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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 4 h. 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. [ABSTRACT FROM AUTHOR]

The active components of turmeric oil (TO) were analyzed using gas chromatography-mass spectrometry (GC-MS), gas chromatography-ion mobility spectrometry (GC-IMS), and electronic nose. The major components of TO were found to be ar-curcumone (23.09%), curcumone (21.36%), and β-curcumone (14.93%). In order to maximize the stability of TO and to mask its irritating substances, a microemulsion encapsulating it (TO-ME) was constructed by the water titration method. Based on the pseudo ternary phase diagram constructed, the optimal process parameters were determined as follows: TO as the oil phase, Tween-80 as the surfactant, propylene glycol as the co-surfactant, deionized water as the aqueous phase, a mass ratio of surfactant to co-surfactant of 4:1, a mass ratio of mixed surfactant to oil phase of 8:2, and a water content of 70% in the microemulsion. The largest area of the microemulsion region was formed under these conditions. The resultant microemulsion had a pH of 6.81 ± 0.02, a density of (1.053 ± 0.001) g/mL, a polydispersity index (PDI) of 0.27 ± 0.11, and an average particle size of (32.81 ± 14.54) nm. The microemulsion was characterized as an oil-in-water (O/W) type microemulsion, with spherical or ellipsoidal droplets. The prepared TO-ME exhibited good centrifugal stability, storage stability, and resistance to oral and gastric digestion, and could be released and utilized in the intestine. The microemulsion system significantly improved the scavenging capacity of TO against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical. In conclusion, microemulsion encapsulation significantly improved the stability and antioxidant activity of TO while effectively facilitating its release and digestion in the intestine. Our research results provide a theoretical basis for the high-value development and utilization of TO.

This study presents results of extracting hydrolyzed collagen peptide from fresh‐water fish scale and using it to prepare a nanoemulsion based on Sacha inchi (Plukenetia volubilis L.) seed oil and collagen peptide. The sacha inchi seed oil is extracted from the seeds of Sacha Inchi (abbreviated as sachi) plant and contains approximate 45 % triple omega 3–6‐9 (ω‐3, ω‐6, ω‐9) content. Pseudo‐ternary phase diagrams of three components: aqueous collagen solution, sachi seed oil, and surfactant/co‐surfactant (Smix) have been constructed. The parameters including the composition of Smix, sachi seed oil, and aqueous collagen solution have been selected to optimize the technology factors for the emulsion process. A quadratic regression equation was chosen, and experimental planning following the Box‐Behnken model using response surface methodology was used to optimize the preparation conditions for the nanoemulsion. The average droplet size of the emulsion systems is the object function for optimization. The Smix is a mixture of surfactant (Tween80) and propylene glycol (PG) with different ratios of Tween80/PG of 1/1, 2/1, 3/1, and 4/1, corresponding to the formation of four emulsion systems, code 1, 2, 3, 4, respectively. The optimal parameters for each emulsion system are different, however, the aqueous collagen solution contains a higher proportion in emulsions. Under the optimal conditions, the predicted values of the objective function of emulsions code 1–code 4 ranged from 95.62 to 185.14 nm, increasing together with the Tween80 ratio in Smix. The experiment values of the objective function of emulsions code 1–code 4 prepared under the optimal conditions are 104.22, 133.70, 159.27, and 207.87 nm, respectively. These values are close to the predicted values, suggesting that the suitability of the experiment and theory. Additionally, the stability of the nanoemulsion prepared under the optimal conditions is also evaluated. A stable nanoemulsion is potentially for loading nutraceuticals and vitamins for applications in personal health care and medicinal fields. [ABSTRACT FROM AUTHOR]

A microemulsion is a stable, homogeneous pesticide formulation, based on an aqueous solvent, which is considered as a suitable alternative to emulsion formulations. In this study, microemulsion formulations of deltamethrin insecticide were designed to control Aphis gossypii Glover (Hemiptera: Aphididae), one of the important pests of many crops and ornamental plants. The solvent was selected based on the higher solubility of deltamethrin, and the appropriate surfactants were selected based on the quality of microemulsion formation. Pseudo‐ternary phase diagrams were constructed by the water titration method. The microemulsion systems were prepared using mixtures composed of deltamethrin, surfactants including Kenon 10 + SDS, Tensiofix 8427 + SDS and Tensiofix 8427 + SLS, and cosurfactant (1‐butanol). The Physico‐chemical properties of the obtained microemulsions were also evaluated. The appearance of microemulsion systems was transparent, and the droplet size of all samples was less than 20 nm. The formulations showed thermodynamic stability and low viscosity. All four microemulsion formulations had high insecticidal activity against A. gossypii, compared with an aqueous solution of pure deltamethrin. In this study, an environment‐friendly microemulsion system was designed to improve the efficacy of deltamethrin for controlling populations of A. gossypii. However, further research could be performed to assess the behaviour and ultimate fate in the environment prior to commercialization. [ABSTRACT FROM AUTHOR]

The active components of turmeric oil (TO) were analyzed using gas chromatography-mass spectrometry (GC-MS), gas chromatography-ion mobility spectrometry (GC-IMS), and electronic nose. The major components of TO were found to be ar-curcumone (23.09%), curcumone (21.36%), and β-curcumone (14.93%). In order to maximize the stability of TO and to mask its irritating substances, a microemulsion encapsulating it (TO-ME) was constructed by the water titration method. Based on the pseudo ternary phase diagram constructed, the optimal process parameters were determined as follows: TO as the oil phase, Tween-80 as the surfactant, propylene glycol as the co-surfactant, deionized water as the aqueous phase, a mass ratio of surfactant to co-surfactant of 4:1, a mass ratio of mixed surfactant to oil phase of 8:2, and a water content of 70% in the microemulsion. The largest area of the microemulsion region was formed under these conditions. The resultant microemulsion had a pH of 6.81 ± 0.02, a density of (1.053 ± 0.001) g/mL, a polydispersity index (PDI) of 0.27 ± 0.11, and an average particle size of (32.81 ± 14.54) nm. The microemulsion was characterized as an oil-in-water (O/W) type microemulsion, with spherical or ellipsoidal droplets. The prepared TO-ME exhibited good centrifugal stability, storage stability, and resistance to oral and gastric digestion, and could be released and utilized in the intestine. The microemulsion system significantly improved the scavenging capacity of TO against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical. In conclusion, microemulsion encapsulation significantly improved the stability and antioxidant activity of TO while effectively facilitating its release and digestion in the intestine. Our research results provide a theoretical basis for the high-value development and utilization of TO. [ABSTRACT FROM AUTHOR]

