Optimal Formulation Research Articles

Prolonged Release Niosomes For Ocular Delivery of Loteprednol: Ocular Distribution Assessment on Dry Eye Disease Induced Rabbit Model.

Loteprednol etabonate (LE) is a topical corticosteroid for the symptomatic management of ocular conditions, encompassing both allergic and infectious etiologies. Owing to the dynamic and static barriers of the eye, LE exhibits significantly low bioavailability, necessitating an increase in the frequency of drug administration. The objective of this study is to overcome the limitations by developing niosomal systems loaded with LE. Design of Experiments (DoE) approach was used for the development of optimal niosome formulation. The optimal formulation was characterized using DLS, FT-IR, and DSC analysis. In vitro and ex vivo release studies were performed to demonstrate drug release patterns. After that HET-CAM evaluation was conducted to determine safety profile. Then, in vivo studies were carried out to determine therapeutic activity of niosomes. Zeta potential (ZP), particle size, polydispersity index (PI), and encapsulation efficacy (EE) were -33.8mV, 89.22nm, 0.192, and 89.6%, respectively. Medicated niosomes had a broad distribution within rabbit eye tissues and was absorbed by the aqueous humor of the bovine eye for up to 6h after treatment. Cumulative permeated drug in the bovine eye and rabbit eye were recorded 52.45% and 54.8%, respectively. No irritation or hemorrhagic situation was observed according to the results of HET-CAM study. Thus, novel LE-loaded niosomal formulations could be considered as a promising treatment option for the dry-eye-disease (DED) due to enhanced bioavailability and decreased side effects.

Microencapsulation of gamma oryzanol using inulin as wall material by spray drying: optimization of formulation and characterization of microcapsules.

The online version contains supplementary material available at 10.1007/s13197-024-05988-0.

Optimization of mature coconut water with calamansi, stevia, and turmeric using mixture design

In the Philippines, the Zero Food Waste Act of 2022 has been proposed with the aim of implementing a system that promotes food waste reduction through redistribution, recycling, and valorization. One of the wastes produced from the coconut industry is the mature coconut water, as the primary focus is on the production of copra, coconut oil, and coconut milk. Further, mature coconut water has poor sensory properties (color/turbidity, aroma, and taste), leading to approximately 2.4 billion liters being discarded annually. One of the proposed solutions is to utilize the D-optimal mixture design, which enables the generation of the best combination of mature coconut water (83.5–91.3 g/100 g), calamansi (8.00–15.00 g/100 g), stevia (0.50–1.50 g/100 g), and turmeric powder (0.20 g). The 'desirability' function was employed to achieve multiresponse optimization, considering parameters such as pH < 4.5; sweetness, sourness, and overall acceptability all equivalent to 6 (like slightly). Significant (p < 0.05) responses indicated that the influence of the raw materials varied, ranging from linear to cubic prediction models, with R2 values ranging from 70.19 to 98.30%. The optimization results revealed that the model successfully predicted the properties of the optimal formulation composed of 90.08 g/100 g mature coconut water, 8.83 g/100 g calamansi, 0.90 g/100 g stevia, and 0.20 g/100 g turmeric powder. The results of this research may help industries valorize mature coconut water instead of discarding it as waste. The developed beverage may be further improved to increase its acceptability and generalizability by increasing the range of the values used and verify results through pilot-scale production.

The gelation characteristics of Torreya grandis wax in diacylglycerol and its preparation of oleogel substitution for shortening

