Optimum Formula Research Articles

Preparation and performance of 10 wt% of chlorantraniliprole Nano-suspension concentrate (SC) using polyether amine-bridged sulfonated alkali lignin (PSAL) as a dispersant

Polyether amine-bridged sulfonated alkali lignin (PSAL) with different sulfonic group contents and molecular weights was firstly synthesized and characterized. Then, 10 wt% of chlorantraniliprole Nano-suspension concentrate (SC) was prepared by the water-based grinding method, and the optimum grinding parameters were explored and obtained. Based on this optimum grinding formula, chlorantraniliprole Nano-SC was prepared and three optimum dispersants were finally obtained as follows: the compounds of polycarboxylate D-2 separately with P1SAL0.68, P1SAL0.84 and TERSPERSE 2500 at the mass ratio of 1:1. All Nano-SC prepared by these three dispersants had a D90 particle size below 200 nm, suspension percentage above 99%, water separation proportion below 1%, excellent thermal storage stability, and also better wettability on banana leaf surface. Additionally, adding glycerin could effectively inhibit the agglomeration and austenogenization of pesticide nanoparticles, and thus improve the stability of Nano-SC. Finally, the farmland experiments indicated chlorantraniliprole Nano-SC prepared in this work had a significantly improved pesticide effect on first-instar rice leaf rollers than traditional micron-sized SC. This work provided a new dispersant with excellent performance for chlorantraniliprole Nano-SC as well as broadened the high value-added utilization of industrial lignin into pesticide Nano-SC field, which had great economic and environmental benefits.

Enhancing collagen based nanoemulgel for effective topical delivery of Aceclofenac and Citronellol oil: Formulation, optimization, in-vitro evaluation, and in-vivo osteoarthritis study with a focus on HMGB-1/RAGE/NF-κB pathway, Klotho, and miR-499a.

The majority of conventional osteoarthritis (OA) treatments are based on molecular adjustment of certain signaling pathways associated with osteoarthritis (OA) pathogenesis, however there is a significant need to search for more effective and safe treatments. This study centers around formulating Aceclofenac (ACF) with high bioavailability in combination with Citronellol oil and collagen. The optimal concentrations of Citronellol oil/D-Limonene oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were studied for thermophysical stability. Thermodynamically stable formula were analyzed for droplet size, zeta potential, and in-vitro permeation. Then, collagen based nanoemulsion were prepared to capitalize on its efficacy in reducing osteoarthritis side effects and characterized for nano size properties. Formulae F10 and F10C were chosen as optimum nanosize formula. Hense, they were prepared and characterized as nanoemulgel dosage form. The nanoemulgel formulae F10NEG1 and F10CNEG1 showed reasonable viscosity and spreadability, with complete drug release after 4h. These formulae were chosen for further In vivo anti-OA study. Collagen based ACF/citronellol emugel were able to modulate HMGB-1/RAGE/NF-κB pathway, mitigating the production of inflammatory cytokine TNF-α. They were also able to modulate Klotho and miR-499, reducing serum CTXII and COMP, by reducing the cartilage destruction. Histological investigations validated the efficacy, safety, and superiority of Aceclofenac in combination with Citronellol oil and collagen (F10CNEG1) over solo the treated group (F10NEG1 and blank). Hence, the findings of the current work encourage the use of this promising combined formula in treatment of OA patients.

Physical and Chemical Characterization of Granules from 70 % Ethanol Extract of Ganitri Leaves (Eleocarpus serratus L.) using Wet Granulation Method as An Anti-Osteoporosis

