D-optimal Mixture Design Research Articles

Quality evaluation and acceptability of cookies produced from wheat (Triticum aestivum) flour substituted with avocado puree as fat substitute

PurposeThe purpose of this study is to evaluate the quality and sensory properties of cookies produced from wheat flour using avocado puree as fat substitute.Design/methodology/approachCookies were produced from wheat flour using avocado puree as fat substitute in ratio 0%, 25%, 50%, 75% and 100%, respectively. The formulation of margarine and avocado puree blends was done by using D-Optimal Mixture Design. In all, 20 samples were produced from each substitution level and analyses were done in triplicates to obtain mean values using standard methods. Means were separated by Duncan’s multiple range test, and significances were accepted at less than 5% confidence level (p < 0.05). Proximate and functional analyses were conducted on the flour samples, while cookie samples were subjected to proximate and sensory analyses.FindingsThe results of this study revealed that the values of loose bulk density, packed bulk density, oil absorption density, water absorption capacity, swelling power, solubility and dispersibility of the flours at p < 0.05 are 0.3–0.4 g/ml, 0.5–0.7 g/ml, 16.9%–94.0%, 39.7%–80.6%, 461.2%–618.2%, 6.0%–29.8% and 69.0%–82.8%, respectively. The moisture, protein, fat, total dietary fiber, total ash and carbohydrate contents of the cookies at p < 0.05 are 3.6%–16.7%, 6.5%–9.9%, 2.5%–19.2%, 1.7%–1.9%, 1.1%–3.0% and 65.0%–70.7%, respectively. The taste, color, crispiness, texture and overall acceptability of the cookies at p < 0.05 are 7.4–7.8, 6.9–7.5, 7.2–7.9, 7.3–7.7 and 7.4–8.3, respectively. The sensory scores showed that panelists preferred the taste, crispiness and texture of the cookies produced from wheat flour using avocado puree as fat substitute at varying proportion. The sensory characteristics of sample WF4 (100% avocado puree) were rated overall best in all the parameters tested followed by sample WF3 (75% avocado puree). Hence, this study established the possibility of producing cookies from wheat flour using avocado puree as fat substitute without a negative impact on the sensory characteristics and the consumers’ acceptability.Practical implicationsThe cookies produced from this study are not meant for vegetarians because eggs were added in the formulations and recipes but could be valuable to ovo-vegetarians that may take food with eggs without restriction. The major challenge of this study was that avocados are very expensive in much of the world, so this is only suitable and viable where there is an excess of the fruit.Originality/valueThis study examined the use of avocado puree as fat substitute in cookie production. Effects of avocado puree on proximate composition and functionality of cookies produced from wheat flour were also determined. This approach was novel, and it will encourage the use of avocado for value-added in industrial food production.

Rapid detection of sesame oil multiple adulteration using a portable Raman spectrometer

Multiple adulteration is a commonly used fraud of illegal traders to mask the traditional adulteration detection methods. In this study, rapid detection of multiple adulteration of sesame oil was proposed using a portable Raman spectrometer. Two strategies including simplex theory of mixtures and D-optimal mixture design were used to conduct variable selection and model evaluation, respectively. Based on simplex theory of mixtures, the important variables were selected by orthogonal partial least squares discriminant analysis of preprocessed Raman spectra of sesame oils and four adulterant oils. Moreover, multiple adulteration identification model was built by one-class partial least squares and validated by representative adulterated samples prepared by D-Optimal mixture design. The validation results show that 40 sesame oils adulterated with four types of adulterant oils can be correctly identified, indicating Raman spectroscopy is an effective tool for the detection of multiple adulteration of sesame oil, especially for on-site applications.

Control Strategy for Excipient Variability in the Quality by Design Approach Using Statistical Analysis and Predictive Model: Effect of Microcrystalline Cellulose Variability on Design Space.