Summary: The antioxidant and anticancer properties of lycopene make it an excellent ingredient for daily food supplements. The present study developed a novel protocol based on crystallisation to produce lycopene of high purity from a complex extract obtained by n‐hexane from tomato peel. The crystallisation process aimed to achieve a higher recovery and purity of lycopene. The crystallisation system was optimised using ethanol and n‐hexane at a volume ratio of 0.8:1 after evaporating the extract to a solid concentration of 66%. The recovery of lycopene reached 78.45% with a purity of 96.12%. The combination of the two crystallisation methods used, antisolvent and evaporation crystallisation, removed most impurities from the lycopene crystals. This novel protocol thus proved to be effective for recovering lycopene from tomato waste. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

A microemulsion is a stable, homogeneous pesticide formulation, based on an aqueous solvent, which is considered a suitable alternative to emulsion formulations. In this study, microemulsion formulations of cypermethrin insecticide were designed to control Aphis gossypii Glover (Hemiptera: Aphididae), one of the important pests of many crops and ornamental plants. Xylene was selected as a suitable solvent based on the higher solubility of cypermethrin. Pseudo-ternary phase diagrams were constructed by the water titration method. The microemulsion system using mixtures composed of cypermethrin, Kenon 10+SDS surfactants, and 1-butanol cosurfactant had the highest microemulsion surface, and the ratio of 50:30:20 was chosen for further experiments. The physical and chemical properties of the obtained microemulsions were also evaluated. Microemulsion formulations were synthesized with 150 and 250 g/L a.i. (active ingredient) of the cypermethrin. The appearance of the microemulsion compounds was transparent and the droplet size of all samples was less than 35 nm. Foliar spraying of compounds including cypermethrin technical material (150 g a.i./L), cypermethrin technical material (250 g a.i./L), cypermethrin microemulsion (150 g a.i./L), and cypermethrin microemulsion (250 g/L a.i.), under greenspace conditions on Hibiscus rosa-sinensis L. (Malvaceae) caused 25.05, 37.54, 60.74, and 83.94% mortality on third instar nymphs 48 hours after treatment, respectively. Therefore, microemulsion formulations had significantly more insecticidal activity against A. gossypii compared to the technical material. In this study, an environment-friendly microemulsion system was designed to improve the efficacy of cypermethrin for controlling populations of A. gossypii. However, further research could be performed to assess the behavior and ultimate fate in the environment prior to commercialization.

Copyright of Journal of South-Central Minzu University (Natural Science Edition) is the property of Journal of South-Central Minzu University (Natural Science Edition) Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

为提高番茄红素的稳定性和水溶性，采用低能乳化法制备番茄红素微乳液，利用伪三元相图优化番茄红素微乳液配方。探讨油相、乳化剂、助乳化剂、乳化剂与助乳化剂质量比(Km值)对微乳液形成的影响，通过计算并比较伪三元相图微乳液区域面积确定各因素的最佳值，并对微乳液的类型、形态、粒径、多分散指数（PDI)和Zeta电位进行测定。结果表明，番茄红素微乳液最佳配方为油相为亚麻籽油、乳化剂为吐温80、助乳化剂为无水乙醇、Km值为2∶ 1，采用最佳配方得到的番茄红素微乳液为O/W型，微乳液液滴呈规则球形，粒径为（167.70±0.45）nm，PDI为0.179±0.006，Zeta电位为（-7.71±0.53） mV。采用该方法制备的番茄红素微乳液均一稳定。 In order to improve the stability and water solubility of lycopene, lycopene microemulsion was prepared by low energy emulsification method. The formulation of lycopene microemulsion was optimized by pseudo-ternary phase diagram.The influences of oil phase,emulsifier,assistant emulsifier,mass ratio of emulsifier to assistant emulsifier(Km value)on the formation of microemulsion were discussed.The optimal value of each factor was determined by calculating and comparing the microemulsion area of the pseudo-ternary phase diagram.The type, morphology, particle size, polydispersity index and Zeta potential of lycopene microemulsion prepared with the optimal formula were measured. The results showed that the best formula of lycopene microemulsion was:oil phase was linseed oil,emulsifier Twain 80, assistant emulsifier anhydrous ethanol, Km value 2∶ 1. Using the best formula, the lycopene microemulsion was O/W type microemulsion in regular spherical shape, and its particle size was (167.70±0.45) nm,the PDI was 0.179±0.006,and the Zeta potential was (-7.71±0.53)mV. The prepared lycopene microemulsion was homogeneous and stable.

