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1.
Front Pharmacol ; 15: 1353791, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38606182

RESUMO

Fungal infections are of major concern all over the globe, and fluconazole is the most prevalently used drug to treat it. The goal of this research work was to formulate a fluconazole-embedded transfersomal gel for the treatment of fungal infections. A compatibility study between fluconazole and soya lecithin was performed by differential scanning calorimetry (DSC). Transfersomes were formulated by a thin-film hydration technique using soya lecithin and Span 80. A central composite design was adopted to prepare different formulations. Soya lecithin and Span 80 were chosen as independent variables, and the effect of these variables was studied on in vitro drug diffusion. Formulations were evaluated for entrapment efficiency and in vitro drug diffusion. The results of in vitro drug diffusion were analyzed using the analysis of variance (ANOVA) test. Optimized formulation was prepared based on the overlay plot and evaluated by scanning electron microscopy, DSC, vesicle size, polydispersity index (PDI), zeta potential, and in vitro drug diffusion studies. An optimized formulation was loaded into xanthan gum gel base and evaluated for pH, viscosity, in vitro and ex vivo drug diffusion, and antifungal activity. DSC studies revealed compatibility between fluconazole and soya lecithin. Entrapment efficiency and in vitro drug diffusion of various formulations ranged between 89.92% ± 0.20% to 97.28% ± 0.42% and 64% ± 1.56% to 85% ± 2.05%, respectively. A positive correlation was observed between in vitro drug diffusion and Span 80; conversely, a negative correlation was noted with soya lecithin. Entrapment efficiency, particle size, zeta potential, PDI, and drug diffusion of optimized formulation were 95.0% ± 2.2%, 397 ± 2 nm, -38 ± 5 mV, 0.43%, and 81 % ± 2%, respectively. SEM images showed well-distributed spherical-shaped transfersomes. In vitro, ex vivo drug diffusion and antifungal studies were conclusive of better diffusion and enhanced antifungal potential fluconazole in transfersomal formulation.

3.
J Ethnobiol Ethnomed ; 20(1): 39, 2024 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-38519994

RESUMO

Traditional cosmetics play a significant role in the cultural practices and personal hygiene of many ethnic groups worldwide. The Oromo, an indigenous community in Ethiopia, has a rich history of utilizing local plants for cosmetic purposes. However, the use of plants as traditional cosmetics has only been poorly investigated as more emphasis was given to traditional medicines. The study thus aimed to identify and document plant species, and parts used in traditional cosmetics and associated knowledge, and practices among Oromo women in the Madda Walabu district, Southeastern Ethiopia. A total of 150 Oromo women were interviewed to gather ethnobotanical information including the plant species used for cosmetics, their preparation methods, and their applications. Ethnobotanical indices were computed to determine the most important species used by the women. A total of 48 plant species belonging to 31 families used as sources of traditional cosmetics were recorded. Most of these plants were trees. Leaves were the most commonly used plant part in traditional cosmetics, and maceration and decoction were the most common preparation methods applied to prepare traditional cosmetics. Topical application of traditional cosmetics was the most common, while oral infusions were rarely reported type of administration. All categories had high informant consensus factor (ICF) values, ranging from 0.80 to 0.98. The highest ICF value was found for skin treatment, followed by the hair, and face mask. Overall, Commiphora habessinica, Gnidia stenophylla, Kalanchoe lanceolata, Mimusops kummel, Sesamothamnus rivae, Terminalia brownii, T. laxiflora, Acacia drepanolobium, A. mellifera, and Aloe citrina were the most frequently cited and culturally important plants by Oromo women for traditional cosmetics in the area. The study highlights the importance of local plant resources for maintaining cultural practices and personal hygiene. However, the cultural heritage associated with traditional cosmetics is facing threats from various factors. Therefore, a continuous effort to document and disseminate knowledge about traditional cosmetics practices to ensure their preservation and transmission and awakening younger generations about the importance of traditional cosmetics and their role in cultural heritage is crucial.


