Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 39
Filtrar
1.
Curr Microbiol ; 79(12): 386, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36329207

RESUMO

This study evaluated the effect of microemulsion (ME) containing Amphotericin B (AmB) alone and associated with Terbinafine (Tbf) on Leishmania major (L. major) using in vitro models. The ME formulations of these drugs were formulated and described. After evaluating their cytotoxicity on the J774A1 macrophage (MΦ), their potency against promastigotes and intracellular amastigotes models was evaluated using an in vitro MTT assay and Giemsa stain, respectively. Based on pseudo ternary phase diagrams, unloaded ME, Tbf-loaded ME (ME-Tbf), and, AmB-loaded ME (ME-AmB) with mean droplet sizes 3.4 ± 0.81, 10.05 ± 0.21, and 8.21 ± 0.46 were successfully prepared, respectively. Concerning toxicity, ME-AmB and ME-Tbf indicated lower toxicity on MΦs compared to the free drugs. The ME formulations showed considerably inhibitory effects compared to the free drug forms when the IC50 was examined. The IC50 values of AmB (59.19 ± 1.74 and 36.4 ± 3.2 µg/mL), ME-AmB (7.5 ± 0.9 and 0.8 ± 0.05 µg/mL), Tbf (234.5 ± 9 and 128.8 ± 0.28 µg/mL), ME-Tbf (26.27 ± 0.2 and 11.97 ± 0.6 µg/mL), AmB + Tbf (30.18 and 24.93 µg/mL), and ME-AmB + ME-Tbf (4.79 and 0.37 µg/mL) were estimated after 48 and 72 h, respectively.


Assuntos
Anfotericina B , Leishmania major , Anfotericina B/farmacologia , Terbinafina/farmacologia
2.
J Wound Care ; 31(Sup10): S16-S27, 2022 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-36240871

RESUMO

OBJECTIVE: For a long time, natural compounds have been used to accelerate wound healing. In this study, the topical effects of ammoniacum gum extract on wound healing were investigated in white male rats. METHOD: Following skin wound induction in aseptic conditions, 48 Wistar rats were divided into six equal groups; phenytoin cream 1% (standard), untreated (control), Eucerin (control), and 5%, 10% and 20% ointments of Dorema ammoniacum gum extract (treatment groups). All experimental groups received topical drugs daily for 14 days. The percentage of wound healing, hydroxyproline content, histological parameters, and growth factors (endothelial growth factor (EGF), platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and transforming growth factor (TGF)-α) were measured in experimental groups. RESULTS: The areas of the wounds in the treatment groups were significantly decreased compared with the wound areas of control groups at 5, 7 and 10 days after wounding. On the 12th day, the wounds in the treatment groups were completely healed. Hydroxyproline contents were significantly increased in the treatment groups compared with the control groups (p<0.001). In histological evaluation, the re-epithelialisation, increasing thickness of the epithelial layer, granulation tissue and neovascularisation parameters in the treatment groups showed significant increases compared with the control groups. Also, serum levels of TGF-ß, PDGF, EGF and VEGF in the treatment groups were significantly increased compared to the control groups. CONCLUSION: The topical application of ammoniacum gum extract significantly increases the percentage of wound healing in rats and reduces the time of wound closure.


Assuntos
Fenitoína , Fator A de Crescimento do Endotélio Vascular , Animais , Fatores de Crescimento Endotelial/farmacologia , Fator de Crescimento Epidérmico , Hidroxiprolina/farmacologia , Masculino , Pomadas , Fenitoína/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Fator de Crescimento Derivado de Plaquetas/farmacologia , Ratos , Ratos Wistar , Fator de Crescimento Transformador beta , Fatores de Crescimento Transformadores/farmacologia , Cicatrização
3.
AAPS PharmSciTech ; 23(7): 280, 2022 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-36241959