In this article, formulation studies for terbinafine hydrochloride nanoemulsions, prepared by high-energy ultrasonication technique, are described. Pseudo-ternary phase diagram was constructed in order to find out the optimal ratios of oil and surfactant/co-solvent mixture for nanoemulsion production. Clove and olive oils were selected as oil phase. Based on the droplet size evaluation, maximum nanoemulsion region were determined for formulation development. Further characterization included polydispersity index (PDI), zeta potential, Fourier transform infrared (FT-IR) spectroscopy, morphology, pH, viscosity, refractive index, ex vivo skin permeation, skin irritation, and histopathological examination. Droplet sizes of optimized formulations were in colloidal range. PDI values below 0.35 indicated considerably homogeneous nanoemulsions. Zeta potential values were from 13.2 to 18.1 mV indicating good stability, which was also confirmed by dispersion stability studies. Ex vivo permeation studies revealed almost total skin permeation of terbinafine hydrochloride from the nanoemulsions (96–98%) in 6 hours whereas commercial product reached only 57% permeation at the same time. Maximum drug amounts were seen in epidermis and dermis layers. Skin irritation and histopathological examination demonstrated dermatologically safe formulations. In conclusion, olive oil and clove oil-based nanoemulsion systems have potential to serve as promising carriers for topical terbinafine hydrochloride delivery.

Copyright of Journal of Central South University is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Methods: Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamic stability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, in vitro solubility of the drug, and emulsification time. Results: F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater in vitro release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). Conclusions: According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

Background: The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Methods: Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamic stability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, in vitro solubility of the drug, and emulsification time. Results: F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater in vitro release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). Conclusions: According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

Background: The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Methods: Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamic stability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, in vitro solubility of the drug, and emulsification time. Results: F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater in vitro release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). Conclusions: According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

The main objective of the proposed work was the development of a thermosensitive gel (containing clove and tea tree oil) for the management of vaginal candidiasis. Both oils have been recommended to be used separately in a topical formulation for vaginal candidiasis. Incorporating two natural ingredients (clove and tea tree oil) into a product give it a broad antimicrobial spectrum and analgesic properties. The two oils were mixed together at a 3:1 ratio and converted into o/w nanoemulsion using the aqueous titration method and plotting pseudo ternary phase diagrams. Further transformations resulted in a gel with thermosensitive properties. To determine the final formulation's potential for further clinical investigation, in vitro analyses (viscosity measurement, MTT assay, mucoadhesion, ex vivo permeation) and in vivo studies (fungal clearance kinetics in an animal model) were conducted. The current effort leveraged the potential of tea tree and clove oils as formulation ingredients and natural therapeutic agents for vaginal infections. Its synergy generated a stable and effective thermosensitive gel that can be utilized for recurrent candidiasis and other infections. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Chinese Institute of Food Science & Technology / Zhongguo Shipin Xuebao is the property of Journal of Chinese Institute of Food Science & Technology Periodical Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This study aims to increase the aqueous solubility of ciprofloxacin (CPN) to improve oral bioavailability. This was carried out by formulating a stable formulation of the Self-Emulsifying Drug Delivery System (SEDDS) using various ratios of lipid/oil, surfactant, and co-surfactant. A pseudo-ternary phase diagram was designed to find an area of emulsification. Eight formulations (F1-CPN-F8-CPN) containing oleic acid oil, silicone oil, olive oil, castor oil, sunflower oil, myglol oil, polysorbate-80, polysorbate-20, PEO-200, PEO-400, PEO-600, and PG were formulated. The resultant SEDDS were subjected to thermodynamic study, size, and surface charge studies to improve preparation. Improved composition of SEDDS F5-CPN containing 40% oil, 60% polysorbate-80, and propylene glycol (Smix ratio 6: 1) were thermodynamically stable emulsions having droplet size 202.6 nm, charge surface -13.9 mV, and 0.226 polydispersity index (PDI). Fourier transform infra-red (FT-IR) studies revealed that the optimized formulation and drug showed no interactions. Scanning electron microscope tests showed the droplets have an even surface and spherical shape. It was observed that within 5 h, the concentration of released CPN from optimized formulations F5-CPN was 93%. F5-CPN also showed a higher antibacterial action against S. aurous than free CPN. It shows that F5-CPN is a better formulation with a good release and high antibacterial activity. [ABSTRACT FROM AUTHOR]

[Display omitted] • BSFL oil was effectively used to create O/W microemulsions with a low-energy emulsification technique. • The minimum particle size of BSFL O/W microemulsions could be as low as 20–25 nm. • HCO-40 served as the most effective surfactant for preparing BSFL O/W microemulsions. • BSFL O/W microemulsion demonstrated favorable stability during storage, centrifugation, and thermal testing. Black Soldier Fly Larvae (BSFL) play an important role in the ecological protection, nutrition security and circular economy, as they consume organic waste and convert it into insect biomass rich in proteins and lipids. Microemulsions (<100 nm) are popular in various fields because of their superior solubilization capacity, stability, transparency, and ease of preparation. Utilizing BSFL oil with great antioxidant properties to develop an oil-in-water (O/W) microemulsion system can release its potential applications. The objective of this research was to establish a method for creating BSFL O/W microemulsion systems through low-energy emulsification, investigate appropriate surfactants, and optimize the formulations. The findings revealed that polyoxyethylene hydrogenated castor oil (HCO-40) was the most effective surfactant, producing a microemulsion with uniform particle size distribution and low polydispersity index (PDI). The optimum surfactant to cosurfactant ratio (Km values) for various systems was determined to be 9:1, allowing for maximum BSFL oil content within the system. Furthermore, the BSFL O/W microemulsions exhibited good stability over a period of 60 days. These results provide valuable support for further exploration of BSFL oil in various applications. [ABSTRACT FROM AUTHOR]

Copyright of China Surfactant Detergent & Cosmetics (1001-1803) is the property of China Surfactant Detergent & Cosmetics Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Purpose: Microemulsion (ME) achieved progressing consequences on both the research and industry levels due to their distinctive properties. ME based-limonene system is considered as a surrogate to the traditional microemulsion composed of conventional oils. Thus, a novel microemulsion based on D-limonene and Gelucire®44/12 had been designed and evaluated with assessing the factors affecting its physicochemical characteristics and in vivo skin irritation. Methods: The impact of microemulsion components and ratios on the isotropic region of the pseudo-ternary phase diagram was investigated. The optimal formula was evaluated in terms of percentage transmittance, average globule size, size distribution, zeta potential, microscopical morphology, stability under different storage conditions and its effect on the mice ear skin. Results: The results demonstrated that Labrasol® and Labrafil® M 1944 CS had been selected as surfactant and co-surfactant, respectively, due to their emulsifying abilities. The largest isotropic area in the pseudo-ternary phase diagram was at a weight ratio of 4:1 for Labrasol® and Labrafil® M 1944 CS. The optimized microemulsion with 25% w/w of the lipid phase and 58.3% w/w of the aqueous phase displayed an optical transparency of 96.5±0.88 %, average globule size of 125±0.123 nm, polydispersity index of 0.272±0.009, zeta potential of -18.9± 2.79 mV with rounded globules morphology and high stability. The in vivo skin irritation and the histopathological evaluation of microemulsion elucidated its safety profile when applied on the skin. Conclusion: The formulated microemulsion is a prospective aid for an essential oil to minimize its volatility, enhance its stability, and mask its dermal irritant.

Water-in-oil (W/O) microemulsions exhibit delivery matrix and exhibit poor lipid solubility. Therefore, increasing the stability of W/O microemulsions is necessary to broaden their applications. In our experiment, a protein microemulsion system was constructed and its stability was investigated. The effects of surfactants, co-surfactants, quality ratio of them (Km) and hydrophilic-lipophilic balance (HLB) values were determined by using the pseudo-ternary phase diagrams and the area of microemulsions (MEs) as the indexes. The results showed that MEs’ stability was the best when the limonene was used as oil phase, Tween 20 + span 80 as the surfactant, and anhydrous alcohol as co-surfactant, if and only if HLB = 6.0 and Km = 3:1. Under this condition, the area of micro-emulsion was the largest, and the quality of microemulsion was better when the mass ratio of oil phase and emulsifier was 7:5.The protein microemulsion was a water-in-oil type, with a particle size of 1.41 ± 0.03 μm, containing 1127.37 ± 30.87 μg/g of proteins. Moreover, the temperature, light, and sample observation tests showed that the solution’s protein retention rate was lower than those in the microemulsion. Low-concentration NaCl, less than 9% of glucose and maltose exerted no significant influence on the protein microemulsion stability.

Crotamiton (CRT) is a commonly approved drug prescribed for the scabies treatment in many countries across the globe. However, poor aqueous solubility and low bioavailability, and side effects restrict its use. To avoid such issues, an appropriate carrier system is necessary which can address the aforementioned challenges for attaining enhanced biopharmaceutical attributes. The current study intends to provide a detailed account on the development and evaluation of CRT-loaded microemulsion (ME) hydrogel formulation containing tea tree oil (TTO) for improved drug delivery for scabies treatment in a safe and effective manner. Pseudo-ternary phase diagrams were constructed with TTO as the oily phase, and Cremophor®EL was used as the surfactant in a mass ratio 2:1 with co-surfactants (mixture of phospholipid 90G and Transcutol®P), and aqueous solution as the external phase. The optimized drug-loaded ME formulation was evaluated for skin penetration, retention, compliance, and dermatokinetics. The nonirritant behavior of the formulation was revealed by skin histopathology, which showed no changes in normal skin histology. In comparison to the conventional product, dermatokinetic experiments revealed that CRT has greater penetration and distribution in the epidermis of the mice skin. The findings imply that the proposed lipid-based ME hydrogel can aid in the resolution of CRT issues by providing a better and safer delivery option to epidermis and deeper epidermis in substantial quantities.

Genipin has attracted much attention for its hepatoprotective, anti-inflammatory, and neuroprotection activities. However, poor water solubility and active chemical properties limit its application in food and pharmaceutical industries. This article aimed to develop a lipid-based microemulsion delivery system to improve the stability and bioavailability of genipin. The excipients for a genipin microemulsion (GME) preparation were screened and a pseudo-ternary phase diagram was established. The droplet size (DS), zeta potential (ZP), polydispersity index (PDI), physical and simulated gastrointestinal digestion stability, and in vitro drug release properties were characterized. Finally, the effect of the microemulsion on its cellular uptake by Caco-2 cells and the protective effect on PC12 cells were investigated. The prepared GME had a transparent appearance with a DS of 16.17 ± 0.27 nm, ZP of −8.11 ± 0.77 mV, and PDI of 0.183 ± 0.013. It exhibited good temperature, pH, ionic strength, and simulated gastrointestinal digestion stability. The in vitro release and cellular uptake data showed that the GME had a lower release rate and better bioavailability compared with that of free genipin. Interestingly, the GME showed a significantly better protective effect against amyloid-β (Aβ1-42)-induced PC12 cell cytotoxicity than that of the unencapsulated genipin. These findings suggest that the lipid-based microemulsion delivery system could serve as a promising approach to improve the application of genipin. [ABSTRACT FROM AUTHOR]

Nanoemulsions (NE) are used widely in pharmaceutical drug formulations and vaccine preparation, and Acanthopanax senticousus polysaccharide (ASPS) is a natural bioactive compound with immunostimulatory activity. Therefore, NE-loaded ASPS is expected to provide immunological enhancement for effective treatment. In the present study, Acanthopanax senticousus polysaccharide (ASPS was encapsulated into nanoemulsions, the resultant ASPS-NE were coated with a negative charge, and the immune enhancement mechanism of these ASPS-NE formulations was analyzed. The immunosuppressive animal models (70 ICR mice, male) for the study were established using cyclophosphamide. In addition, the activation of splenocyte proliferation, phagocytosis of the macrophages, the ratio of CD4+ to CD8+, the concentrations of the cytokines in serum, Western blot analysis was used for the analysis of the P65/JNK/ikk α signaling pathway in the peritoneal macrophage s. The results revealed that the ASPS-NE could stimulated the proliferation of splenocytes and enhance immunity. The ASPS-NE induced the expression of different cytokines (TNF-α, IFN-γ, IL-2, and IL-6), could activate the expressions of P65, JNK, and ikkα, and regulated the Th1/Th2 cytokines. These findings demonstrated the potential of ASPS-NE formulations for drug delivery and to induce potent and sustained immune responses. [ABSTRACT FROM AUTHOR]

