Bortezomib (BTZ) is a potent anticancer agent whose clinical application is limited by poor aqueous solubility. We engineered a sulfobutylether-β-cyclodextrin (SBE-β-CD) inclusion complex via aqueous complexation and freeze-drying to enhance BTZ solubility and therapeutic performance. Phase solubility analysis demonstrated a 25.7-fold increase in BTZ solubility at a 1:20 molar ratio (F1), in 25 °C. Complex formation was confirmed by differential scanning calorimetry (DSC) and Fourier-transform infrared (FTIR) spectroscopy. The F1 formulation exhibited sustained drug release at physiological pH of 7.4. Although F1 showed slightly reduced in vitro cytotoxicity compared with conventional BTZ (cBTZ) in C26 and U266 cell lines, it significantly improved in vivo antitumor efficacy in C26 tumor-bearing mice, achieving a tumor growth delay (TGD) of 52.14% versus 29.34% for cBTZ. Furthermore, a calcein/SBE-β-CD complex (F1', 1:20 molar ratio, as a fluorescent model drug) demonstrated enhanced cellular uptake and tumor accumulation in C26 tumor-bearing mice. These findings highlight SBE-β-CD as a promising platform for BTZ encapsulation, enabling improved drug delivery and anticancer efficacy and merits further investigation.
This study aimed to prepare and characterize Diosmin-loaded nanostructured lipid carriers (Diosmin-NLCs) as a novel antioxidant formulation for topical drug delivery. Diosmin-NLCs were prepared and characterized for particle size, zeta potential, stability, crystal properties, morphology, and encapsulation efficiency (EE
Palmitoyl tripeptide-38 (PT-38) is a bioactive signal peptide widely used in topical anti-aging formulations. PT-38 stimulates fibroblast proliferation and extracellular matrix (ECM) synthesis; however, its clinical efficacy is limited and inevitably leads to poor stability and insufficient skin permeability. In the present study, a citrate-buffered nano-liposomal formulation of PT-38 (LC-PT-38) was developed to enhance peptide stability, skin penetration, and biological activity against UVB-induced skin damage. Liposomes were prepared using a fusion method and characterized regarding particle size, zeta potential, encapsulation efficiency, rheological behavior, and long-term stability. The optimized formulation was exhibited and characterized for desirable size (68.6±7.07 nm), PDI (0.28±0.01), zeta potential (-28.60±6.30 mV), encapsulation efficiency (approximately complete encapsulation), pseudoplastic behavior, and high stability with the absence of microbial growth. Franz diffusion indicated appropriate skin penetration in comparison with conventional cream. Biological evaluation revealed that LC-PT-38 significantly promoted fibroblast proliferation, accelerated wound closure, reduced intracellular reactive oxygen species (ROS), and enhanced collagen synthesis in HFFF-2 and HaCaT without inducing cytotoxicity. In a UVB-induced BALB/c mouse model of photoaging, topical administration of LC-PT-38 preserved dermal collagen architecture, reduced epidermal thickness, and attenuated wrinkle formation in both preventive and therapeutic settings. These findings demonstrate that nano-liposomal encapsulation significantly potentiates the antioxidant, regenerative, and collagen-stimulating activities of PT-38 through improved dermal delivery. LC-PT-38 represents a promising transdermal nanotherapeutic platform for the prevention and treatment of photoaging-associated skin degeneration.
This paper investigates the insertion of dissolvable microneedles into skin, which is a challenging topic in the design and application of dissolvable microneedles. Traditionally, this phenomenon has been evaluated through mechanical tests and experimental studies. To address this issue, this paper presents mathematical equations for predicting the insertion of pyramid shape dissolvable microneedles into skin by comparing the failure (buckling) force, which causes microneedle deformation, with the insertion force required for penetration. These equations enable the prediction of microneedle insertion into skin without necessitating microneedle fabrication. The derivation of these equations employed both analytical studies and numerical simulations using ABAQUS software based on the Finite Element Method (FEM). To validate the proposed equations, experimental investigations were also performed on microneedle insertions; obtained results were aligned closely with outcomes predicted by the equations. The results indicate that the insertion of dissolvable microneedles into skin is influenced by the geometry and the mechanical properties of the microneedle. Additionally, a key finding of this study is that the effects of additives and active pharmaceutical ingredients (APIs) must be considered when assessing the insertion of dissolvable microneedles into skin. Additionally, the findings have been distilled into general statements that encapsulate the core principles, offering practical recommendations and design considerations for researchers to enhance the likelihood of successful microneedle insertion. To further assist researchers in utilizing the presented equations, a proposed protocol is provided, serving as a roadmap for effectively applying the information presented.
