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1.
J Colloid Interface Sci ; 677(Pt B): 504-512, 2025 Jan.
Article in English | MEDLINE | ID: mdl-39154443

ABSTRACT

The commonly used artificial light sources, such as fluorescent lamps and white light-emitting diodes, often have a high ratio of blue light emission, which poses potential blue light hazards, especially one of the main culprits leading to eye diseases. Therefore, developing novel white lighting sources with low blue-hazard is highly appreciated. In this work, an air-stable and color-tunable triplet-triplet annihilation upconversion (TTA-UC) mechanism was proposed to realize the low blue-hazard white-light emission. The proposed design was composed of three primary RGB colors from the annihilator (9,10-diphenylanthracene, DPA), the laser excitation source, and the photosensitizer (palladium (II) octaetylporphyrin, PdOEP), respectively. The introduction of oil-in-water (o/w) microemulsion can effectively block the potential oxygen-induced triplet-quenching and benefit high UC efficiency. Moreover, either raising ambient temperatures or adding isobutanol can activate the UC process to yield white-light emission. Notably, the white-light emission with a Commission Internationale de l'Eclairage (CIE) coordinate of (0.33, 0.33) as well as a low ratio of blue emission (14.2 %) was achieved at an ambient temperature of 42 °C. Therefore, the proposed air-stable TTA-UC mechanism can significantly lower the blue-hazard and provide a novel solution for applications in lighting and display.

2.
Sci Rep ; 14(1): 23168, 2024 10 05.
Article in English | MEDLINE | ID: mdl-39369062

ABSTRACT

Limited solubility is the main cause of the low local availability of anti-candidiasis drug, miconazole nitrate (MN). The study's objective was to develop and characterize microemulsion (ME) based temperature-triggered in situ gel of MN for intravaginal administration to enhance local availability and antifungal activity. The solubility of MN was initially studied in different oils, surfactants, and co-surfactants. Then, pseudo-ternary phase diagrams were constructed to select the best ratio of various components. The ME formulations were characterized by thermodynamic study, droplet size, polydispersity index (PDI), viscosity, and in-vitro antifungal mean inhibition zone (MIZ). Selected MEs were incorporated into different in situ gel bases using a combination of two thermosensitive polymers (poloxamer (PLX) 407 and 188), with 0.6% of hydroxypropyl methylcellulose (HPMC K4M) and gellan gum (GG) as mucoadhesive polymer. ME-based gels (MG) were investigated for gelation temperature, gelation time, viscosity, spreadability, mucoadhesive strength, in vitro release profile, and MIZ test. Furthermore, the optimum MG was assessed for in vivo animal irritation test and FESEM investigation. Tea tree oil, lavender oil, tween 80, and propylene glycol (PG) were chosen for ME preparation for the optimal formulation; formulation ME7 and ME10 were chosen. After incorporation of the selected formulation into a mixture of P407 and P188 (18:2% w/w) with 0.6% mucoadhesive polymer, the resultant MG formulation (MG1) revealed optimum gelation temperature (33 ± 0.01℃) and appropriate viscosity with enhanced sustained release (98%) and retention through sheep vaginal mucosa, MG1 exhibited a better MIZ compared to the 2% MN gel formulation and the marketed MN product, and no rabbit vagina irritation. In conclusion, the miconazole nitrate-loaded MG-based formula sustained the duration of action and better antifungal activity than the marketed miconazole nitrate formulation.


Subject(s)
Antifungal Agents , Candidiasis, Vulvovaginal , Emulsions , Gels , Miconazole , Miconazole/chemistry , Miconazole/administration & dosage , Miconazole/pharmacology , Female , Antifungal Agents/pharmacology , Antifungal Agents/chemistry , Antifungal Agents/administration & dosage , Emulsions/chemistry , Animals , Candidiasis, Vulvovaginal/drug therapy , Gels/chemistry , Viscosity , Administration, Intravaginal , Candida albicans/drug effects , Solubility , Poloxamer/chemistry
3.
J Appl Microbiol ; 135(9)2024 Sep 02.
Article in English | MEDLINE | ID: mdl-39237458

