Formulation Factors Research Articles

Antibacterial Activity and Sensory Characteristics of Low Calories Functional Candy Contains Trigona’s Honey (Trigona Itama) and Patchouli Oil (Pogostemon Cablin Benth)

Candy is a product made from sugar which can cause health problems. The proportion of sugar with high calories can be replaced with isomalt which is low in calories, and honey which is beneficial to health. In addition, the use of synthetic flavours in candy can be replaced with essential oils such as patchouli oil. Product analysis was in the form of salivary bacterial growth inhibition and hedonic organoleptic tests to determine the samples' antibacterial activity and sensory characteristics. This research was conducted using two factors of a sugar formulation consisting of 3 levels, namely, G1, G2, and G3. The second factor was patchouli oil concentration consisting of 4 levels, namely N1, N2, N3, and N4. Data on the results of the antibacterial and hedonic activity tests were analyzed using a factorial, Completely Randomized Design (CRD). From the analysis of variance, it can be concluded that sugar formulation, patchouli oil concentration, and their interactions had a significant effect (P0.05) on the growth of salivary bacteria, patchouli oil concentration had a significant effect (P0.05) on hedonic aroma, sugar formulation had a significant effect (P0.05) P0.05) on hedonic texture and had no significant effect (P0.05) on hedonic colour and taste. The best treatment was obtained from the G2N2 sample with salivary bacterial growth of 34.50 ± 6.02 colonies and an overall hedonic value of 3.05 (likes).

Floating Drug Delivery System: As A Novel Approach for Drug Delivery

The retention period of the drug and dosage form in the stomach is very challenging for the treatment of gastrointestinal disease. To solve this problem and improve the efficacy and bioavailability of the drug, most researchers develop a novel carrier system that is called a Floating drug delivery system (FDDS). The goal of this review on floating drug delivery systems (FDDS) is to synthesise contemporary material with a particular concentration on the main mechanism of flotation for stomach retention. The physiology of the stomach (including gastric pH and movement) has been shown a major effect on gastrointestinal holding period and drug delivery behaviour in both intra- and inter-subject variability. The most recent advancements in the Floating drug delivery system (FDDS) are thoroughly reviewed, including the physiological and formulation factors that influence stomach retention, design methods for single-unit and multiple-unit floating systems, and their categorization and formulation characteristics. A synopsis of the research that has been done to determine the effectiveness and utility of floating systems, as well as uses for such systems, is also included in this review. This study covers the most recent Floating drug delivery system (FDDS) technology advances, including patented delivery techniques and commercial devices, along with their benefits and potential applications for oral controlled drug administration in the future.
 Keywords: Floating drug delivery system, Gastric-emptying time, Inter-digestive myoelectric cycle (IDMC), Polymers, Bioavailability, Membrane permeability.

Quality by Design approach for Optimization and Development of Cyclodextrin-Surfactant Complex Based Formulations for Bioavailability Enhancement of Valsartan

The main objective of the present research is to increase the oral bioavailability of Valsartan by inclusion complexes (ICVs) with a cyclodextrin-surfactant combination followed by the formulation of fast-dissolving tablets (FDTs). The solvent evaporation method was used for the preparation of ICVs. Methyl-ß-cyclodextrin and Hydroxypropyl-ß- cyclodextrin were evaluated with the combination of poloxamer 188 to get the formulations with the desired solubility. Central composite design (CCD) was used as the experimental design as a part of the quality by design (QbD) approach. The optimized ICVs were further developed into FDTs by direct compression technique. Taking concentration of povidone, type and concentration of disintegrant as the formulation factors, the FDTs were optimized using CCD. In-vivo bioavailability study in rats was performed for the optimized FDTs against the marketed tablets. The optimized ICVs were found to have a 3.12 mg/mL solubility. The optimized FDTs were found to be disintegrated in 18.7 sec and dissolved 90% of the dose in 6.3 min. The In-vivo results indicated that the FDTs exhibited rapid absorption and an increase in bioavailability by 24.1% against the marketed tablets. The results indicated that the QbD approach successfully improved Valsartan's oral bioavailability through cyclodextrin-surfactant complexation.

