Search Results (74)

This study investigates the Quality by Design (QbD)-driven development and optimization of a nanoemulgel incorporating Kunzea ericoides oil for transdermal therapy. Nanoemulgels enhance percutaneous drug delivery, sustain release profiles, and improve bioavailability. A central composite design was employed to optimize critical formulation parameters, with ANOVA confirming a statistically significant impact on particle size and drug release kinetics (p < 0.05). The optimized formulation exhibited a particle size of 112.38 nm, a polydispersity index of 0.203, and a zeta potential of −29.0 mV, ensuring colloidal stability. In vitro drug release followed the Higuchi model (R² = 0.989, kH = 4.776), indicating diffusion-controlled kinetics, while the Korsmeyer–Peppas model (n = 0.88) suggested an anomalous transport mechanism. Antibacterial studies determined minimum inhibitory concentrations of 250 µg/mL for Staphylococcus aureus and 500 µg/mL for Escherichia coli, indicating greater susceptibility in S. aureus. In vivo anti-inflammatory evaluation using a carrageenan-induced paw edema model demonstrated a statistically significant reduction in inflammation (p = 0.005 at 60 min), with a near-complete resolution by 240 min. These findings underscore the potential of Kunzea ericoides nanoemulgel as a promising transdermal therapeutic, integrating controlled drug release with potent anti-inflammatory and antibacterial properties for dermatological and inflammatory conditions. Full article

Periodontitis is a prevalent oral condition worldwide. Azithromycin, a conventional lipophilic drug for periodontal treatment, often causes systemic side effects when administered orally. To address this, azithromycin-loaded nano-emulgels were developed using olive oil as a carrier within a xanthan gum aqueous gel phase. This oil-in-aqueous gel emulsion was actuated into a foam for localized drug delivery in gingival and periodontal disease. The solubility of azithromycin in various vehicles was tested, with olive oil showing the best solubility (0.347 mg/mL). Thermodynamic stability testing identified viable nano-formulations, with encapsulation efficiencies ranging from 98 to 100%. These formulations exhibited rapid drug release within 2–8 h. Muco-adhesion studies and ex vivo permeability tests on porcine buccal mucosa highlighted the beneficial properties of xanthan gum for local drug retention within the oral cavity. Antimicrobial efficiency was assessed using minimum inhibitory concentrations against various oral pathogens, where the formulation with equal surfactant and co-surfactant ratios showed the most potent antibacterial activity, ranging from 0.390 to 1.56 µg/mL. This was supported by the shear-thinning, muco-adhesive, and drug-retentive properties of the xanthan gel base. The study also examined the influence of the oil phase with xanthan gum gel on foam texture, rheology, and stability, demonstrating a promising prototype for periodontitis treatment. Full article

Background/Objectives: Raynaud’s phenomenon (RP) is characterized by an exaggerated vasoconstrictive response of small blood vessels in the fingers and toes to cold or stress. Oral therapy with tadalafil (TDL), a phosphodiesterase-5 inhibitor, is limited by systemic side effects and reduced patient compliance. This study aimed to develop and evaluate a TDL-loaded nanoemulgel for transdermal delivery as a non-invasive treatment alternative for cold-induced vasoconstriction. Methods: TDL-loaded nanoemulsions were prepared using the aqueous titration method with cinnamon oil as the oil phase and Cremophor RH40 and Transcutol as the surfactant–cosurfactant system. The optimized nanoemulsion was incorporated into a carbopol-based gel to form a nanoemulgel. The formulation was characterized for droplet size, morphology, thermodynamic stability, rheological properties, in vitro drug release, skin permeation, and pharmacokinetic behavior. Infrared thermography was employed to assess in vivo efficacy in cold-induced vasoconstriction models. Results: The optimized TDL nanoemulsion exhibited a spherical morphology, a nanoscale droplet size, and an enhanced transdermal flux. The resulting nanoemulgel displayed suitable physicochemical and rheological properties for topical application, a short lag time (0.7 h), and a high permeability coefficient (Kp = 3.59 × 10⁻² cm/h). Thermal imaging showed significant vasodilation comparable to standard 0.2% nitroglycerin ointment. Pharmacokinetic studies indicated improved transdermal absorption with a higher C_max (2.13 µg/mL), a prolonged half-life (t_1/2 = 16.12 h), and an increased AUC_0–24 compared to an oral nanosuspension (p < 0.001). Conclusions: The developed TDL nanoemulgel demonstrated effective transdermal delivery and significant potential as a patient-friendly therapeutic approach for Raynaud’s phenomenon, offering an alternative to conventional oral therapy. Full article