Torreya grandis wax (TGW), a new nut wax and by-product of refined Torreya grandis oil, lacks sufficient research and application. In this study, the gelling behavior in diacylglycerol (DAG) and chemical compositions of TGW were investigated. Compared with four typical natural waxes, TGW exhibited the lowest critical gelling concentration (Cg, 1 %wt) in DAG. The results performed that TGW-DAG oleogels at Cg possessed the highest G′LVR and G″, highest critical stress, good thermal stability, moderate viscosity recovery, and osc. yields stress, indicating strong gel. The microstructure and correlation analysis revealed that excellent gelling behaviors of TGW-DAG oleogels were due to the solid three-dimensional network formed by rod-like TGW crystal, and the higher hydrocarbon compound (HC) content and HC/wax ester in TGW. Formulation optimization suggested that oleogel containing 3.2 % TGW and 1.0 % diosgenin (DSG) better mimicked the characteristics of shortening in terms of hardness, adhesiveness, spreadability. The bread prepared with TGW/DSG-DAG oleogel owned uniform and dense pores, the best moisture retention capability, and soft and firm taste, demonstrating that TGW/DSG-DAG oleogel was a good shortening substitute. Therefore, this study provides the systematically fundamental knowledge of TGW and develops DSG-TGW-DAG oleogels as promising shortening substitutions.

Elucidating the Impact of Polyol Functional Moieties on Exothermic Poly(urethane-urea) Polymerization: A Thermo-Kinetic Simulation Approach

The pursuit of sustainable polyurethane (PU) product development necessitates a profound understanding of precursor materials. Particularly, polyol plays a crucial role, since PU properties are heavily influenced by the type of polyol employed during production. While traditional PUs are solely derived from hydroxyl functionalized polyols, the emergence of amine-hydroxyl hybrid polyols has garnered significant attention due to their potential for enhancing PU product properties. These hybrid polyols are characterized by the presence of both amine and hydroxyl functional groups. However, characterizing these polyols remains a daunting challenge due to the lack of established experimental testing standards for properties, such as fractional hydroxyl and amine moieties and thermo-kinetic parameters for amine reactions with isocyanates. Additionally, characterization methods demand extensive time and resources and pose risks to health and the environment. To bridge these gaps, this study employed computational simulation via MATLAB to determine the moieties’ fractions and thermo-kinetic parameters for hybrid polyols. The computational method integrated energy balance and reaction kinetics analysis for various polyols to elucidate the influence of functional moieties on the thermo-kinetic behavior of PU formations. Validation of the simulated results was conducted by comparing their experimental and simulated prepolymer and foam temperature profiles, highlighting the direct influence of fractional moieties on PU formations. The comparisons revealed an average relative error of less than 5%, indicating the accuracy and credibility of the simulation. Thus, this study represents a pivotal opportunity for advancing knowledge and driving sustainable developments in bio-based polyol characterization for PU production streamlining and formulation optimization.

Formulation Development and Optimization of Orodispersible Tablet of Loratadine

Loratadine, a histamine H1 receptor antagonist, is used to treat urticaria and allergic rhinitis. Children who have trouble swallowing tablets make it difficult to administer loratadine orally. F1-F9 batches of Loratadine Tablets (ODTs) 10 mg dose were developed and tested in the present research. In this research, super disintegrants such as croscarmellose sodium, sodium starch glycolate, and crosspovidone were used to manufacture fast-dissolving tablets utilising the direct compression method. In phosphate buffer pH 6.8, the impact of various super disintegrants on tablet dissolving behaviour was examined.

Quality by Design (QbD) Aided Formulation Optimization of Amlodipine Besylate Oral Thin Film

Quality by Design (QbD) Aided Formulation Optimization of Amlodipine Besylate Oral Thin Film

Low drug load, high retention mometasone furoate cream with polyglyceryl − 3 oleate as a chemical enhancer: Formulation development, in vivo and in vitro evaluation and molecular mechanisms

The study aimed to create a low loading, high retention, easier to apply O/W mometasone furoate (MF) cream using a chemical enhancer (CE) approach to provide more options for patients with atopic dermatitis (AD) and to investigate molecular mechanisms of its increased release and retention. A Box-Behnken design determined the optimal formulation based on stability and in vitro skin retention. Evaluations included appearance, rheological properties, irritation, in vivo tissue distribution and pharmacodynamics. Molecular mechanisms of enhanced release were studied using high-speed centrifugation, molecular dynamics and rheology. The interaction between the CE, MF and skin was studied by tape stripping, CLSM, ATR-FTIR and SAXS. The formulation was optimized to contain 0.05% MF and used 10% polyglyceryl-3 oleate (POCC) as the CE. There was no significant difference from Elocon® cream in in vivo retention and pharmacodynamics but increased in vivo retention by 3.14-fold and in vitro release by 1.77-fold compared to the basic formulation. POCC reduced oil phase cohesive energy density, enhancing drug mobility and release. It disrupted skin lipid phases, aiding drug entry and formed hydrogen bonds, prolonging retention. This study highlights POCC as a CE in the cream, offering insights for semi-solid formulation development.