The aim of this article was to design a self-emulsifying drug delivery system (SEDDS) of loaded cepharanthine (CEP) to improve the oral bioavailability in rats. Based on the solubility determination and pseudo-ternary phase diagram, isopropyl palmitate (IPP) was chosen as the oil phase. Meanwhile, Cremophor RH40 and Macrogol 200 (PEG 200) were chosen as the emulsifier and co-emulsifier, respectively. This prescription was further optimized by using central composite design of response surface methodology. The optimized condition was CEP:IPP:Cremophor RH40:PEG 200=3.6:30.0:55.3:11.1 in mass ratio with maximum drug loading (36.21 mg/mL) and the minimum particle size (36.70 nm). The constructed CEP-SEDDS was characterized by dynamic light scattering, transmission electron microscopy, in vitro release and stability studies. The dissolution level of CEP-SEDDS was nearly 100% after 30 min in phosphate-buffered saline (PBS, pH 6.8) which was higher than that of the pure CEP (approximately 20%). In addition, in vivo pharmacokinetic study in rats showed that CEP-SEDDS dramatically improved bioavailability compared with active pharmaceutical ingredient (API) (the relative bioavailability was 203.46%). In this study, CEP-SEDDS was successfully prepared to enhance the oral bioavailability which might facilitate to increase its better clinical application. [ABSTRACT FROM AUTHOR]

The main objective of the proposed work was the development of a thermosensitive gel (containing clove and tea tree oil) for the management of vaginal candidiasis. Both oils have been recommended to be used separately in a topical formulation for vaginal candidiasis. Incorporating two natural ingredients (clove and tea tree oil) into a product give it a broad antimicrobial spectrum and analgesic properties. The two oils were mixed together at a 3:1 ratio and converted into o/w nanoemulsion using the aqueous titration method and plotting pseudo ternary phase diagrams. Further transformations resulted in a gel with thermosensitive properties. To determine the final formulation’s potential for further clinical investigation, in vitro analyses (viscosity measurement, MTT assay, mucoadhesion, ex vivo permeation) and in vivo studies (fungal clearance kinetics in an animal model) were conducted. The current effort leveraged the potential of tea tree and clove oils as formulation ingredients and natural therapeutic agents for vaginal infections. Its synergy generated a stable and effective thermosensitive gel that can be utilized for recurrent candidiasis and other infections.

This study was aimed at improving the water solubility and oral bioavailability of Chl by self-microemulsifying drug delivery system (Chl-SMEDDS). Compatibility experiments, pseudo-ternary phase diagram and central composite design were used to optimize the formulation. The selected systems were further evaluated for physical characteristics, including particle size, zeta potential, and appearance. The stability, in vitro dispersion test, and in vivo intestinal perfusion experiments were used to evaluate the SMEDDS. The optimal composition of Chl-SMEDDS included: Labrafil M 1944 CS (35%), kolliphor RH 40 (46%), Transcutol HP (19%) and 60 mg/g Chl. The appearance of water emulsified Chl-SMEDDS was green and transparent. The particle size, ζ-potential, and transmission electron microscopy studies showed that spherical globules of Chl-SMEDDS with a size of about 22.82 ± 1.29 nm and a negative surface charge of −24.21 ± 3.45 mV were obtained. Chl-SMEDDS could remain stable at 25 °C and 4 °C for at least 6 months. The dispersion test showed that Chl-SMEDDS dispersed spontaneously to form microemulsion after disintegration of capsule shell and 90% drug dispersed in just 30 min in pH 1.2 HCl without any drug precipitation during the test period. In vivo intestinal perfusion experiment revealed that the main absorption site for Chl-SMEDDS was duodenum. This study indicates that SMEDDS formulation could be an effective strategy for the oral administration of Chl. [ABSTRACT FROM AUTHOR]

Purpose: Microemulsion (ME) achieved progressing consequences on both the research and industry levels due to their distinctive properties. ME based-limonene system is considered as a surrogate to the traditional microemulsion composed of conventional oils. Thus, a novel microemulsion based on D-limonene and Gelucire®44/12 had been designed and evaluated with assessing the factors affecting its physicochemical characteristics and in vivo skin irritation. Methods: The impact of microemulsion components and ratios on the isotropic region of the pseudo-ternary phase diagram was investigated. The optimal formula was evaluated in terms of percentage transmittance, average globule size, size distribution, zeta potential, microscopical morphology, stability under different storage conditions and its effect on the mice ear skin. Results: The results demonstrated that Labrasol® and Labrafil® M 1944 CS had been selected as surfactant and co-surfactant, respectively, due to their emulsifying abilities. The largest isotropic area in the pseudo-ternary phase diagram was at a weight ratio of 4:1 for Labrasol® and Labrafil® M 1944 CS. The optimized microemulsion with 25% w/w of the lipid phase and 58.3% w/w of the aqueous phase displayed an optical transparency of 96.5±0.88 %, average globule size of 125±0.123 nm, polydispersity index of 0.272±0.009, zeta potential of -18.9± 2.79 mV with rounded globules morphology and high stability. The in vivo skin irritation and the histopathological evaluation of microemulsion elucidated its safety profile when applied on the skin. Conclusion: The formulated microemulsion is a prospective aid for an essential oil to minimize its volatility, enhance its stability, and mask its dermal irritant. [ABSTRACT FROM AUTHOR]