ABSTRACT

AIMS: Evaluate the in vitro efficacy of the essential oils derived from Aloysia citrodora (Verbenaceae), Cymbopogon winterianus (Poaceae), and Ocimum gratissimum (Lamiaceae) against Acanthamoeba polyphaga trophozoites. Additionally, microemulsions formulated with these essential oils, along with their major components, were analyzed. METHODS AND RESULTS: The prepared microemulsions were characterized using polarized light microscopy and rheological techniques. The amoebicidal activity was determined by measuring the inhibitory concentration (IC50). Flow cytometry was employed to detect membrane damage and alterations in trophozoites size. The results revealed transparent and thermodynamically stable microemulsions. The essential oil from O. gratissimum exhibited a lower IC50, with values of 280.66 and 47.28 µg ml-1 after 24 and 48 h, respectively. When microemulsions containing essential oils were tested, the IC50 values exhibited a reduction of over 80% after 24 h. Particularly, eugenol, a constituent of the O. gratissimum essential oil, displayed higher amoebicidal activity. The essential oils also caused damage to the cell membrane, resulting in the subsequent death of the trophozoites. CONCLUSIONS: The EOs of A. citrodora, C. winterianus, and O. gratissimum and their microemulsions showed antiparasitic effect against A. polyphaga trophozoites, representing promising alternatives for the treatment of diseases caused by this protozoan.


Subject(s)
Acanthamoeba , Cymbopogon , Emulsions , Ocimum , Oils, Volatile , Trophozoites , Verbenaceae , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Cymbopogon/chemistry , Ocimum/chemistry , Emulsions/pharmacology , Trophozoites/drug effects , Acanthamoeba/drug effects , Verbenaceae/chemistry , Amebicides/pharmacology , Plant Oils/pharmacology , Plant Extracts/pharmacology
4.
Curr Drug Deliv ; 2024 Sep 03.
Article in English | MEDLINE | ID: mdl-39230000

ABSTRACT

BACKGROUND: Eczema, an inflammatory skin disease causing intense itching, is a function of a range of internal and external factors, impacting individuals of all ages and leading to economic loss. Inflammation is the most important manifestation of eczema, and Matricaria recutita essential oil (MREO) extracted from Matricaria recutita possesses excellent antibacterial and anti-inflammatory properties. METHODS: In this study, Matricaria recutita microemulsions were prepared by the trans-phase emulsification method and their stability was determined by evaluating the relevant indexes. Establishment of 2,4-dinitro-chlorobenzene-induced AD model in mice. Detection of serum indexes of IL-6, IL-17, and TNF-α, and on pathological tissue sections, the HE staining, toluidine blue staining, immunohistochemistry, and observation were performed. RESULTS: The study obtained optimal conditions for the preparation of microemulsion formulations of Matricaria recutita. Through quality evaluation, it was found that the microemulsion increased stability, reduced irritation, and retained anti-inflammatory activity and therapeutic effects on eczema compared to Matricaria recutita essential oil (MREO). Studies have demonstrated that microemulsion formulations of Matricaria recutita and Matricaria recutita significantly down regulate the proinflammatory factors TNF-α, IL-17, and IL-6. It was shown by hematoxylin-eosin (HE) staining that both Matricaria recutita essential oil (MREO) and Matricaria recutita microemulsion (MRME) improved the inflammatory status of eczematous skin tissues in mice. The number of mast cells expressed in the tissues was decreased in the surface-treated group, as shown by toluidine blue staining. Additionally, the number of mast cells expressed in the tissues in the surface-treated group was reduced, as demonstrated by immunohistochemistry. Furthermore, immunohistochemistry revealed that MREO and MRME have immunomodulatory effects on the tissues. CONCLUSION: The study showed that microemulsion formulations of Matricaria recutita may serve as a novel remedy for eczema.

5.
AAPS PharmSciTech ; 25(7): 203, 2024 Sep 05.
Article in English | MEDLINE | ID: mdl-39237802

ABSTRACT

Normal skin is the first line of defense in the human body. A burn injury makes the skin susceptible to bacterial infection, thereby delaying wound healing and ultimately leading to sepsis. The chances of biofilm formation are high in burn wounds due to the presence of avascular necrotic tissue. The most common pathogen to cause burn infection and biofilm is Pseudomonas aeruginosa. The purpose of this study was to create a microemulsion (ME) formulation for topical application to treat bacterial burn infection. In the present study, tea tree oil was used as the oil phase, Tween 80 and transcutol were used as surfactants, and water served as the aqueous phase. Pseudo ternary phase diagrams were used to determine the design space. The ranges of components as suggested by the design were chosen, optimization of the microemulsion was performed, and in vitro drug release was assessed. Based on the characterization studies performed, it was found that the microemulsion were formulated properly, and the particle size obtained was within the desired microemulsion range of 10 to 300 nm. The I release study showed that the microemulsion followed an immediate release profile. The formulation was further tested based on its ability to inhibit biofilm formation and bacterial growth. The prepared microemulsion was capable of inhibiting biofilm formation.