Although various quality by design (QbD) approaches have been used to establish a design space to obtain robust drug formulation and process parameters, the effect of excipient variability on the design space and drug product quality is unclear. In this study, the effect of microcrystalline cellulose (MCC) variability on drug product quality was examined using a design space for immediate-release tablets of amlodipine besylate. MCC variability was assessed by altering the manufacturer and grade. The formulation was developed by employing the QbD approach, which was optimized using a D-optimal mixture design. Using 36 different MCCs, the effect of MCC variability on the design space was assessed. The design space was shifted by different manufacturers and grades of MCC, which resulted in associations between the physicochemical properties of MCC and critical quality attributes (CQAs). The correlation between the physicochemical properties of MCCs and CQAs was assessed through a statistical analysis. A predictive model correlating the physicochemical properties of MCCs with dissolution was established using an artificial neural network (ANN). The ANN model accurately predicted dissolution with low absolute and relative errors. The present study described a comprehensive QbD approach, statistical analysis, and ANN to comprehend and manage the effect of excipient variability on the design space.

Augmented Oral Bioavailability and Prokinetic Activity of Levosulpiride Delivered in Nanostructured Lipid Carriers.

The present study is aimed to develop and optimize levosulpiride-loaded nanostructured lipid carriers (LSP-NLCs) for improving oral bioavailability and prokinetic activity of LSP. LSP-NLCs were optimized with D-optimal mixture design using solid lipid, liquid lipid and surfactant concentrations as independent variables. The prepared LSP-NLCs were evaluated for physicochemical properties and solid-state characterization. The in vivo oral pharmacokinetics and prokinetic activity of LSP-NLCs were evaluated in rats. LSP-NLCs formulation was optimized at Precirol® ATO 5/Labrasol (80.55/19.45%, w/w) and Tween 80/Span 80 concentration of 5% (w/w) as a surfactant mixture. LSP-NLCs showed a spherical shape with a particle size of 152 nm, a polydispersity index of 0.230 and an entrapment efficiency of 88%. The DSC and PXRD analysis revealed conversion of crystalline LSP to amorphous state after loading into the lipid matrix. LSP-NLCs displayed a 3.42- and 4.38-flods increase in AUC and Cmax after oral administration compared to LSP dispersion. In addition, LSP-NLCs showed enhanced gastric emptying (61.4%), intestinal transit (63.0%), and fecal count (68.8) compared to LSP dispersion (39.7%, 38.0% and 51.0, respectively). Taken together, these results show improved oral bioavailability and prokinetic activity of LSP-NLCs and presents a promising strategy to improve therapeutic activity of LSP for efficient treatment of gastric diseases.

Investigation of the use of various fruit juice concentrates instead of corn syrup in marshmallow type products: A preliminary study

In this study, the effects of using various fruit juice concentrates (pomegranate, grape and sour cherry) instead of corn syrup in marshmallows on the physico-chemical, textural and microstructural properties of the products were investigated. Experimental points of the study were determined by D-optimal mixture design, and accordingly, special cubic, linear and quadratic models were used for the effects on physico-chemical, color and texture parameters according to independent variables. Considering the results, pH, water activity and density values of the marshmallow samples were found to be in the range of 2.54–3.21, 0.48–0.55 and 0.44–0.66 g/mL, respectively. As expected, the use of fruit juice concentrates affected the visual properties of marshmallows, and in particular sour cherry and pomegranate juice concentrates caused a positive increase in the +a* values of the samples. According to the texture profile analysis, the hardness, springiness, cohesiveness, gumminess and resilience values of the samples were determined as 6.43–10.5 N, 0.84–97, 0.74–0.90, 5.18–8.22 g, 0.34–0.81, respectively. R2 values of investigated parameter models were determined between 0.4971 and 0.8901. It was concluded that fruit juice concentrates can be used instead of corn syrup in marshmallows to meet consumer demands and expectations. Finally, it is thought that it will be useful to investigate the effects of various hydrocolloids on the color, texture stability and sensory properties of the products with further studies using fruit juice concentrates in marshmallow production.

A Highly Efficient Biomass Compound Aerosol Suppressant in Purifying Radioactive Cesium Droplet Aerosols.