Water-in-oil (W/O) microemulsions exhibit delivery matrix and exhibit poor lipid solubility. Therefore, increasing the stability of W/O microemulsions is necessary to broaden their applications. In our experiment, a protein microemulsion system was constructed and its stability was investigated. The effects of surfactants, co-surfactants, quality ratio of them (Km) and hydrophilic-lipophilic balance (HLB) values were determined by using the pseudo-ternary phase diagrams and the area of microemulsions (MEs) as the indexes. The results showed that MEs' stability was the best when the limonene was used as oil phase, Tween 20 + span 80 as the surfactant, and anhydrous alcohol as co-surfactant, if and only if HLB = 6.0 and Km = 3:1. Under this condition, the area of micro-emulsion was the largest, and the quality of microemulsion was better when the mass ratio of oil phase and emulsifier was 7:5.The protein microemulsion was a water-in-oil type, with a particle size of 1.41 ± 0.03 μm, containing 1127.37 ± 30.87 μg/g of proteins. Moreover, the temperature, light, and sample observation tests showed that the solution's protein retention rate was lower than those in the microemulsion. Low-concentration NaCl, less than 9% of glucose and maltose exerted no significant influence on the protein microemulsion stability. [ABSTRACT FROM AUTHOR]

Genipin has attracted much attention for its hepatoprotective, anti-inflammatory, and neuroprotection activities. However, poor water solubility and active chemical properties limit its application in food and pharmaceutical industries. This article aimed to develop a lipid-based microemulsion delivery system to improve the stability and bioavailability of genipin. The excipients for a genipin microemulsion (GME) preparation were screened and a pseudo-ternary phase diagram was established. The droplet size (DS), zeta potential (ZP), polydispersity index (PDI), physical and simulated gastrointestinal digestion stability, and in vitro drug release properties were characterized. Finally, the effect of the microemulsion on its cellular uptake by Caco-2 cells and the protective effect on PC12 cells were investigated. The prepared GME had a transparent appearance with a DS of 16.17 ± 0.27 nm, ZP of −8.11 ± 0.77 mV, and PDI of 0.183 ± 0.013. It exhibited good temperature, pH, ionic strength, and simulated gastrointestinal digestion stability. The in vitro release and cellular uptake data showed that the GME had a lower release rate and better bioavailability compared with that of free genipin. Interestingly, the GME showed a significantly better protective effect against amyloid-β (Aβ1-42)-induced PC12 cell cytotoxicity than that of the unencapsulated genipin. These findings suggest that the lipid-based microemulsion delivery system could serve as a promising approach to improve the application of genipin.

Anthocyanins exhibit natural antioxidants but exhibit poor stability and low oil solubility. Therefore, increasing the stability and fat solubility of anthocyanins is necessary to broaden their applications. In our experiment, an anthocyanin microemulsion system was constructed and its stability was investigated. At an oil phase and emulsifier ratio of 7:3, the hydrophilic oil-wet value reached 7.5 and the Km was 2:1. Furthermore, the microemulsion area was the largest. The bicontinuous region of the microemulsion exhibited optimal experimental conditions and resulted in a microemulsion containing 425.54 ± 1.58 μg/g anthocyanins. The anthocyanin microemulsion was a water-in-oil type, with a particle size of 0.07 ± 0.009 μm. Moreover, the temperature, light, and sample observation tests showed that the anthocyanin retention rate in the microemulsion was higher than that in the anthocyanin solution. Low-concentration NaCl and less than 9% of glucose and sucrose exerted no significant influence on the anthocyanin microemulsion stability.

Beta vulgaris L. (beetroot) is a vegetable plant rich in phytochemical compounds such as phenolic acids, carotenoids and flavonoids. The objective of the current study is the development and optimization of self-nanoemulsifying drug delivery systems (SNEDDSs) to enhance the hepatoprotective activity of beet leaf (BL) extract. Total flavonoids content was estimated in the BL extract and its solubility was evaluated in various vehicles to select proper component combinations. Pseudo-ternary phase diagrams were constructed employing olive, linseed, castor and sesame oils (oil phase), Tween® 20 (Tw20) and Tween® 80 (Tw80) (surfactants (SAs)) as well as dimethyl sulfoxide (DMSO) and propylene glycol (PG) (co-surfactants (Co-SAs)). Optimization of formulations from the phase diagrams took place through testing their thermodynamic stability, dispersibility and robustness to dilution. Four optimized BL-SNEDDS formulations, comprising linseed oil or olive oil, Tw80 and DMSO at two SA/Co-SA ratios (2:1 or 3:1) were chosen. They exhibited high cloud point and percentage transmittance values with spherical morphology of mean droplet sizes ranging from 14.67 to 16.06 nm and monodisperse distribution with negatively charged zeta potential < −9.51 mV. The in vitro release profiles of the optimized formulations in pH 1.2 and 6.8 were nearly similar, with a non-Fickian release mechanism. In vivo evaluation of BL-SNEDDSs hepatoprotective activity in a thioacetamide-induced hepatotoxicity rat model depicted promoted liver functions, inflammatory markers and histopathological findings, most prominently in the group treated by F7. The results indicate that SNEDDS, as a nanocarrier system, has potential to improve the hepatoprotective activity of the BL extract. [ABSTRACT FROM AUTHOR]

In this paper, the components of blank nanoemulsion were screened by pseudo-ter­nary phase diagram method to prepare O/W nanoemulsion. The structure ? conductivity ? vis­cosity and stability of the nanoemulsion were determined. The micromorphology and distri­bution characteristics were characterized and investigate the solubilization effect of nanoe­mulsion on the insoluble drug quercetin. The results show the components of quercetin nano­emulsion was ethyl acetate/emulsifier OP-10/anhydrous ethanol/pure water, the quercetin nanoemulsion prepared was clear and transparent yellowish liquid. Its viscosity was 0. 024 Pa • s?conductivity was 99. 0 /s/cm. Through observation by transmission electron micros­copy? the nanoemulsion exhibited spherical morphology; The prepared nanoemulsion had an average particle diameter of(14. 43 士 0. 25) nmand a polydispersity index (PDI) of 0. 157 ; its Zeta potential wasmeasured to be 1 25±0. 45 mV. It has nano-sized particle size and exhib­its a stable normal particle size distribution ofO/W emulsion characteristics. By loading the insoluble drug quercetin, the content of quercetin in the stable nanoemulsion system was 354. 84 /g/mL. Compared with the solubility of quercetin in water (0. 17 〜7. 7 /g/mL)，the water solubility of quercetin was significantly improved. [ABSTRACT FROM AUTHOR]