Subject(s)
Anti-Bacterial Agents , Biofilms , Burns , Drug Delivery Systems , Emulsions , Pseudomonas aeruginosa , Biofilms/drug effects , Burns/drug therapy , Burns/microbiology , Pseudomonas aeruginosa/drug effects , Drug Delivery Systems/methods , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/pharmacology , Particle Size , Drug Liberation , Surface-Active Agents/chemistry , Polysorbates/chemistry , Tea Tree Oil/administration & dosage , Tea Tree Oil/chemistry , Tea Tree Oil/pharmacology , Chemistry, Pharmaceutical/methods , Humans
6.
Biotechnol J ; 19(9): e2400387, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39295572

ABSTRACT

21-Hydroxy-20-methylpregn-4-en-3-one (4-HBC, bisnoralcohol) is a crucial intermediate for the synthesis of steroidal drugs. Significant challenges including by-products formation and poor substrate solubility were still confronted in its main synthetic route by microbial conversion from phytosterol. Construction of a direct bioconversion pathway to 4-HBC and an efficient substrate emulsion system is therefore urgently required. In this study, three novel isoenzymes of 3-ketosteroid-Δ1-dehydrogenase (KstD) and 3-ketosteroid 9α-hydroxylase (KsH) in Mycobacterium neoaurum were excavated and identified as KstD4, KstD5, and KsHA3. A strain capable of fully directing the synthesis of 4-HBC was metabolically engineered via serial genetic deletion combined with enhanced expression of cholesterol oxidase (ChOx2) and enoyl-CoA hydratase (EchA19). Moreover, a micro-emulsion system combined with soybean oil and hydroxypropyl-ß-cyclodextrin improved substrate solubility and bioavailability. In batch fermentation, molar yield of 96.7% with 39.5 g L-1 4-HBC was obtained from 50 g L-1 phytosterol. Our findings demonstrate the potential for industrial-scale biosynthesis of 4-HBC.


Subject(s)
Emulsions , Metabolic Engineering , Mycobacteriaceae , Phytosterols , Metabolic Engineering/methods , Phytosterols/metabolism , Emulsions/metabolism , Mycobacteriaceae/genetics , Mycobacteriaceae/metabolism , Mycobacteriaceae/enzymology , Oxidoreductases/metabolism , Oxidoreductases/genetics , Bacterial Proteins/genetics , Bacterial Proteins/metabolism , Fermentation , Soybean Oil/metabolism
7.
Article in English | MEDLINE | ID: mdl-39325151

ABSTRACT

Psoriasis, a chronic skin condition, affects around 2-5% of the population. Topical corticosteroids treat the vast majority of cases (> 80%). Because of the physicochemical characteristics of the damaged stratum corneum, all treatments are ineffective. Nevertheless, systemic immunosuppression, the oral strategy, has substantial adverse effects that may be avoided using the topical procedure. The research sought to determine if a salicylic acid-loaded microemulsion-based gel (emulgel) could successfully infiltrate and maintain salicylic acid in skin tissue for psoriasis treatment. The pseudo-ternary phase was generated in different Smix ratios (1:1, 2:1, and 3:1; Labrasol:Transcutol® P). At a 3:1 ratio, the Smix had a substantial microemulsion area. Microemulsion was characterized for particle size, pH, etc. For topical application, the selected microemulsion was combined with Carbopol 940 gel, and ex vivo permeation and drug retention study were conducted. The effectiveness of the developed gel was checked using the IMQ-induced psoriatic plaque model. Salicylic acid microemulsion has an average globule size of 79.72 nm, pH 5.93, and 100% transmittance. In an ex vivo diffusion study, emulgel revealed greater penetration and more drug retention than ordinary salicylic acid gel. The emulgel was non-irritating on the skin of rats. In vivo studies revealed significant antipsoriatic activity of microemulsion-loaded gel compared to the marketed product. Developed emulgel was considered a potential product for an effective and safe way to administer salicylic acid for the treatment of skin diseases such as psoriasis.

8.
Antioxidants (Basel) ; 13(8)2024 Jul 27.
Article in English | MEDLINE | ID: mdl-39199153

ABSTRACT

Numerous approaches targeting hepatic stellate cells (HSCs) have emerged as pivotal therapeutic strategies to mitigate liver fibrosis and are currently undergoing clinical trials. The investigation of herbal drugs or isolated natural active compounds is particularly valuable, due to their multifaceted functions and low risk of side effects. Recent studies have hinted at the potential efficacy of verbascoside (VB) in ameliorating renal and lung fibrosis, yet its impact on hepatic fibrosis remains to be elucidated. This study aims to evaluate the potential effects of VB on liver fibrosis by assessing its ability to inhibit HSC activation. VB demonstrated significant efficacy in suppressing the expression of fibrogenic genes in activated LX-2 cells. Additionally, VB inhibited the migration and proliferation of these activated HSCs by scavenging reactive oxygen species (ROS) and downregulating the AMPK pathway. Furthermore, a biosafe reverse microemulsion loaded with VB (VB-ME) was developed to improve VB's instability and low bioavailability. The optimal formulation of VB-ME was meticulously characterized, revealing substantial enhancements in cellular uptake, ROS-scavenging capacity, and the suppression of HSC activation.