Development of Ciprofloxacin-Loaded Bilosomes In-Situ Gel for Ocular Delivery: Optimization, In-Vitro Characterization, Ex-Vivo Permeation, and Antimicrobial Study.

Conventional eye drops are most commonly employed topically in the eye for the management of bacterial conjunctivitis. Eye drops have a low corneal residence time and 90-95% of the administered dose is eliminated from the eye by blinking and the nasolacrimal drainage system. This problem can be minimized by formulating a mucoadhesive ocular in-situ gel system that undergoes sol-gel transition upon stimulation by temperature, pH, and ions. The goal of this study was to develop ciprofloxacin (CIP) loaded bilosomes (BLO) in-situ gel for the improvement of therapeutic efficacy. The BLO was prepared by the thin-film hydration method and optimized by the Box-Behnken design. Cholesterol (CHO), surfactant (Span 60), and bile salt (sodium deoxycholate/SDC) were used as formulation factors. The vesicle size (nm) and entrapment efficiency (%) were selected as responses (dependent factors). The optimized CIP-BLO (CIP-BLO-opt) formulation displayed a vesicle size of 182.4 ± 9.2 nm, a polydispersity index of 0.274, a zeta potential of -34,461.51 mV, and an entrapment efficiency of 90.14 ± 1.24%. Both x-ray diffraction and differential scanning calorimetry spectra did not exhibit extensive peaks of CIP in CIP-BLO-opt, revealing that CIP is encapsulated in the BLO matrix. The CIP-BLO-opt formulation was successfully incorporated into an in-situ gel system using a gelling agent, i.e., Carbopol 934P and hydroxyl propyl methyl cellulose (HPMC K100 M). CIP-BLO-opt in-situ gel formulation (CIP-BLO-opt-IG3) was evaluated for gelling capacity, clarity, pH, viscosity, in-vitro CIP release, bio-adhesive, ex-vivo permeation, toxicity, and antimicrobial study. The CIP-BLO-opt-IG3 exhibited satisfactory gelling properties with a viscosity of 145.85 ± 9.48 cP in the gelling state. CIP-BLO-opt-IG3 displayed sustained CIP release (83.87 ± 5.24%) with Korsmeyer-Peppas kinetic as a best-fitted model (R2 = 0.9667). CIP-BLO-opt-IG3 exhibited a 1.16-fold than CIP-IG and a 2.08-fold higher permeability than pure CIP. CIP-BLO-opt-IG3 displayed a significantly greater bio-adhesion property (924.52 ± 12.37 dyne/cm2) than tear film. Further, CIP-BLO-opt-IG3 does not display any toxicity as confirmed by corneal hydration (76.15%), histology, and the HET-CAM test (zero scores). CIP-BLO-opt-IG3 shows significantly higher (p < 0.05) antimicrobial activity against P. aeruginosa and S. aureus than pure CIP. From all these findings, it could be concluded that CIP-BLO-opt-IG3 might be an effective strategy for the increment of corneal residence time and therapeutic activity of CIP.

3D bioprinted microparticles: Optimizing loading efficiency using advanced DoE technique and machine learning modeling