Elaeocarpus serratus L. leaves have been used as an antiosteoporosis treatment and it contains active compounds such as quercetin, rutin, and myricetin. The pre-formulation study was done by making granules from 70 % ethanol extract of this plant through the wet granulation method. These granules were determined by physical characteristics including organoleptic, flow properties, real and incompressible specific gravity, moisture, particle size distribution, and chemical characteristics including flavonoid content. The organoleptic result showed that all formulas had a strong characteristic odor and a slightly bitter taste. Formula A had a dark brown color, while formulas B and C were whitish brown. Based on the results of the flow properties test, all formulas had good flow properties because they had gone through the granulation process. The compressibility index, Hausner ratio, and % moisture content displayed that all formulas met the requirements and had almost the same value. In the assay process, the average % w/w content of formula A was 0.68 ± 0.017 %, formula B was 0.66 ± 0.044 %, and formula C was 0.16 ± 0.006 %. The most optimum formula was formula C with whitish brown color, slightly bitter taste, and strong odor, 10.90 ± 0.000 g/s of flow rate, 25.41 ± 0.000 ° of angle, 4.36 ± 0.214 % of moisture content, 13.80 % compressibility index, 1.1601 of Hausner ratio, 1772.04 µm of particle average distribution, and 0.66 ± 0.044 % w/w of percent routine flavonoid content. HIGHLIGHTS   This study aims to determine the characteristics of granules from 70 % ethanol extract of ganitri leaves (Elaeocarpus serratus), the optimal formula to make granule preparations with active ingredients of ganitri leaves, and the levels of flavonoids using the spectrophotometer method. It also determined the characteristic physics of granule preparations including flow properties, organoleptic, moisture, particle size distribution, and real and incompressible specific gravity. GRAPHICAL ABSTRACT

Fabricating pentaazatetraethylene modified sulfonated polyacrylamide for dye adsorption from aqueous media: isotherms and kinetics models.

In this study, pentaazatetraethylene-modified sulfonated polyacrylamide (PAm-SO3-N5) was synthesized and used as a novel efficient adsorbent to remove calmagite from aqueous media. To this end, a central composite design (CCD) was applied to reduce the number of reaction variables (i.e., adsorbent concentration, temperature, initial concentration, and pH) on calmagite removal. The results showed that calmagite was entirely adsorbed by the PAm-SO3-N5 within 30 min. In addition, a pseudo-second-order (PSO) model was prepared as the optimum formula to fit the kinetics information. The modeling results revealed that film diffusion and adsorption are rate-limiting stages to remove the dyes. Using a Langmuir isotherm to fit the equilibrium data, the highest equilibrium adsorption was calculated to be 1732.5 mg/g. In the present study, the ΔH value indicates that the adsorption is of chemical type. Also, the negative sign of ΔS° shows that PAm-SO3-N5 removes calmagite during a relatively stable process with randomness in the system. The increase in ΔG° values with increasing temperature indicates a descending trend in the feasibility degree of calmagite adsorption. Eventually, recycling the adsorbent for 7 cycles to adsorb calmagite dye showed no remarkable activity loss.

Fucoidan-incorporated dissolving microneedles: A novel approach to anticoagulant transdermal delivery

Cardiovascular disease (CVD) is the leading cause of global mortality, particularly in Indonesia. Vascular disorders, including thrombosis and atherosclerosis, have been implicated as potential contributors to the development and progression of CVDs. Anticoagulant agents, such as heparin, have been commonly used to treat vascular disorders. Nevertheless, this agent may result in a hazardous adverse effect. Bioactive substances like fucoidan (FC) have emerged as an alternative, with anticoagulant and antithrombotic properties similar to heparin. However, FC was often found in oral, injectable, and transdermal dosage forms, which has considerable limitations due to its low bioavailability alongside with poor patient comfort and compliance. To overcome these issues, FC was further incorporated into dissolving microneedles (DMN) that can facilitate transdermal delivery of FC by penetrating the stratum corneum. Fucoidan Dissolving Microneedle (FC-DMN) was fabricated using gelatin and polyvinyl pyrrolidone (PVP) as polymers with various concentrations. Following several evaluations, FC-DMN exhibited good stability, mechanical resistance, and penetration ability. Ex vivo permeation study revealed that 91.23 ± 0.12 % of FC was released from the optimum formula. Furthermore, the hemolytic activity demonstrated that FC-DMN did not induce notably hemolytic, confirming its safe applicability. The in vivo anticoagulant activity test showed increased aPTT and PT values following a 7-day regimen of FC-DMN application. Interestingly, there were no significant differences (p > 0.05) were observed between FC-DMN and heparin injection (dosage 200 IU/Kg). In contrast, significant differences (p < 0.05) were observed when comparing FC-DMN to healthy controls, negative controls, and heparin gel. These findings suggested that FC-DMN offers a promising alternative to conventional anticoagulant therapies and can effectively deliver FC into systemic circulation. This study successfully developed a safe, painless, and nonirritating FC-DMN with promising results for enhancing the efficacy of anticoagulant therapy through the transdermal route.