Assuntos
Etnobotânica , Plantas Medicinais , Humanos , Feminino , Fitoterapia , Etiópia , Medicina Tradicional
4.
J Pharmacol Sci ; 154(4): 326-333, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38485351

RESUMO

PURPOSE: To determine whether combination of topical ripasudil and brimonidine has more effective neuroprotection on retinal ganglion cells (RGCs) following injury to axons composing the optic nerve. METHODS: Topical ripasudil, brimonidine, or mixture of both drugs were administered to adult mice after optic nerve injury (ONI). The influence of drug conditions on RGC health were evaluated by the quantifications of surviving RGCs, phosphorylated p38 mitogen-activated protein kinase (phospho-p38), and expressions of trophic factors and proinflammatory mediators in the retina. RESULTS: Topical ripasudil and brimonidine suppressed ONI-induced RGC death respectively, and mixture of both drugs further stimulated RGC survival. Topical ripasudil and brimonidine suppressed ONI-induced phospho-p38 in the whole retina. In addition, topical ripasudil suppressed expression levels of TNFα, IL-1ß and monocyte chemotactic protein-1 (MCP-1), whereas topical brimonidine increased the expression level of basic fibroblast growth factor (bFGF). CONCLUSIONS: Combination of topical ripasudil and brimonidine may enhance RGC protection by modulating multiple signaling pathways in the retina.


Assuntos
Isoquinolinas , Traumatismos do Nervo Óptico , Sulfonamidas , Camundongos , Animais , Tartarato de Brimonidina , Traumatismos do Nervo Óptico/tratamento farmacológico , Traumatismos do Nervo Óptico/metabolismo , Neuroproteção , Combinação de Medicamentos
5.
Heliyon ; 10(6): e28096, 2024 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-38545140

RESUMO

Objective: To systematically evaluate the efficacy and safety of topical application of botanical (TAB) adjuvants in the treatment of melasma and provide evidence-based medical evidence for their clinical application. Methods: Medline, Web of Science, EMBASE, Cochrane Library, CNKI, VIP, Wanfang Data, and SinoMed, databases were searched to identify all randomized controlled clinical trials on TAB adjuvant treatment for melasma from inception to May 2023. The primary outcomes included clinical efficacy, adverse effects, recurrence rate, and melanin index. Subgroup analyses were performed using the Melasma Area Severity Index (MASI) scores. Results: This study included 16 randomized trials with 1386 participants. Eligible trials demonstrated that topical phytomedicine adjuvant treatment for melasma increased clinical effectiveness (RR = 1.14, 95% CI (1.10, 1.19), P <0.00001), decreased recurrence rate (RR = 0.28, 95% CI (0.13, 0.59), P = 0.0009), and decreased melanin index (MI) (MD = -22.2,95% CI (-31.79, -12.61), P < 0.00001). In addition, subgroup analysis showed that topical phytomedicines reduced MASI scores (I2 = 0%, MDI = -0.95, 95% CI (-1.23,0.67), P < 0.00001), but when scored as the rate of decrease in MASI, topical phytomedicines had high MASI scores (I2 = 15%, MD = 0.3, 95% CI (0, 0.59), P = 0.05), indicating a slower rate of melasma mitigation when botanicals were applied topically. Although burning pain, redness and other mild adverse reactions may occur during the treatment period, they can be recovered on their own, and there is no statistical significance in the comparison of the two groups (RR = 0.95, 95% CI (0.42, 2.51), P = 0.91). Conclusion: TAB for melasma has a clear adjuvant clinical efficacy, a low recurrence rate, and does not cause serious adverse effects. An appropriate administration method may achieve better efficacy; however, this requires further verification.

6.
Dermatol Ther (Heidelb) ; 14(2): 521-532, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38345680

RESUMO

INTRODUCTION: Involvement of the scalp is common in psoriasis and severely affects the quality of life of those affected. It is difficult to treat and places special demands on the galenics of a drug formulation. Tacrolimus is a calcineurin inhibitor and is approved as an ointment formulation for the treatment of atopic dermatitis. The efficacy and safety of topically applied tacrolimus have also been studied and proven for psoriasis. However, no proprietary pharmaceutical product is currently approved for this indication. METHODS: A multicenter, double-blind, vehicle-controlled phase 3 study was conducted to evaluate the efficacy and safety of 0.1% tacrolimus microemulsion when applied topically twice daily in 128 patients independently of sex with scalp psoriasis. RESULTS: The primary efficacy analysis showed a scalp Investigator Global Assessment (s-IGA) of 0 (absence of disease) or 1 (very mild disease) at 8 weeks in 28.6% of subjects in the tacrolimus group, indicating a significantly better response (p = 0.0476, chi-square test) versus 12.7% of subjects in the placebo group (difference of 15.9%-points). The Dermatology Life Quality Index (DLQI) improved over time and was more pronounced in the group treated with tacrolimus-containing microemulsion than in the placebo group, but showed no statistically significant difference after 8 weeks of use (p = 0.193, ANCOVA). The safety analysis revealed no evidence of cutaneous side effects other than those known. Toxicologically relevant serum levels of tacrolimus could be excluded. CONCLUSION: The study data show that 0.1% tacrolimus microemulsion has good efficacy and safety in the treatment of scalp psoriasis.