Current microparticle (MP) development still strongly relies on the laborious trial-and-error approach. Herein, we developed a systemic method to evaluate the significance of MP formulation factors and predict drug loading efficiency (DLE) using design of experiment (DoE) and machine learning modeling. A first-in-class 3D printing concept was initially employed to fabricate polymeric MPs by a 3D printer. Sprayed Multi Adsorbed-droplet Reposing Technology (SMART) was developed to combine extrusion-based printing with emulsion evaporation technique to fabricate a small molecule drug i.e., 6-thioguanine (6-TG) loaded poly (lactide-co-glycolide) (PLGA) MPs. Compared to conventional emulsion evaporation method, SMART employs the shear force exerted by the printing nozzle rather than the sonication energy to generate smaller emulsion droplets in a single step. Furthermore, the applied shear force in the 3D printing process reported herein is controllable since the emulsion is extruded through the nozzle under preset printing conditions. The formulated MPs exhibited spherical structure with size distribution ∼ 1-3μ m in diameter and reached ∼ 100 % drug release at 10 h. Also, the papain-like protease (PLpro) inhibition efficacy of 6-TG in formulated MPs was maintained even after the printing process under different printing conditions. Furthermore, the formulation factor importance was assessed by DoE statistical analysis and further validated by machine learning modeling. Among the four process parameters (drug amount, printing speed, printing pressure, and nozzle size), drug amount was the most influential formulation factor. Moreover, it is interesting that nearly all the machine learning models, especially decision tree (DT), demonstrated superior performance in predicting DLE compared to DoE regression models. Overall, incorporating DoE and machine learning modeling shows great promises in the prediction and optimization of MP formulations factors by means of a novel SMART technology. Moreover, this systemic approach helps streamline the development of MP with programmable pharmaceutical attributes, representing a new paradigm for digital pharmaceutical science.

Preparation and optimization of glyceryl monooleate-low molecular weight chitosan nanoparticles for delivery of morpholinopyrrolizine derivative

Purpose: To develop and optimize glyceryl monooleate–low-molecular-weight chitosan (GMO-LMWC) nanoparticles loaded with morpholinopyrrolizine derivative (NPM).
 Methods: Molecular mechanics was used to determine the main driving force for the complexation between glyceryl monooleate (GMO) and chitosan. Nanoparticles were fabricated using a modified film-rehydration method. Optimization was carried out using a statistical design approach. The effects of formulation factors (concentrations of GMO, LMWC and Tween 80) on zeta potential and particle size were investigated using a 23 factorial design.
 Results: A steady increase in binding energy was observed when chitosan length was increased from 22 to 142 Å, and thereafter it remained almost constant. The examined independent variables had significant effects on particle size and zeta potential. The particle size of the nanoparticles varied from 265 to 1270 nm while zeta potential was in the range of 3 – 12 mV. The optimized preparation showed a significantly low half-maximal inhibitory concentration (IC50) when compared to a free anticancer agent in the hepatocellular carcinoma (HePG-2) cell line.
 Conclusion: A nanoparticulate system composed of GMO and LMWC is a potential nanocarrier for delivery of morpholinopyrrolizine derivative.

Ferrofluid high internal phase emulsion polymer foams for soft, magnetic materials

Magnetic components are an essential part of current electronics, although the materials used to make magnetic components are almost exclusively rigid and non-deformable. The high modulus and inflexible behavior of typical magnetic materials makes their integration into soft, deformable electronics challenging. Soft electronics, however, is a dynamic field pushing forward the state-of-the-art in wearable sensors, human-machine interaction, and biomimetic robots. In order to access the wide range of functionality of rigid electronics, magnetic materials must be made that are high performing and deformable. One previously unexplored route to creating such materials is the encapsulation of a high concentration of magnetic fluids, such as ferrofluids (FF), into an elastomer using high internal phase emulsification. In this work, the formulation factors required to make an effective ferrofluid high internal phase emulsion polymer foam (polyHIPE) utilizing polydimethylsiloxane (PDMS) were investigated such as the emulsifiers, polyHIPE curing kinetics, and the interaction of emulsified nanoparticles. The porous structure, magnetic properties, and mechanical properties of the final, successful FF/PDMS polyHIPE were subsequently characterized. Pores ranged between 10 and 50 μm with visible nanoparticle aggregation. FF/PDMS polyHIPE had an Ms of 18 A∙m2/kg and susceptibility of 0.69, which is reduced as compared to neat ferrofluid, as expected, but an improvement on ferrofluid polymer dispersions found in the literature. Coercivity and magnetic remanence also decreased with respect to the neat ferrofluid. Rheology demonstrated that the polyHIPE had a significantly lower modulus than the neat PDMS as well as a lower modulus than any magnetic composite material currently published. The FF/PDMS polyHIPE created in this work not only demonstrates the potential for deformable magnetic materials based on the emulsification of high concentrations of magnetic fluid into elastomers, but also the potential to create even higher performing materials using a higher concentration of magnetic fluid or ferrofluids with superior magnetic properties.