9.
Sci Rep ; 14(1): 19819, 2024 Aug 27.
Article in English | MEDLINE | ID: mdl-39191832

ABSTRACT

Ecofriendly ionic liquids (ILs) were synthesized through amidation of ricinoleic acid, the main fatty acid in castor oil, followed by a quaternization reaction to solubilize ethanol in IL/diesel blends at different ratios. As a result, stable and highly renewable, low viscous microemulsion biofuels with high oxygen content were prepared. The prepared fuel samples combine the advantages of green ionic liquids and microemulsion properties. The chemical structures of ILs were confirmed with the aid of NMR and FTIR spectroscopy. DLS analysis revealed that the ethanol particles ranged in size from 8 to 18.1 nm in all samples. As ILs ratios decrease in microemulsion from 37 to 69%, the ethanol particle sizes increase from 10 to 25%. Ethanol shows good solubilization in diesel and IL-1 is more effective than IL-2 in ethanol solubilization at low percentages of ethanol due to more oxygen atoms besides three hydroxyl groups. The ternary phase diagram indicated that the microemulsion area in the case of using IL-1 is larger than that of IL-2. The fuel properties of the prepared microemulsions are nearly close to those of neat diesel and fall within the permitted range of ASTM D975. The viscosity and density values at low ratios of ILs are found to be very close to the values of the neat diesel at different temperatures. The prepared samples show a slight decrease in cetane number and heating value compared to diesel. However, they have improved flash points, cloud points, sulfur content, and acid value. The particle sizes were checked every week and the prepared samples showed high stability with the aid of the synthesized ILs. Moreover, the prepared microemulsions stayed in a transparent appearance for more than a year and no phase separation was observed.

10.
Poult Sci ; 103(10): 104121, 2024 Oct.
Article in English | MEDLINE | ID: mdl-39121643

ABSTRACT

The overuse of antibiotics has resulted in a surge of drug-resistant bacteria, making the pursuit of natural antimicrobials an urgent and significant trend. Encapsulation and nanoparticulation are effective ways to enhance the antibacterial properties of natural drugs. In this study, we encapsulated tannic acid (TA) with chitosan (CS) and poly (lactide-co-glycolide) (PLGA) using the emulsion-solvent evaporation method to enhance the antimicrobial effect of TA. We prepared a bilayer membrane spherical nanoemulsion of TA-PLGA-CS (TPC) with uniform size of 559.87 ± 1.16 nm, and zeta potential of 59.53 ± 1.07 mV. TPC could be stably stored for 90 days at 4°C without affecting the properties of the emulsion, and the minimum bactericidal concentration against four strains of Escherichia coli (E. coli) remained unchanged for 60 d. The results indicated that TPC enhanced the inhibitory effect of TA against E. coli. Scanning electron microscope images revealed that TPC treatment caused damage to the bacterial cell membrane. In addition, in vivo experiments indicated that TPC exhibited a superior therapeutic effect on artificial colibacillosis in chickens infested with Avian pathogenic Escherichia coli, as evidenced by the changes in body weight and a reduction bacterial load in heart. Furthermore, TPC reversed the down-regulation of catalase, glutathione peroxidase1 (GPX1), and GPX7 gene expression levels in intestinal tissues. Compared to the model group, TPC treatment elevated serum glutathione peroxidase activities and lowered myeloperoxidase and lactate dehydrogenase levels, offering antioxidant protection that was slightly better than that of doxycycline hydrochlorid group. In summary, we prepared a novel TA antimicrobial preparation with significant antioxidant potential and inhibitory effect against E. coli both in vitro and in vivo.


Subject(s)
Anti-Bacterial Agents , Chickens , Chitosan , Emulsions , Escherichia coli Infections , Escherichia coli , Polylactic Acid-Polyglycolic Acid Copolymer , Poultry Diseases , Tannins , Chitosan/pharmacology , Chitosan/administration & dosage , Chitosan/chemistry , Animals , Escherichia coli/drug effects , Tannins/pharmacology , Tannins/chemistry , Tannins/administration & dosage , Emulsions/chemistry , Emulsions/pharmacology , Escherichia coli Infections/veterinary , Escherichia coli Infections/drug therapy , Polylactic Acid-Polyglycolic Acid Copolymer/chemistry , Polylactic Acid-Polyglycolic Acid Copolymer/administration & dosage , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/chemistry , Poultry Diseases/drug therapy , Poultry Diseases/microbiology , Poultry Diseases/prevention & control , Polyphenols
11.
Int J Pharm ; 663: 124585, 2024 Sep 30.
Article in English | MEDLINE | ID: mdl-39147248