Advancement of an Environmentally Friendly and Innovative Sustainable Rubber Wrap Film with Superior Sealing Properties.

Common kitchen wraps like plastic and aluminum foil create significant environmental burdens. Plastic wrap, typically made from non-renewable fossil fuels, often ends up in landfills for centuries, breaking down into harmful microplastics. Aluminum foil, while effective, requires a large amount of energy to produce, and recycling it at home can be impractical due to food residue. A promising new alternative, low-nitrosamine rubber wrap film, aims to reduce waste by offering a reusable option compared to traditional single-use plastic wrap. The film is environmentally friendly, durable, and effective in sealing containers and keeping food fresh or crispy. The raw materials used to make the product were studied, namely fresh and concentrated natural rubber latex. No nitrosamines were found in either the fresh or concentrated latex, which is important as nitrosamines are known to be carcinogenic. The absence of nitrosamines in the raw materials suggests that the universal rubber wrap film is safe for use. In this study, the rubber formulation and properties of rubber used to make rubber wrap film were studied. The content of additives affecting the rubber properties was varied to find the optimum rubber formulation for making rubber wrap films. The rubber formulation with the least amount of chemicals that met the following criteria was selected: tensile strength of at least 15 MPa, elongation at break of at least 600%, and nitrosamine content below 6 ppm. It was found experimentally that the optimum rubber formulation for making a translucent rubber film had 0.7 phr zinc oxide and 1.0 phr sulfur. Performance tests revealed the rubber wrap film's superior sealing capabilities. Its elasticity allows for a tighter fit on containers, effectively conforming to various shapes and creating an optimal seal compared to plastic wrap and aluminum foil. The results of this study provide valuable information for developing a universal rubber wrap film that is safe with low nitrosamines.

A novel inorganic phosphate-based adhesive for bonding archaeological pottery: a preliminary exploration

Damage and fracture of archaeological potteries not only jeopardize the long-term preservation but also hinder their exhibition. To repair these pottery sherds effectively, this study introduces a novel inorganic phosphate-based adhesive and evaluates its effectiveness through a series of experiments. To determine the optimal base adhesive, the paper investigates the influence of varying weight ratios of the H2O–H3PO4 system and the Al(OH)3–H3PO4 system on properties including tensile lap-shear strength, microstructure, high-temperature resistance and phase composition. However, the original black color of the traditional CuO–phosphate adhesive limits its application. The innovation of this study lies in the addition of nano-TiO2 to the adhesive, which not only improves the bonding strength but also adjusts the color of the adhesive. This study has defined the optimal formulation (i.e., base adhesive = m[Al(OH)3]:m[H3PO4] = 7:100, filler = 10wt% nano-TiO2), and the final product shows no residual acid in adhesives. Additionally, the fracture surfaces are successfully bonded with a high strength of 3.56 MPa. Various ageing tests including dry-thermal ageing, hygrothermal ageing and UV irradiation ageing are conducted to assess the ageing resistance of the inorganic phosphate-based adhesive. The results indicate strong tolerance of adhesive to high temperature and high humidity environment. Preliminary applications in archaeological pottery restoration suggest that the inorganic phosphate-based adhesive offers considerable promise for repairing shattered pottery.Graphical

Comparison of the heat resistance of flame retardants of various classes for polymer cable channels

The article presents a comparison of different classes of flame retardants, the mechanisms of their action and their effect on the physico-chemical properties of polymer materials. Based on studies of the heat resistance of flame retardants, an optimal formulation for the manufacture of polymer cable channels has been proposed.