To prepare, characterize, and clinically evaluate postbiotic creams containing Lactobacillus ferment lysate in pediatric patients with atopic dermatitis (AD). After preparing different formulations, the formulations were evaluated for stability and physicochemical properties for semisolids, such as physical properties, viscosity, temperature cycle, and pH. Finally, a formulation that showed better physical properties was chosen for further investigation. A randomized clinical trial study was performed with AD referred to the outpatient allergy clinic. The primary outcomes were assessed with the SCORAD index and changes in the proportion of children with clinical improvement/no improvement, deterioration, and recurrence rate. A total of 52 patients (27 vs 25 participants in intervention and placebo groups) were recruited in the study. The pH of creams was 6.00 ± 0.02, which is safe for human skin. In addition, the centrifugation test showed that this formulation was completely homogeneous after centrifugation. The temperature cycle test indicated no change in the structure of the cream. After a 2-month follow-up, the mean SCORAD score was 50 ± 14.5 at baseline and 27.8 ± 10 at the final visit in the postbiotic group. It was also 43 ± 12 at baseline and 28.2 ± 6 at the final visit in the placebo group. After 4 months, 11 patients had a recurrence in lesions: 2 (6.9%) in the postbiotic group, versus 9 (30%) in the placebo group. This study demonstrated that postbiotic formulation is cutaneously acceptable and showed a clinically significant improvement, especially in long-term follow-up.
Introduction:Lawsone (LWS), a naphthoquinone dye known for its anticancer properties, faces challenges with aqueous solubility, which restricts its therapeutic use. Solid lipid nanoparticles (SLNs) are recognized for enhancing the bioavailability of poorly soluble drugs, supporting in targeted drug delivery and reducing toxicity to normal tissues. The purpose of this study was to develop chitosan-coated solid lipid nanoparticles that were loaded with lawsone and conjugated with the AS1411 aptamer (LWS-SLN-Chit-Apt) for evaluating the cytotoxic effects on mouse colon adenocarcinoma cells (C26). Methods:High-shear homogenization and ultrasound methods were used for producing the LWS-SLNs nanoparticles. Several considerations, including dynamic light scattering (DLS), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR), were directed to characterize the properties of the nanoparticles. Next, the nanoparticles were coated with chitosan, then conjugated to AS1411 aptamer, which was confirmed with DLS and gel electrophoresis. Additionally, the encapsulation efficiency of LWS and its release profile were investigated. Cytotoxicity and cellular uptake were evaluated on C26 cells and Chinese hamster ovary (CHO) cells. Results:The LWS-SLNs and LWS-SLN-Chit-Apt formulations revealed particle sizes of 160±14.8 nm and 350±22.5 nm, with encapsulation efficiencies of 70.72±2.64% and 70.00±4.3%, respectively. Both formulations exhibited a sustained drug release profile over 120 hours. Targeted nanoparticles displayed higher cellular uptake and cytotoxicity in nucleolin-positive cells (C26 cells) compared to nucleolin-negative cells (CHO cells), with no substantial differences observed. Conclusion:These results illustrated that LWS-SLN-Chit-Apt could be considered as a great candidate for further studies and in vivo trials.
Background:: Commercial Minoxidil (MXD) is commonly used as a vasodilator agent of hair follicles for providing direct dermal papilla cell proliferation and consequently enhancing the rate of hair growth. Objective:: The current study attempted to improve the bioactivity and water solubility of MXD by producing nanocrystal structures and investigating the obtained hair growthstimulating activity on C57BL/6 mice. Method:: The MXD nanoparticles (MXD-NPs) were prepared through a bead mill and ultrasonic process and characterized by DLS, XRD, UV-Vis, FTIR, FESEM, TEM, and Zeta-potential techniques. Result:: The cytotoxicity of MXD-NPs was studied on human dermal fibroblast (HDF) by MTT assay. Lastly, we analyzed the comparative hair growth inductive activity of certain MXD-NPs concentrations on C57BL/6 mice. The stabled MXD-NPs (-46 mV, 21.9 nm) caused a significant increase in the hair growth rate of C57BL/6 mice by running a safe site-specific delivery mechanism on the targeted pilosebaceous follicles when compared to MXD. Conclusion:: The MXD-NPs-receiving mice exhibited a greater rate of anagen/telogen follicular when compared with MXD-treated types, which verified the improvement of their hair re-growing and follicular-stimulative activities. Therefore, these outcomes confirmed the potential of MXD-NPs for substituting its commercial solution format as a safe and efficient iso-formulation structure.