RESUMO

Intracellular parasitic protozoa of Leishmania sp. causes leishmaniasis. The restricted access of the drugs to affected cells in the treatment of intracellular infections such as leishmaniasis is frequently hampered. Furthermore, most of today's drugs have limited uses due to some containing toxic compounds, and drug resistance is on the rise. In the present investigation, Amphotericin B (AmB) and Terbinafine (Tbf) were loaded in microemulsion (ME) in combination and alone, and the in vivo efficacy was considered in BALB/c mice infected with Leishmania major (L. major). The wound size at the base of the mouse tail was measured, and real-time PCR was performed to quantify the parasite load after the infection challenge. The study demonstrated that the ME-AmB and ME-Tbf formulations are safe and effective compounds for the treatment of cutaneous leishmaniasis by enhancing the effectiveness of AmB and Tbf in reducing the parasite burden.


Assuntos
Leishmania major , Leishmaniose Cutânea , Anfotericina B/farmacologia , Anfotericina B/uso terapêutico , Animais , Leishmaniose Cutânea/tratamento farmacológico , Camundongos , Camundongos Endogâmicos BALB C , Terbinafina/uso terapêutico
4.
J Liposome Res ; 31(3): 246-254, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32594811

RESUMO

The aim of the present study was to develop a topical liposomal formulation as a transdermal delivery of rivastigmine for the treatment of Alzheimer's disease as an alternative to the oral dosage form and to achieve smooth continuous drug delivery and maintain plasma levels within the therapeutic window. Rivastigmine-loaded liposomes were prepared by a thin layer hydration technique that was applied in ex vivo-in vivo correlation study. Permeability parameters through rat skin in ex vivo study and pharmacokinetic parameters in the in vivo study were evaluated. The ex vivo permeation study showed that liposomes provided steady-state flux 0.11 ± 0.01 mg/cm.h that were more than 2-fold the aqueous control. In the in vivo experiments, after topical application of optimized rivastigmine liposomes, the Cmax 208 ng/ml and AUC0-24 3605 (ng.h/ml) were also significantly higher than the control group (both p < 0.01). A point-to-point significant linear correlation was found between ex vivo and in vivo parameters, meaning in vivo pharmacokinetic parameters can be predicted by ex vivo permeation parameters. These data suggest that a liposomal formulation could be an effective carrier to enhance rivastigmine permeation through the skin and maintain plasma levels within the therapeutic window.


Assuntos
Lipossomos , Absorção Cutânea , Administração Cutânea , Animais , Correlação de Dados , Lipossomos/metabolismo , Ratos , Rivastigmina/metabolismo , Pele/metabolismo
5.
Molecules ; 23(8)2018 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-30065147

RESUMO

The low oral bioavailability of ciprofloxacin is associated with two distinct challenges: its low aqueous solubility and efflux by p-glycoproteins (P-gp) in the intestinal membrane. Several studies were conducted in order to improve its solubility and permeability through the gastrointestinal membrane. In this study, in a full factorial design study, eight polymeric micelles were prepared and their characteristics, including particle size, loading and release rate were evaluated. Polymeric micelles demonstrated particle sizes below 190 nm and 27⁻88% loading efficiency. Drug release was affected by drug solubility, polymeric micelle erosion and swelling in simulated gastrointestinal fluids. An optimized polymeric micelle was prepared based on appropriate characteristics such as high drug loading and low particle size; and was used for a permeation study on Caco-2 cells. Optimized polymeric micelles with and without ginsenoside and ginsenoside alone enhanced drug permeability through Caco-2 cells significantly in the absorptive direction. The effect of ginsenoside was dose dependent and the maximum effect was seen in 0.23 mg/mL concentration. Results showed that P-gp may not be responsible for ciprofloxacin secretion into the gut. The main mechanism of ciprofloxacin transport through Caco-2 cells in both directions is active diffusion and P-gp has inhibitory effects on ciprofloxacin permeability in the absorptive direction that was blocked by ginsenoside and micelles without ginsenoside.