Background: Acne is a prevalent dermatological condition characterized by the blockage of hair follicles and sebaceous glands, leading to the formation of acne. The anaerobe pathogen Cutibacterium acnes (formerly known as Propionibacterium acnes) plays an essential role in the pathogenesis of acne, for which generally antimicrobial treatment is required. Acne is a substantial health concern, and continuing research is being conducted to discover novel and efficacious remedies. The antimicrobial activity of plants has been demonstrated in numerous studies, and they are still targeted organisms in drug development. Studies showing that plants are effective against acne pathogens have also been reported. Methods: The antimicrobial activity of the hydroethanolic extracts prepared from 30 plant species was determined against C. acnes standard strains (C. acnes Scholz and Kilian ATCC 11827 and ATCC 11828) and 30 clinical isolates in our preliminary screening. Since acne is an inflammatory skin disease, the anti-inflammatory effect of six active extracts against C. acnes was determined through the in vitro inhibition of collagenase, lipoxygenase (LOX), hyaluronidase and xanthine oxidase (XO) enzymes. Results: Cotinus coggygria Scop. leaf extract displayed the highest hyaluronidase and collagenase inhibition (79.75% and 52.52%, respectively), while the extract from the aerial parts of Helichrysum arenarium (L.) Moench demonstrated a potent XO inhibitory effect (82.51%). Therefore, these two extracts have been chosen for further studies, and LC/MS-MS was used to determine the phenolic profiles of these extracts. Conclusions: Subsequently, nanoemulgels were formulated with the active extracts to develop a prototype herbal anti-acne product, and characterization studies of the formulations were conducted. Full article

Aim: To investigate the anti-inflammatory, antioxidant, and diabetic wound healing properties of the novel topical formulation [Ferulic acid-loaded nanoemulgel (DLMGO-G)]. Methods: Ferulic acid nanoemulsion developed with lemongrass oil is investigated in diabetic wound healing. Further nanoemulsion is incorporated into 1% carbopol^® 934 to obtain the DLMGO-G. Nanoemulsion was characterized for particle size, and polydispersity index (PDI) was obtained by Malvern Zetasizer (Zetasizer Nano ZS, Malvern, AL, USA), and morphology by TEM (JEM 1400, JOEL, Akishima, Japan). Furthermore, in vitro cell line and in vivo studies were carried out. Results: The developed nanoemulsion showed a globule size of 28.04 ± 0.23 nm and PDI of 0.07 ± 0.01. The morphology of nanoformulations by TEM confirmed the spherical and uniform nature. Further, the nanoformulation in in vitro cell line experiments revealed that the IC50 value was increased by 1.52 times compared to the drug solution. The treatment groups have shown that fibroblast morphologies were spindle-shaped, suggesting that nanoformulation was compatible with the cells and developed normally on nanoformulation. It also reduced ROS with improved internalization more than the control group. The in vitro wound healing model also revealed that nanoformulation had better wound healing activity. In the in vivo diabetic wound studies on male SD rats, the levels of inflammatory markers such as TNF-α, IL-6, IL-22, and IL-1β declined significantly when treated with DLMGO-G. IL-10 levels significantly increased compared to the diseased group, and MMP-9 levels were remarkably decreased compared to the diseased group. Furthermore, histopathological studies showed the regeneration and granulation of tissues. Conclusions: Thus, these findings indicate that FA-loaded nanoemulgel greatly accelerates the healing of wounds in diabetic rats. Full article

Background/Objectives: Ivermectin gained widespread attention as the “miracle drug” during the coronavirus disease 2019 (COVID-19) pandemic. Its inclusion in the 21st World Health Organization (WHO) List of Essential Medicines is attributed to its targeted anti-helminthic response, high efficacy, cost-effectiveness and favorable safety profile. Since the late 2000s, this bio-inspired active pharmaceutical ingredient (API) gained renewed interest for its diverse therapeutic capabilities. However, producing ivermectin formulations does remain challenging due to its poor water solubility, resulting in low bioavailability after oral administration. Therefore, the transdermal drug delivery of ivermectin was considered to overcome these challenges, which are observed after oral administration. Methods: Ivermectin was incorporated in a nano-emulsion, nano-emulgel and a colloidal suspension as ivermectin-loaded nanoparticles. The nano-drug delivery vehicles were optimized, characterized and evaluated through in vitro membrane release studies, ex vivo skin diffusion studies and tape-stripping to determine whether ivermectin was successfully released from its vehicle and delivered transdermally and/or topically throughout the skin. This study concluded with cytotoxicity tests using the methyl thiazolyl tetrazolium (MTT) and neutral red (NR) assays on both human immortalized epidermal keratinocytes (HaCaT) and human immortalized dermal fibroblasts (BJ-5ta). Results: Ivermectin was successfully released from each vehicle, delivered transdermally and topically throughout the skin and demonstrated little to no cytotoxicity at concentrations that diffused through the skin. Conclusions: The type of nano-drug delivery vehicle used to incorporate ivermectin influences its delivery both topically and transdermally, highlighting the dynamic equilibrium between the vehicle, the API and the skin. Full article