Pharmacokinetics and Anti-Diabetic Studies of Gliclazide Nanosuspension.

Gliclazide (GCZ), an antidiabetic medication, has poor solubility and limited oral bioavailability due to substantial first-pass metabolism. Thus, the purpose of the current study was to optimize and formulate a GCZ nanosuspension (NS) employing the antisolvent precipitation technique. A three-factor, three-level Box–Behnken design (BBD) was used to examine the impact of the primary formulation factors (drug concentration, stabilizer, and surfactant %) on particle size. The optimized NS contains 29.6 mg/mL drug, 0.739% lecithin, and 0.216% sodium dodecyl sulfate (SDS). Under scanning microscopy, the topography of NS revealed spherical particles. Furthermore, NS had a much better saturation solubility than the pure material, which resulted in a rapid dissolving rate, which was attributed to the amorphous structure and smaller particle size of the NS particles. Studies on intestinal permeability using the in vitro noneverted intestinal sac gut method (duodenum, jejunum, and ileum) and single-pass intestinal permeability (SPIP) techniques showed that the effective permeability was also increased by more than 3 fold. In the pharmacokinetic study, the Cmax and AUC0–t values of NS were approximately 3.35- and 1.9-fold higher than those of the raw medication and marketed formulation (MF). When compared to plain drug and commercial formulations, the antidiabetic efficacy of NS demonstrated that it had a significant impact on lowering glucose levels.

DEVELOPMENT AND OPTIMIZATION OF ASTRAGALIN-LOADED POLYMERIC NANOPARTICLES USING CENTRAL COMPOSITE FACTORIAL DESIGN

Objective: The objective of the present study was to develop and optimize Astragalin-loaded polymeric nanoparticles (AST-NPs) using a central composite factorial design (CCD). Methods: AST-NPs were prepared by the dialysis method. CCD was employed to study the influence of formulation factors, polymer concentration, aqueous organic phase ratio, and process parameter stirring time on dependent physicochemical characteristics, particle size, zeta potential, and percentage entrapment efficiency (%EE) of the drugs. The optimized formulation was evaluated for in vitro release studies and subjected to stability studies. Results: Polymer concentration and process parameters were optimized to produce nanoparticles with desired parameters. The prepared NPs were characterized by Fourier transmission infrared (FT-IR), differential scanning calorimetry (DSC), drug loading, entrapment efficiency, particle size, zeta potential, and in vitro studies. FT-IR and DSC studies indicated that there was no interaction between the drug and polymer. The optimized NPs exhibits stability. Optimized NPs exhibited spherical and porous surfaces with a mean PS of 118 nm, the zeta potential of-25 mV, and %EE of 89%. Conclusion: Astragalin-loaded nanoparticles prepared with optimized formulation composition and process parameters.

Box-Behnken Design: Optimization of Proanthocyanidin-Loaded Transferosomes as an Effective Therapeutic Approach for Osteoarthritis.