Nuclear accidents and decommissioning in the nuclear industry would release a large number of radioactive aerosols which endangers the natural environment and the health of workers. Therefore, there is an urgent need for environment-friendly aerosol suppressants to control and handle environmental pollution problems caused by radioactive aerosols. In this paper, sodium alginate (SA), a type of polyphenol material (TP), and alkyl glycosides (APGs) were selected as the components of the compound aerosol suppressant and the optimal proportion was generated via the method of D-optimal mixture design. Furthermore, the cesium aerosol sedimentation effect of the optimized compound aerosol suppressants was evaluated via sedimentation efficiency, the change in particle concentration cumulative concentration fraction of the cesium aerosol sedimentation process. The results showed that the aerosol sedimentation efficiency was 99.82% which was much higher than nature settlement, 18.6% and water spraying sedimentation, 43.3%. Moreover, after spraying the compound suppressant, it displayed a good effect on settling the cesium aerosol particles with a diameter of less than 1 µm, as the concentration of particles was reduced from 55.49% to 44.53%. Finally, the sedimentation mechanism of the compound aerosol suppressant and cesium aerosol particles, such as the coagulation effect, was analyzed using the particle size distribution.

Effect of Oromo Dinich (Plectranthus edulis) flour supplemented on quality characteristics of teff-maize composite injera

Blending Oromo dinich flours with cereals-based flours significantly enhances the nutritional potential of cereals-based products. Therefore, this study aimed to develop and evaluate the quality of teff-based injera supplemented by underutilized indigenous tuber Oromo dinich (Plectranthus edulis) and maize flours. Fourteen formulations were generated using D-optimal constrained mixture design with a range of maize (5–15%), Plectranthus edulis (5–15%), and teff (70–90%). Statistical evaluation and optimization were done using D-optimal mixture design expert software. The results showed that the supplementation of more Plectranthus edulis flour in the formulations indicated better improvements in terms of protein (10–10.8%), fat (2.4–2.8%), gross energy contents (380.7–391.9 kcal/100g), total phenolic content (8.6–15.8 mg GAE/g) and total antioxidant capacity (66.20–82.7%) at the concentration of 3.32 mg/mL. The sensory acceptability of the injera was significantly (p < 0.05) liked in terms of aroma with increasing the ratio of Plectranthus edulis and maize flours. The optimum value of the blending ratio was 77.6% teff, 13.1% maize, and 9.3% Plectranthus edulis flours with desirable nutritional composition of injera, which varied for protein (10.7–10.8%), fat (2.62–2.8%) and energy (388.3–391.9 kcal/100g) and overall acceptance (5.5–6.3) with the desirability of 0.66. The optimization results indicated that supplementing Plectranthus edulis flour up to 10% with teff-maize composite flours were acceptable in terms of nutritional composition and sensory quality. Thus, supplementing underutilized indigenous Plectranthus edulis tuber flour with teff-maize flours significantly enhanced the nutritional potential of injera products.

Nutritional, physical, microbial, and sensory characteristics of gluten-and sugar-free cereal bar enriched with spirulina and flavored with neroli essential oil

This study aims to formulate a gluten- and sugar-free cereal bars, enriched with spirulina and flavored with neroli essential oil. The basic formula consists of gluten-free cereals (SCB). Then, sugar and glucose syrup are replaced by a mixture of three sweeteners (maltodextrin, sorbitol and, maltitol syrup). The D-optimal mixture design was used to optimize the influence of these three sweeteners on the sensory quality of cereal bars. The optimized mixture fractions of the best formulation, containing 10 g/100 g maltodextrin, 10 g/100 g sorbitol, and 80 g/100 g maltitol syrup of the total sweeteners. The best formulation was flavored with 20 μL/100 g of neroli essential oil (CB), and enriched with 2 g/100 g spirulina (CBS). Formulations were compared in terms of nutritional, physical, microbial, and sensory characteristics. The addition of spirulina increases the nutritional content and antioxidant inhibition. Then, CB and CBS were found in Nutri-Score category A. In addition, they are very natural, and stable for 60 days storage at room temperature.