7.
Allergol Int ; 73(2): 323-331, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38350816

RESUMO

BACKGROUND: Selective activator protein (AP)-1 inhibitors are potentially promising therapeutic agents for atopic dermatitis (AD) because AP-1 is an important regulator of skin inflammation. However, few studies have investigated the effect of topical application of AP-1 inhibitors in treating inflammatory skin disorders. METHODS: Immunohistochemistry was conducted to detect phosphorylated AP-1/c-Jun expression of skin lesions in AD patients. In the in vivo study, 1 % T-5224 ointment was topically applied for 8 days to the ears of 2,4 dinitrofluorobenzene challenged AD-like dermatitis model mice. Baricitinib, a conventional therapeutic agent Janus kinase (JAK) inhibitor, was also topically applied. In the in vitro study, human epidermal keratinocytes were treated with T-5224 and stimulated with AD-related cytokines. RESULTS: AP-1/c-Jun was phosphorylated at skin lesions in AD patients. In vivo, topical T-5224 application inhibited ear swelling (P < 0.001), restored filaggrin (Flg) expression (P < 0.01), and generally suppressed immune-related pathways. T-5224 significantly suppressed Il17a and l17f expression, whereas baricitinib did not. Baricitinib suppressed Il4, Il19, Il33 and Ifnb expression, whereas T-5224 did not. Il1a, Il1b, Il23a, Ifna, S100a8, and S100a9 expression was cooperatively downregulated following the combined use of T-5224 and baricitinib. In vitro, T-5224 restored the expression of FLG and loricrin (LOR) (P < 0.05) and suppressed IL33 expression (P < 0.05) without affecting cell viability and cytotoxicity. CONCLUSIONS: Topical T-5224 ameliorates clinical manifestations of AD-like dermatitis in mice. The effect of this inhibitor is amplified via combined use with JAK inhibitors.


Assuntos
Azetidinas , Benzofenonas , Dermatite Atópica , Isoxazóis , Purinas , Pirazóis , Sulfonamidas , Animais , Humanos , Camundongos , Citocinas/metabolismo , Dermatite Atópica/metabolismo , Inflamação/tratamento farmacológico , Interleucina-33 , Pele/patologia , Fator de Transcrição AP-1/antagonistas & inibidores
8.
Int J Mol Sci ; 25(3)2024 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-38338918

RESUMO

Due to prolonged forced positioning, the incidence of intraoperative pressure injuries is high. This study aimed to explore the impact of small-molecule antiplatelet drugs on pressure injuries by locally applying them before an injury occurs. In the first part of this study, water-soluble tracers with different molecular weights were applied to normal and early-stage pressure-injured skin. Through digital cameras, spectrophotometers, and histological observations, the penetration of tracers into the epidermis was clarified. In the second part of this study, a water-soluble antiplatelet drug called Trapidil (molecular weight = 205 Da) was applied to the left side of the back of a rat before, during, and after compression, and the contralateral side served as a non-intervention control group. The differences in pressure injuries between the two groups were observed through a digital camera, an ultraviolet camera, and temperature measurement, and skin circulation and perfusion were assessed via an intravenous injection of Evans Blue. The first part of this study found that water-soluble tracers did not easily penetrate normal skin but could more easily penetrate pressure-damaged skin. The smaller the molecular weight of the tracer, the easier it penetrated the skin. Therefore, in the next step of research, water-soluble drugs with smaller molecular weights should be selected. The second part of this study found that, compared with the control group, the occurrence rates and areas of ulcers were lower, the gray value was higher, and the skin temperature was lower in the Trapidil group (p < 0.05). After the intravenous Evans Blue injection, skin circulation and perfusion in the Trapidil group were found to be better. In conclusion, this study found that the topical skin application of a small-molecule antiplatelet agent may have significant effects against pressure injuries by improving post-decompression ischemia, providing new insights into the prevention and treatment of intraoperative pressure injuries.


Assuntos
Lesões por Esmagamento , Lesão por Pressão , Trapidil , Ratos , Animais , Inibidores da Agregação Plaquetária/farmacologia , Inibidores da Agregação Plaquetária/uso terapêutico , Lesão por Pressão/tratamento farmacológico , Trapidil/farmacologia , Azul Evans/farmacologia , Pele , Água/farmacologia
9.
Eur J Pharm Sci ; 195: 106636, 2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38185273

RESUMO

Doxycycline hyclate (DOXH) is a broad-spectrum antibiotic derived synthetically from tetracycline. Despite its use in clinical practice for more than 40 years, DOXH remains an effective antibiotic with retained activity. The potential advantages of DOXH for wound healing therapy include its mechanisms of action, such as anti-inflammatory effects, antioxidant properties, modulation of cellular processes, stimulation of collagen synthesis, and antimicrobial activity. As current standards of care aim to improve wound healing by promoting rapid closure, a relevant direction is the development of novel DOXH formulations for parenteral delivery that enhance both skin regeneration and control of infectious conditions. Oral delivery is the most common and commercially available route for administering DOXH therapeutic agents. However, parenteral delivery of DOXH, where the antibiotic substance is not in a solid state (as in powdered or compressed solid form) but rather dissolved in any carrier, presents challenges regarding DOX solubility and the stability of DOXH solutions, which are major factors complicating the development of new formulations for parenteral administration. This review discusses the achievements in research strategies and the development of new pharmaceutical formulations for the delivery of doxycycline in the treatment of wounds of various etiologies.


Assuntos
Antibacterianos , Doxiciclina , Doxiciclina/uso terapêutico , Composição de Medicamentos , Antibacterianos/farmacologia , Pele , Cicatrização
10.
Pharmaceutics ; 15(12)2023 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-38140024

RESUMO

Organogels have importance for topical applications because they can be used to deliver drugs in a controlled and prolonged fashion. These are materials consisting of a three-dimensional network of organic molecules dispersed in a solvent. Recent studies have demonstrated that the solvent could be replaced by oils from non-conventional biologic sources. There is a diversity of not-explored species in the Amazon that are promising sources of vegetable oils with a promising composition. This study developed an organogel with buriti (Mauritia flexuosa L.f) and cacay (Caryodendron orinocense Karst.) oils, using cetostearyl alcohol as an organogelator due to its compatibility, stability, security, affordability, and it is readily available. The oils were characterized, and the organogels were synthesized by studying their crystal evolution and oil-binding capacity. The microstructure was evaluated with polarized light microscopy, fractal dimension, FTIR spectroscopy, XRD, and thermal and rheological analyses. It was found that the critical gelation concentration was higher for cacay oil as it possessed a higher amount of polyunsaturated triacylglycerols. The crystals of the buriti organogel had a smaller lamellar shape, a greater surface area, and physical and thermal stability; although, it presented a slower crystal evolution due to the low number of minor compounds and a greater number of saturated triacylglycerols. The polar fraction of the organogelators as well as triacylglycerol and minor polar compounds are important in forming crystallization nuclei. The study showed that Amazonian oils in crystallization processes form microstructures with differentiating physicochemical properties.

11.
Skin Pharmacol Physiol ; 36(5): 235-248, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38008088

RESUMO

BACKGROUND: Curcumin is a polyphenolic compound present in turmeric (Curcuma longa). Curcumin, turmeric powder, and extracts are widely used in traditional Indian medicine and are active ingredients of dietary supplements and cosmeceutical products. The pharmacological properties of curcumin/turmeric as well as the studies performed in vitro, in animal models, and in volunteers have been the objects of a vast literature. Most of the clinical studies report on the effects of curcumin/turmeric administered orally, while only a few describe its topical applications. SUMMARY: This review focuses on clinical studies in which curcumin/turmeric was applied topically to treat various skin conditions based on its antioxidant, anti-inflammatory, and antimicrobial properties. KEY MESSAGES: The clinical studies employing curcumin/turmeric as the only active ingredient allow us to appreciate its therapeutic potential without confounding contributions coming from additional pharmacologically active substances present in the same formulation. Curcumin/turmeric was regarded as an attractive alternative to conventional drugs, such as corticosteroids and antibiotics, thanks to its characteristics of a safe and well-tolerated natural substance.