Effective acne treatment is critical due to its profound impact on physical and psychological well-being. It was shown that severe systemic side effects, including teratogenicity, ovarian reserve reduction, depression, dry skin, hypertriglyceridemia, and intracranial hypertension limited oral isotretinoin usage. Therefore, this study addresses these challenges by developing isotretinoin-loaded lipid liquid crystal (LLC-IT) nanoparticles for topical application, aiming to enhance localized delivery while minimizing systemic exposure. LLC-IT nanoparticles were prepared using a top-down method and evaluated for their physicochemical properties, photostability, cytotoxicity, antimicrobial activity, in-vitro drug release, and in-vivo therapeutic efficacy. A testosterone-induced acne mouse model was used to compare LLC-IT treatment with untreated and commercial isotretinoin gel-treated groups. LLC-IT nanoparticles exhibited a uniform particle size (69.57 ± 0.51 nm), low polydispersity index (0.264 ± 0.01), and stable zeta potential (- 19.3 ± 0.2 mV). High encapsulation efficiency (95% ± 3) and effective loading capacity (1.15% ± 0.13) were achieved. Drug release was diffusion-controlled with minimal UV-induced degradation. Stability assessments over 12 months confirmed consistent properties across varying storage temperatures. LLC-IT displayed significant antibacterial activity and reduced skin irritation in Draize tests compared to commercial gels. In-vivo , LLC-IT reduced inflammation significantly more than untreated or commercial gel-treated groups, indicating enhanced therapeutic efficacy of LLC-IT formulation. The isotretinoin-loaded lipid liquid crystal formulation shows superior stability and efficacy with reduced side effects compared to conventional treatments, offering a more effective and patient-friendly solution, as well as a promising alternative for industrial production in acne management. Graphical Abstract
BACKGROUND:Alleviating inflammation should be considered as one of the first steps of the treatment plan in patients with acute rotator cuff related shoulder pain (RCRSP). OBJECTIVE:To compare the effects of triamcinolone/lidocaine ultrasonophoresis, injection on pain, disability, and quality of life in patients with acute RCRSP. METHODS:A total of 28 acute RCRSP patients were randomly allocated into two groups of ultrasonophoresis and injection. Both groups received vitamin C and shoulder care education for 10 days and then were subjected to therapeutic interventions. Ultrasonophoresis group received triamcinolone (16 mg) and lidocaine (2mg) using ultrasonophoresis (frequency: 3 MHz, intensity: 1.50 W/Cm2), while the injection group received a single subacromial injection of triamcinolone (80 mg) and lidocaine (10 mg). The main outcomes measures were pain assessed by two scales (visual analog scale), and shoulder pain and disability index (SPADI), disability (SPADI), and quality of life (Western Ontario rotator cuff questionnaire). RESULTS:Although the main effect of time was statistically significant for all dependent variables (P< 0.01), no significant interaction was found between group and time (P-value (0.12-0.55)). The ultrasonophoresis effect, size for pain, disability, and quality of life were 2.58, 1.43, 1.78, and 1.35, respectively. The injection effect, size for pain, disability, and quality of life were 1.98, 2.02, 1.40, and 1.60, respectively. CONCLUSIONS:Triamcinolone/lidocaine ultrasonophoresis demonstrated similar outcomes to injection in reducing pain, improving disability, and enhancing quality of life in patients with acute RCRSP in short time. According to our findings, ultrasonophoresis with triamcinolone/lidocaine cream is as effective as triamcinolone/lidocaine injection and can be proposed as a potential adjunctive treatment for patients with acute RCRSP.
