Effects of lecithin-based nanoemulsions on skin: Short-time cytotoxicity MTT and BrdU studies, skin penetration of surfactants and additives and the delivery of curcumin (original) (raw)
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In Vivo Assessment of Clobetasol Propionate-Loaded Lecithin-Chitosan Nanoparticles for Skin Delivery
International Journal of Molecular Sciences, 2016
The aim of this work was to assess in vivo the anti-inflammatory efficacy and tolerability of clobetasol propionate (CP) loaded lecithin/chitosan nanoparticles incorporated into chitosan gel for topical application (CP 0.005%). As a comparison, a commercial cream (CP 0.05% w/w), and a sodium deoxycholate gel (CP 0.05% w/w) were also evaluated. Lecithin/chitosan nanoparticles were prepared by self-assembling of the components obtained by direct injection of soybean lecithin alcoholic solution containing CP into chitosan aqueous solution. Nanoparticles obtained had a particle size around 250 nm, narrow distribution (polydispersity index below 0.2) and positive surface charge, provided by a superficial layer of the cationic polymer. The nanoparticle suspension was then loaded into a chitosan gel, to obtain a final CP concentration of 0.005%. The anti-inflammatory activity was evaluated using carrageenan-induced hind paw edema test on Wistar rats, the effect of formulations on the barrier property of the stratum corneum were determined using transepidermal water loss measurements (TEWL) and histological analysis was performed to evaluate the possible presence of morphological changes. The results obtained indicate that nanoparticle-in-gel formulation produced significantly higher edema inhibition compared to other formulations tested, although it contained ten times less CP. TEWL measurements also revealed that all formulations have no significant disturbance on the barrier function of skin. Furthermore, histological analysis of rat abdominal skin did not show morphological tissue changes nor cell infiltration signs after application of the formulations. Taken together, the present data show that the use of lecithin/chitosan nanoparticles in chitosan gel as a drug carrier significantly improves the risk-benefit ratio as compared with sodium-deoxycholate gel and commercial cream formulations of CP.
Pharmaceutics, 2021
Tetrahydrocurcumin (THC) has been well known for its superior antioxidant properties. Therefore, it is speculated that it might be effective to relieve oxidative stress-induced diseases, such as skin hyperpigmentation. In this work, an in vitro B16F10 melanoma cell model was used to study the impact of THC on the melanogenic process under stressed conditions. It was demonstrated that THC could effectively inhibit the α-MSH (melanocyte-stimulating hormone) induced melanin production in B16F10 melanoma cells and the expressions of three key enzymes involved with the biosynthetic process of melanin, tyrosinase (TYR), tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2), were all significantly reduced. In addition, an in vitro human keratinocyte cell model was used to investigate the potential protective role of THC on H2O2-induced cytotoxicity. It was found that THC could prevent H2O2-induced oxidative stress based on the results of both the cell viability stu...
International Journal of Pharmaceutics, 2018
Nanostructured lipid carriers (NLC) and nano-sized emulsions based on monoacyl-phosphatidylcholine (MAPL) were tested for their effect on physiological skin parameters in vivo during daily application over four weeks. The influence of the basic formulations on transepidermal water loss (TEWL), skin hydration, sebum content and pH was determined once per week and after a recovery period of three weeks. In addition, confocal Raman spectroscopy was employed to evaluate natural moisturising factor and urea content. The results showed that the tested NLC systems with different MAPL content led to increased TEWL and decreased stratum corneum hydration, NMF and urea content. This effect was more pronounced for NLC with higher MAPL content and less pronounced for corresponding emulsions with increased oil phase volume. The observed effects indicate temporarily impaired barrier function; however, all effects were reversible after the treatment was finished. Additional tape stripping penetration experiments were performed on intact human forearm skin in vivo using the model substance curcumin. Higher total penetrated curcumin amounts were found for NLC-based formulations when compared to the emulsion. Comparative in vitro tape stripping data on porcine ear skin confirmed the trends observed in vivo. In summary, these findings suggest that the effect of the developed MAPLbased NLC and nano-sized emulsion on skin barrier function differs mildly in a one-time application setup, but may increase strongly during daily application over a longer treatment period. Having explored different surfactants for the production of these
A soybean lecithin microemulsion gel has been studied as a possible matrix for transdermal drug delivery. This gel is transparent and viscous, and it is composed of soybean phosphatidylcholine (lecithin), isopropyl palmitate and a small amount of water. In vitro percutaneous penetration studies of two anti-inflammatory drugs, indomethacin and diclofenac, dissolved in the gel-system resulted in steady state fluxes of about 1 Ixg h -~ cm -2. In order to estimate the function of the gel as a potential transdermal penetration enhancing system, interaction studies with isolated human stratum corneum were performed using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) as well as low-temperature scanning electron microscopy. These studies indicated that the lecithin gel, in particular isopropyl palmitate, affects the stratum corneum lipid organization even after 1-day incubation (FFIR, DSC), whereas recent in vivo human skin irritation tests showed no significant irritancy.