Modern bioeconomy and sustainability demands lead food technology in the development of novel biobased edible food preservatives. Herein, the development and characterization of novel polysaccharide (xanthan gum and kappa-carrageenan)-based nanoemulgels (NGs) enhanced with essential oil derivatives; pure citral (CT); pure carvacrol (CV); and various CT:CV ratios (25:75, 50:50, and 75:25) are presented. The obtained NGs are applied as active edible coatings for extending the shelf life of Protected Designation of Origin (PDO) green table olives of Chalkidiki. The zeta potential demonstrated the high stability of the treatments, while light scattering measurement and scanning electron microscopy images confirmed the <100 nm droplet size. EC₅₀ indicated high antioxidant activity for all the tested samples. The fractional inhibitory concentration (FIC) confirmed the synergistic effect of NG with a CT:CV ratio at 50:50 against Staphylococcus aureus and at CT:CV ratios 25:75 and 75:25 against E. coli O157:H7. NG coatings with CT:CV ratios at 50:50 and at 25:75 effectively controlled the weight loss at 0.5%, maintained stable pH levels, and preserved the visual quality of green olives on day 21. The synergistic effect between CT and CV was confirmed as they reduced the spoilage microorganisms of yeasts and molds by 2-log [CFU/g] compared to the control and almost 1 log [CFU/g] difference from pure CT and CV-based NGs without affecting the growth of beneficial lactic acid bacteria crucial for fermentation. NGs with CT:CV ratios at 50:50 and at 25:75 demonstrated superior effectiveness in preventing discoloration and maintaining the main sensory attributes. Overall, shelf life extension was achieved in 21 compared to only 7 of the uncoated ones. Finally, this study demonstrates the potential of polysaccharide-based NGs in mixtures of CT and CV for the shelf life extension of fermented food products. Full article

The aim of this study is to develop a nanoemulgel encapsulating a Tunisian Prickly Pear (Opuntia ficus-indica L.) seed oil (PPSO) to assess, for the first time, the in vivo efficacy of this nanoformulation on wound healing. Phytocompounds of this oil have been reported in the literature as having powerful pharmacological activities. However, it remains poorly exploited due to low bioavailability. A nanoemulsion (NE) was designed by determining the required hydrophilic–lipophilic balance (HLB) and subsequently characterized. The mean droplet size was measured at 56.46 ± 1.12 nm, with a polydispersity index (PDI) of 0.23 ± 0.01 using dynamic light scattering. The zeta potential was −31.4 ± 1.4 mV, and the morphology was confirmed and assessed using transmission electron microscopy (TEM). These characteristics align with the typical properties of nanoemulsions. The gelification process resulted in the formation of a nanoemulgel from the optimum nanoemulsion. The high wound healing efficiency of the nanoemulgel was confirmed compared to that of a medicinally marketed cream. The outcomes of this research contribute valuable insights, for the first time, into the potential therapeutic applications of PPSO and its innovative pharmaceutical formulation for wound healing. Full article

The combination of nanoemulgel and phytochemistry has resulted in several recent discoveries in the field of topical delivery systems. The present study aimed to prepare nanoemulgel based on turmeric (Curcuma longa) and neem (Azadirachta indica) against microbial infection as topical drug delivery. Olive oil (oil phase), Tween 80 (surfactant), and PEG600 (co-surfactant) were used for the preparation of nanoemulsion. Carbopol 934 was used as a gelling agent to convert the nanoemulsion to nanoemulgel and promote the control of the release of biological properties of turmeric and neem. The nanoemulsion was characterized based on particle size distribution, PDI values, and compatibility using FTIR analysis. In contrast, the nanoemulgel was evaluated based on pH, viscosity, spreadability, plant extract and excipient compatibility or physical state, in vitro study, ex vivo mucoadhesive study, antimicrobial properties, and stability. The resulting nanoemulsion was homogeneous and stable during the centrifugation process, with the smallest droplets and low PDI values. FTIR analysis also confirmed good compatibility and absence of phase separation between the oil substance, surfactant, and co-surfactant with both plant extracts. The improved nanoemulgel also demonstrated a smooth texture, good consistency, good pH, desired viscosity, ex vivo mucoadhesive strength with the highest spreadability, and 18 h in vitro drug release. Additionally, it exhibited better antimicrobial properties against different microbial strains. Stability studies also revealed that the product had good rheological properties and physicochemical state for a period of over 3 months. The present study affirmed that turmeric- and neem-based nanoemulgel is a promising alternative for microbial infection particularly associated with microorganisms via topical application. Full article