Formulation of functional gummy candies containing natural antioxidants and stevia

The research aimed to enhance the nutritional value of gummy candies by incorporating pistachio green hull extract (PGHE), stevia, and starch into the formulations. The gummy candies formulations were optimized using PGHE (1–5 %), stevia (0.013–0.040 %) and gelatin-to-starch ratio (9:1, 2:8, and 3:7) by response surface methodology (RSM), central composite design (CCD), with six center points. The physicochemical and textural properties of the gummy candies were assessed. Three optimal formulations were determined, which were preferred by the majority of panelists. One of them was selected for testing total phenolic content (680.31 ± 0.6 mg GAE/100g gummy candy), antioxidant activity (IC50 = 277 μg/mL), FTIR analysis, morphology examination, and storage stability. This study resulted in the development of gummy candies that not only offer a reduced-sugar product (50 %; equal to 12 % of sucrose) with high antioxidant activity but also eliminate the need for artificial flavors and synthetic colorants in the formulation.

Vegan gummy candies with low calorie based on celery (Apium graveolens) puree and boswellia gum (Boswellia thurifera).

Gummy candy is one of the main snacks for children, and conventional samples with high calorie illustrate no nutritional value; therefore, the aim of present research was to develop functional product on priority. Celery (Apium graveolens) puree (25%-50%), boswellia gum (10%-20%), lemon essential oil (0.25%-0.50%), and sugar (10%-20%) in two levels were considered for vegan gummy candy production. Based on central composite design, the 30 types of gummy candies were prepared; afterward, response surface methodology was applied to optimize results determined by texture (hardness, springiness, adhesiveness, gumminess, chewiness, and elasticity characteristics), physicochemical attributes (pH, sugar content, water activity, antioxidant function, and calorie restriction), and also sensory evaluation. In general, elevated concentration of celery puree and boswellia gum-enhanced hardness, chewiness, and also gumminess for treated products. On the other hand, higher sugar with lemon essential oil improved adhesion, springiness, and elasticity features. More boswellia gum, celery, lemon essential oil, and reduction in sugar elevated water activity and also declined pH for treated samples. The celery puree, boswellia gum, and lemon essential oil significantly enhanced antioxidant function of treated gummy candies. According to attained results, sugar had a remarkable influence on acceptability and in treated samples calorie decreased. Based on all investigated factors, optimal formulation was achieved including 25% celery puree, 20% boswellia gum, 0.450% lemon essential oil, and 13.55% sugar. Regarding the results, obtained gummy candy with high nutritional value and low calorie demonstrated the potential to produce extensively in food sector.

Optimization of Antioxidant Activity of Water-Soluble Fraction of Wader Pari Fish (Rasbora Argyrotaenia) Fermentation Using Response Surface Methodology

Rusip processed by fermentation can potentially contain bioactive peptides as antioxidants and antimicrobials. This study aims to optimize the bioactive content in producing rusip from wader pari fish with the Response Surface Methodology (RSM) method. There were 20 recommended formulas based on factors such as sugar concentration, salt concentration, and fermentation duration. The results showed that salt concentration, fermentation duration, and sugar concentration significantly affected antioxidant activity in rusip. The optimal formulation produced involves the addition of liquid palm sugar with a concentration of 11.22%, salt concentration of 15%, and fermentation duration of 8.9 days. Verification of activity response showed results with antioxidant activity of 56.78%.

Enhancing Effector Jurkat Cell Activity and Increasing Cytotoxicity against A549 Cells Using Nivolumab as an Anti-PD-1 Agent Loaded on Gelatin Nanoparticles.