Transferosomes are one of the vesicular carriers that have received extensive research and attention recently because of their capacity to get beyond the barriers posed by the stratum corneum to penetration. The intent of the current study is to optimize and evaluate proanthocyanidin (PAC) containing transferosomal transdermal gels. PAC-containing transferosomes were prepared using the film hydration method and then loaded into a 4% methylcellulose gel. A 23 Box–Behnken design was used to optimize the PAC-loaded transferosomal gel, where the effects of phospholipid 90 G (X1), Tween 80 (X2), and sonication time (X3) were evaluated. The formulation factors, such as the drug entrapment efficiency percentage (PEE) and in vitro drug release, were characterized. A PEE of 78.29 ± 1.43% and a drug release in vitro at 6 h of 24.2 ± 1.25% were obtained. The optimized transferosomal-loaded proanthocyanidin (OTP) formulation penetrated the porcine skin at an excellent rate (0.123 ± 0.0067 mg/cm2/h). Stability tests were conducted for OTP to predict the effects of various temperature conditions on the physical appearance, drug content, and PEE for periods of 15, 30, and 45 days. Finally, this transferosomal system for transdermal PAC delivery may be a suitable alternative to the conventional treatment for osteoarthritis.

QUALITY BY DESIGN APPROACH FOR OPTIMIZATION AND DEVELOPMENT OF ORODISPERSIBLE FILMS OF LORNOXICAM INCLUSION COMPLEXES

Lornoxicam is a non-steroidal anti-inflammatory drug, indicated in the treatment of osteoarthritis and rheumatoid arthritis. Lornoxicam is a poor water-soluble drug and hence possesses dissolution limited bioavailability. The aim of the current research work was to develop and characterize orodispersible films of Lornoxicam to enhance its bioavailability by employing Quality-by-Design (QbD) approach. Solvent casting method was used to formulate the Lornoxicam mouth dissolving films. Three formulation factors viz. amount of polymer, amount of PEG 400 and type of polymer were varied at different levels. The responses selected were disintegration time and percent drug dissolved after 5mins. Under the response surface methodology, historical data design was employed to perform the statistical analysis using Design Expert software. The developed films were found to have good elasticity, folding endurance and favorable tensile strength. The disintegration time was found to be 9 to 17 seconds and drug dissolved after 5 minutes was 49 to 95%. The statistical analysis of the results by ANOVA elucidated that there was a significant effect of all the formulation factors on the selected responses (p

Nose to brain delivery of donepezil through surface modified NLCs: Formulation development, optimization, and brain targeting study

The research was aimed to formulate the Donepezil (DPZ)-loaded nanostructured lipid carriers (NLCs) and coated with chitosan (CH) for brain targeting through the intranasal route. NLCs were prepared by homogenization & sonication technique and optimized by three factors-three levels Box-Behnken design (BBD). The composition of DPZ-loaded CH-NLCs was established by using a mixture of Compritol & Capryol 90 as lipid, poloxamer 188 as a surfactant, and CH as a coating agent. The effect of formulation factors was evaluated on particle size, entrapment efficiency, and polydispersity index (PDI). Finally, ex-vivo permeation, in-situ perfusion as well as in-vivo study was conducted on albino Wistar rats for the detection of pharmacokinetic and neuropharmacokinetic parameters like drug targeting efficiency (% DTE), nose to brain drug transport percentage (DTP), etc of the optimized formulation. Optimized formulation (DPZ-CH-NLCs-OPT2) exhibited an acceptable particle size (192.5 ± 7.3 nm) with 89.85 ± 2.17% entrapment efficiency, 0.298 ± 0.021 PDI, and 38.9 mV zeta potential and particles were spherical shape as shown by TEM. DSC thermogram displayed that the drug existed in amorphous form within the NLCs matrix. Permeability coefficient (Papp) of DPZ-CH-NLCs-OPT2 formulation (10.14 ± 1.73 × 10−3 cm h−1) was two folds than DPZ-Sol (4.55 ± 1.18 × 10−3 cm h−1). The nasal absorption rate constant for DPZ-CH-NLCs-OPT2 (1.4 × 10−3 h−1) was found to be significantly higher than DPZ-Sol (0.5 × 10−3 h−1). The bioavailability of DPZ-CH-NLCs was 2.02 fold than that of DPZ-Sol administered intranasally and 2.41 fold than DPZ-CH-NLCs administered via the intravenous route. Efficient brain targeting and targeting potential was observed as showed by DTE (321.21%) and DTP (74.55%) after intranasal administration of DPZ-CH-NLCs as compared to DPZ-Sol (DTE 158.52% and DTP 36.92%). From the findings, it could be concluded that DPZ-CH-NLCs might be an effective strategy for the brain targeting of DPZ through the intranasal route for the treatment of Alzheimer's disease.