Assuntos
Subfamília B de Transportador de Cassetes de Ligação de ATP/antagonistas & inibidores , Antibacterianos/metabolismo , Ciprofloxacina/metabolismo , Difusão/efeitos dos fármacos , Portadores de Fármacos , Ginsenosídeos/antagonistas & inibidores , Subfamília B de Transportador de Cassetes de Ligação de ATP/genética , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Antibacterianos/farmacologia , Disponibilidade Biológica , Transporte Biológico , Células CACO-2 , Permeabilidade da Membrana Celular/efeitos dos fármacos , Ciprofloxacina/farmacologia , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Expressão Gênica , Ginsenosídeos/farmacologia , Humanos , Absorção Intestinal/fisiologia , Cinética , Micelas , Modelos Biológicos , Tamanho da Partícula
6.
Pharm Dev Technol ; 23(8): 741-750, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27871215

RESUMO

The aim of this study was to develop a new microemulsion formulation for topical application of poorly soluble drug named quercetin. In order to design suitable microemulsion system, the pseudo-ternary phase diagrams of microemulsion systems were constructed at different surfactant/co-surfactant ratios using tween 80 as surfactant, transcutol® P as a co-surfactant and oleic acid as an oil phase. Some physicochemical properties such as droplet size, density, refractive index, electrical conductivity, pH, surface tension, and viscosity of the microemulsion systems were measured at 298.15 K. The average hydrodynamic droplet size of the optimized microemulsions was obtained by dynamic light scattering method. Morphology assessment of the optimized quercetin-loaded microemulsion by transmission electron microscopy analysis indicated that the particles have the size of about 25 nm and spherical with narrow size distribution. Equilibrium solubility, in vitro drug release at a 24 h time period, release kinetic evaluation as well as ex vivo permeation and retention of quercetin-loaded microemulsions through rat skin has been investigated. The obtained results showed a slow release behavior without any transdermal delivery. Most of the formulations fitted best with zero-order kinetic model with a non-Fickian mechanisms. This study illustrated that the proposed QU-microemulsion has a good potential for use in sunscreen formulations. [Formula: see text].


Assuntos
Antioxidantes/administração & dosagem , Antioxidantes/farmacocinética , Emulsões/química , Quercetina/administração & dosagem , Quercetina/farmacocinética , Absorção Cutânea , Administração Cutânea , Animais , Antioxidantes/química , Liberação Controlada de Fármacos , Etilenoglicóis/química , Masculino , Ácido Oleico/química , Veículos Farmacêuticos/química , Polissorbatos/química , Quercetina/química , Ratos Wistar , Tensoativos/química
7.
Molecules ; 22(10)2017 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-29053620

RESUMO

The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions 4 and 8 due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of Plantago lancolata extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner.


Assuntos
Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem , Otopatias/tratamento farmacológico , Edema/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Plantago/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Otopatias/induzido quimicamente , Edema/induzido quimicamente , Emulsões , Humanos , Hidrólise , Nanopartículas/química , Tamanho da Partícula , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Xilenos/efeitos adversos
8.
J Cosmet Dermatol ; 23(1): 289-295, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37462297

RESUMO

INTRODUCTION: Acne vulgaris can be treated topically with adapalene, a synthetic derivative of naphthoic acid with retinoid activity. Adapalene has a very low rate of percutaneous absorption and is almost completely insoluble in water. To obviate this problem, microemulsion (ME) carrier is used. The study's goals were to create and characterize adapalene-loaded ME and assess the drug's transfollicular route of penetration to see if hair follicles can serve as a conduit for the drug to enter the skin. METHODS: Adapalene microemulsions (MEs) are made by combining the right amounts of the cosurfactant (propylene glycol), surfactant (Tween 80 and Span 20), and oil phase (oleic acid-Transcutol P (10:1)). Physical and chemical characteristics of MEs, including droplet size, stability, viscosity, drug release, and in vitro skin permeability via guinea pigs' hairy and non-hairy skin, were assessed. RESULTS: The range of 13.86-56.16 nm was found to be the average droplet size of ME formulations. The range of viscosities was 117-240 cps. The drug release profile reveals that 95.374 percent of the drug was released within the experiment's first 24 h. Compared to the adapalene control (aqueous suspension), all MEs enhanced the adapalene flow through both hairy and non-hairy skin. The surfactant/cosurfactant ratio had an impact on the amount of drug that passed through both skins because a larger ratio enhanced the adapalene affinity in the follicular route. CONCLUSION: Furthermore, the proportions of the water and oil phases in formulations, as well as the S/C ratio, have a significant impact on the physicochemical characteristics and adapalene permeability across both pathways.