The current research investigated the use of gelatin nanoparticles (GNPs) for enhancing the cytotoxic effects of nivolumab, an immune checkpoint inhibitor. The unique feature of GNPs is their biocompatibility and functionalization potential, improving the delivery and the efficacy of immunotherapeutic drugs with fewer side effects compared to traditional treatments. This exploration of GNPs represents an innovative direction in the advancement of nanomedicine in oncology. Nivolumab-loaded GNPs were prepared and characterized. The optimum formulation had a particle size of 191.9 ± 0.67 nm, a polydispersity index of 0.027 ± 0.02, and drug entrapment of 54.67 ± 3.51%. A co-culture experiment involving A549 target cells and effector Jurkat cells treated with free nivolumab solution, and nivolumab-loaded GNPs, demonstrated that the latter had significant improvements in inhibition rate by scoring 87.88 ± 2.47% for drug-loaded GNPs against 60.53 ± 3.96% for the free nivolumab solution. The nivolumab-loaded GNPs had a lower IC50 value, of 0.41 ± 0.01 µM, compared to free nivolumab solution (1.22 ± 0.37 µM) at 72 h. The results indicate that administering nivolumab-loaded GNPs augmented the cytotoxicity against A549 cells by enhancing effector Jurkat cell activity compared to nivolumab solution treatment.

Preparation, characterization, and in vitro evaluation of microemulsion based cream formulations for the topical treatment of acne vulgaris

AbstractBy lowering the significant adverse effects of traditional medications, this study intends to create cream formulations based on microemulsions that contain extract from Allium sativum L. for the treatment of acne vulgaris. Characterization experiments were carried out on the developed cream formulations based on microemulsions. Textural profile analysis and spreadability tests were conducted. Furthermore, cell culture studies and toxicity analysis were performed. As a result, the pH and viscosity values of the developed formulations were found between 6.43 ± 0.00 and 6.66 ± 0.01, and between 13.90 ± 0.080 and 137.20 ± 8.02 P, respectively. The highest‐performing empty and loaded cream formulations in terms of spreadability and textural profile analysis were those with the highest beeswax content. The highest‐performing empty and loaded cream formulations in terms of spreadability and textural profile analysis were those with the highest beeswax content. According to the visual physical evaluation of the formulations, it was observed that the developed formulations were neat, smooth, and homogeneous. The optimum formulation developed was non‐cytotoxic, which maintained cell viability by over 90%. Additionally, the skin irritation experiment was also non‐irritant with a relative cell viability of 92.6%. In conclusion, the developed A. sativum extract‐loaded microemulsion‐based cream formulations appear to be promising formulations for the acne vulgaris treatment, without malodors.

Cellulose fibres enhance the function of hemostatic composite medical sealants.

Tissue adhesives and sealants offer promising alternatives to traditional wound closure methods, but the existing trade-off between biocompatibility and strength is still a challenge. The current study explores the potential of a gelatin-alginate-based hydrogel, cross-linked with a carbodiimide, and loaded with two functional fillers, the hemostatic agent kaolin and cellulose fibres, to improve the hydrogel's mechanical strength and hemostatic properties for use as a sealant. The effect of the formulation parameters on the mechanical and physical properties was studied, as well as the biocompatibility and microstructure. The incorporation of the two functional fillers resulted in a dual micro-composite structure, with uniform dispersion of both fillers within the hydrogel, and excellent adhesion between the fillers and the hydrogel matrix. This enabled to strongly increase the sealing ability and the tensile strength and modulus of the hydrogel. The fibres' contribution to the enhanced mechanical properties is more dominant than that of kaolin. A combined synergistic effect of both fillers resulted in enhanced sealing ability (247%), tensile strength (400%), and Young's modulus (437%), compared to the unloaded hydrogel formulation. While the incorporation of kaolin almost did not affect the physical properties of the hydrogel, the incorporation of the fibres strongly increased the viscosity and decreased the gelation time and swelling degree. The cytotoxicity tests indicated that all studied formulations exhibited high cell viability. Hence, the studied new dual micro-composite hydrogels may be suitable for medical sealing applications, especially when it is needed to get a high sealing effect within a short time. The desired hemostatic effect is obtained due to kaolin incorporation without affecting the physical properties of the sealant. Understanding the effects of the formulation parameters on the hydrogel's properties enables the fitting of optimal formulations for various medical sealing applications.