The aim of present study was to prepare a self nano-emulsifying drug delivery system (SNEDDS) of ketoconazole for topical administration. Ketoconazole is an excellent antifungal agent that is useful in treatment of fungal infections due to Candida species, but it is a BCS class II drug and hence has poor water solubility which limits its efficacy. SNEDDS is a system consisting of oil, surfactant and co-surfactant that spontaneously emulsify on dilution. A pseudo-ternary phase diagram was plotted to determine the exact concentration of components to be mixed in order to obtain a stable SNEDDS preconcentrate. The design of experiment was carried out using Design Expert® 7.0 (State-Ease Inc. Minneapolis, USA) software and using a D-optimal design the entire study design was developed. The statistical tool helped in optimization of the formulation and achieving a formula which is most desirable. Particle size analysis and Polydispersity Index depicted that the optimized SNEDDS formulation produced a nanoemulsion upon dilution with a globule size of 13.87 nm and a polydispersity index of 0.086 which indicates high degree of uniformity in globule size. Accelerated stability studies showed that the formulation is able to withstand temperature fluctuations on storage for long durations of time. Antifungal activity showed enhanced performance of the drug compared to standard. In vivo skin irritability studies were performed that indicated that the formulation does not produce any skin irritability and is suitable for topical administration. [ABSTRACT FROM AUTHOR]

The Imiquimod (IMQ) formulation for cutaneous administration is challenging due to its very low solubility and its poor penetration properties. The purpose of this study was to develop medium or high fluidity microemulsions (ME) to increase the solubility and modulate the release for the topical administration of Imiquimod (IMQ), thus increasing the therapeutic efficacy of the drug. Ginger oil was selected as the oil phase, Polysorbate 80/Triton X-100 1:1 as the surfactant system, and water as the aqueous phase. From the construction of a pseudo-ternary phase diagram, it was possible to obtain ME in a wide range of combinations with medium to high density. Five ME were subjected to conductivity, drug incorporation, and in vitro release assays. From conductivity determinations, it was established that ME exhibited a characteristic profile of percolative conductivity, suggesting a phase inversion of W/O to direct micelles O/W. The release assay demonstrated the ability of the ME to deliver IMQ, where the ME 1–3 had a high rate of release as a function of time, and the ME 4–5 , released the drug in a sustained manner. These results indicate that the ME studied may be a promising vehicle for increasing the effectiveness of IMQ in topical dosage forms. [Display omitted] • Fluid and semisolid transparent formulations were found by PTPD. • The maximum apparent solubilities (Sapp) for IMQ observed was 59 × 101 mg/g. • The average droplet size was lower than 20 nm. • An important increase in the released IMQ was observed from F1 and F2 after 4 h. [ABSTRACT FROM AUTHOR]

Abstract Nanoemulsion is considered to be a new and exciting field of research that seeks to exploit the attractive properties of components to improve oral delivery of drugs like candesartan cilexetil used in the management of chronic diseases. Candesartan cilexetil is a lipophilic acidic drug with a half-life of about (5–10) hour and absolute bioavailability of (14–40%). For this reason, the study target was to formulate and characterize candesartan cilexetil nanoemulsions that could improve solubility, dissolution and stability of the lipophilic drug candesartan cilexetil. The solubility of candesartan cilexetil was checked in various vehicles in order to choose the best solubilizing components for building up an efficient nanoemulsion based on regulating hydrophilic/lipophilic balance (HLB) value above 10, and then pseudo-ternary phase diagram was used as a useful tool to evaluate the nanoemulsion domain. The nanoemulsion formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer mixture and transcutol HP as oil, surfactant mixture and co-surfactant respectively by aqueous titration method at surfactant/co-surfactant ratios of 3:1 and 4:1 and varying the type of poloxamer in each ratio. The prepared nanoemulsions were tested for nanodispersion stability studies, droplet size distribution, polydispersity index, zeta potential, viscosity, filter paper spreadability, dye miscibility, electroconductivity, pH, percent transmittance, surface tension, refractive index, morphology and drug dissolution. It was found that release rate and extent for all prepared nanoformulations were significantly higher (p

Abstract Candesartan cilexetil is an ester prodrug antagonist to angiotensin II receptor type 1 (AT1) used in management of many cardiovascular diseases. The absolute bioavailability of candesartan cilexetil is about (14–40%). Therefore, the paper aim was to prepare and evaluate solid self-nanoemulsifying drug delivery systems for candesartan cilexetil in order to improve its solubility, dissolution and stability. Solubility study was run in different vehicles to select the best excipients for dissolving candesartan cilexetil. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios and four formulations were prepared using various concentrations of cinnamon oil, tween 80 with poloxamer 407 mixture and transcutol HP as oil, surfactant mixture and co-surfactant, respectively. After this step about (0.2 milliliter) of each formulation was adsorbed on to two different adsorbent mixtures set which were: avicel 101 with aerosil 200 and avicel 101 with dibasic calcium phosphate anhydrous resulted in eight solid nanoformulations. All prepared formulations were evaluated for particle size distribution, polydispersity index, zeta potential, scanning probe microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffractometry and in vitro drug dissolution. It was found that release rate and extent for all prepared formulations were significantly higher (p

