Pseudo-ternary Phase Diagrams Research Articles

Study the Effective Role of Metronidazole Nanoemulsion for the Treatment of Skin Lesions in Mice Induced by Entamoeba Histolytica

The current study aimed to create a metronidazole nanoemulsion and then use it in the treatment of skin lesions in mice caused by Entamoeba histolytica. We used parasite isolates which taken from the Department of Biology, College of Science, University of Kirkuk. It was rediagnosed by conventional methods. After prepared metronidazole nanoemulsion. We selected 24 healthy males Mus musculus with an average weight of 20-25 grams mice aged 9-12 weeks from, the animals were randomly divided into four groups, with six animals in each group, as follows Control group which injected with normal saline in a volume of 0.1 ml. The second group was injected with a suspension of E. histolytica in a volume of 0.1 ml and at a concentration of 1 x 108 CFU. The third group was injected with Mt-nanoemulsion 0.1 ml. The fourth group was injected with a suspension of E. histolytica and treated with Mt-nanoemulsion. The solubility investigation was conducted using a variety of vehicles to determine the optimal solvent for isradipine's dissolution. Pseudo ternary phase diagrams are created at surfactant and co-surfactant mix related ratios of (1:1, 1:2, 1:3, 1:4, and 2:1). Eight nano emulsions were created by combining several amounts of (Transcutol, Tween20, and Triacetin). The findings indicated that Triacetin was included in the formulations to preserve the medication in a solubilized state and prevent precipitation of the drug because Triacetin had a better solubility of metronidazole. The results of the in vitro study showed that the levels of Malondialdehyde were substantially greater (P >0.05) in the E. histolytica group than in the normal mouse group. Glutathione and catalase levels in the E. histolytica group were substantially lower (P>0.05) than those of normal mice. MDA, GSH, and catalase levels did not differ significantly between the Mt-nanoemulsion-treated group and the control group (P<0.05).

The construction and mechanisms of a O/W microemulsion acid blockage remover system for low permeability reservoirs

Segmental injection as well as high corrosion of the conventional matrix acidizing treatment is harmful to the environment. In this work, a new O/W microemulsion acid (MEA) blockage removal system was developed combining slow-release acid and microemulsion to address these problems. This system could further reduce corrosion, showed great blockage removing ability, and be injected uniformly. HLB and pseudo-ternary phase diagram methods were used to optimize the components of the MEA system and lab tests were used to measure its effective performances and mechanisms. The results indicated 1.5 wt% D-limonene, 0.9 wt% Sodium dodecyl sulfate (SDS), 0.6 wt% JFC, 3.5 wt% N-butanol and 30 wt% slow-release acid was the ideal formulation for the MEA system. The MEA system outperformed the traditional toluene-mud acid system in laboratory settings, with blockage removing efficiency exceeding 8%, and its corrosion rate was just 6.34% of pure mud acid. The blockage removal mechanisms for the MEA system were the synergistic effects of the dilution modification effects of the light oil phase, the emulsification carrying effect of the emulsifiers and slow-release acidification effects of the acid system.

Spinel-trirutile microwave dielectric ceramics with high Q and excellent temperature stability based on MgO-Al2O3-Ta2O5 ternary systems

(1-x)MgAl2O4-xMgTa2O6 composite ceramics based on the MgO-Al2O3-Ta2O5 pseudoternary phase diagram were prepared by the solid-state reaction. MgAl2O4 and MgTa2O6 could coexist due to their different crystal structures. MgAl2O4 inhibited the rapid growth of MgTa2O6 grains, and dense microstructures (ρ > 95%) with a uniform grain size distribution was obtained, with an optimal densification temperature of 1550 - 1575 °C. The temperature coefficient of resonant frequency (τf) and quality factor (Q×f) were optimized by introducing MgTa2O6 phases with low dielectric loss and positive τf. In addition, the partial solid solutions of Al3+ into Ta5+ sites resulted in loosening bonds within [Al/TaO6] octahedra and abnormally large polarizabilities, which was confirmed by the decrease in VTa-O and the redshift of A1 g(Ta-O) mode. Consequently, the relative permittivity (εr) and τf values of MgAl2O4-MgTa2O6 composite ceramics were further enhanced, exceeding the predicted ones. The 0.6MgAl2O4-0.4MgTa2O6 composition sintered at 1550 °C achieved excellent performance, with a near-zero τf value of 3.3 ± 1.7 ppm/°C, a low εr of 16.4 ± 0.3 and an ultra-high Q×f of 179,000 ± 6700 GHz @ 8.94 ± 0.04 GHz. These findings hold promising applications in the field of 5 G/6 G high-frequency communication.

