetry, Scanning electron microscopy and evaluated for in vitro dissolution rate. Fourier Transform Infrared Spectroscopy studies confirmed the absence of chemical interactions between drug, polymers and cross-linking agent. Differential scanning calorimetric results indicated amorphous dispersion of Diclofenac Sodium into Interpenetrating Polymer Network matrix. Scanning electron microscopy pictures showed that microparticles did not agglomerate and had a rough surface. Hydrated surface after swelling showed spongy porous surface which indicated the mechanism of drug release as diffusion. Particle size ranged between 294 to 366 µm. DS percentage encapsulation efficiency ranged from 84.09 to 96.81%. In vitro release studies indicated a dependence of drug release rates on both the amount of CS and GG used in preparation of microparticles. The release was extended up to 12 h and release rates indicated a non-Fickian and super case II mechanism.

Surfactant-free suspension polymerization of hydrophilic monomers with an oil-in-water system for the preparation of microparticles toward the selective isolation of tumor cells

Polymer microparticles, composed of water-soluble hydrophilic monomers, are synthesized via surfactant-free suspension polymerization with an oil-in-water system. Microparticles formed from PMEA have potential as a platform to capture tumor cells.

Robust and scalable production of emulsion-templated microparticles in 3D-printed milli-fluidic device

Emulsions are ideal templates for preparation of functional microparticles in food, cosmetics, and pharmaceutics. However, the lack of a simple and robust platform that allows mass production of oil-in-water (O/W) emulsions has been considered as a practical hurdle for broader applicability of these emulsion-based technologies. Herein, we report a novel 3D-printed milli-fluidic device (3D-PMD) for robust and scalable production of water-in-oil (W/O) as well as O/W emulsions. By using an additive manufacturing method with one-step prototyping capability, 3D-PMD integrates an array of 40 drop-makers with a 3D void geometry and a flow distributor in a compact fashion, which has been difficult to achieve using conventional methods. Experimental results as well as the computational fluid dynamics simulation confirm the validity in the design of the drop-maker and the flow distributor, as well as the hydrophilic surface modification process for the robust and controllable production of poly(ethylene glycol) microgels and polycaprolactone microparticles, prepared from W/O and O/W emulsions, respectively. We anticipate that the simplicity, low-cost ($150/per device), facile manufacturability, and versatile emulsion production capability of our 3D-PMD method offers a unique route to produce W/O and O/W emulsions in a robust and in a scalable manner, providing new and exciting opportunities in various applications involving functional microparticles such as cosmetic products, optical displays, controlled reactions, and drug delivery systems to name a few.

Preparation and Characterization of Fenofibrate Microparticles with Surface-Active Additives: Application of a Supercritical Fluid-Assisted Spray-Drying Process.

In this study, supercritical fluid-assisted spray-drying (SA-SD) was applied to achieve the micronization of fenofibrate particles possessing surface-active additives, such as d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), sucrose mono palmitate (Sucroester 15), and polyoxyethylene 52 stearate (Myrj 52), to improve the pharmacokinetic and pharmacodynamic properties of fenofibrate. For comparison, the same formulation was prepared using a spray-drying (SD) process, and then both methods were compared. The SA-SD process resulted in a significantly smaller mean particle size (approximately 2 μm) compared to that of unprocessed fenofibrate (approximately 20 μm) and SD-processed particles (approximately 40 μm). There was no significant difference in the effect on the particle size reduction among the selected surface-active additives. The microcomposite particles prepared with surface-active additives using SA-SD exhibited remarkable enhancement in their dissolution rate due to the synergistic effect of comparably moderate wettability improvement and significant particle size reduction. In contrast, the SD samples with the surface-active additives exhibited a decrease in dissolution rate compared to that of the unprocessed fenofibrate due to the absence of particle size reduction, although wettability was greatly improved. The results of zeta potential and XPS analyses indicated that the surface-active additive coverage on the surface layer of the SD-processed particles with a better wettability was higher than that of the SA-SD-processed composite particles. Additionally, after rapid depletion of hydrophilic additives that were excessively distributed on the surfaces of SD-processed particles, the creation of a surface layer rich in poorly water-soluble fenofibrate resulted in a decrease in the dissolution rate. In contrast, the surface-active molecules were dispersed homogeneously throughout the particle matrix in the SA-SD-processed microparticles. Furthermore, improved pharmacokinetic and pharmacodynamic characteristics were observed for the SA-SD-processed fenofibrate microparticles compared to those for the SD-processed fenofibrate particles. Therefore, the SA-SD process incorporating surface-active additives can efficiently micronize poorly water-soluble drugs and optimize their physicochemical and biopharmaceutical characteristics.

Novelkaraya gum micro-particles loaded Ganoderma lucidum polysaccharide regulate sex hormones, oxidative stress and inflammatory cytokine levels in cadmium induced testicular toxicity in experimental animals

Presented research aimed to develop a spray drying process without the use of organic solvents for the preparation of novel Karaya gum polymer microparticles (MPs) of Ganoderma lucidum polysaccharide (GLP). The prepared microparticles were characterized and evaluated. Prepared novel karaya gum micro-particles loaded Ganoderma lucidum polysaccharide (GLP MPs) were observed an effect on cadmium (CAD) induced testicular toxicity. A total of 40 rats (male) was divided into 4 groups viz. 1. Control group, 2. GLP MPs (250 mg/kg, 60 days of b.w per day), 3. CAD (60 days of 30 mg/l/day), 4. GLP MPs + CAD. CAD was responsible for altering the sex hormones, oxidative stress and inflammatory cytokines. Furthermore, elevated levels of indicator of oxidative stress, malondialdehyde, and a reduced action of SOD, GSH, and CAT (antioxidant enzymes), were observed in the tissues of the testicles of CAD- treated group. Such harmful occurrences were followed by an up-regulation in proinflammatory cytokines (TNF-α, IL-1β) levels, protein expression of Nrf2, and HO-1 expression was decreased. GLP MPs pre-treatment significantly abrogated these toxic effects which were confirmed histologically. This study concluded that pre-treatment with GLP MPs exerts a protective effect against CAD-induced male reproductive testicular toxicity.