ABSTRACT

The etiology of alopecia is so complex that current therapies with single-mechanism and attendant side-effects during long-term usage, are insufficient for treatment. Panax notoginseng saponins (PNS) is supposed to treat alopecia with multiple mechanisms, but difficult to penetrate skin efficiently due to water-solubility. Here, we designed water-in-oil microemulsion (PNS ME) using jojoba oil, fractioned coconut oil, RH 40 + Span 80 and cosurfactant D-panthenol, to help PNS penetrating the skin. Particularly, D-panthenol not only enlarges the microemulsion area, reduces the usage amounts of surfactants thus relieves skin irritation, but stimulates the migration of dermal papilla cells (DPCs), displaying cooperative effects on anti-alopecia. PNS ME penetrates through sebum-rich corneum via high-affinity lipid fusion, targets to hair follicles (HFs), where it resides in skin for sustained drug release, accelerates angiogenesis to build well-nourished environment for HFs, and facilitates the proliferation and migration of DPCs in vitro. PNS ME markedly improved hair density, skin pigmentation, new hair weight, skin thickness, and collagen generation of telogen effluvium mice. Moreover, PNS also took outstanding curative effects on androgenetic alopecia mice. Upon further exploration, PNS ME caused dramatic upregulations of ß-catenin, VEGF and Ki67, suggesting it might function by triggering Wnt/ß-catenin pathway, accelerating vessels formation, and activating the hair follicle stem cells. Notably, PNS ME indicated longer-term safety than minoxidil tincture. Together, PNS ME provides a comprehensive strategy for alopecia, especially it avoids defects by high-proportioned surfactants in traditional microemulsion, exhibiting milder and safer, which shows bright prospect of applying microemulsion in hair growth promotion.


Subject(s)
Alopecia , Emulsions , Hair Follicle , Panax notoginseng , Saponins , Surface-Active Agents , Alopecia/drug therapy , Alopecia/chemically induced , Animals , Mice , Saponins/administration & dosage , Saponins/pharmacology , Saponins/chemistry , Hair Follicle/drug effects , Panax notoginseng/chemistry , Surface-Active Agents/chemistry , Surface-Active Agents/administration & dosage , Female , Skin/drug effects , Skin/metabolism , Cell Movement/drug effects , Male , Skin Absorption/drug effects , Water/chemistry , Administration, Cutaneous
12.
Int J Biol Macromol ; 279(Pt 1): 134879, 2024 Nov.
Article in English | MEDLINE | ID: mdl-39168198

ABSTRACT

This context summarizes a detail on the fabrication of Acacia senegal Gum Hydrogel (ASGh) within well-engineered microemulsion, and thereafter chemical modification for environmental remediation. In brief, Divinylsulfone was used to crosslink polymeric chains and produce ASGh in ˂50 µm size within the reverse-microemulsion of Natrium-bis-(2-ethylhexyl) sulfosuccinate in gasoline. ASGh were subjected to chemical modification via versatile diethylenetriamine to produce m-[ASGh] for adsorptive removal of methyl orange (MO), eosin Y (EY) and congo red (CR) from waste-water. ASGh and m-[ASGh] were characterized through Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), and zeta potential measurements. For instance, FT-IR spectra depicted new bands upon Diethylenetriamine modification. The zeta potential measurements confirm a positively charged surface of m-[ASGh] upon Diethylenetriamine addition. Interestingly, 0.05 g m-[ASGh] demonstrated 91.0, 84.1, and 73.0 % removal efficiency towards MO, EY and CR, respectively in 2 h equilibrium time. Langmuir, Freundlich and modified-Freundlich isotherms were applied to further delineate adsorption data. Modified-Freundlich model depicted comparatively more agreeable fit, and delivered R2 value nearer to unity. Further, 143 mg·g-1, 130 mg·g-1 and, 116 mg·g-1 maximum adsorption capacity (QM) was represented by m-[ASGh] towards MO, EY and CR, respectively in 2 h. Interestingly, real water sample were tested whereby, the QM against MO, EY and CR was 146 mg·g-1, 132 mg·g-1 and, 111 mg·g-1, respectively in 2 h equilibrium time. To conclude, m-[ASGh] could be treated as decolorizing agent in real waste-water polluted through negatively charged organic pollutants, particularly MO.