Assuntos
Curcumina , Dermatopatias , Animais , Humanos , Curcumina/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia
13.
Pharmaceutics ; 15(10)2023 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-37896197

RESUMO

This study aimed to develop novel topical formulations based on a natural component (0.5% of Siberian pine essential oil) and to assess its wound-healing capacity through macroscopic, histopathological, and biochemical examination. The phytochemical profile of Pinus sibirica essential oil (PSEO) and rheological analysis and safety potential of formulations were determined. The wound-healing effect was evaluated on an excision wound model in diabetic Wistar albino rats randomly divided into the following groups topically treated with (1) untreated, (2) 1% silver sulfadiazine, (3) ointment base, (4) gel base, (5) PSEO ointment, and (6) PSEO gel. Formulations containing PSEO were stable and safe for skin application. Three weeks of treatment with both PSEO formulations (ointment and gel) led to a significant reduction in wound size (98.14% and 96.28%, respectively) and a remarkably higher level of total hydroxyproline content (9.69 µg/mg and 7.26 µg/mg dry tissue, respectively) relative to the control group (65.97%; 1.81 µg/mg dry tissue). These findings were in correlation with histopathological results. Topically applied PSEO formulations were associated with a significant reduction in most of the measured pro-oxidants and enhanced activity of the antioxidant defense system enzymes (p < 0.05). Our findings showed that gel and ointment with PSEO demonstrated significant wound-repairing capabilities in the excision wound model.

14.
Drug Des Devel Ther ; 17: 3139-3149, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37876501

RESUMO

Background: Postoperative sore throat is a frequent adverse event after double-lumen endobronchial tube (DLT) intubation. The aim of this study was to investigate whether esketamine gargle has a preventive effect on the incidence of postoperative sore throat in patients undergoing DLT intubation. Methods: This trial included 140 patients undergoing elective thoracic surgery at the third affiliated hospital of Sun Yat-Sen University. Patients were randomly allocated into the following two groups of 70 patients each: the control group, gargling with saline of 30 mL, and the esketamine group, gargling with an esketamine solution of 30 mL (2 mL/50 mg esketamine in 28 mL saline), 5 min prior to anaesthesia induction. The primary outcome was the incidence of sore throat 24 h after surgery. The main secondary outcomes included the incidence of sore throat and hoarseness at 1 h and 48 h after surgery, as well as the intraoperative haemodynamic responses. Results: The incidence of sore throat was significantly higher in the control group (47.1%, 33/70 patients) compared with the esketamine group (12.9%, 9/70 patients) at 24 h after surgery (RD, 0.41; 95% confidence interval, 0.26-0.57; p < 0.001). Furthermore, the incidence of sore throat at 1 h (p = 0.027), 24 h (p = 0.019), and seventh day (p = 0.031) as well as hoarseness at 1 h (p = 0.027), 24 h (p = 0.019), and 48 h (p = 0.031) after surgery were reduced in the esketamine group. Significant differences were seen in the peak levels of systolic blood pressure, mean arterial blood pressure, and heart rate between the groups during the intubation (p < 0.05). Besides, no patient developed an adverse reaction to esketamine. Conclusion: Preoperative gargling of esketamine can provide an effect against sore throat after DLT intubation without adverse side effects and effectively inhibit sharp elevations in heart rate and blood pressure during double-lumen intubation procedures.