Enhanced oral absorption of insulin: hydrophobic ion pairing and a self-microemulsifying drug delivery system using a D-optimal mixture design

The lipophilicity of a peptide drug can be considerably increased by hydrophobic ion pairing with amphiphilic counterions for successful incorporation into lipid-based formulations. Herein, to enhance the oral absorption of insulin (INS), a self-microemulsifying drug delivery system (SMEDDS) formulation was developed. Prior to optimization, INS was complexed with sodium n-octadecyl sulfate (SOS) to increase the loading into the SMEDDS. The INS–SOS complex was characterized via scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and its dissociation behavior. The SMEDDS was optimized using a D-optimal mixture design with three independent variables including Capmul MCM (X 1, 9.31%), Labrasol (X 2, 49.77%), and Tetraglycol (X 3, 40.92%) and three response variables including droplet size (Y 1, 115.2 nm), INS stability (Y 2, 46.75%), and INS leakage (Y 3, 17.67%). The desirability function was 0.766, indicating excellent agreement between the predicted and experimental values. The stability of INS-SOS against gastrointestinal enzymes was noticeably improved in the SMEDDS, and the majority of INS remained in oil droplets during release. Following oral administration in diabetic rats, the optimized SMEDDS resulted in pharmacological availabilities of 3.23% (50 IU/kg) and 2.13% (100 IU/kg). Thus, the optimized SMEDDS is a good candidate for the practical development of oral delivery of peptide drugs such as INS.

Solubility Enhancement of Ebastine by Formulating Microemulsion Using D-Optimal Mixture Design: Optimization and Characterization.

Ebastine, a histamine H1 antagonist, nonsedating, belonging to BCS class II is used in the treatment of allergic rhinitis and chronic idiopathic urticaria. The current study was intended in augmenting the aqueous solubility and dissolution rate of ebastine, by formulating a microemulsion system using oleic acid, Transcutol® HP, and Tween®80 as oily phase, cosurfactant, and surfactant, respectively, by the phase titration method. A custom mixture design with optimality D was used to design the formulation by using the Design Expert® Software (Version 11; Stat-Ease, Inc., Minneapolis, MN, USA). Optimization of formulation was performed using the numerical optimization technique, where optimization is based upon the desirability. The optimized formulation was evaluated for transmittance, viscosity, globule size, polydispersity index, zeta potential, drug content, morphological studies, and in vitro studies. The optimized formulation displayed percent cumulative drug release, ranging from 82.9% to 90.6% obtained after dissolution studies and the percent cumulative drug release after diffusion studies ranged from 83.3% to 100%. The in vitro release data were subjected to kinetic treatment. The zero-order and first-order plots were linear and showed the highest values for R2, which indicated mixed-order release. The Higuchi plot was linear, indicating diffusion as the mechanism of release. From Peppas plot, it was further confirmed that the release for dissolution studies was anomalous and for diffusion studies it was zero order. Thus, the studies concluded that the microemulsion technique is a very good approach for enhancing the solubility and dissolution rate of the BCS class II drug ebastine.

Olive Oil-Based Oleogel as Fat Replacer in a Sponge Cake: A Comparative Study and Optimization.

Oleogels (defined as structured solid-like materials with a high amount of oil entrapped within a three-dimensional network of gelator molecules) represent a healthy alternative to fats that are rich in saturated and trans fatty acids. Given its fatty acids composition (oleic, linoleic, and linolenic acids), olive oil is an excellent candidate for the use of oleogels in the food industry. In this study, a D-optimal mixture design was employed to optimize the replacement of butter with olive oil-based oleogel in a type of sponge cake formulation: the plum cake. In addition, emulsifiers and whey proteins were used as recipe ingredients to extend the product’s shelf life by delaying staling phenomena and mold growth. In the experimental design, oleogel, emulsifier, and whey protein variables were set as the ingredients that change in specific ranges, while hardness, porosity, water activity, and moistness were used to characterize the obtained formulations. The experimental data of each response were fitted through polynomial regression models with the aim of identifying the best plum cake formulation. The results revealed that the best mixture was the formulation containing 76.98% olive oil-based oleogel, 7.28% emulsifier E471, and 15.73% whey protein. We stored the optimized plum cake for 3 months at room temperature and then checked for any hardness and moistness changes or mold spoilage.

Evaluation of Phytochemical, Nutritional and Antioxidant Properties of a Functional Tea Prepared from Blends of Local Spices Utazi (Gongronema latifolium), Nchanwu (Ocimum gratissium) and Tumeric (Curcuma longa)

The study assessed the phytochemical, nutritional and antioxidant properties of a functional tea made from mixture of Utazi leaf Gongronema latifolium), Nchanwu leaf (Ocimum gratissimum) and Turmeric rhizome (Curcuma longa). The three spices were individually processed by drying and mincing before combining them at different ratios that resulted to 16 samples. The samples were generated through D-optimal mixture design using statistical software (Design Expert version 12). The samples were evaluated for phytochemical, nutritional and antioxidant properties. The fresh raw materials were destalked (for the leaves), sorted, washed, withered, oxidized for 24 h, oven dried at 60oC for 30 min, cooled and milled, and packaged. Fresh turmeric rhizome were sorted, washed blanched at 90oC for 2 min, cooled, peeled, sliced, oven dried at 60oC for 30 min, cooled, milled and packaged in teabags and high density polyethylene. The alkaloids, saponin, phenol, cardiac glycoside, flavonoid, tannin, steroid and anthocyanin content ranged from 12.00-22.00, 0.42-1.15, 11.67-15.63, 0.06-0.67, 12.67-22.00, 0.56-0.89, 1.00-1.67, 46.00-54.00 mg/100g respectively. The vitamin C and E content ranged from 3.03-4.13, 0.31-0.64 mg/100g respectively. The minerals iron and zinc content of the tea samples ranged from 3.53-4.70, 0.06-0.78 ppm respectively. The sensory evaluation score of the tea infusion of the sample AB and DA were ‘liked very much’ with the rating of 8.60 and 8.20 respectively, these samples were more acceptable to the panelist. The antioxidant scavenging activity ranged from 42.00-47.00% with sample EC exhibiting the highest level of activity, and the proportion was 70g, 24.62g, 5.38g of Utazi leave, Nchanwu leave, and Turmeric rhizome.

In silico-assisted development of supersaturable preconcentrated isotropic mixture of atazanavir for augmenting biopharmaceutical performance in the presence of H2-receptor antagonist.

The therapeutic potential of atazanavir (BCS Class II drug), a highly selective inhibitor of human immunodeficiency virus (HIV-1), has been largely limited due to its low intrinsic solubility at elevated pH resulting in low oral bioavailability. Thus, the current work describes the systematic development, optimization, and evaluation of hydroxypropyl methylcellulose acetate succinate (HPMC-AS)-based supersaturable preconcentrate isotropic mixture (SP-IM) containing long-chain triglyceride to improve intestinal lymphatic transport and augment oral bioavailability of atazanavir (ATZ). A D-optimal mixture design was employed for optimization of plain IM containing corn oil, oleic acid, Tween 80, and propylene glycol, evaluating various critical quality attributes (CQAs) like particle size, polydispersity index, self-emulsification time, % transmittance, and drug content. In silico analysis and in vitro supersaturation test facilitated the selection of HPMC-AS as a best suited polymeric precipitation inhibitor (PPI) for formulating ATZ loaded SP-IM (ATZ-SP-IM). In vitro dissolution data indicated that ATZ-SP-IM exhibits superior performance in 0.025N HCl and pH 6.8 over pure drug. Ex vivo permeation and in vivo pharmacokinetic study of ATZ-SP-IM corroborated enhanced permeation (2.03 fold) and improved drug absorption via lymphatic transport in Wistar rats. Further, the pharmacokinetic performance of ATZ-SP-IM was not affected in presence of H2 receptor antagonist. Therefore, the results showed that ATZ-SP-IM can significantly improve the biopharmaceutical attributes of ATZ so as to lay a foundation of further research on the new dosage form of ATZ.