Subject(s)
Gum Arabic , Hydrogels , Water Pollutants, Chemical , Water Purification , Adsorption , Hydrogels/chemistry , Hydrogels/chemical synthesis , Water Pollutants, Chemical/chemistry , Water Pollutants, Chemical/isolation & purification , Gum Arabic/chemistry , Kinetics , Water Purification/methods , Industrial Waste , Acacia/chemistry , Spectroscopy, Fourier Transform Infrared , Wastewater/chemistry , Congo Red/chemistry , Azo Compounds/chemistry , Azo Compounds/isolation & purification
13.
Iran J Pharm Res ; 23(1): e139381, 2024.
Article in English | MEDLINE | ID: mdl-39140102

ABSTRACT

Background: This study aimed to develop a microemulsion (ME)-based skin delivery platform containing sildenafil citrate (SC)-ME and evaluate its in vitro skin permeability. Methods: Accurate MEs were prepared using pseudo-ternary phase diagrams and a full factorial design with three variables at two levels. After the design phase, suitable ratios of oil, water, and a mixture of surfactant (S) and cosurfactant (CS) were selected to prepare various SC-ME formulations. These SC-MEs were analyzed for stability, droplet size, in vitro SC release, skin permeability, and viscosity properties. Results: The droplet size of the ME samples ranged from 6.24 to 32.65 nm, with viscosities between 114 to 239 cps. Release profiles indicated that 26 to 60% of SC was released from the different SC-MEs within 24 hours. All ME formulations significantly enhanced the permeability coefficient (P) through rat skin. Specifically, the flux (Jss) in SC-ME7 increased by approximately 117 times (Jss = 0.0235 mg/cm2.h) compared to the control sample (0.0002 mg/cm2.h). Conclusions: The study concluded that the proportions of the water or oil phase and the S/CS mixture in the MEs significantly influenced the physicochemical characteristics and permeation parameters. The selected MEs improved both the permeability coefficient and the rate of permeation through rat skin. The enhanced drug delivery through and into deep skin layers is a key attribute of an ideal dermal ME. These findings suggest that MEs could serve as effective transdermal delivery systems for SC and similar drugs. However, in vivo assays and clinical research are needed to confirm the therapeutic efficacy of MEs.

14.
Curr Pharm Des ; 2024 Aug 01.
Article in English | MEDLINE | ID: mdl-39092731

ABSTRACT

Microemulsion gel, as a promising transdermal nanoparticle delivery system, addresses the limitations of microemulsions and enhances their performance in drug delivery and release. This article aims to discuss the advantages of microemulsion gel, including improved drug bioavailability, reduced drug irritation, enhanced drug penetration and skin adhesion, and increased antimicrobial properties. It explores the methods for selecting microemulsion formulations and the general processes of microemulsion preparation, as well as commonly used oil phases, surfactants, and co-surfactants. Additionally, the biomedical applications of microemulsion gel in treating conditions, such as acne and psoriasis, are also discussed. Overall, this article elucidates the significant potential of microemulsion gel in topical drug delivery, providing insights into future development and clinical applications.

15.
Biomed Pharmacother ; 178: 117253, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39111084

ABSTRACT

Malignant ascites effusion (MAE) is a common complication of advanced malignant tumors with limited treatments. Euphorbia lathyris (EL) has a long history of application in patients with edema and ascites. Herein, we reported for the first time a mode in which EL and EL Pulveratum (PEL) spontaneously formed natural microemulsions (ELM and PELM) without the addition of any carriers and excipients, and found that the protein and phospholipid contained in them encapsulated fatty oil and diterpenoid esters through non-covalent interactions. The denaturation and degradation of protein in PELM resulted in stronger binding of diterpenoid esters to the hydrophobic region of protein, which facilitated the sustained and slow release of diterpenoid esters and improved their bioavailability in vivo, thereby retaining the efficacy of preventing MAE while alleviating the irritation of intestinal mucosa. The mechanism by which PELM retained efficacy might be related to increased feces moisture and urine volume, and decreased expression of AVPR2, cAMP, PKA and AQP3 in MAE mice. And its mechanism of reducing intestinal mucosal irritation was related to decreased cell apoptosis, amelioration of oxidative stress, elevation of mitochondrial membrane potential, and up-regulation of Occludin and Claudin-1 expression in IEC-6 cells. This nano-adjuvant-free natural microemulsions may be a promising therapeutic strategy in the field of phytochemistry for promoting the application of natural and efficient nano-aggregates spontaneously formed by medicinal plants in MAE, and provide a new perspective for advancing the development of the fusion of Chinese herbal medicine and nanomedicine and its clinical translation.