BACKGROUND:Drug resistance has been a problem in cancer chemotherapy, which often causes shortterm effectiveness. Further, the literature indicates that telomere G-quadruplex could be a promising anti-cancer target. OBJECTIVE:We synthesized and characterized two new pyrimidine derivatives as ligands for G-quadruplex DNA. METHODS:The interaction of novel non-cationic and cationic pyrimidine derivatives (3a, b) with G-quadruplex DNA (1k8p and 3qsc) was explored by circular dichroism (CD) and ultraviolet-visible spectroscopy and polyacrylamide gel electrophoresis (PAGE) methods. The antiproliferative activity of desired compounds was evaluated by the MTT assay. Apoptosis induction was assessed by Propidium iodide (P.I.) staining and flow cytometry. Computational molecular modeling (CMM) and molecular dynamics simulation (MD) were studied on the complexes of 1k8p and 3qsc with the compounds. The van der Waals, electrostatic, polar solvation, solventaccessible surface area (SASA), and binding energies were calculated and analyzed. RESULTS:The experimental results confirmed that both compounds 3a and 3b interacted with 1k8p and 3qsc and exerted cytotoxic and proapoptotic effects on cancer cells. The number of hydrogen bonds and the RMSD values increased in the presence of the ligands, indicating stronger binding and suggesting increased structural dynamics. The electrostatic contribution to binding energy was higher for the cationic pyrimidine 3b, indicating more negative binding energies. CONCLUSION:Both experimental and MD results confirmed that 3b was more prone to form a complex with DNA G-quadruplex (1k8p and 3qsc), inhibit cell growth, and induce apoptosis, compared to the non-cationic pyrimidine 3a.
We developed novel and optimal Q10-NLC/SLN formulations as antioxidant and anti-tyrosinase agents. The formulations were analyzed for particle size, morphology, entrapment efficiency (EE %), and long-term stability. The in vitro drug release and in vivo skin penetration were evaluated using dialysis bag diffusion and Sprague Dawley (SD) rats, respectively. Cytotoxicity and protecting effects were assessed by AlamarBlue (R) assay, ROS level by DCFH-DA, and tyrosinase activity by L-DOPA assay, measuring the absorbance at 470 nm. The selected formulations had optimal surface characterizations, including Z-average size, PDI, and Zeta potential ranging from 125 to 207 nm, 0.09-0.22, and -7 to -24, respectively. They also exhibited physiochemical stability for up to 6 months and EE% above 80 %. The lipids ratio and co-Q10 amount as variable factors significantly affected particle size and zeta potential but were insignificant on PDI. The in vitro release diagram showed that Q10-NLC/SLN revealed a fast release during the first 8 h and prolonged release afterward. The in vivo skin permeation revealed a higher accumulative uptake of co-Q10 in the skin for Q10-NLC/SLN compared to Q10 emulsions. Both selected Q10-NLC and Q10-SLN could reduce intracellular ROS after exposure to H2O2. The Q10-NLC was found to be more potent for inhibiting the tyrosinase activity compared to O10-SLN. The results suggest that the new formulations are promising carriers for topical delivery of co-Q10 as an anti-aging and skin-whitening agent.
Hair loss and hirsutism have been major complaints due to increased concentrations of dihydrotestosterone. The plant Platycladus orientalis, with 5-alpha reductase inhibitor properties, has been used to treat these disorders. Its formulation with lipophilic carriers in SLN possesses high loading capacity and greater permeability to hair follicles. The present study aimed to determine the content of active ingredients in the extract of P. orientalis L. and to prepare and characterize the solid lipid nanoparticles (SLN) of Platycladus orientalis L. extract as a 5-alpha reductase inhibitor. The total methanolic extract was obtained following the maceration technique. This preparation was analyzed by HPLC using Quercetin and Cedrol as standard components. SLNs were prepared by high-shear homogenization and ultrasound. Four Glucire-GMS-Compritol-Precirol lipids and three poloxamer-tween80-Labrasol surfactants were further used in the formulations. Particle size, zeta potential, nanoparticle morphology, encapsulation percentage, crystal structure, physical stability, size, and zeta potential were studied 0, 3, and 6 months after preparation. Within 1-7 days after preparation, formulations containing GMS and compritol lipids became solid and jelly. Meanwhile, the formulations with Precirol as the lipid and Poloxamer as the surfactant with 0.3% extract exhibited desirable properties such as average particle size (192 nm), the encapsulation of the extract inside the nanoparticles was almost 71%, and good zeta potential. This formulation containing precirol as a lipid, poloxamer as a surfactant, and 0.3% plant extract exhibited greater 5-alpha reductase inhibitor activity, and it can be recommended to treat hair loss and hirsutism.
The cherry tomato is a nutritious product commonly used in salads or consumed as a dietary supplement. However, improper storage after harvesting can lead to a decrease in its quality and shelf-life. In this study, we aimed to assess the effects of free essential oil of Mentha x Piperita L. and solid lipid nanoparticles containing free essential oil at concentrations of 0.025%, 0.05%, 0.075%, 0.1%, and 0.2% on the microbial load and post-harvest quality of Solanum lycopersicum cv. Santiago F1 during 28 days of storage at 8 degrees C. Fruits coated with solid lipid nanoparticles containing essential oil at 0.075%, 0.1%, and 0.2% maintained their quality attributes, including firmness at approximately 50%, ascorbic acid at about 80%, phenolic compounds, color parameters, antioxidant activity at around 71%, and sensory properties compared to the control groups or fruits treated with free essential oil of Mentha x Piperita L. This coating also effectively suppressed cellulase and polyphenol oxidase activity, reducing microbial load and weight loss percentages to under 10%. However, it's important to note that fruits coated with free essential oil of Mentha x Piperita L. at 0.1% and 0.2% showed visible tissue damage. Our research demonstrated that the combination of solid lipid nanoparticles and free essential oil of Mentha x Piperita L. resulted in a decrease in microbial load, an extension of shelf-life, and improvements in the quality characteristics of cherry tomato fruits.
Due to its involvement in skin maintenance and repair, topical administration of recombinant human growth hormone (rhGH) is an interesting strategy for therapeutic purposes. We have formulated and characterized a topical rhGH-loaded liposomal formulation (rhGH-Lip) and evaluated its safety, biological activity, and preventive role against UVB-induced skin damage. The rhGH-Lip had an average size and zeta potential of 63 nm and -33 mV, respectively, with 70 % encapsulation efficiency. The formulation was stable at 4 °C for at least one year. The SDS-PAGE and circular dichroism results showed no structural alterations in rhGH upon encapsulation. In vitro, studies in HaCaT, HFFF-2, and Ba/F3-rhGHR cell lines confirmed the safety and biological activity of rhGH-Lip. Franz diffusion cell study showed increased rhGH skin permeation compared to free rhGH. Animal studies in nude mice showed that liposomal rhGH prevented UVB-induced epidermal hyperplasia, angiogenesis, wrinkle formation, and collagen loss, as well as improving skin moisture. The results of this study show that rhGH-Lip is a stable, safe, and effective skin delivery system and has potential as an anti-wrinkle formulation for topical application. This study also provides a new method for the topical delivery of proteins and merits further investigation.
Fungal rot is a major global health concern, particularly in delicate and soft-textured fruits such as strawberries. This study aimed to assess the effectiveness of coatings containing different levels of free essential oil of Mentha x piperita L. (MEO) and solid lipid nanoparticles carrying MEO (MEO-SLNs) on the microbial load, storage quality, and shelf life of strawberries (Fragaria x ananassa cv. Camarosa) for 20 days at 8 degrees C. The study evaluated several factors, including weight loss, firmness, color, ascorbic acid, phenolic content, antioxidant activity, microbial load, cellulase, catalase, polyphenol oxidase, and sensory properties at regular intervals. The results indicated that strawberries treated with MEO-SLN at a concentration of 0.2% exhibited the lowest weight loss (approximately 78%), the highest firmness (around 45%), the greatest antioxidant activity (about 98%), and the highest ascorbic acid content (approximately 41%) compared to the control group. This treatment also preserved the levels of total phenol and catalase activity, reduced the activity of cellulase and polyphenol oxidase, and delayed color development. Furthermore, strawberries treated with MEO-SLN at a concentration of 0.2% received higher ratings for texture firmness, freshness, taste, appearance, and overall acceptance, and showed a lower number of cfu (colony-forming units) on day 20 of storage. MEO-SLN treatments showed no signs of soft spoilage in artificially contaminated strawberries during storage. These findings suggest that the use of MEO-SLN coatings can effectively maintain the postharvest quality of strawberries, decrease spoilage, and extend the shelf life and nutritional value of the fruits during cold storage.
Purpose: Melasma is a persistent skin condition caused by excessive melanin production, particularly affecting women’s quality of life. It can result from various factors like sun exposure, genetics, hormones, medications, or inflammation. Effective melasma treatment requires products that can deeply penetrate the skin. The outermost skin layer, known as the stratum corneum (SC), plays a crucial role in delivering topical and transdermal drugs. Researchers have developed numerous strategies to enhance skin permeability and drug efficacy. Methods: This review delves into energy-based techniques and nanocarrier systems for treating melasma, specifically focusing on improving drug delivery to the viable epidermis (EP) while overcoming the SC barrier. Results: Physical methods offer benefits such as enhanced skin penetration but come with drawbacks like frequent visits, high costs, and the need for specialized equipment and skilled operators. Microneedle patches are gaining attention as a convenient physical treatment option for delivering multiple medications effectively, offering targeted delivery and minimal side effects. Nanocarrier systems like transferosomes demonstrate promise in enhancing skin penetration for treating melasma and skin hyperpigmentation. While they offer advantages such as high drug entrapment and improved bioavailability, challenges like stability issues and scalability hinder their widespread adoption. Conclusion: Energy-based techniques enhance drug penetration but can lead to scarring and burns, while dissolvable micro-needles offer a convenient and effective alternative. Nano-drug carriers, like nanostructured lipid carriers (NLCs) and transferosomes, show promise for improved skin drug delivery with their flexible structures and enhanced penetration capabilities, yet further clinical research is needed for definitive conclusions
Nanoencapsulation of essential oils is a promising strategy for extending their antifungal activity and addressing evaporation and decomposition in unfavorable environmental conditions. This research aimed to synthesize and compare the physical properties of solid lipid nanoparticles (SLNs) containing peppermint essential oil (PE) during 12 months of storage at various temperatures (4°C, 25°C, 27°C with 60% relative humidity, 37°C, and 40°C with 75% relative humidity), and to investigate their antifungal activity compared to free PE. The SLN formulations were prepared using high-shear homogenization and ultrasound techniques and were analyzed using a particle size analyzer, differential scanning calorimetry, transmission electron microscopy, and microscopic images of fungal mycelium to assess encapsulation efficacy. The results showed that the PE-SLNs had a size of 164.2 ±5.8 nm, a PDI value of 0.176 ±0.01, a zeta potential value of –11.3 mV, and an encapsulation percentage of approximately 75 ±0.5%. Overall, the physical properties of the formulations showed a slight and acceptable increase over the 12-month storage period at all investigated temperatures. Furthermore, the in vitro inhibition percentage of free PE at a concentration of 2000 μL L–1 against Penicillium italicum and P. digitatum was 66.7% ±2.6 and 66.8% ±0.8, respectively, while for PE-SLNs it was 88.8% ±0.9 and 89.9% ±1.4. These results demonstrate the potential of SLNs as an effective carrier for sustained delivery of PE with improved antifungal activity during storage.
PURPOSE:This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation. METHODS:Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using Dynamic Light Scattering (DLS). The best formulation was chosen for further surface characterization, including Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), and Fouriertransform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation. RESULTS:Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic. CONCLUSION:The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.
This study aimed to enhance the effectiveness and water solubility of Minoxidil (MXD) by producing its nanocrystal structure, which improves its vasodilator properties and promotes hair growth. In the current study, the hair growth-stimulating activity of the MXD nanoparticles (MXD-NPs) was compared with the hydroethanolic rosemary (RSY) extract on the C57BL/6 mice. The MXD-NPs were produced through a bead mill and ultrasonic process and characterized using various techniques. The cytotoxicity of MXD-NPs was studied on human dermal fibroblasts, and their hair growth-stimulating activity was analyzed in C57BL/6 mice. The results showed that MXD-NPs significantly increased the hair growth rate in mice compared to commercial MXD and hydroethanolic rosemary extract as they were delivered safely and specifically to the target pilosebaceous follicles. The follicular uptake of MXD-NPs was also increased compared to commercial MXD, leading to improved pilosebaceous follicle re-growth and hair growth in treated mice. Therefore, MXD-NPs have the potential to be a safe and efficient iso-formulation structure for hair growth promotion.