Formulation Development and Optimization of Blonanserin Liquid SMEDDS using D-Optimal Mixture Design

Background: Blonanserin is an atypical antipsychotic potent antagonist of dopamine-D2 and D3 receptors with low aqueous solubility BCS class II drugs. Objective: The present research aims to develop and optimize the Blonanserin-loaded liquid selfmicro emulsifying drug delivery system (SMEDDS) to improve its in vitro drug release by D-optimal mixture design. Methods: Saturation solubility of Blonanserin was checked in various oils, surfactants, and cosurfactants. The pseudo-ternary phase diagram was developed to identify the region of the microemulsion. Trial batches were designed to determine dependent and independent variables in the formulation. DOptimal Mixture design applies for optimization and minimized trials. The amount of oil(X1), surfactant( X2), and co-surfactant(X3) were selected as independent variables, and solubility(Y1) and in vitro percentage cumulative drug release(Y2) and size of globule(Y3) after 250 times dilution were selected as the dependant variable. The level of the independent variables in the design will be selected based on the drug's phase diagram, trial batches, and solubility. The developed SMEDDS was then evaluated for globule size, transparency, self-emulsification time, in vitro dissolution, and relative dissolution of the final formulation with marketed products and a pure drug. Results: BLN shows the highest solubility in (1:1) Captex 200P: Capmul MCM (oil), Tween 20 (surfactant), and Ethanol (cosurfactant). Trial batches were shown at 1:9, 2:8, and 3:7 oil to surfactant and cosurfactant ratios suitable for optimization. Optimization using a D-optimal mixture design gives 11 run batches and the resulting surface and contour plot suggest the best design space. The optimized formula given by the mixture design of the target formulation had maximum drug solubility, maximum drug release, and minimum globule size. Optimized formula containing Blonanserin, Captex 200P: Capmul MCM (1:1) Mixture (23% v/v), Tween 80 (57% v/v), and Ethanol (20% v/v) having 94.72% in vitro diffusion within 30 min with 21 nm globule size. Optimized liquid SMEDDS have a higher in-vitro diffusion rate than marketed products and pure drugs. Conclusion: Blonanserin liquid SMEDDS was successfully developed with high solubility, nanoglobule size, and improvement in in-vitro diffusion rate and vice versa for improvement in bioavailability of the drug.

Preparation and Characterization of Clopidogrel Bisulfate-hydroxypropyl-β-Cyclodextrin Mixed Inclusion Complex for Improved Intestinal Solubility and Anti-Thrombotic Efficacy

The study aimed to increase the intestinal solubility and absorption of orally bioavailable clopidogrel-bisulfate (CPB) by complexing with hydroxypropyl-β-cyclodextrin (HCD) to form a binary inclusion complex that was stabilized by Tween 80 (T80) resulting into mixed inclusion complex. The results of phase solubility studies and molecular docking of CPB with β-cyclodextrin (β-CD) and HCD suggested higher solubility and binding energy of the stable CPB: HCD complex in the presence of T80 as compared to the CPB: β-CD complex. The D-Optimal mixture design was used to optimize the formulation containing the CPB: HCD: T80 mixed inclusion complex. The results suggest the enhanced stability of the CPB: HCD inclusion complex in the presence of T80. The spectral attributes confirmed the inclusion complexation and pointed out the central position of CPB in a hydrophilic cavity of HCD. Further, the prepared soft gelatin capsule successfully confirmed the importance of obliterating the intestinal precipitation associated problem of CPB through an in-vitro release study. The anticoagulant activity in rabbits confirmed that soft gelatin capsules showed 1.2 folds and 1.3 folds increase in clotting time, 1.2 fold and 1.5 folds increase in bleeding time when compared to marketed formulation and pure drug, respectively. Conclusively, soft gelatin capsules exhibit the potential to enhance the oral bioavailability of CPB, leading to reduction of the dose and dose-related side effects.

Optimized self-microemulsifying drug delivery system improves the oral bioavailability and brain delivery of coenzyme Q10

Our study aimed to develop a self-microemulsifying drug delivery system for the poorly aqueous-soluble drug Coenzyme Q10, to improve the dissolution and the oral bioavailability. Excipients were selected based on their Coenzyme Q10 solubility, and their concentrations were set for the optimization of the microemulsion by using a D-optimal mixture design to achieve a minimum droplet size and a maximum solubility of Coenzyme Q10 within 15 min. The optimized formulation was composed of an oil (omega-3; 38.55%), a co-surfactant (Lauroglycol® 90; 31.42%), and a surfactant (Gelucire® 44/14; 30%) and exhibited a mean droplet size of 237.6 ± 5.8 nm and a drug solubilization (at 15 min) of 16 ± 2.48%. The drug dissolution of the optimized formulation conducted over 8 h in phosphate buffer medium (pH 6.8) was significantly higher when compared to that of the Coenzyme Q10 suspension. A pharmacokinetic study in rats revealed a 4.5-fold and a 4.1-fold increase in the area under curve and the peak plasma concentration values generated by the optimized formulation respectively, as compared to the Coenzyme Q10 suspension. A Coenzyme Q10 brain distribution study revealed a higher Coenzyme Q10 distribution in the brains of rats treated with the optimized formulation than the Coenzyme Q10 suspension. Coenzyme Q10-loaded self microemulsifying drug delivery system was successfully formulated and optimized by a response surface methodology based on a D-optimal mixture design and could be used as a delivery vehicle for the enhancement of the oral bioavailability and brain distribution of poorly soluble drugs such as Coenzyme Q10.

Yenilebilir mantar (Pleurotus ostreatus) için tahılsız misel geliştirilmesi: D-optimal karışım tasarımı yaklaşımı

Objective: The objective of this study was to develop a non-grain spawn formulation for Pleurotus ostreatus with the D-optimal mixture design approach. The developed spawn was compared with the traditionally used grain spawn in terms of spawn running time and biological efficiency. Material and Methods: Non-grain spawn was produced in 25 different formulations using wheat bran, poplar sawdust, perlite, CaCO3, CaSO4 components. In addition, oat spawn containing 1% CaSO4 and 0.5% CaCO3 from cereals was used as the control group. Spawn running times and the biological efficiencies of the samples were determined. Results: The optimum mixing ratios for wheat bran, poplar sawdust, perlite, CaCO3, and CaSO4 used in the formulation of non-grain spawn production were determined as 11.44%, 28.87%, 50.74%, 5.89%, and 3.07%, respectively. The spawn running time of the improved non-grain spawn produced according to the above formulation was shortened by 20.16% as compared to the grain-derived spawn. This shows that the non-grain as one of the two different spawn production methods is technologically superior. Conclusion: In the leading countries in mushroom production, new technologies and formulations are being developed day by day to shorten the spawn running time and increase biological efficiency and mushroom yield. It is thought that this study will contribute to the development of spawn technology, which is an essential input in mushroom cultivation.

A Cosmeceutical Topical Water-in-Oil Nanoemulsion of Natural Bioactives: Design of Experiment, in vitro Characterization, and in vivo Skin Performance Against UVB Irradiation-Induced Skin Damages.