Lecithin microemulsion based systems for dermal delivery of drugs: a review
The purpose of this review is to give an insight into the considerable potential of lecithin based nanocarriers. The lecithin microemulsion and closely related microemulsion based systems are currently of interest to pharmaceutical researchers. Conventional systems for topical delivery of drugs meet many hindrances like reduced permeation and entrapment efficiency. Lecithin nanocarriers with their enhanced bioavailability of drugs present a viable option to address the drawbacks of conventional formulations. Soya and egg lecithin are widely being explored. However, the purity of lecithin plays a significant role in gelation process. The review encompasses lecithin microemulsions, lecithin based microemulsion gels, pluronic lecithin gels and lecithin stabilized microemulsion based hyrogels in improving the topical delivery of drugs. Biocompatible lecithin based systems are known to furnish ways of many promising discoveries in the field of safe and efficacious topical dosage forms.
Lecithin/chitosan nanoparticles of clobetasol-17-propionate capable of accumulation in pig skin
Journal of Controlled Release, 2010
In this study, clobetasol-17-propionate (CP) loaded lecithin/chitosan nanoparticles were studied with special attention to the transport of the active agent across the skin in vitro. Nanoparticles were characterized by measuring particle size, zeta potential, polydispersity index and encapsulation efficiency. The morphology of nanoparticles was evaluated by transmission electron microscopy. Encapsulation experiments with CP showed high encapsulation efficiency (92.2%). To assess the advantages of this carrier-based formulation in topical administration, the accumulation in and permeation across pig ear skin were compared with chitosan gel and commercially available cream of CP. The results obtained indicate that the incorporation of drug into nanoparticles induced an accumulation of CP especially in the epidermis without any significant permeation across the skin. Dilution of CP loaded nanoparticles with chitosan gel (1:9) produced the same amout of CP in the skin compared with commercial cream, although the former contained ten times less CP. This is a remarkable point for the reduction of the side effects of CP. These results demonstrated the suitability of lecithin/chitosan nanoparticles to induce epidermal targeting and to improve the risk-benefit ratio for topically applied CP.
International Journal of Pharmaceutics, 2019
Nanostructured lipid carriers (NLC) and nanoemulsions (NE) are colloid carriers which could improve dermal delivery of tacrolimus. The aims of this study were to evaluate effects of different formulation and process parameters on physicochemical characteristics and stability of lecithin-based NLC with glyceryl palmitostearate as solid and propylene glycol monocaprylate as liquid lipid and to compare the influence of different inner structure of tacrolimus-loaded NLC and corresponding NE on physicochemical characteristics, stability, entrapment efficiency, in vitro drug release and overall skin performance. Solid/liquid lipid ratio, total amount of lipids, homogenization pressure and cooling after the preparation were identified as critical variables in NLC development. Moreover, tacrolimus-loaded NLC emerged as more stabile carrier than NE. Differential stripping performed on porcine ear skin revealed significantly higher tacrolimus amount in stratum corneum from nanocarriers compared to referent ointment (Protopic®). Similarly the highest amount of tacrolimus in hair follicles was obtained using NLC (268.54 ± 92.38 ng/cm 2), followed by NE (128.17 ± 48.87 ng/cm 2) and Protopic® (77.61 ± 43.25 ng/cm 2). Contrary, the highest permeation rate through full-thickness porcine ear skin was observed for Protopic®, implying that the selection of experimental setup is critical for reliable skin performance assessment. Overall, developed NLC could be suggested as promising carrier in a form of lotion for tacrolimus dermal delivery.
Colloids and Surfaces B-biointerfaces, 2006
Effect of composition of lecithin water-in-oil and oil-in-water microemulsion on in vitro transdermal permeation of tetracaine hydrochloride was studied on mice model. The results were compared with an aqueous solution of tetracaine hydrochloride (2.7 mg/ml). In vitro skin flux and permeability coefficients were obtained using the Franz diffusion cell. Differential scanning calorimetry (DSC), transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM) were used to study the mechanism of action of the microemulsion. Micrographs of TEM and CLSM studies were analyzed by using Image Pro Plus image software. Skin flux of tetracaine hydrochloride was found to be dependent on the composition of lecithin/n-propanol/isopropyl myristate/water microemulsions. At lower K m ratio (i.e. 0.5:1 and 0.8:1) of microemulsion, the rate of permeation of tetracaine hydrochloride was higher when compared to the microemulsion of higher K m ratio (1:1 and 1.5:1). Image analysis of TEM micrograph, 6 h after application of lecithin microemulsion, showed 3.5 ± 0.75-fold (p < 0.001) increase in the intercellular space in the epidermis and 3.8 ± 0.4-fold (p < 0.001) enhancement in upper dermis. CLMS results show that sweat gland and hair follicles also provided path for permeation of the drug through the skin.
International Journal of Pharmaceutics, 2017
After the publication of the General Principles of the Civil Law of the People's Republic of China (General Principles of the Civil Law), The rights and obligations of the civil affairs departments in carrying out the duties of the guardians or supervising the guardians should be implemented and the norms should be refined so that the law will not become a dead letter. This paper mainly demonstrates by a method of literature research and case analysis. Articles on the guardianship function of civil affairs departments are mainly published in recent three years, and there were very few disputes cases with civil affairs departments involved. Legislation has attached importance, but the legal principle researches and judicial practices are still not enough.