Formulation of Itraconazole Loaded Clove Oil based Nanoemulsion using Pseudoternary Phase Diagram for Improved Thermodynamic Stability

Formulation of Itraconazole Loaded Clove Oil based Nanoemulsion using Pseudoternary Phase Diagram for Improved Thermodynamic Stability

Formulation And Evaluation of Diclofenac Sodium-Loaded Self-Microemulsifying Gel for Enhanced Topical Drug Delivery

Objective: This study aimed to develop a topical gel formulation of diclofenac sodium (DFS) utilizing a self-micro emulsifying drug delivery system (SMEDDS) to enhance solubility, bioavailability, and patient compliance while minimizing systemic side effects associated with oral administration. Methods: DFS solubility was evaluated in various oils, surfactants, and co-surfactants. A pseudo-ternary phase diagram guided the selection of optimal SMEDDS components. The SMEDDS formulation, comprising cinnamon oil, Tween 20, and propylene glycol, was converted into a gel using Carbopol 940. Both the liquid SMEDDS and gel underwent extensive physicochemical characterization, including drug content, pH, viscosity, spreadability, and in vitro/ex vivo diffusion studies. Key Findings: Cinnamon oil, Tween 20, and propylene glycol exhibited the highest DFS solubility and emulsification efficiency. The optimized SMEDDS formulation showed robust stability, rapid self-emulsification, high drug loading, and favorable droplet size (112.8 nm) and zeta potential (-11.36 mV). The gel demonstrated consistent drug release (79.70% over 1440 minutes) and improved skin permeation (71.30% over 1440 minutes). Conclusions: The DFS-loaded SMEDDS gel formulation significantly enhances the solubility, dissolution, and topical bioavailability of DFS, providing a promising alternative for managing arthritic pain and inflammation with reduced systemic side effects.

다공성의 콜로이드성 이산화규소를 이용한 닐로티닙 함유 고형의 자가미세유화 약물전달시스템의 개발

The objective of this study was to develop a novel nilotinib HCl-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) formulation with enhanced solubility and dissolution rate. Various oils and surfactants were screened, resulting in the selection of Peceol (oil) and Tween 80 (surfactant) and Transcutol P (co-surfactant). Pseudoternary phase diagram was constructed to detect the nanoemulsion zone. Among the SNEDDS formulations tested, the SNEDDS consisting of Peceol (oil), Tween 80 (surfactant), and Transcutol P (co-surfactant) at a weight ratio of 30/50/20 produced an emulsion droplet size of 182.1±1.0 nm. The spray drying technique, using mesoporous silicon dioxide as an inert carrier, was employed to solidify the selected nilotinib HCl-loaded SNEDDS. The resulting nilotinib HCl-loaded solid SNEDDS (S-SNEDDS) was characterized by scanning electron microscopy (SEM), powder X-ray diffractometry (PXRD), dynamic light scattering, saturation solubility and in vitro dissolution study. The S-SNEDDS produced an emulsion droplet size of 185.2±0.9 nm and there was no change in emulsion particle size upon the addition of drug. SEM and PXRD results suggested that nilotinib HCl existed in an amorphous form in nilotinib HCl-loaded S-SNEDDS. Solubility tests across various pH levels showed a significant improvement in nilotinib HCl solubility. Similarly, dissolution tests demonstrated enhanced dissolution rates in all tested solutions, consistent with the solubility results. These results indicate that the employed methodologies were effective in increasing both the solubility and dissolution rates of nilotinib HCl across different pH environments, suggesting a successful enhancement of its bioavailability.