Optimizing Intranasal Amisulpride Loaded Nanostructured Lipid Carriers: Formulation, Development, and Characterization Parameters

Background: Nanostructured lipid carriers (NLCs) are lipid-based nanoparticles composed of a mixture of solid and liquid lipids, which are stabilized by the outer surface of a surfactant. Objective: This research aimed to prepare intranasal nanostructured lipid carriers loaded with amisulpride to enhance its dissolution and bioavailability using different formulation compositions. Methods: Amisulpride nanostructured lipid carriers were formulated using ultra-sonication methods. Solid lipids like stearic acid, palmitic acid, and glyceryl monostearate were used, while liquid lipids like oleic acid, Imwitor 988, and isopropyl myristate were employed. Surfactants used were cremophor®EL, tween 80, and span 20 with different co-surfactants: Transcutol HP, triacetin, and propylene glycol in different ratios. The key metrics used in this study's evaluation were particle size, polydispersity index, zeta potential, entrapment efficiency, and loading efficiency. The formulations with the best characteristics were also subjected to an in-vitro release test. Results: The results showed a significant shift in some evaluation criteria with a non-significant change in other characterizations upon switching between different types and ratios of compositions. A biphasic release pattern was also observed. The optimum formula F19 was found to have 68.309±0.38 nm, 0.2408±0.004, -20.64±0.11 mV, 95.75±0.26 and 18.07±0.36, respectively. It was safe on the sheep nasal membrane. result: The results showed a significant shift in some evaluations criteria with a non-significant change in other characterizations upon switching between different types and ratios of compositions. A biphasic release pattern was also observed. The optimum formula F19 was found to have 68.309±0.38 nm, 0.204±0.004, -20.64±0.11, 95.75±0.26 and 18.07±0.36, respectively. It was safe on the sheep nasal membrane. Conclusion: The right combination of the formulation compositions based on studying the effect of each factor on the main formulation characteristics can serve as the basis for a successful intranasal amisulpride-loaded nanostructured lipid carrier.

LIQUID SOAP FORMULATION FROM ETHANOLIC EXTRACT OF CASSAVA LEAVES (Manihot esculenta Crantz) WITH COCAMIDE DEA AS SURFACTANT

The ethanol extract of cassava leaves contains various secondary metabolites that have antibacterial activity against Escherichia coli, Staphylococcus aureus, and Shigella sp., and thus can be used as active ingredients in liquid soap preparation. Liquid soap formulations generally use sodium lauryl sulfate (SLS) as a surfactant, which can cause irritation and skin dryness. This study aimed to formulate an ethanol extract from cassava leaves into a liquid soap preparation using cocamide DEA as a surfactant to reduce skin irritation. The study was conducted in an experimental laboratory. Cassava leaves were extracted by maceration using ethanol. Three liquid soap formulas from cassava leaf extract were developed with different extract concentrations: F1 (1%), F2 (3%), and F3 (5%). The liquid soaps were evaluated in terms of organoleptic properties, pH, homogeneity, viscosity, foam height, and foam stability. The study showed that cassava leaves extract could be formulated into a homogeneous liquid soap with a pH range of 7.0–7.5, viscosity of 143.6–306.2 cps, foam height of 53.33–60.00 mm, and foam stability of 75.01–82.36%. F3 is the optimum formula with the best physical characteristics of the preparation in terms of organoleptic properties, foam height, and foam stability. Keywords: cocamide DEA, cassava leaves, liquid soap, surfactant