Assuntos
Pele , Tensoativos , Animais , Cobaias , Adapaleno , Administração Cutânea , Pele/metabolismo , Água/metabolismo
9.
Iran J Pharm Res ; 23(1): e139381, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39140102

RESUMO

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.

10.
J Cosmet Dermatol ; 2024 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-39135289

RESUMO

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.

11.
J Cosmet Dermatol ; 23(5): 1816-1827, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38193246

RESUMO

BACKGROUND: The purpose of this study was to investigate the protective effect of Silibinin-loaded polymeric micelles from human hair against UV-B radiation. METHODS: Eight formulations with different concentrations of Silibinin, Pluronic F-127, and Labrasol-Labrafil were made by a solvent evaporation method, and the selected formulation was chosen by examining their properties like particle size and loading efficiency. Six groups of human hair, including a group that received the selected formulation, were exposed to UV-B radiation and by calculating its factors such as peak-to-valley roughness, RMS roughness, FTIR, and the amount of protein loss, the protective effect of the selected formulation was judged. RESULTS: According to the results, the loading efficiency and particle size of the selected formulation were 45.34% and 43.19 nm. The Silibinin release profile had two parts, fast and slow, which were suitable for creating a drug depot on hair. Its zeta potential also confirmed the minimum electrostatic interference between the formulation and hair surface. The zeta potential of selected formulation was -5.9 mv. Examination of AFM images showed that the selected formulation was able to prevent the increase in peak-to-valley roughness and RMS roughness caused by UV-B radiation. RMS roughness after 600 h of UV radiation in Groups 5 and 6 was significantly lower than the negative control group and the amount of this factor did not differ significantly between 0 and 600, so it can be concluded that the selected formulation containing Silibinin and the positive control group was able to prevent the increase of RMS roughness and hair destruction. In other hands, the two positive control groups and the selected formulation containing Silibinin were able to effectively reduce hair protein loss. CONCLUSION: Silibinin-loaded polymeric micelles were able to effectively protect hair from structural and chemical changes caused by UV-B radiation.


Assuntos
Cabelo , Micelas , Tamanho da Partícula , Silibina , Raios Ultravioleta , Humanos , Raios Ultravioleta/efeitos adversos , Silibina/farmacologia , Silibina/administração & dosagem , Silibina/química , Cabelo/efeitos dos fármacos , Cabelo/efeitos da radiação , Silimarina/farmacologia , Silimarina/administração & dosagem , Silimarina/química , Polímeros/química , Liberação Controlada de Fármacos/efeitos da radiação , Antioxidantes/farmacologia , Antioxidantes/administração & dosagem , Portadores de Fármacos/química , Portadores de Fármacos/efeitos da radiação
12.
J Drug Target ; 32(1): 74-79, 2024 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38009711

RESUMO

Background: Long contact of UV causes skin damage. Glycolic acid (GA) as an alpha hydroxy acid is used to treat photodamaged skin. However, GA leads to side effects including; burning, erythema and peeling.Purpose: The aim of this study was to develop a controlled delivery systems loading GA in order to increasing its efficacy and lowering its side effects.Methods: Liposomes were evaluated for encapsulation efficiency, size and morphology. Optimized formulation was dispersed in HPMC gel bases and drug release kinetics were also studied. Clinical efficacy and safety of GA-loaded liposomal gel and GA gel formulation were evaluated in patients with photodamaged skin.Results: The EE% and average particle size of liposomes were 64 ±2.1 % and 317±3.6 nm, respectively. SEM image showed that liposomes were spherical in shape. In vitro release kinetics of GA from both formulations followed Weibull model. Clinical evaluation revealed that GA-loaded liposomal gel was more effective than GA gel formulation. Treatment with GA-loaded liposomal gel resulted in a statistically significant reduction in the scores of hyperpigmentation, fine wrinkling and lentigines. Moreover, liposomal gel formulation was able to minimize side effects of GA.Conclusion: According to the obtained results, the liposome-based gel formulation can be used as potential drug delivery system to enhance permeation of GA through skin layers and also reduce its side effects.