Subject(s)
Emulsions , Euphorbia , Intestinal Mucosa , Euphorbia/chemistry , Animals , Mice , Intestinal Mucosa/drug effects , Intestinal Mucosa/metabolism , Intestinal Mucosa/pathology , Ascites/drug therapy , Ascites/pathology , Male , Apoptosis/drug effects , Plant Extracts/pharmacology , Oxidative Stress/drug effects
16.
AAPS PharmSciTech ; 25(7): 195, 2024 Aug 21.
Article in English | MEDLINE | ID: mdl-39168904

ABSTRACT

Psoriasis is a chronic inflammatory disorder affecting over 100 million people, requires long-term therapy. Current treatments offer only symptomatic relief. However, phytoconstituents-based therapies like Silymarin (SLM) have shown promising effects. The study aims to develop, optimize, and evaluate a novel stable SLM NLC gel to improve anti-psoriatic activity by enhancing its permeability and retention into the dermal layer. SLM NLC formulation was prepared and optimized using 32 full factorial designs. The formulation was evaluated for the particle size, PDI, zeta potential, and % entrapment efficiency, evaluated by Transmission electron microscopy and thermal analysis. The freeze dried and prepared NLC-loaded gel was evaluated for physicochemical parameters, ex-vivo, and in-vivo studies. SLM-loaded NLC shows 624 nm particle size, 0.41 PDI, 92.95% entrapment efficiency, and -31.6 mV zeta potential. The sphere form of NLCs was confirmed using TEM. Controlled drug release was observed in ex vivo studies, low PASI score compared to disease control. Further, the levels of IL-6, TNF-α, and NF-κB were also reduced. The results are supported by histopathology showing minimal parakeratosis indicated in the SLM NLC-treated group. Prepared NLC-based shows enhance topical penetration and decrease the thickness of psoriatic plaques in the in vivo study.


Subject(s)
Gels , Particle Size , Psoriasis , Silymarin , Silymarin/pharmacology , Silymarin/administration & dosage , Silymarin/chemistry , Silymarin/pharmacokinetics , Psoriasis/drug therapy , Animals , Skin Absorption , Drug Liberation , Skin/metabolism , Skin/drug effects , Administration, Cutaneous , Chemistry, Pharmaceutical/methods , Nanoparticles/chemistry , Male , Mice
17.
J Cosmet Dermatol ; 2024 Aug 12.
Article in English | MEDLINE | ID: mdl-39135289

ABSTRACT

BACKGROUND: Methimazole, an oral antithyroid drug, has recently gained attention for its skin-brightening effects when applied topically to treat melasma. This study aims to develop, optimize, and characterize a methimazole microemulsion as a novel, safe approach for local melasma treatment. MATERIALS AND METHODS: We prepared microemulsion formulations containing 3% methimazole by combining appropriate amounts of surfactants (Tween 80 and Span 20), propylene glycol cosurfactant, and an oil phase (oleic acid-transcutol p at a 1:10 ratio). We then assessed droplet size, stability, viscosity, and skin permeation using rat skin models. RESULTS: The microemulsions' droplet sizes ranged from 7.06 to 28.13 nm, with viscosities between 120 and 254 centipoises. Our analysis identified droplet size, viscosity, and membrane release as significant independent variables. We determined the permeability parameters of the optimal formulation through rat skin, including steady-state permeability rate (Jss), permeability coefficient (p), lag time (Tlag), and apparent diffusion coefficient (Dapp). CONCLUSION: We found that the microemulsions' characteristics, physicochemical properties, and in vitro release depended on the surfactant-to-cosurfactant ratio, water content, and oil content. We developed an optimal formulation with a high surfactant-to-cosurfactant ratio and low water and oil percentages. This formulation shows potential for commercialization and manufacturing of final products.

18.
Int J Pharm ; 661: 124447, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-39002820

ABSTRACT

None of transitional lipid-based drug delivery systems (LBDDS) includes compositions containing one lipid and one water-soluble surfactant that form stable microemulsions. The conversion of liquid LBDDS to solid LBDDS has been limited by low drug loading. Previously, we have developed drug solid microemulsions containing one lipid and TPGS (a water-soluble surfactant) that achieved high drug loading and remarkably increased oral bioavailability. This study aimed to test if binary lipid systems (BLS), composed of one lipid and one water-soluble surfactant that form stable self-emulsifying microemulsions, is not an exclusive but widely applicable type of LBDDS for other lipids and surfactants and evaluate the influences of chemical structures of lipids and surfactants on microemulsions and solid microemulsions. We systemically identified new BLS by using a library of lipids and surfactants. Propylene glycol diesters and glycerol triesters were favorable for forming stable microemulsions with Tween 80, Cremophor EL, or TPGS. To the best of our knowledge, this is the first report exploring and confirming that the BLS is a new addition to traditional LBDDS, provides a promising option for researchers, and has the potential to increase drug loading to facilitate the development of solid microemulsions.