IntroductionDamage to human skin occurs either chronologically or through repetitive exposure to ultraviolet (UV) radiation, where collagen photodegradation leads to the formation of wrinkles and skin imperfections. Consequently, cosmeceutical products containing natural bioactives to restore or regenerate collagen have gained a remarkable attention as an ameliorative remedy.MethodsThis study aimed to develop and optimize collagen-loaded water-in-oil nanoemulsion (W/O NE) through a D-optimal mixture design to achieve an ideal multifunctional nanosystem containing active constituents. Vit E was included as a constituent of the formulation for its antioxidant properties to minimize the destructive impact of UV radiation. The formulated systems were characterized in terms of their globule size, optical clarity, and viscosity. An optimized system was selected and evaluated for its physical stability, in vitro wound healing properties, and in vivo permeation and protection against UV radiation. In addition, the effect of collagen-loaded NE was compared to Vit C-loaded NE and collagen-/Vit C-loaded NEs mixture as Vit C is known to enhance collagen production within the skin.ResultsThe optimized NE was formulated with 25% oils (Vit E: safflower oil, 1:3), 54.635% surfactant/cosurfactant (Span 80: Kolliphor EL: Arlasolve, 1:1:1), and 20.365% water. The optimized NE loaded with either collagen or Vit C exhibited a skin-friendly appearance with boosted permeability, and improved cell viability and wound healing properties on fibroblast cell lines. Moreover, the in vivo study and histopathological investigations confirmed the efficacy of the developed system to protect the skin against UV damage. The results revealed that the effect of collagen-/Vit C-loaded NEs mixture was more pronounced, as both drugs reduced the skin damage to an extent that it was free from any detectable alterations.ConclusionNE formulated using Vit E and containing collagen and/or Vit C could be a promising ameliorative remedy for skin protection against UVB irradiation.

Polydextrose and guar gum as a fat substitute in rice cookies and its physical, textural, and sensory properties

This study was to investigate the combined effect of polydextrose and guar gum, as a fat replacer, on physical, chemical, textural, and sensory properties of developed Sungyod rice cookies (SYRC). The variation of polydextrose (5.00-9.50%), guar gum (0.50-1.00%), and butter (12.00-16.50%) were optimized using a d-optimal mixture design with 3 center points. The suitable formulation for SYRC with the optimized quantity of polydextrose (5.00%), guar gum (1.00%), and butter (16.00%) was obtained and can substitute the fat content in control SYRC up to 6%. The substitution of polydextrose and guar gum significantly affected the physical, chemical, textural, and sensory properties, especially fat content which could be reduced by 27.86% as compared with control SYRC formulation. The consumer acceptance of optimized SYRC was in the range of like slightly to like very much (6.7–7.4). The research outcomes indicated that polydextrose and guar gum can substitute fat content in SYRC and can be applied to create bakery products which can further recommend the exploitation of various ingredients to deliver reduced-fat products.

D-optimal mixture design optimized solid formulation containing fruits extracts of Momordica charantia and Abelmoschus esculentus.

Fruit extracts of Momordica charantia L. (Cucurbitaceae) and Abelmoschus esculentus (L.) Moench (Malvaceae) have shown promising antidiabetic activities in clinical trials. However, they remain underutilized due to insufficient standardization and lack of formulation containing their mixture. This study’s overall purpose was to develop and optimize a capsule dosage form containing dried fruit extracts of M. charantia and A. esculentus. The design of the experiment involved two steps; first, response surface methodology (RSM) with a five-level two-factor central composite rotatable design (CCRD) was employed to determine the optimal dose of a mixture of extracts for adequate glycemic control. The extract of M. charantia and A. esculentus were the independent variables while fasting plasma glucose (FPG) was the dependent factor. In the second step, a D-optimal mixture design was applied to study the interaction effect of the optimal dose and selected excipients on granules flowability and capsules’ disintegration time. Moreover, a second-order quadratic model determined the interrelationship of excipients and the desired capsules’ quality attributes. The validity of the predicted models was confirmed. The findings indicated that a combined dose of 175 A. esculentus and 281 M. charantia (mg/kg) significantly reduced the FPG level compared to vehicle at day 14 (mean difference -2.7 ± 0.21, p < 0.001). This dose was used to make a 600 mg capsule (DM083) with 76% drug loading. The DM083 had 40.4 ± 0.62 mg GAE/gDW total polyphenols, 12 peaks HPLC fingerprint, and 26.6 ± 4.75 min average disintegration time. Together, these findings showed that a mixture of M. charantia and A. esculentus fruit extracts could be formulated in a stable capsule dosage form with acceptable quality standards. Further biological studies such as toxicity assays and long-term efficacy studies of the developed capsules could be carried out before large-scale commercial production.