Optimization of Hydroxypropyl Methylcellulose (HPMC) and Carbopol 940 in Clindamycin HCl Ethosomal Gel as Anti-acne

Clindamycin HCl has anti-acne properties because it can inhibit the growth of Propionibacterium acnes (P. acnes) bacteria. However, the bioavailability of clindamycin HCl is less than 13% of the given dose, so it needs to be developed in the form of ethosomes to increase its bioavailability. This study aimed to create a clindamycin HCl ethosomal gel preparation with varying hydroxypropyl methylcellulose (HPMC) and carbopol-940 as a gelling agent using a factorial design to obtain 4 formulas. The concentrations of HPMC and carbopol 940 used were 0.5% and 1%. The optimum formula was determined based on the pH response, viscosity, spreadability, and adhesion of the clindamycin HCl ethosomal gel preparation. Based on the factorial design analysis, HPMC and Carbopol-940 have an influence on the pH response and adhesion, while the interaction between HPMC and Carbopol-940 influences the spreadability and viscosity responses. The optimum formula was obtained with a desirability value of 0.994 at a concentration of HPMC was 1%, and Carbopol 940 was 0.5%. The minimum inhibitory concentration of the optimum clindamycin HCl ethosomal gel was 60 µg/mL. So, the clindamycin HCl ethosomal gel had a strong antibacterial activity.

Pharmacodynamic Studies of Pravastatin Sodium Nanoemulsion Loaded Transdermal Patch for Treatment of Hyperlipidemia

Pravastatin sodium (PVS) is a hypolipidemic drug with poor oral bioavailability due to the first-pass effect. Therefore, this study aims to formulate and evaluate transdermal patches containing PVS-loaded nanoemulsions (PVS-NEs) to increase PVS’s hypolipidemic and hepatoprotective activities. PVS-NEs were prepared using the aqueous titration method, where oleic acid was chosen as an oil phase, and span 80 and tween 80 were used as surfactant and cosurfactant respectively. Droplet size (DS), polydispersity index (PDI), zeta potential (ZP), clarity, and thermodynamic stability of NEs were all characterized. Also, PVS-NEs (NE2) with 50% oil phase, 40% SC mix 2:1, and 10% water were selected as an optimum formula based on the results of DS (251 ± 16), PDI (0.4 ± 0.16), and ZP (-70 ± 10.4) to be incorporated into a transdermal patch, and PVS-NE2 loaded transdermal patches (PVS-NE2-TDPs) were prepared by solvent evaporation method. F1 patch with HPMC E15 and PVP K30 in a ratio of 3:1 represented satisfactory patch properties with good drug-excipients compatibility. Thus, it was selected as an optimum patch formula. The optimized F1 patch was characterized for thickness, moisture content, weight variation, and drug-excipients incompatibility. Therefore, it was subjected to ex vivo skin permeation and finally pharmacodynamic studies. Ex vivo permeation studies of F1 revealed that the cumulative amount of PVS permeated across rat skin was 271.66 ± 19 µg/cm2 in 72 h, and the pharmacodynamic studies demonstrated that the F1 patch was more effective in treating hyperlipidemia than PVS-TDP (control patch) based on both blood analysis and histopathological examination. Graphical

Capped flexosomes for prominent anti-inflammatory activity: development, optimization, and ex vivo and in vivo assessments.