Essential oils (EOs) are concentrated, hydrophobic volatile compounds derived from different parts of plants. They are recognized for their diverse and versatile functional properties. Approximately 90% of EOs are administered via topical or transdermal routes. However, EOs are susceptible to oxidation, and their high volatility often poses a challenge to the transdermal delivery of their bioactive constituents. Additionally, the direct application of pure EOs on the skin may result in irritating effects. Hence, various novel carrier systems have been explored for the topical application of EOs. Among these, nanoemulgel has received particular attention from the cosmeceutical industry. It is a hybrid technology combining nanoemulsion and a gelling phase, which can enhance the bioadhesivity of EOs, at the same time minimizing their irritating effects. This review summarizes the methods of EO extraction, steps and factors influencing the preparation of EO nanoemulgel, and characterization parameters for nanoemulgel studies. The potential cosmeceutical applications of EO nanoemulgels as an anti-inflammatory, antimicrobial, antioxidant, and penetration enhancer are also compiled and discussed. Full article

This study explores developing and optimizing a nanoemulsion (NE) system loaded with dipyridamole and roflumilast, aiming to improve skin penetration and retention. The NE formulation was further transformed into a nanoemulgel to enhance its application as a topical treatment for psoriasis. Solubility studies were conducted to select the oil, surfactant, and co-surfactant. Phase diagrams were constructed using the aqueous phase titration method. All the formulations were in nanoscale, and Formula (F2) (which contains oleic acid oil as the oil phase, a mixture of Surfactant Tween 80 and co-surfactant (ethanol) at a ratio of 1:2 in addition to distilled water as an aqueous phase in a ratio of 1:5:4, respectively) was the selected formula depending on the particle size, PDI, and zeta potential. Formula (F2) has the best ratio because it gives the smallest nanoemulsion globule size (particle size average of 167.1 nm), the best homogenicity (lowest PDI of 0.195), and the highest stability (higher zeta potential of −32.22). The selected formula was converted into a nanoemulgel by the addition of 0.5% (w/w) xanthan gum (average particle size of 172.7 nm) and the best homogenicity (lowest PDI of 0.121%) and highest stability (higher zeta potential of −28.31). In conclusion, the selected formula has accepted physical and chemical properties, which enhanced skin penetration. Full article

In this study, we present a new type of polymer-free hydrogel made only from nonionic surfactants, oil, and water. Such a system is produced by taking advantage of the physicochemical behavior and interactions between nonionic surfactants and oil and water phases, according to a process close to spontaneous emulsification used in the production of nano-emulsions. Contrary to the classical process of emulsion-based gel formulation, we propose a simple one-step approach. Beyond the originality of the concept, these nanoemulgels appear as very promising systems able to encapsulate and deliver various molecules with different solubilities. In the first section, we propose a comprehensive investigation of the gel formation process and its limits through oscillatory rheological characterization, characterization of the sol/gel transitions, and gel strength. The second section is focused on the follow-up of the release of an encapsulated model hydrophilic molecule and on the impact of the rheological gel properties on the release profiles. Full article

This research aimed to evaluate the efficacy of a nanoemulgel (NE) containing Cananga odorata (Ylang-Ylang) oil for managing scalp psoriasis and dandruff through various assessments. The study involved phytochemical screening, characterization, stability testing, in vivo performance evaluation, dermatokinetic analysis, central composite rotatable design (CCRD) optimization, in vitro release profiling, and antioxidant and antimicrobial activity assessment of the NE. The NE exhibited excellent stability and maintained physical parameters over a three-month period. In vivo studies showed no skin irritation, maintenance of skin pH (4.55 to 5.08), and improvement in skin hydration (18.09 to 41.28 AU) and sebum content (26.75 to 5.67 mg/cm²). Dermatokinetic analysis revealed higher skin retention of C. odorata in the NE (epidermis: 71.266 µg/cm², dermis: 60.179 µg/cm²) compared to conventional formulations. CCRD optimization yielded NE formulations with the desired particle size (195.64 nm), entrapment efficiency (85.51%), and zeta potential (−20.59 mV). In vitro release studies indicated sustained release behavior, and antioxidant and antimicrobial properties were observed. This study demonstrates the stability, skin-friendliness, therapeutic benefits, and controlled release properties of the NE. The NE presents a promising option for various topical applications in treating bacterial and fungal diseases, potentially enhancing drug delivery and treatment outcomes in pharmaceuticals and cosmetics. Full article