Formulation and Evaluation of Minoxidil Loaded Submicron Emulsion Based Topical Gel for Treatment of Alopecia

Introduction: Alopecia is a benign hair condition that causes reduced hair growth on the scalp and has afflicted populations worldwide. Aim: The present study is designed to formulate and characterize submicron emulsion-based topical gel containing an anti-hypertensive drug like minoxidil to overcome the adverse effects of conventional oral dosage forms & to provide an improved, targetted therapy for the treatment of alopecia. Methods: The minoxidil-loaded submicron emulsion was prepared by aqueous titration method using a suitable combination of Clove oil (oil phase), Tween 20 (surfactant), and Transcutol P (co-surfactant). Results: The maximum submicron emulsion area obtained after constructing pseudo-ternary phase diagrams was found in S\(_{\text{mix}}\) ratio 4:1. The optimized submicron emulsion formulation (M5) exhibited a pH of 5.4 \(\pm\) 0.17, in vitro release of 95.08 \(\pm\) 0.36%, ex vivo permeation of 79.36 \(\pm\) 0.18%, the particle size of 181.3nm with an uniform particle size distribution \((<1)\) and optimum zeta potential (-8.80 mV). The optimized formulation (M5) was then converted to intogel formulation by adding different concentrations (1%, 1.5%, and 2% w/v) of gelling agents like Carbopol 934. Among them, M5\(_{2 w/v}\) was considered to be the optimized gel formulation based on different evaluation studies. The optimized submicron emulsion-based gel formulation also showed an inherited anti-oxidant potential and remained stable for three months at \(4^{\circ}\). Conclusion: The minoxidil-loaded submicron emulsion-based topical gel formulation could be considered a beneficial nano-approach in contrast to other traditional topical dosage forms for treating alopecia.

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from biopharmaceutics classification system (BCS) class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability. Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections. Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study. Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity. Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.

Microemulgel-based Hydrogel of Diclofenac Sodium using Lipidium sativum as a Gelling Agent

Aim was to prepare hydrogel containing diclofenac sodium using Lipidium sativum as a gelling agent within a micro emulsion-based system. The oil phase consisted of soybean oil, while surfactants, namely Span 80 and Tween 20, were employed in the formulation. Absolute ethanol was used as a co-surfactant and were characterized by a phase diagram. The in-vitro permeation information is derived from the Franz diffusion. Different microemulsion was designed by screening of various components by performing pseudo-ternary phase diagram and then a solubility study. From this psudo-ternary phase diagram was constructed. In-vitro permeation data was screened from these results the topical delivery of diclofenac sodium microemulsion was clearly confirmed as being by means of w/o microemulsion systems. The optimized formulation of the microemulsion consist of soya bean oil 1.25 mL, span:Tween 20 : 2.5 mL, ethanol 1-mL, water 0.2 mL, L. sativum mucilage and it is compared with the marketed preparation. So, the micro emulsion-based hydrogel of diclofenac using L. sativum mucilage can be used as a gelling agent for a topical drug delivery system.

Development of microemulgel formulations with varied permeation enhancers for transungual delivery of luliconazole in onychomycosis management

Luliconazole-loaded microemulgels containing different permeation enhancers were formulated for transungual drug delivery for the management of onychomycosis, onychomycosis, which affects nails. The physicochemical properties like droplet size, zeta potential, pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, and microscopic study were evaluated. The Pseudo-ternary phase diagram was constructed for the formulation of microemulsions (MEs) by keeping the Km ratio constant at 3:1 and characterized for clarity, mean droplet size, zeta potential, viscosity, pH, transmittance, refractive index, and stability. The ME mean droplet size and zeta potential were found in the range of 38.78 to 171.4 nm, and 0.00 to − 6.6 mV, respectively. Prepared MEs were converted into microemulgel by adding a 2.5% gelling agent (Carbapol 934) in the external phase, and a drug release study was conducted. Formulation E3 showed better drug release and was chosen as the control. Four different penetration enhancers were added separately within E3 and further evaluated for pH, viscosity, spreadability, extrudability, oil binding capacity, drug content, microscopic study, Compatibility study, XRD, and DSC. A favorable docking score was observed between luliconazole and Lanosterol 14-alpha-demethylase. In-vitro cumulative drug release at the end of 24 h from E3-SS, containing sodium sulfide as a penetration enhancer, was found to be 94.70% and was 2 times more than the control formulation. Ex-vivo transungual permeation studies through cutting nail clippings were found to be in the range of 28.18 - 36.52 µg/mm2. The microemulgels tagged as E3, E3-SS, and E3-SL showed a significant zone of inhibition against Candida albicans and Aspergillus fumigatus as compared to the marketed formulation.

Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions

This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram and Box-Behnken design successively. MTGME was characterized by dynamic laser light scattering (DLS), zeta potential and transmission electron microscopy (TEM), moreover, the storage stability, pharmacodynamics and pharmacokinetics were investigated. The optimal prescription for MTGME consisted of Maisine 35–1 (oil), Cremophor EL (surfactant) and propylene glycol (PG, cosurfactant). MTGME with a spherical dimension of 58.1 ± 5.86 nm was stable when stored at 4 °C for 3 months. The blood glucose levers (BGL) of diabetic mice were uniformly and significantly decreased by intragastric (i.g.) administration of 1–4 mg/kg MTGME, in which BGL (i.g. 4 mg/kg MTGME) was reduced by 69% during 24 h. The pharmacokinetics study of MTGME (i.g., 20 mg/kg) in Wistar rats showed higher plasma drug concentration (Cmax, 2.9 folds), larger area under curve (AUC, 4.6 folds) and oral bioavailability than those of MTG suspensions. Generally, the MTGME (o/w) showed good effect on controlling hyperglycemia. Therefore, microemulsion can be used as an effective oral drug delivery system to improve the bioavailability of MTG.

Itraconazole Self-Nano Emusifying Drug Delivery System for Enhancement of Solubility

The main objective of formulation is to enhance the bioavailability of the drug within the body. Some of the challenging subjects associated with poorly water-soluble drugs concern solubility and bioavailability factors. To overcome these problems, new technologies, such as lipid-based drug delivery systems including micro or nano emulsifying drug delivery system, have obtained importance in recent years, due to their enhanced solubility and bioavailability in the gastrointestinal tract. Such systems are solubilized within the lipid excipients or mixed with oils or surfactants/co-solvents to facilitate the solubility and absorption rate, which can enhance the bioavailability of the targeted drug. The research was targeted to develop a self-Nano Emulsifying drug delivery system (SNEDDS) for oral bioavailability enhancement of BCS II antifungal drug Itraconazole. Nano Emulsions are consignment methods that improve the solubility and distribution of lipid medicines to the intended areas. SNEDDS of Itraconazole were developed using Castor oil, Tween 20 as surfactant and PEG 200 as co-surfactant. SNEDDS formulation can be obtained through phase diagram approach. Pseudo Ternary phase diagrams were constructed, using Chemix software, to optimize the concentrations of excipients. Thermodynamic stability studies were satisfactory. Robustness to dilution did not exhibit phase separation and drug precipitation. The Among 4 formulations, B1F3 formulation showed more than 95% of drug content and were considered superior and subjected to droplet size analysis and zeta potential measurement. Droplet size ranged from 120 nm to 505 nm. The Nano size was obtained for formulation. The zeta-potential results indicated the range -35 mV. Based on all evaluation tests, formulation B2F3 was chosen as the best. Thus, this self-Nano Emulsifying drug delivery system should be an effective oral dosage form for improving oral bioavailability of lipophilic drug Itraconazole.

Design, optimization, and evaluation for a long-time-released transdermal microneedle delivery system containing estradiol.

Transdermal drug delivery systems (TDDS) have drawbacks such as poor absorption, low blood concentration, and delayed effects. Dissolving microneedle has sharp tips and short length, which overcome patients' pain and improve transdermal efficiency but has low mechanical strength and drug loading capacity. This study thereby proposes a microemulsion-encapsulated and long-time-released transdermal microneedle (MN) delivery system with estradiol (Es) as the model drug. The microemulsion (ME) was optimized by utilizing the pseudo-ternary phase diagram and D-optimal mixture design. The estradiol microemulsion-encapsulated microneedle (Es-ME-MN) was optimized by Box-Behnken design and prepared by freeze-thaw method. The Es-ME-MN obtained was characterized and evaluated through a large variety of studies. Es-ME-MN had sufficient mechanical strength to pierce skin and was safe enough, the length of which was 600 μm, and the Es content was 177.12 ± 0.72 μg/patch without drug-excipient chemical interaction. In vitro permeation study showed that Es-ME-MN has a higher transdermal efficiency and lower retention capacity than commercial estradiol patch and conventional MN. Es plasma concentration began to increase at 3 h and remained at 12.98-23.52 ng/mL until 72 h by pharmacokinetic experiments in the Es-ME-MN group. Es-ME-MN rapidly achieves effective blood concentrations through needle puncture and microemulsion delivery and maintains blood concentrations through the baseplate long-time release. Microemulsion-encapsulated, organic solvent-free, and long-time-released transdermal microneedle will make progress and provide a new idea for transdermal delivery of lipophilic drugs.