Formulation and characterization of immediate-release oral dosage forms with zolpidem tartrate fabricated by digital light processing (DLP) 3D printing technique

The introduction of three-dimensional (3D) printing in the pharmaceutical field has made great strides towards innovations in the way drugs are designed and manufactured. In this study, digital light processing (DLP) technique was used to fabricate oral dosage forms of different shapes with zolpidem tartrate (ZT), incorporated within its therapeutic range. Formulation factors, such as poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) 400 (PEG 400) ratio, as well as water content, were varied in combination with the surface area/volume (SA/V) ratio to achieve immediate drug release. Hypromellose (HPMC) was used as a stabilizing agent of photoreactive suspensions in an attempt to prevent drug sedimentation and subsequent variations in drug content uniformity. Oral dosage forms with doses in the range from 0.15 mg to 6.37 mg, showing very rapid and rapid drug dissolution, were successfully fabricated, confirming the potential of this technique in drug manufacturing with the ability to provide flexible dose adjustments and desirable release profiles by varying formulation factors and geometry of 3D models. DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction) and scanning electron microscopy (SEM) showed that ZT remained in a crystalline form within printed dosage forms and no interactions were found between ZT and polymers.

Sustainable Release of Propranolol Hydrochloride Laden with Biconjugated-Ufasomes Chitosan Hydrogel Attenuates Cisplatin-Induced Sciatic Nerve Damage in In Vitro/In Vivo Evaluation.

Peripheral nerve injuries significantly impact patients’ quality of life and poor functional recovery. Chitosan–ufasomes (CTS–UFAs) exhibit biomimetic features, making them a viable choice for developing novel transdermal delivery for neural repair. This study aimed to investigate the role of CTS–UFAs loaded with the propranolol HCl (PRO) as a model drug in enhancing sciatica in cisplatin-induced sciatic nerve damage in rats. Hence, PRO–UFAs were primed, embedding either span 20 or 60 together with oleic acid and cholesterol using a thin-film hydration process based on full factorial design (24). The influence of formulation factors on UFAs’ physicochemical characteristics and the optimum formulation selection were investigated using Design-Expert® software. Based on the optimal UFA formulation, PRO–CTS–UFAs were constructed and characterized using transmission electron microscopy, stability studies, and ex vivo permeation. In vivo trials on rats with a sciatic nerve injury tested the efficacy of PRO–CTS–UFA and PRO–UFA transdermal hydrogels, PRO solution, compared to normal rats. Additionally, oxidative stress and specific apoptotic biomarkers were assessed, supported by a sciatic nerve histopathological study. PRO–UFAs and PRO–CTS–UFAs disclosed entrapment efficiency of 82.72 ± 2.33% and 85.32 ± 2.65%, a particle size of 317.22 ± 6.43 and 336.12 ± 4.9 nm, ζ potential of −62.06 ± 0.07 and 65.24 ± 0.10 mV, and accumulatively released 70.95 ± 8.14% and 64.03 ± 1.9% PRO within 6 h, respectively. Moreover, PRO–CTS–UFAs significantly restored sciatic nerve structure, inhibited the cisplatin-dependent increase in peripheral myelin 22 gene expression and MDA levels, and further re-established sciatic nerve GSH and CAT content. Furthermore, they elicited MBP re-expression, BCL-2 mild expression, and inhibited TNF-α expression. Briefly, our findings proposed that CTS–UFAs are promising to enhance PRO transdermal delivery to manage sciatic nerve damage.

Formulation and Optimization of Gastro retentive Glimepiride Floating Matrix Tablets

The main objective of this research investigational studies is to formulate floating matrix tablets of glimipride by applying simplex centroid design for optimization technique and by direct compression method. The simplex Centroid configuration was drilled as an enhancement strategy by adjusting the amount of three components all the while and holding back their total concentration constant. Ingredients HPMC K15m, Kappa-carrageenan and sodium bicarbonate as X1,X2,X3 independent Variables while response variables Y1 floating lag time Y1, Percentage drug released after 1 hour Y2% and t90 time required for 90% were considered as response variable factors for formulation and optimization of total 14 formulations simplex centroid design was applied. The measures of HPMC K15M (X1), kappa-Carrageenan (X2) and sodium bicarbonate (X3) were utilized as the autonomous factors while coasting slack time (Y1), Percentage drug discharged after 1 hour(Y2) and time required for 90% (t90) were taken as the reaction factors. According to the simplex centroid configuration complete 14 formulations were formulated. Matrices were evaluated for physical parameters, in-vitro buoyancy, swelling ability and adhesion retention period. It was inferred that the blend of kappa carrageenan and HPMC K 15 M builds the adaptability in the release pattern of the drug. This examination sets up the utilization of simplex centroid structure in the advancement of coasting network tablets with least experimentation.

Design and Optimization of Floating Microspheres Using Abelmoschus esculentus Natural Polymer

The main objective of the present research study was to fabricate Vildagliptin floating microspheres by ionotropic gelation using natural polymer, Abelmoschus esculentus obtained from the fruits of Abelmoschus esculentus in combination with sodium alginate. Microspheres were prepared and optimized using central composite rotatable design model using design expert software version 12 .The study is focussed on the interaction effects of the three independent variables, natural polymer concentration, sodium alginate concentration and crosslinker concentration, optimization of formulations response surface methodology was used . drug –excipient compatibility studies were carried out by infrared spectroscopic studies. Infrared spectroscopic studies clearly shown that drug and excipients were compatible. Totally 15 formulations were generated taking 8 factorial points, 6 axial points and 1 centre point. Response surface methodology was used to optimize the formulations. To investigate the responses %cumulative drug release, floating time and floating lag time Response surface methodology was used Polynomial equations and model plots of 3 dimensional model surface plots were generated. Vildagliptin optimized microspheres were formulated and a second order, model quadratic model was used to study influence of formulation factors on response variables. Experimental data of Statistical analysis exhibited good coefficient of regression for cumulative in vitro drug release Regression F –ratios for the experimental variables were significant. The experimental values and predicted values are agreed. All fifteen formulations exhibited % yield of 94.35-99.99%, particle size of 124-441µm, %swelling index 64.52-89.65%, floating time of 10.16 to 13.16 and floating lag time of 30.31 to 46.98 sec. F4 formulation is optimized based on cumulative % in-vitro drug release at 2nd hour, 12th hour, floating lag time and floating time values. Predicted and observed results are in agreement 95% confidence intervals. Based on investigation, RSM is the good tool for optimization of formulations.

Potential of some Rhizobacteria Isolates Antagonists in Various Formulation to Control Sheat Root Disease (Sarocladium oryzae) on Rice Plants

The reserach aims to determine the potential of antagonistic rhizobacteria and is appropriate formulations used to control sheat root disease (Sarocladium oryzae). This research was carried out in July to December 2019 in the Plant and Disease Laboratory and the Greean House Faculty of Agriculture Jember University. The experiment was conducted using a completely randomized design (CRD) 2 factors, namely isolates and formulation. Isolates factors have 4 factors levels; control, Bacillus sp. isolate, Pseudomonas fluorescens isolate, and Bacillus sp. + Pseudomonas fluorescens isolate. The formulation factors has 4 factors levels; glucose 10% + potato water 70% + bacterial starter 20%, Fructose 20% + coconut water 60% + bacteria; starter 20%, glucose 10% + CMC 2% + monmorilonite 68% + bacterial starter 20%, fructose 20% + CMC 2% + kaolin 58% + bacterial starter 20%. The result showed that the treatment of Bacillus sp. with formulation glucose 10% + CMC 2% + monmorilonite 68% + bacterial starter 20%, showed the best result, with a control effectiveness of 78.31%.Key word; Formulation, Rhizobacteria antagonist, Sarocladium oryzae

Quality-by-design-based engineered liposomal nanomedicines to treat cancer: an in-depth analysis.

Engineered nano-sized liposomes have attained the highest success rate in commercialization among the reported nanomedicines. However, developing industrially acceptable nanoliposomes is still challenging because the process, formulation factors and even their properties may critically influence the desired attributes of the final nanoliposomal product. Implementation of quality-by-design (QbD) in nanoliposomal fabrication has led to revolutionary advancement int better analysis of the interacting factors (drug and lipid ratio, hydration, sonication, etc), which, in turn, leads to better product performance with predefined attributes (entrapment efficiency percentage, drug release time and pattern, vesicles size, polydispersity index, surface chargeand surface morphology). This review provides a summary of decade of researchand an in-depth analysis of QbD-based nanoliposomes developed to address different cancers. The review aims to provide complete details of QbD-inspired nanoliposomal development from process to application.

The development of formulation for curd products based on the methodology of risk qualimetry

The authors suggest a new approach to the development of curd products formulation. The approach is based on the methodology of "risk qualimetry" which uses information-matrix models. Defect names are revealed and ranked by the detection rate, as well as reasons for the complaints about the curd products quality that had been coming from retail chains within 5 years. Moreover, the information-matrix model of the influence of the recipe ingredients on the risks of complaints about the curd product quality was presented. The values of the importance indicators were determined and the formulation factors were ranked: low-fat cottage cheese (185.8 points), a structurant (153.9), a functional ingredient (100.3), sugar syrup (60.0) and cream (54.2). The choice of a functional component and a structure former was substantiated. Those components would not only increase the nutritional value of the product, but also minimize the risks of inconsistencies. The formulation of a new curd product with functional components was developed: fat-free curd (65.0%), cream (24.3%), sugar syrup (8.0%), oats cryopowder (1.2%) and red grapes cryopowder (1.5%). The organoleptic evaluation of the prototype model showed high consumer properties.

Semi-analytical estimation of Helmholtz resonators’ tuning frequency for scalable neck-cavity geometric couplings

Innovative meta-materials offer great flexibility for manipulating sound waves and assure unprecedented functionality in the context of acoustic applications. Indeed, they can exhibit extraordinary properties, such as broadband low-frequency absorption, excellent sound insulation, or enhanced sound transmission. These amazing properties have drawn the eye of the transport industry, especially for aeronautic applications where objects like these can be combined and coupled with primary structures aiming to reduce exterior and interior noise without increasing weight. However, the design of acoustic meta-materials with exciting functionality still represents a challenge, therefore there is a huge interest about the conceptualization and design of innovative acoustic solutions making use of meta-material resonance effects. The main target of the present research work is to obtain an accurate prediction of the tuning frequency of a Helmholtz-resonating device, whose resonance properties are exploited in a wide part of acoustic meta-material design. In this context, an investigation on a correction factor for the classical formulation used to estimate the Helmholtz resonance frequency starting from its geometric characteristics, accounting for different-shaped resonators with varying neck/cavity ratios, is performed. More specifically, a set of numerical simulations for several geometric configuration is considered in order to demonstrate the limits of pre-existing formulas, and a new correction factor formula is developed after theoretical considerations where it is possible. In the end, results in terms of correction factors are provided in both graphical and semi-analytical form, compared with Finite Element data.