Carriers For Topical Application Research Articles

Encapsulation of Vitamin C by Glycerol-Derived Dendrimers, Their Interaction with Biomimetic Models of Stratum corneum and Their Cytotoxicity.

Vitamin C is one of the most sensitive cosmetic active ingredients. To avoid its degradation, its encapsulation into biobased carriers such as dendrimers is one alternative of interest. In this work, we wanted to evaluate the potential of two biobased glycerodendrimer families (GlyceroDendrimers-Poly(AmidoAmine) (GD-PAMAMs) or GlyceroDendrimers-Poly(Propylene Imine) (GD-PPIs)) as a vitamin C carrier for topical application. The higher encapsulation capacity of GD-PAMAM-3 compared to commercial PAMAM-3 and different GD-PPIs, and its absence of cytotoxicity towards dermal cells, make it a good candidate. Investigation of its mechanism of action was done by using two kinds of biomimetic models of stratum corneum (SC), lipid monolayers and liposomes. GD-PAMAM-3 and VitC@GD-PAMAM-3 (GD-PAMAM-3 with encapsulated vitamin C) can both interact with the lipid representatives of the SC lipid matrix, whichever pH is considered. However, only pH 5.0 is suggested to be favorable to release vitamin C into the SC matrix. Their binding to SC-biomimetic liposomes revealed only a slight effect on membrane permeability in accordance with the absence of cytotoxicity but an increase in membrane rigidity, suggesting a reinforcement of the SC barrier property. Globally, our results suggest that the dendrimer GD-PAMAM-3 could be an efficient carrier for cosmetic applications.

Histological assessment of follicular delivery of flutamide by solid lipid nanoparticles: potential tool for the treatment of androgenic alopecia

Context: Flutamide is a potent anti-androgen with the several unwanted side effects in systemic administration, therefore, it has attracted special interest in the development of topically applied formulations for the treatment of androgenic alopecia.Objective: The purpose of this study was to prepare and characterize the solid lipid nanoparticles (SLNs) of Flutamide for follicular targeting in the treatment of the androgenic alopecia.Methods: Flutamide-loaded SLNs, promising drug carriers for topical application were prepared by hot melt homogenization method. Drug permeation and accumulation in the exercised rat skin and histological study on the male hamsters were performed to assess drug delivery efficiency in vitro and in vivo, respectively.Results: The optimized Flutamide-loaded SLNs (size 198 nm, encapsulation efficiency percentage 65% and loading efficiency percentage 3.27%) exhibited a good stability during the period of at least 2 months. The results of X-ray diffraction showed Flutamide amorphous state confirming uniform drug dispersion in the SLNs structure. Higher skin drug deposition (1.75 times) of SLN formulation compared to Flutamide hydroalcoholic solution represented better localization of the drug in the skin. The in vivo studies showed more new hair follicle growth by utilizing Flutamide-loaded SLNs than Flutamide hydroalcoholic solution which could be due to the higher accumulation of SLNs in the hair follicles as well as slowly and continues release of the Flutamide through the SLNs maximizing hair follicle exposure by antiandrogenic drug.Conclusion: It was concluded Flutamide-loaded SLN formulation can be used as a promising colloidal drug carriers for topical administration of Flutamide in the treatment of androgenic alopecia.

Mesoporous silica as a carrier for topical application: the Trolox case study

As part of a recent research effort aimed at employing mesoporous materials for controlled drug delivery, this paper presents MCM-41 as a carrier for topical application, using Trolox as a model unstable guest molecule. The complexes between Trolox and MCM-41 were prepared by employing different inclusion procedures, varying solvent, method and pretreatment of the silica matrix. The objectives of this study were to determine Trolox loading, analyze its integrity and availability after immobilization on mesoporous silica, evaluate MCM-41 influence on Trolox photodegradation and establish whether the preparation method significantly influences complex properties. The characterization analyses (XRD, TGA, DSC and FTIR) confirmed the hydrogen-bonding interaction and Trolox structure preservation. Gas-volumetric analysis showed a consistent decrease in surface area and in pore volume and diameter with respect to bare MCM-41 indicating that Trolox was mainly located within mesopores. In vitro diffusion tests showed a slower release of Trolox after inclusion in the MCM-41 matrix; at the same time UV irradiation studies highlighted an increased photostability for the complex particularly in O/W emulsion. Moreover the radical scavenging activity of Trolox was maintained after immobilization. In all cases, differences were observed in all tested samples, suggesting that results could be optimized by modifying the inclusion procedure and by improving the guest loading.

Nanostructured novel carrier for topical application

Nanoemulsions have attracted considerable attention in recent years for application in personal care products as potential vehicles for the controlled delivery of cosmetics and the optimized dispersion of active ingredients in particular skin layers. Of the many techniques that have been developed to measure droplet size of emulsions, 2 are of interest: laser light scattering and energy-filtering transmission electron microscopy used to measure the size of droplets in a nanoemulsion formed by a novel emulsifying agent that is able to spontaneously create emulsions with droplet sizes smaller than 300 nm .