Subject(s)
Drug Delivery Systems , Emulsions , Lipids , Polyethylene Glycols , Polysorbates , Solubility , Surface-Active Agents , Vitamin E , Water , Surface-Active Agents/chemistry , Drug Delivery Systems/methods , Lipids/chemistry , Polysorbates/chemistry , Polyethylene Glycols/chemistry , Water/chemistry , Vitamin E/chemistry , Glycerol/analogs & derivatives
19.
Ther Deliv ; 15(7): 521-544, 2024.
Article in English | MEDLINE | ID: mdl-38949622

ABSTRACT

Aim: The current study aims to develop and optimize microemulsions (ME) through Quality-by-Design (QbD) approach to improve the aqueous solubility and dissolution of poorly water-soluble drug disulfiram (DSF) for repurposing in melanoma and breast cancer therapy.Materials & methods: The ME was formulated using Cinnamon oil & Tween® 80, statistically optimized using a D-optimal mixture design-based QbD approach to develop the best ME with low vesicular size (Zavg) and polydispersity index (PDI).Results: The DSF-loaded optimized stable ME showed enhanced dissolution, in-vitro cytotoxicity and improved cellular uptake in B16F10 and MCF-7 cell lines compared with their unformulated free DSF.Conclusion: Our investigations suggested the potential of the statistically designed DSF-loaded optimized ME for repurposing melanoma and breast cancer therapy.


Identifying new medicinal uses of an existing marketed drug can save both money and time in the process of drug development. From many of the recently reported literature, disulfiram (a drug used for alcoholism) has shown its activity against various cancers, including breast and skin cancer. However, it possesses poor water solubility and absorption, leading to low medicinal activity. The current study aims to develop a novel microemulsion dosage form through a statistical design approach to enhance the solubility, dissolution and anticancer activity for repurposing in melanoma and breast cancer treatment. The novel microemulsion was prepared, statistically analyzed and optimized. The optimized microemulsion was found to be stable and showed improved medicinal activity against breast and skin cancer compared with the pure drug. Our research showed the potential of the developed microemulsion of the disulfiram for its new therapeutic use in skin cancer and breast cancer.


Subject(s)
Breast Neoplasms , Disulfiram , Drug Repositioning , Emulsions , Disulfiram/chemistry , Disulfiram/administration & dosage , Disulfiram/pharmacology , Emulsions/chemistry , Humans , Breast Neoplasms/drug therapy , Breast Neoplasms/pathology , Animals , MCF-7 Cells , Mice , Female , Solubility , Melanoma/drug therapy , Melanoma/pathology , Melanoma, Experimental/drug therapy , Melanoma, Experimental/pathology , Cell Line, Tumor , Cell Survival/drug effects , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology
20.
Environ Res ; 260: 119626, 2024 Nov 01.
Article in English | MEDLINE | ID: mdl-39019143

ABSTRACT

The utilization of bio-oil derived from biomass presents a promising alternative to fossil fuels, though it faces challenges when directly applied in diesel engines. Microemulsification has emerged as a viable strategy to enhance bio-oil properties, facilitating its use in hybrid fuels. This study explores the microemulsification of Jatropha bio-oil with ethanol, aided by a surfactant, to formulate a hybrid liquid fuel. Additionally, a bio-nano CaO heterogeneous catalyst synthesized from eggshells is employed to catalyse the production of Jatropha biodiesel from the microemulsified fuel using microwave irradiation. The catalyst is characterized through UV-Vis, XRD, and SEM analysis. The investigation reveals a significant reduction in CO, CO2, and NOX emissions with the utilization of microemulsion-based biodiesel blends. Various blends of conventional diesel, Jatropha biodiesel, and ethanol are prepared with different ethanol concentrations (5, 10, and 20 wt%). Engine performance parameters, including fuel consumption, NOX emission, and brake specific fuel consumption, are analyzed. Results indicate that the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend exhibits superior performance compared to conventional diesel, Jatropha biodiesel, and other blends. The fuel consumption of the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend is measured at 554.6 g/h, surpassing that of conventional diesel and other biodiesel blends. The presence of water (0.14 %) in the blend reduces the heating value, consequently increasing the energy requirement. CO and CO2 emissions for the conventional diesel/Jatropha biodiesel/ethanol (10 wt%) blend are notably lower compared to conventional C-18 hydrocarbons and various biodiesel blends. These findings accentuate the efficacy of the microemulsion process in enhancing fuel characteristics and reducing emissions. Further investigations could explore optimizing the emulsifying agents and their impact on engine performance and emission characteristics, contributing to the advancement of sustainable fuel technologies.


Subject(s)
Biofuels , Egg Shell , Jatropha , Oxides , Biofuels/analysis , Egg Shell/chemistry , Jatropha/chemistry , Catalysis , Oxides/chemistry , Animals , Emulsions , Calcium Compounds/chemistry , Ethanol/chemistry , Vehicle Emissions/analysis
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