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Copyright of Shipin Kexue/ Food Science is the property of Food Science Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The oral administration of celecoxib (CLX) is a real problem because of its low aqueous solubility that results in high variability in absorption and its severe adverse effect such as cardiotoxic effects and gastrointestinal toxicity. Self-nanoemulsifying drug delivery systems (SNEDDS) can enhance the poor dissolution and erratic absorption of poorly water-soluble drugs such as CLX. This study was conducted to investigate the potential of SNEDDS to enhance the efficacy of CLX on inflamed mucous tissue and reduce systemic adverse effects by increasing its poor dissolution properties. A pseudo-ternary phase diagram was derived from the results of CLX solubility experiments in various excipients. These studies revealed the use of Labrafil M 2515 CS as oil, tween 80 as a surfactant, and polyethylene glycol 400 as a co-surfactant for the optimization of SNEDDS formulations. Eight formulations were formulated and characterized by their particle size, polydispersity index, viscosity, globular shape, drug solubility, self-emulsification efficiency, in vitro drug release, and permeation. The anti-inflammatory effect of CLX-SNEDDS was evaluated by carrageenan-induced cheek oedema in rats. The cheeks were treated with CLX-SNEDDS before oedema induction and then noticed for narrow periods (2 h) followed by histopathological studies to determine the efficacy of treatment. The selected formulations (F3 and F5) showed spherical morphologies under transmission electron microscopy, mean droplet sizes of 116.9 ± 1.78 and 124 ± 1.87 nm, respectively, complete in vitro drug release, and high cumulative amounts of drug permeation in 8 h. They also showed significant remarkable cheek oedema inhibition in comparison with the control groups (p < 0.05). CLX-SNEDDS was found to achieve effective local therapeutic concentration and intended to reduce cheek oedema, congestive capillary, inflammatory cells, and side effects due to lower dose size. [ABSTRACT FROM AUTHOR]

Zingeber officinale is a commonly used plant which has been shown to possess anti-inflammatory activity. The active compounds present in ginger are gingerols, shagaols and paradol. The aim of this study was formulation of topical microemulsion system to enhance the solubility and stability of ginger extract, as it is unstable in the presence of light, air, heat and long term storage, and to evaluate its anti-inflammatory activity. The solubility of ginger extract in different oils, surfactants, and co-surfactants was determined in order to find the optimal components for microemulsion. IPM was selected as oil phase, tween 80 and PEG 400 were selected as surfactant and co-surfactant respectively based on highest solubility values. Pseudo-ternary phase diagram was constructed in order to find out the microemulsion region. The prepared microemulsions were evaluated for pH, viscosity, conductivity, refractive index, globular size, zeta potential, polydispersity index, ginger extract content. The formulation F1 showed best physicochemical properties with smallest globular size. It also showed significant (p<0.05) anti-inflammatory effect as compared to reference piroxicam drug solution. Based on the results, it is concluded that ginger extract can be used to develop stable microemulsion system and promising anti-inflammatory activity. [ABSTRACT FROM AUTHOR]

The effective components of flavonoids in the &quot;Pueraria lobata-Hovenia dulcis&quot; drug pair have low bioavailability in vivo due to their unstable characteristics. This study used microemulsions with amphoteric carrier properties to solve this problem. The study drew pseudo-ternary phase diagrams through titration compatibility experiments of the oil phase with emulsifiers and co-emulsifiers and screened the prescription composition of blank microemulsions. The study used average particle size and PDI as evaluation indicators, and the central composite design-response surface method(CCD-RSM) was used to optimize the prescription; high-dosage drug-loaded microemulsions were obtained, and their physicochemical properties, appearance, and stability were evaluated. The results showed that when ethyl butyrate was used as the oil phase, polysorbate 80(tween 80) as the surfactant, and anhydrous ethanol as the cosurfactant, the maximum microemulsion area was obtained. When the difference in results was small, K&#95;(m )of 1∶4 was chosen to ensure the safety of the prescription. The prescription composition optimized by the CCD-RSM was ethyl butyrate(16.28%), tween 80(9.59%), and anhydrous ethanol(38.34%). When the dosage reached 3% of the system mass, the total flavonoid microemulsion prepared had a clear and transparent appearance, with average particle size, PDI, and potential of(74.25±1.58)nm, 0.277±0.043, and(-0.08±0.07) mV, respectively. The microemulsion was spherical and evenly distributed under transmission electron microscopy. The centrifugal stability and temperature stability were good, and there was no layering or demulsification phenomenon, which significantly improved the in vitro dissolution of total flavonoids.

A pseudo-ternary phase experimental approach was used to model the influence of the mixture components concentration on the nanoemulsions properties as ternary systems. For this, several types of essential oils (EO) were used as lipid phase, being oregano (OR-EO), thyme (TH-EO), lemongrass (LG-EO) and mandarin (MN-EO), while pectin and Tween 80 were studied as emulsifiers. All formulations were processed by microfluidization at 150 MPa and 5 cycles. Polynomial models were fitted to experimental data and their adjusted R 2 and p-values were obtained. Remarkably, a pectin concentration of 1% ( w/w ) allowed the formation of submicron emulsions between 350 and 850 nm in the absence of Tween 80 for all the studied EOs, thus confirming its emulsification capacity. In general, increasing the pectin concentration up to 2% ( w/w ) enlarged the particle size of emulsions and their viscosity thus suggesting decreased emulsification efficiency during microfluidization. Nonetheless, nanoemulsions with particle sizes below 500 nm were obtained when a minimum Tween 80 concentration of 1.8% ( w/w ) was used, regardless the pectin or EO concentrations. The modest decrease in the ζ-potential that was observed depending on the type of EO at increasing pectin concentrations indicated that pectin is not or weakly adsorbed at the oil-water interface. All nanoemulsions were transparent at high surfactant and low EO concentrations due to a weak light scattering of the nano-sized oil droplets. Thus, this work contributes in elucidating the role of pectin and small molecule non-ionic surfactants on the formation of submicron emulsions and nanoemulsions containing essential oils. [ABSTRACT FROM AUTHOR]