Improved Therapeutic Efficacy of MT102, a New Anti-Inflammatory Agent, via a Self-Microemulsifying Drug Delivery System, in Ulcerative Colitis Mice.

MT-102 is a new anti-inflammatory agent derived from Juglans mandshurica and Isatis indigotica. Its therapeutic potential is hindered by low aqueous solubility, impacting its in vivo efficacy. Therefore, this study aimed to develop a self-microemulsifying drug delivery system (SMEDDS) for MT-102 to enhance its oral efficacy in treating ulcerative colitis. Solubility assessment in different oils, surfactants, and cosurfactants led to a SMEDDS formulation of MT-102 using Capmul MCM, Tween 80, and propylene glycol. Based on a pseudoternary phase diagram, the optimal SMEDDS composition was selected, which consisted of 15% Capmul MCM, 42.5% Tween 80, and 42.5% propylene glycol. The resulting optimized SMEDDS (SMEDDS-F1) exhibited a narrow size distribution (177.5 ± 2.80 nm) and high indirubin content (275 ± 5.58 µg/g, a biomarker). Across an acidic to neutral pH range, SMEDDS-F1 showed rapid and extensive indirubin release, with dissolution rates approximately 15-fold higher than pure MT-102. Furthermore, oral administration of SMEDDS-F1 effectively mitigated inflammatory progression and symptoms in a mouse model of ulcerative colitis, whereas pure MT-102 was ineffective. SMEDDS-F1 minimized body weight loss (less than 5%) without any significant change in colon length and the morphology of colonic tissues, compared to those of the healthy control group. In addition, oral administration of SMEDDS-F1 significantly inhibited the secretion of pro-inflammatory cytokines such as IL-6 and TNF-α. In conclusion, the SMEDDS-F1 formulation employing Capmul MCM, Tween 80, and propylene glycol (15:42.5:42.5, w/w) enhances the solubility and therapeutic efficacy of MT-102.

Lopinavir-Loaded Self-Nanoemulsifying Drug Delivery System for Enhanced Solubility: Development, Characterisation and Caco-2 Cell Uptake.

The antiretroviral protease inhibitor drug, lopinavir (LPV), is used to treat HIV-1 infection. LPV is known to have limited oral bioavailability, which may be attributed to its poor aqueous solubility, low efficacy and high first-pass metabolism. Self-nanoemulsifying drug delivery systems (SNEDDS) for LPV have been developed and optimised to counter the current issues. The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS. The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension). The LPV-SNEDDS could be a potential carrier for LPV oral delivery.

Preparation of Self-microemulsion Solids of Kaempferia galanga (L.) Volatile Oil and Its Effect on Rats with Gastric Ulcer.

Kaempferia galanga volatile oil (KVO), the main effective component of the medicinal plant Kaempferia galanga L., possesses a variety of pharmacological activities such as anti-inflammatory, antioxidant, and anti-angiogenic activities and has therapeutic potential for gastric ulcer (GU). However, poor solubility as well as instability limits the clinical application of KVO. In this study, K. galanga volatile oil self-microemulsion solids (KVO-SSMEDDS) were prepared to improve its bioavailability and stability, and the therapeutic effects were evaluated in a rat model with GU. The ratio of oil phase, emulsifier, and co-emulsifier in the KVO-SMEDDS prescription were optimized by plotting the pseudo-ternary phase diagram with the star point design-response surface method. Based on the optimal prescription, self-microemulsifying drug delivery system (SMEDDS) was prepared as solid particles (S-SMEDDS). The prepared KVO-SSMEDDS had a rounded and non-adhesive appearance, formed an O/W emulsion after dissolution in water, and had a uniform particle size distribution with good stability and solubility. It was administered to GU model animals, and the results showed that a certain dose of KVO-SSMEDDS solution could increase the content of gastric mucosal protective factors PGE2, TGF-α, and EGF in gastric tissues and serum, and the expression of inflammatory factors IL-8 and TNF-α was downregulated. Meanwhile, the expression of the NF-κB/COX-2 pathway proteins was inhibited. In conclusion, the prepared KVO-SSMEDDS has good dispersion, solubility, and stability and has a therapeutic effect on rats with GU.

Preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin for potential oral applications

Phytochemicals as therapeutic alternatives can have a fundamental impact on the various stages of inflammation and its resolution. Prunetin is a naturally occurring isoflavone and has been claimed to have numerous therapeutic potentials. The objective of this study is preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin (PMF) for potential oral applications. With this research, it was targeted to emphasize the way of improving the therapeutic efficacy of natural biomolecules with a nontoxic and effective formulation. In the study, the pseudo-ternary phase diagram was developed and PMF was characterized by conductivity, droplet size, viscosity and pH. Effects against to cytokines (IL-1β and IL-6) and TNF-α levels of the PMF were determined by ELISA technique. Genotoxicity and acute oral toxicity tests were carried out according to OECD guidelines. The results showed that PMF is a colloid system that reduced proinflammatory cytokine levels in LPS-induced macrophage cells compared to the control group. PMF demonstrated no mutagenic activity against TA98, TA100, TA1535, and TA1537 Salmonella strains. The in vivo oral acute toxicity test results indicated that PMF did not show mortality or significant side effects even at 2000 mg/kg bw. This study represents PMF showed a good safety profile in animal study. It is thought that this formulation may have anti-inflammatory potential with further in vivo testing.

A new stable and bioactive formulation of Geniotrigona thoracia propolis microemulsion for oral delivery

Propolis, particularly those produced by stingless bees, is known to have a broad range of medicinal benefits due to its antioxidant properties. However, its strong and unpleasant flavour and sticky texture make it less palatable. This study aimed to improve the oral administration of stingless bee propolis extract for nutraceutical use by formulating it into a microemulsion. The microemulsion was created using a water titration method and a pseudo-ternary phase diagram to determine the optimal surfactant: co-surfactant ratio. The formulation was then characterized for its globule size, pH, viscosity, and phenolic content, and subjected to stability tests under ambient and accelerated conditions. Anti-microbial and antioxidant activity were evaluated through the disk diffusion method and the ABTS assay. The microemulsion had an average droplet size of 229.2 nm, a pH of 4.78 ± 0.18, and a viscosity of 0.149 Pa, which falls within the typical range for oral formulations. The microemulsion successfully preserved the antioxidant and antibacterial properties of the propolis extract. Long-term and accelerated stability studies indicated that the microemulsion's pH, appearance, and viscosity remained stable for up to 12 months, although there was a 24 % loss in phenolic activity over the same period. Overall, a stable and potent propolis microemulsion was successfully developed using pharmaceutical and food-grade ingredients, providing a safe and effective way to orally deliver propolis.

Formulation and stability study of vitamin E microemulsion with green surfactant

To satisfy the urge for green life, the preparation of various microemulsions using green surfactants has become a new research hotspot. To improve the utilization of vitamin E (VE) oil, the O/W microemulsions of VE were successfully prepared by a pseudo-ternary phase diagram method with three green surfactants. All of the microemulsions are transparent and uniform-looking. The average size of spheres is in the range of 30–75 nm. The stability of microemulsions was determined by storage, temperature and centrifugation. They remained stable for up to 4 months. The antioxidant capacity of microemulsions was 2.99 times higher than that of ordinary VE, and they were less susceptible to oxidative inactivation. This work has successfully constructed food-grade microemulsions with high VE content and free of other oil phases by simple stirring using a completely green surfactant and cosurfactant, which is one more step towards the better application of VE products in food, medicine and industrial fields.

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

Self-nanoemulsifying drug delivery systems are innovative methods that have the potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and highly selective H1-antihistamine. The aim of this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability from prepared formulas and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulae of liquid SNEDDS were created utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zetapotential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SMEDDS formulations showed enhanced drug release. This study's findings showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size and higher zetapotential with acceptable drug content compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble. Keywords: Bilastine, SNEDDS