Assessing nutritional probing and storage stability of functional Aloe vera (Aloe barbadensis) based guava jam: a machine learning approach for predictive modelling

SummaryThis research aimed to explore the influence of nutritional adjustments and storage stability on a functional, reduced‐calorie guava jam incorporating Aloe vera. Over two months, comprehensive analysis assessed physicochemical properties, sensory traits, microbial stability, and shelf‐life. The addition of Aloe vera gel resulted in significant improvements in pH (3.00 to 3.65), total soluble solids (40.10 to 42.20°Brix), antioxidant activity (36.85% to 81.09%), moisture content (29.48% to 38.82%), water activity (0.78 to 0.84), ash content (0.29% to 0.45%), fat content (0.14% to 0.19%), fibre content (1.05% to 1.86%), and the colour values. Moreover, b* scores for colour indication improved from 15.09 to 18.86. Texture attributes of cohesiveness and firmness improved significantly. Sensory evaluation favoured the T2 variant (20% Aloe vera gel), suggesting it as the optimal formulation. Furthermore, artificial neural networks (ANNs), a technique of machine learning, were utilised to predict guava jam behaviour, with 99% accuracy. The study discovered substantial changes in pH, total soluble solids, antioxidant activity, moisture content, and textural qualities, indicating that Aloe vera supplementation could improve guava jam quality and shelf‐life. The results of ANN predictions about antioxidants and cohesiveness provide information about the product's performance during storage.

Unveiling Garlic's Arsenal: A Comprehensive Review of Antifungal and Antibacterial Cream

Garlic (Allium sativum) has long been recognized for its medicinal properties, particularly its antimicrobial effects. In this comprehensive review, we explore the therapeutic potential of garlic in the formulation of creams targeting fungal and bacterial infections. We discuss the rising prevalence of fungal infections, particularly those caused by Candida species, and the challenges they pose in healthcare settings. Furthermore, we delve into the diverse biochemical composition of garlic, including sulfur compounds, enzymes, carbohydrates, minerals, amino acids, flavonoids, and vitamins, which contribute to its antimicrobial activity. The synthesis of allicin, a key bioactive compound in garlic, and its mechanism of action against various pathogens are elucidated. Additionally, we examine the dermatological applications of topical garlic in treating fungal skin infections, wound healing, antioxidant protection, UVB shielding, and anti-aging benefits. Clinical evidence supporting the efficacy of garlic extracts in managing viral skin conditions is also discussed. Finally, we highlight the need for further research and clinical trials to fully explore garlic's therapeutic potential, safety profile, and optimal formulations, thereby enhancing patient outcomes in the management of infectious diseases.

Optimization of polydimethylsiloxane (PDMS) surface chemical modification and formulation for improved T cell activation and expansion

Adoptive T cell therapy has undergone remarkable advancements in recent decades; nevertheless, the rapid and effective ex vivo expansion of tumor-reactive T cells remains a formidable challenge, limiting their clinical application. Artificial antigen-presenting substrates represent a promising avenue for enhancing the efficiency of adoptive immunotherapy and fostering T cell expansion. These substrates offer significant potential by providing flexibility and modularity in the design of tailored stimulatory environments. Polydimethylsiloxane (PDMS) silicone elastomer stands as a widely utilized biomaterial for exploring the varying sensitivity of T cell activation to substrate properties. This paper explores the optimization of PDMS surface modification and formulation to create customized stimulatory surfaces with the goal of enhancing T cell expansion. By employing soft PDMS elastomer functionalized through silanization and activating agent, coupled with site-directed protein immobilization techniques, a novel T cell stimulatory platform is introduced, facilitating T cell activation and proliferation. Notably, our findings underscore that softer modified elastomers (Young’ modulus E∼300 kPa) exhibit superior efficacy in stimulating and activating mouse CD4+ T cells compared to their stiffer counterparts (E∼3 MPa). Furthermore, softened modified PDMS substrates demonstrate enhanced capabilities in T cell expansion and Th1 differentiation, offering promising insights for the advancement of T cell-based immunotherapy.