Assuntos
Glicolatos , Lipossomos , Absorção Cutânea , Humanos , Lipossomos/metabolismo , Pele/metabolismo , Sistemas de Liberação de Medicamentos , Tamanho da Partícula
13.
J Family Med Prim Care ; 13(2): 640-646, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38605791

RESUMO

Background: Due to the increasing resistance of bacteria to antibiotics and anti-bacterial compounds in plants, Allium jesdianum Boiss plant extract can be used in mouthwash compounds with its anti-microbial activity. Methods and Materials: The anti-bacterial and anti-fungal activity of A. jesdianum mouthwash was investigated on Streptococcus mutans, Streptococcus sanguis, S. salivarius and Candida albicans, and Candida tropicalis. To analyse the anti-microbial effect of this mouthwash, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined by the broth microdilution method. Results: The average MIC and MBC of A. jesdianum mouthwash for S. mutans were 1.56 and 3.12 (mg/ml), respectively, for S. salivarius, 0.25 and 0.65 (mg/ml), and for S. sanguis, respectively, 0.25 and 0.65 (mg/ml). The highest MIC and MBC values were for S. mutans, and the MIC and MBC values were equal for S. sanguis and S. salivarius. Average MIC and MBC were determined as 2.41 and 4.16 (mg/ml) for C. albicans and 2.34 and 5.72 (mg/ml) for C. tropicalis, respectively. MIC values of mouthwash were higher for C. albicans and MBC values for C. tropicalis. Conclusion: Our results showed a promising anti-fungal-anti-bacterial effect of A. jesdianum extract. A. jesdianum extract may be used as an alternative to chemical mouthwashes.

14.
Turk J Pharm Sci ; 20(2): 108-114, 2023 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-37161659

RESUMO

Objectives: Mefenamic acid (MA) is a strong non-steroidal anti-inflammatory drug, but because of its limited oral bioavailability and the side effects that come with taking it systemically, it is better to apply it topically. The major goal of this study was to see how certain permeation enhancers affected MA is in vitro skin permeability. In manufactured Franz diffusion cells, MA permeability tests using rat skin pretreatment with several permeation enhancers such as corn oil, olive oil, clove oil, eucalyptus oil, and menthol were conducted and compared to hydrate rat skin as a control. Materials and Methods: The steady-state flux (Jss), permeability coefficient (Kp), and diffusion coefficient are among the permeability metrics studied. The permeability enhancement mechanisms of the penetration enhancer were investigated using fourier transform infrared spectroscopy (FTIR) to compare changes in peak position and intensities of asymmetric and symmetric C-H stretching, C=O stretching, C=O stretching (amide I), and C-N stretching of keratin (amide II) absorbance, as well as differential scanning calorimetry (DSC) to compare mean transition temperature and their enthalpies. Results: Clove oil, olive oil, and eucalyptus oil were the most effective enhancers, increasing flux by 7.91, 3.32, and 2.6 times, as well as diffusion coefficient by 3.25, 1.34, and 1.25, respectively, when compared to moist skin. FTIR and DSC data show that permeation enhancers caused lipid fluidization, extraction, disruption of lipid structures in the SC layer of skin, and long-term dehydration of proteins in this area of the skin. Conclusion: According to the findings, the permeation enhancers used improved drug permeability through excised rat skin. The most plausible mechanisms for greater ERflux, ERD, and ERP ratios were lipid fluidization, disruption of the lipid structure, and intracellular keratin irreversible denaturation in the SC by eucalyptus oil, menthol, corn oil, olive oil, and clove oil.