This study aimed to formulate diacerein (DCN)-loaded flexosomes for enhanced efficacy against osteoarthritis. A 23 D-optimal design was employed, investigating the impact of surfactant type (A), surfactant concentration (%w/v) (B), and oleylamine amount (mg) (C). Flexosomes were formulated using a rotary evaporator, and Design-Expert® software was utilized to statistically analyze entrapment efficiency (EE%), zeta potential (ZP), poly-dispersity index (PDI), and particle size (PS) to determine the optimum formula. The selection criteria prioritized increased ZP (as absolute value) and EE%, coupled with decreased PDI and PS. Rigorous physicochemical, in vivo, and ex vivo tests were conducted to validate the safety, stability, and activity of the optimal formula. Physicochemical assessments encompassed pH measurement, transmission electron microscopy, differential scanning calorimetry, release profiles, storage effects, and Fourier transform infrared spectroscopy. In vivo tests included permeation studies, histopathology, anti-inflammatory activity, and skin irritancy, while ex vivo tests focused on permeation parameters and skin deposition. The optimum formula demonstrated high desirability (0.931), along with favorable EE% (90.93%), ZP (- 40.4mV), particle size (188.55nm), and sustained behavior. Notably, improved in vivo permeation (132µm), skin deposition (193.43µg/cm2), and antinociceptive activity (66%) compared to DCN suspension (48µm, 66.31µg/cm2, and 26%, respectively) were observed. The optimal formula also exhibited excellent safety and storage characteristics. In conclusion, DCN-loaded flexosomes exhibit significant potential for effectively managing osteoarthritis.

FORMULATION AND PHYSICAL PROPERTIES TESTS OF FACIAL WASH FROM OLIVE OIL AND NIACINAMIDE

&lt;p class="MsoNormal" style="margin: 0in; margin-bottom: .0001pt; text-align: justify; text-indent: -.1pt; line-height: normal;"&gt;&lt;span style="font-size: 11.0pt; font-family: 'Calibri','sans-serif'; mso-fareast-font-family: Calibri;" lang="IN"&gt;Problems on facial skin that often occur are caused by free radicals. Free radicals can cause cell damage in the form of premature aging which is characterized by a lack of elasticity in the skin, black spots appear, skin looks duller and there is pigmentation. Free radicals can be counteracted by giving antioxidants. Antioxidants are molecular compounds that can release electrons and neutralize free radicals in order to prevent cell damage. One of the natural ingredients that can be used to treat premature aging is olive oil. Olive oil is believed to help maintain skin moisture and elasticity as well as expedite the skin regeneration process, so that the skin is not easily dry and wrinkled. The aim of the research was to determine the results of the physical properties test of olive oil and niacinamide facial wash preparations and to determine the right and optimum formula for the surfactant combination of sodium lauryl sulfate (SLS) and cocamidopropyl betaine. The type of research used is laboratory experimental with the Simplex Lattice Design (SLD) method. According to the results of the physical properties of the 8 formulas, the facial wash preparations met the physical properties tests such as organoleptic, homogeneity, pH, foam stability, spreadability and viscosity which met the requirements according to SNI. Olive oil and niacinamide facial wash preparations have an optimum formula at a concentration of 0.75% SLS and 0.25% cocamidopropyl betaine.&lt;/span&gt;&lt;/p&gt;&lt;em&gt;&lt;span style="font-size: 11.0pt; line-height: 115%; font-family: 'Calibri','sans-serif'; mso-fareast-font-family: Calibri; position: relative; top: .5pt; mso-text-raise: -.5pt; mso-ansi-language: IN; mso-fareast-language: EN-US; mso-bidi-language: AR-SA;" lang="IN"&gt;Facial Washes; olive oil; Niacinamide&lt;/span&gt;&lt;/em&gt;

Utilization of composite flour (red bean, catfish, oyster mushroom and tempeh formula flour) in making cookies

Local food ingredients can be used as alternative ingredients for cookie products to help ending hunger and overcome malnutrition are the objectives of SDG 2 and 3. This study aims to obtain the optimum cookie formula using composite flour from local food ingredients consisting of red bean flour, catfish flour, oyster mushrooms flour, and tempeh formula flour using the design expert program v.13 Response Surface Methodology (RSM) Box Behnken Design/BBD. Independent variables are different levels of red bean flour (20-45 g), catfish flour (10-45 g), oyster mushroom flour (5-25 g), and tempeh formula flour (5-35 g) with 29 (twenty-nine) different runs of 4 (four) similar center points. Using goal settings for each response based on proximate composition achieved from the best definition of each response to achieve high-quality cookies, an optimum formulation of cookies was obtained at 44.21% red bean flour, 34.39% catfish flour, 7.46% oyster mushroom flour, and 20.52% tempeh formula flour, with a desirability level of 1.00.