Assuntos
Rouquidão , Faringite , Humanos , Rouquidão/epidemiologia , Rouquidão/etiologia , Rouquidão/prevenção & controle , Intubação Intratraqueal/efeitos adversos , Intubação Intratraqueal/métodos , Complicações Pós-Operatórias/tratamento farmacológico , Complicações Pós-Operatórias/epidemiologia , Dor/etiologia , Faringite/etiologia , Faringite/prevenção & controle
15.
Innate Immun ; 29(7): 135-149, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37605866

RESUMO

In the mammary glands, production of antimicrobial components and formation of less-permeable tight junctions (TJs) are important for safe milk production. Previously, we reported that local heat treatment of udders using disposable heating pad enhances the components of innate immunity in lactating goat mammary glands. Gingerol is a polyphenol present in ginger that can induce heat-like effects. However, oral administration of polyphenols causes a decrease in biological activity through conjugation and metabolic conversion. Here, we investigated the effects of gingerol on antimicrobial components and TJs by topically applying it to lactating goat udders. Gingerol application increased the somatic cell count, cathelicidin-2 concentration, and proportion of polymorphonuclear cells in the milk and interleukin-8 production. Moreover, gingerol treatment enhanced ß-defensin-1 production in milk, cultured mammary epithelial cells, and cultured somatic cells. Contrastingly, gingerol treatment did not affect the concentrations of blood-derived components (Na+, albumin, and IgG) in the milk or the TJ barrier function of cultured mammary epithelial cells. These findings suggest that the topical application of gingerol, similar to local heat treatment, to udders enhances the components of innate immunity in mammary glands. These findings may be useful for the prevention of mastitis in milk-producing animals and, hence, safe and stable dairy production.

16.
Peptides ; 169: 171078, 2023 11.
Artigo em Inglês | MEDLINE | ID: mdl-37579838

RESUMO

Skin aging refers to a degenerative process that can be affected and regulated by intrinsic and extrinsic factors. The mesenchymal stem cell secretome covers a considerable number of regenerative molecules with anti-aging effects in a wide variety of circumstances. However, it is complex, time-consuming, and costly to identify specific compounds from thousands of natural molecules using conventional methods. With the development of computational biology and machine learning, an efficient workflow was generated to identify novel peptides with anti-aging and skin restoration potential. One of the candidate peptides was discovered and subsequently truncated to a novel peptide named EQ-9, with promising anti-aging effects for topical applications at a concentration of 10 ppm validated by experimental validation. The above-described paradigm is expected to be further applied to the virtual screening of novel peptide molecules targeting specific biological functions from a wide variety of natural resources.


Assuntos
Células-Tronco Mesenquimais , Medicina Regenerativa , Medicina Regenerativa/métodos , Secretoma , Peptídeos/farmacologia
17.
Front Pharmacol ; 14: 1230728, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37593173

RESUMO

Although medical cannabis was legalized in Czechia in 2013 and its use in topical treatments of skin disorders is now allowed, galenic formulations prepared from medical cannabis have not been widely implemented in the Czech healthcare system. One of the main reasons is the lack of a straightforward standardized protocol for their preparation. Cannabinoids, e.g., cannabidiol (CBD) and tetrahydrocannabinol (THC), have been shown to have therapeutic effects on various skin conditions, such as atopic dermatitis, psoriasis, scleroderma, acne and skin pigmentation. Recognizing the potential of dermatological treatment with medical cannabis, the present study aimed to evaluate the extraction capacity of various pharmaceutical bases for cannabinoids and the stability of prepared galenic formulations for dermatological applications with respect to cannabinoid content. The results showed that the stability of cannabinoids in formulations depended on the bases' physical and chemical properties. The highest THC decomposition was observed in cream bases and Vaseline, with estimated percentage loss of total content of up to 5.4% and 5.6% per week, respectively. In contrast, CBD was more stable than THC. Overall, the tested bases were comparably effective in extracting cannabinoids from plant material. However, olive oil and Synderman bases exhibited the highest cannabinoid extraction efficiencies (approximately 70%) and the best storage stabilities in terms of the content of monitored compounds. The proposed preparation protocol is fast and easily implementable in pharmacies and medical facilities.

18.
Eur J Pharm Biopharm ; 190: 24-34, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37433416

RESUMO

The development of biocompatible delivery systems is a necessity for medical and topical applications. Herein, the development of a new bigel for topical application is described. It is composed of 40% colloidal lipid hydrogel and 60% olive oil and beeswax oleogel. Its characterization and the potential of the bigel as a drug carrier through the skin was evaluated in vitro using fluorescence microscopy and two phases of the bigel were labeled with two fluorescent probes: sodium fluorescein (hydrophilic phase) and Nile red (lipophilic phase). The structure of the bigel showed two phases with fluorescence microscopy in which the hydrogel phase was incorporated into a continuous oleogel matrix. Attenuated Total Reflectance Fourier Transform Infrared Spectroscopy (ATR-FTIR) presented a combination of vibrations characteristic of the different molecules forming the bigel, and Differential Scanning Calorimetry (DSC) showed different transitions attributed to beeswax lipids. Small-angle and wide-angle X-ray scattering (SAXS and WAXS) indicated a predominant lamellar structure with orthorhombic lateral packing that could be related to the arrangement of beeswax crystals. Bigel enables deeper penetration of hydrophilic and lipophilic probes into deeper layers, making it a promising candidate for effective topical carriers in medical and dermatological applications.


Assuntos
Hidrogéis , Pele , Espalhamento a Baixo Ângulo , Difração de Raios X , Hidrogéis/química
19.
Plant Cell Rep ; 42(10): 1571-1587, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37482559

RESUMO

KEY MESSAGE: We report the size dependent uptake of dsRNA loaded MSNPs into the leaves and roots of Nicotiana benthamiana plants and accessed for their relative reduction in Tomato leaf curl New Delhi viral load. A non-GMO method of RNA interference (RNAi) has been recently in practice through direct delivery of double stranded RNA into the plant cells. Tomato leaf curl New Delhi virus (ToLCNDV), a bipartitie begomovirus, is a significant viral pathogen of many crops in the Indian subcontinent. Conventional RNAi cargo delivery strategies for instance uses viral vectors and Agrobacterium-facilitated delivery, exhibiting specific host responses from the plant system. In the present study, we synthesized three different sizes of amine-functionalized mesoporous silica nanoparticles (amino-MSNPs) to mediate the delivery of dsRNA derived from the AC2 (dsAC2) gene of ToLCNDV and showed that these dsRNA loaded nanoparticles enabled effective reduction in viral load. Furthermore, we demonstrate that amino-MSNPs protected the dsRNA molecules from nuclease degradation, while the complex was efficiently taken up by the leaves and roots of Nicotiana benthamiana. The real time gene expression evaluation showed that plants treated with nanoparticles of different sizes ~ 10 nm (MSNPDEA), ~ 32 nm (MSNPTEA) and ~ 66 nm (MSNPNH3) showed five-, eleven- and threefold reduction of ToLCNDV in N. benthamiana, respectively compared to the plants treated with naked dsRNA. This work clearly demonstrates the size dependent internalization of amino-MSNPs and relative efficacy in transporting dsRNA into the plant system, which will be useful in convenient topical treatment to protect plants against their pathogens including viruses. Mesoporous silica nanoparticles loaded with FITC, checked for its uptake into Nicotiana benthamiana.


Assuntos
Begomovirus , Nanopartículas , Doenças das Plantas , RNA de Cadeia Dupla , Begomovirus/genética , Doenças das Plantas/prevenção & controle , Interferência de RNA , RNA de Cadeia Dupla/genética , Sistemas de Liberação de Medicamentos , Dióxido de Silício
20.
Pharmaceuticals (Basel) ; 16(7)2023 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-37513911

RESUMO

Microemulsions (MEs) have gained prominence as effective drug delivery systems owing to their optical transparency, low viscosity, and thermodynamic stability. MEs, when stabilized with surfactants and/or co-surfactants, exhibit enhanced drug solubilization, prolonged shelf life, and simple preparation methods. This review examines the various types of MEs, explores different preparation techniques, and investigates characterization approaches. Plant extracts and bioactive compounds are well established for their utilization as active ingredients in the pharmaceutical and cosmetic industries. Being derived from natural sources, they serve as preferable alternatives to synthetic chemicals. Furthermore, they have demonstrated a wide range of therapeutic effects, including anti-inflammatory, antimicrobial, and antioxidant activities. However, the topical application of plant extracts and bioactive compounds has certain limitations, such as low skin absorption and stability. To overcome these challenges, the utilization of MEs enables enhanced skin absorption, thereby making them a valuable mode of administration. However, considering the significant surfactant content in MEs, this review evaluates the potential skin irritation caused by MEs containing herbal substances. Additionally, the review explores the topical application of MEs specifically for herbal substances, with an emphasis on their anti-inflammatory properties.

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