15.
Adv Pharm Bull ; 13(1): 96-103, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36721808

RESUMO

Purpose: Finasteride is a 5-alpha reductase inhibitor used to treat hair loss and acne. The skin permeation of finasteride is one of the main challenges associated with dermal drug delivery. One way to overcome the skin barrier is to use penetration enhancers. The purpose of this study was to investigate the effect of some penetration enhancers on finasteride permeability on the skin, as well as the effect of pretreatment time on their efficacy. Methods: In order to determine the effect of penetration enhancers on the skin permeability of finasteride, the skin was exposed to clove oil, urea, and lyophilized powder of grape seed extract (LPGSE) at different pretreatment times (2, 4 h), and then the permeability parameters were determined by passing the drug through the skin. Results: The results of this study showed that clove oil, urea, and LPGSE increased the transfer of finasteride from the skin. The highest rate of permeation was observed with clove oil (4 h), and the least permeability was observed with urea (4 h). Conclusion: Increasing the pretreatment time with clove oil and LPGSE increases the permeability of finasteride. Meanwhile, the increase in pretreatment time with urea reduces the penetration of finasteride from the skin due to reversible effects.

16.
Iran Biomed J ; 26(5): 366-73, 2022 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-36403103

RESUMO

Background: Flavonoids are a large group of phenolic compounds possessing anti-inflammatory and antioxidant effects. NAR is a flavonoid with various pharmacological properties. Using pharmaceutical compounds on skin is one of the routes of administration to achieve local and systemic effects. The aim of this study was to develop a topical formulation of NAR by the preparation of a NAR ME, which was further tested its skin permeability in rats. Methods: Eight 0.5% NAR MEs were prepared by mixing appropriate amounts of surfactant (Tween 80 and Labrasol), cosurfactant (Capryol 90) and the oil phase (oleic acid-Transcutol P in a ratio of 1:10). The drug was dissolved in the oil phase. The physicochemical properties of MEs such as droplet size, viscosity, release, and skin permeability were assessed using Franz Cells diffusion. Results: Based on the results, the droplet size of MEs ranged between 5.07 and 35.15 nm, and their viscosity was 164-291 cps. Independent factors exhibited a strong relationship with both permeability and drop size. The permeability findings revealed that the diffusion coefficient of NAR by the ME carrier increased compared to the drug saturation solution. Conclusion: The most validated results were obtained for Jss and particle size. Optimal formulations containing MEs with Jss and particle sizes varying between minimum and maximum amounts are suitable for topical formulations of NAR.


Assuntos
Flavanonas , Ratos , Animais , Administração Cutânea , Emulsões/química , Flavanonas/farmacologia , Pele
17.
Iran J Pharm Res ; 21(1): e127486, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36945341

RESUMO

Background: The goal of this research was to design and characterize quercetin microemulsions (MEs) to resolve water solubility issues related to quercetin and improve transcorneal permeation into the eye. Methods: MEs were prepared by the phase diagram method. Oily phase (oleic acid-Transcutol P), surfactant (Tween 80, Span 20), and co-surfactant (propylene glycol) were used to make a quercetin-loaded ME. The size of the droplets, their viscosity, pH, release, flux, and diffusivity were all measured. Results: Droplet diameters in ME samples ranged from 5.31 to 26.07 nanometers. The pH varied from 5.22 to 6.20, and the release test revealed that 98.06 percent of the medication was released during the first 24 hours. The flux and diffusivity coefficients of the ME-QU-8 formulation were 58.8 µg/cm2.h and 0.009 cm2/h, respectively, which were 8.8 and 17.9 times greater than the quercetin aqueous control (0.2 percent). The maximum percentage of drug permeated through rabbit cornea after five hours was 16.11%. Conclusions: It is concluded that ME containing quercetin could increase transcorneal permeation and that permeation could be altered by any change in the composition of the ME formulation. This effect might be caused by structural alterations in the cornea caused by ME components.