Screening of Antagonistic Bacillus against Brown Rot in Dendrocalamus latiflorus and Preparation of Applying Bacterial Suspension.

The aim of this study was to isolate biocontrol bacteria that could antagonize brown rot of Dendrocalamus latiflorus, optimize the culture conditions, and develop an effective biocontrol preparation for brown rot of D. latiflorus. This study isolated a bacterium with an antagonistic effect on bamboo brown rot from healthy D. latiflorus rhizosphere soil. Morphology, molecular biology, and physiological biochemistry methods identified it as Bacillus siamensis. The following culturing media and conditions improved the inhibition effect of B. siamensis: the best culturing media were 2% sucrose, 1.5% yeast extract, and 0.7% potassium chloride; the optimal culturing time, temperature, pH, and inoculation amount were 48 h, 30℃, 6, and 20%. The optimum formula of the applying bacterial suspension was 14% sodium dodecyl benzene sulfonate emulsifier, 4% Na2HPO4·2H2O, 0.3% hydroxypropyl methylcellulose thickener, and 20% B. siamensis. The pot experiment results showed the control effect of applying bacterial suspension, diluted 1,000 times is still better than that of 24% fenbuconazole suspension. The applying bacterial suspension enables reliable control of brown rot in D. latiflorus.

INKORPORASI MIKROEMULSI EKSTRAK ETANOL AKAR KELAKAI (Stenochlaena Palustris (Burn. F) Bedd.) PADA FORMULASI TONER WAJAH DENGAN VARIASI KONSENTRASI GLISERIN

The face is one part of the human body that needs to be kept healthy and clean. Efforts can be made to maintain facial cleanliness by using facial toner. The extract of kelakai root has activity as an antioxidant. Incorporation of kelakai root extract microemulsion in the toner formulation will increase the cleaning ability and optimal absorption of active substances. This research aims to obtain an optimum face toner formula. The kelakai roots were macerated with 70% ethanol solvent. The kelakai microemulsion consisted of Tween 80 35% w/v and PEG 400 15% w/v. Incorporation of 2% w/v microemulsion into the toner formula with varying glycerin concentrations of 2%, 3%, 4%, and 5% w/v. Evaluation through stability tests with organoleptic, homogeneity, pH, viscosity, clarity, and density. Organoleptic, homogeneity, and clarity before and after the stability test provide a liquid form, odorless, clear, and homogeneous color. In the pH test, the pH value of the preparation was stable in the pH range of 4.5-6.5. The viscosity of toner preparations is in a range of 1-24.5 cPs. The density stability with a range of 1.003-1.015 gr/mL. The optimum formula, namely F2 with 3% glycerin, provides good toner stability based on physical quality tests.

OPTIMIZATION OF DICLOFENAC POTASSIUM TRANSDERMAL PATCH FORMULA USING A COMBINATION OF POLYVYNIL PYRROLIDONE K 30, ETHYL CELLULOSE AND MENTHOL WITH SIMPLEX LATTICE DESIGN METHOD

Diclofenac potassium is one of the NSAID drugs which can cause gastrointestinal irritation and damage to the small intestinal mucosa including erosion and ulceration. The purpose of this study was to determine the effect of the combination of PVP K 30, ethyl cellulose and menthol on organoleptic, thickness, weight uniformity, moisture and folding resistance of diclofenac potassium transdermal patch.This research is an experimental study that includes an experiment to optimize the formulation of a transdermal patch preparation with the active ingredient potassium diclofenac and a combination of PVP K 30, ethyl cellulose and menthol. The optimization method uses the simplex lattice design method. There are 13 formula designs consisting of a combination of PVP K 30, ethyl cellulose and menthol. Each formula was tested for organoleptic, thickness, weight uniformity, moisture and folding resistance. Then the optimum formula was determined and analyzed using the simplex lattice design method. The combination of PVP K 30, ethyl cellulose and menthol with a simplex lattice design has an effect on the transdermal patch of diclofenac potassium which increases the consistency of the patch surface, reduces the thickness directly proportional to the weight of the patch and increases folding resistance. The proportion of PVP K 30, ethyl cellulose and menthol that can produce the optimum formula for diclofenac potassium transdermal patches with the simplex lattice design on the critical parameters of thickness, moisture, folding resistance and penetration tests, namely PVP K 30 of 14.87%, ethyl cellulose of 10.00% and 5.13% menthol.

The Effect of Diet Consistency on the Craniofacial Morphology: A review Article.

Mastication is a chewing route, that implicates a group of muscles that are responsible for moving the mandible condyle in the temporomandibular joint (TMJ) to chore food between the teeth in the maxillary and mandibular arches (1) .Regarding the growth of the craniofacial system (CFS),there are an agreement which is strongminded via genetic and ecological aspects (2) . Masticatory forces considered as one of the chief environmental incentives that produce craniofacial difference amongst modern humans. New researeches on a broad variety of creatures, counting those having retro-gnathic post canine teeth, expect that retorts to the force of mastication that determined the superior in the occlusal plane (3) . The effect of masticatory stroke induced by the muscles of the mastication on the development of the morphology of craniofacial portion, has established significant attention in the recent oral invistigations (4) . Meanwhile the skeletal of the CFS adapts to the applied loads by bone remodeling in order to get the optimum formula to resist loads according to Wollf ’s law (5) . CFS has been assumed that it formula is mainly resolute by loading induced by mucsles of mastication. This has been reinforced by numerous clinical and experimental readings (6-9) . Investigational studies displayed that the reduced stresses induced by function on the animals mandibles, whose nourished a lenient diet outcomes in organizational variations in their masticatory systems (10) , in addition to morphological modifications of the lower jaw, like diminished of the alveolar bone size (11, 12) .Diet could be considered as a element of masticatory magnitude. Recent humans in developed countries eat an additional treated and softer diet rather than old humans. The change from hard to soft nourishment has been join by reduce in mandibular dimension and the growth of the alveolar bone, along with enlarged occurrence of malocclusion (1,5,7).

FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES FROM ELEUTHERINE BULBOSA URB. BULB EXTRACT WITH PLASTICIZER VARIATIONS

Objective: This research aimed to develop a transdermal drug delivery system from Eleutherine bulbosa Urb. bulbs as an alternative treatment with minimum side effects compared to other pain medications and increased drug penetration by determining the optimum formula(s) for transdermal patches prepared with varying plasticizer concentrations. Methods: Eleutherine bulbosa Urb. bulbs were extracted by maceration using 96% ethanol. The extract was formed into transdermal patches using the solvent casting method with six formulations (F1-F6) and different types and concentrations of the plasticizer: polyethylene glycol (PEG) 400 or dibutyl phthalate. The derived patches were then evaluated for their organoleptic properties, homogeneity, weight uniformity, thickness, folding endurance, pH level, moisture content, and acceptability (hedonic scale). Results: The evaluation of the physical properties found that all patches were dark brown, opaque, smooth-textured, and had a typical odor of the bulb’s ethanol extract and uniform weight and thickness. Other characteristics included pH ranging from 5.0±0.00 to 5.86±0.04 and a moisture content between 1.04±0.04% and 4.13±0.08%. In addition, the folding endurance was 267 times for F1 and &gt;300 times for F2-F6. The acceptability test using the five-point hedonic scale showed different preferences for these formulas. Conclusion: F6 is the optimum formula for producing transdermal patches with excellent physical properties.

IMPROVED SOLUBILITY OF CHOLECALCIFEROL AS BOVINE SERUM ALBUMIN (BSA) NANOPARTICLES

Objective: This study aims to report the optimum formula for BSA nanoparticles cholecalciferol (BSA-NP cholecalciferol), which can increase the solubility of cholecalciferol.Methods: BSA cholecalciferol nanoparticles was prepared by desolvation method with variations in solvent/non-solvent ratio, BSA concentration, pH of BSA solution, and cholecalciferol concentration. For this purpose, particle size, polydispersity index, and zeta potential were measured. Furthermore, the solubility test of the best BSA-NPs cholecalciferol formula was carried out.Results: The most optimal BSA nanoparticle cholecalciferol characterization results have a particle size of 166.6±50.3 nm, a zeta potential of-32.1 mV, and a percentage encapsulation efficiency (%EE) for cholecalciferol of 82.9±0.72%. The solubility of BSA-NP cholecalciferol is four times higher than that of pure cholecalciferol.Conclusion: The optimum formula for BSA-NP cholecalciferol with a solvent/non-solvent ratio of 1/2, a concentration of BSA of 2.5%, a BSA solution pH 6, and a cholecalciferol concentration of 0.1% will increase the solubility of cholecalciferol by four times compared to pure cholecalciferol.

Preparation, In-vitro, Ex-vivo, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based In Situ Gel.

Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%. This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits. Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by L. Santosh Kumar. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5. The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066±242 ng/ml, 0.75±0.05 h, 19616.86±589 ng. h/ml, and 7975.67±239 ng/ml, 1.0±0.05 h, 17912.36±537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09±125 ng/ml, 2±0.2 h, and 8852.27±266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p<0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one to be selected as the optimum formula. NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula that will be ready for further clinical study is NEIG 2.

Formulation, Nutritional and Sensory Evaluation of Mocaf (Modified Cassava Flour) Noodles with Latoh (Caulerpa lentillifera) Addition

Instant noodles gained widespread popularity, resulting in a surge in global wheat consumption. However, concerns about the health implications of wheat-based products spurred the need for alternative ingredients in noodle production. The substitution of wheat flour with local resources, such as mocaf flour, and the enrichment of noodles with latoh (Caulerpa lentillifera), provided an opportunity to reduce wheat imports while enhancing the quality and potential health benefits of noodles. This study aimed to determine the optimal formulation, assess the characteristics, and evaluate the functional properties of wheat noodles that were substituted with mocaf flour and supplemented with latoh. The formulation of these noodles was conducted using design expert. The research encompassed a comprehensive analysis of physical, chemical, and organoleptic properties. The presence of latoh, in terms of chemical characteristics, increased the water and protein content in the noodles. On the physical side, it increased the final viscosity, setback, peak time, and elongation, as well as reduced the peak viscosity and breakdown. Meanwhile, the presence of mocaf increased carbohydrate content, peak viscosity, and breakdown value. The variations in noodle formulas only affected consumer acceptance of the appearance of the noodles; the noodle formula 99:1 (Mocaf:Latoh) had the most preferred appearance. Based on the sensory test parameters, the elongation value, and the tensile strength, noodles with optimal formulas were obtained, namely mocaf 63%, wheat 36% and latoh 1%. The optimum formula was similar to sample 10 (60:39:1) which exhibited characteristics such as a bright color, a rather smooth appearance with no cracks, a very soft mouthfeel, a bit springiness and elasticity, and a slightly non-sticky texture to the teeth without a fishy aroma. The essential and non-essential amino acids with the highest concentration contained in the Mocaf Noodles’ optimum formula were glutamate and leucine. Mocaf noodles with added latoh had low fat content but high carbohydrates and were rich in essential amino acids compared to other noodles. Additionally, they possessed sensory characteristics that were deemed acceptable by the panelists.