18.
Adv Pharm Bull ; 12(1): 102-108, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35517878

RESUMO

Purpose: Cystic echinococcosis (CE) is a serious contemporary public health problem. Different CE treatment methods are of considerable importance, with albendazole (ABZ) being one of the most preferred drugs for CE treatment and prophylaxis. In this study, we evaluated the nephrotoxicity caused by ABZ and ABZ-loaded solid lipid nanoparticles (SLNs) in mice with experimental hydatid cyst. Methods: ABZ-loaded SLNs were produced by micro-emulsification and a high shear homogenization technique. Thereafter, we evaluated the physicochemical characterization of the product. Live protoscolices were injected into mice to induce experimental hydatidosis. Mice were then treated with ABZ and ABZ-loaded SLNs. The nephrotoxicity effects were evaluated by biochemical and histopathological surveys. Results: Significantly different blood urea nitrogen (BUN) levels were observed between the two infected groups (ABZ treatment and ABZ-loaded SLN treatment) and the control group. The kidney malondialdehyde (MDA) and glutathione (GSH) levels of the infected groups were not significantly different from those of the control group. The histopathological study revealed nephropathic and pathologic changes in the ABZ and ABZ-loaded SLN groups. Conclusion: ABZ formulated for ABZ-loaded SLNs had a more prominent chemoprophylactic efficacy on CE and fewer side effects than ABZ alone. Neither ABZ nor ABZ-loaded SLNs caused significant biochemical and histopathological defects on the kidney, and all functional biochemical markers stayed within the normal range. Therefore, ABZ-loaded SLNs could be a potential new product for CE treatment.

19.
J Cosmet Dermatol ; 20(9): 3011-3017, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33528091

RESUMO

BACKGROUND: Acne is one of the skin diseases that include abnormalities in the production of sebum, changes in the microbial flora, abnormal keratinization, and inflammation. Adapalene is a good choice in the treatment of acne with fewer side effects and high effectiveness. However, the absorption of adapalene through human skin is low. We investigated the effect of several enhancers on the skin absorption of adapalene. METHODS: For the preparation of a topical formulation, this drug needs proper skin absorption. Therefore, to increase the effect of chemical absorption of the Adapalene skin permeability, it should first be put on the skin in a touch of some absorption like Eucalyptus, Urea, Clove oil, propylene glycol, and oleic acid for 1 and 2 hours and was then examined for the passing of the drug on the treated skin and for the effect of absorptions by calculating of the permeability parameters using DSC and FT-IR techniques. RESULT AND CONCLUSION: The results show that the enhancers used increased the permeability of the drug adapalene to water. Several mechanisms including lipid liquefaction, degradation of the fat structure, as well as irreversible denaturation of intracellular creatine caused by Eucalyptus, urea clove oil, PG, and oleic acid are the main mechanisms of drug penetration. Based on the results, it was found that among the enhancers studied, eucalyptus and urea had the highest and the lowest absorption effect in 2- and 1-hour pre-contact, respectively.


Assuntos
Acne Vulgar , Absorção Cutânea , Acne Vulgar/tratamento farmacológico , Acne Vulgar/metabolismo , Adapaleno , Humanos , Pele/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier
20.
J Cosmet Dermatol ; 20(1): 181-187, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-32413183

RESUMO

BACKGROUND: Shampoos remove fat and pus from the skin and hair. The most critical part of these products is their cleansing properties; therefore, the amount of shampoo cleanser plays an essential role in consumer acceptance. AIM: The production of herbal shampoos from root saponins in Hawthorn can lead to the removal of these substances from shampoos. Squarrosum is one of the 23 Acanthophyllum species that is native to Iran. The root of this plant has been used traditionally as a consumption detergent due to the presence of saponins. METHOD: To make the shampoo, saponins were extracted through several steps by a solvent after Acanthophyllum squarrosum scientific specimens had been prepared and identified The shampoo's fatigue strength was tested using the Ross-Miles method, and its cleansing power was assessed using Thompson's test. RESULTS: The optimum formula with 15% total saponins content was evaluated. CONCLUSION: This liquid shampoo has an excellent cleansing effect, is suitable for regular hair; has pseudoplastic rheology; and has acceptable pH, surface tension, and organoleptic stability characteristics.


Assuntos
Preparações para Cabelo , Saponinas , Cabelo , Humanos , Irã (Geográfico) , Tensoativos
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA