Development and characterization of solid lipid microparticles containing vitamin C for topical and cosmetic use

Abstract

Solid lipid microparticles (SLMs), combined with the advantages of double emulsions (W/O/W) and water-in-oil micro emulsions, are developed for transdermal administration. A modified one-step emulsification method was introduced, which made the industrial production of SLMs easier. Variables involved in preparation that may affect the solubility, stability, and entrapment efficiency of SLMs were investigated. With vitamin C as a model active, the advantages of SLMs in transdermal administration were studied further. Vitamin C, encapsulated by SLMs, exhibited an enhanced storage stability up to 1 month under 25°C and a sustained releasing profile over 24 h. Furthermore, the SLMs was very helpful in delivering vitamin C molecules into skin through stratum corneum. The result showed 5.52-fold (p < 0.05) increased absorption of vitamin C, compared to the vitamin C solution. These studies demonstrate that SLMs could be a promising method for facilitating transdermal penetration of active ingredients with high solubility and low permeability.Practical applications: SLMs could be used as a drug delivery system for hydrophilic active ingredients with low permeability. Experiments have shown better stability and skin permeability of vitamin C incorporated in SLMs when compared with pure vitamin C. Furthermore, the method of producing SLMs is simple and can be realized in a way of industrial production. Since SLMs can dissolve in water, SLMs can be directly used on wet skin with excellent skin-touch feel. As a result, SLMs could be a practical delivery system for hydrophilic compounds with low permeability in many applications such as pharmaceuticals and cosmetics.

Encapsulating plant ingredients for dermocosmetic application: an updated review of delivery systems and characterization techniques

“…However, the direct utilization of vitamin C in cosmetic or pharmaceutical products is limited by its poor fat solubility and dermal absorbability. Liposomes , microcapsules and chitosan‐grafted cellulose nanocrystals have been reported as promising delivery systems for stabilizing vitamin C for cosmetic dermal application. Moreover, the storage stability and skin permeation of vitamin C‐loaded liposomes can be improved by coating them with natural antioxidant polymers of chitosan or pectin .…”

“…The microstructure of most carrier systems can be investigated by microscopic techniques, including optical microscopy , scanning electron microscopy (SEM) , transmission electron microscopy (TEM) and confocal laser scanning microscopy (CLSM) . For lipid‐based carriers, samples usually need to be immobilized by freezing before observation by cryo‐electron microscopy .…”

“…Photon correlation spectroscopy (PCS), dynamic light scattering (DLS), laser diffraction (LD) and nano‐tracking analysis (NTA) are commonly used techniques to determine the size distribution of capsules, particles and emulsion droplets . For micro‐sized liposomes and emulsions, the shape, size and distribution of droplets can be observed by fluorescence microscopy after dyeing the oil phase with Nile red and the water phase with rhodamine B . For porous micro‐/nanospheres, total surface area, average pore diameter and size distribution are also key parameters affecting the stability and functionality of the encapsulated core material, which can be measured by mercury porosimetry .…”

Sistemas de entrega de fármacos autoemulsificables: una plataforma de desarrollo alternativa para la industria farmacéutica colombiana

“…Los sistemas autoemulsificables se pueden definir como mezclas isotrópicas de aceites naturales o sintéticos, tensioactivos, en algunas ocasiones, cosolventes y un principio activo, que son capaces de formar emulsiones finas de aceite en agua cuando se introducen en medio acuoso bajo agitación suave [46][47][48]. La motilidad del tracto gastrointestinal proporciona la agitación necesaria para la autoemulsificación, por lo cual estos sistemas emulsionan espontáneamente al exponerse a los fluidos gastrointestinales [40,49].…”

Vitamins in cosmetic products: Current opinions and practice

“…Pravilnim izborom vrste i koncentracije hidrofilnih i lipofilnih surfaktanata, kao i sa odgovarajućim odnosom vodene i masne faze, SLM mogu samoemulgovanjem u vodenom medijumu formirati v/u/v emulzije. Ovakve višestruke v/u/v emulzije, koje su nastale samoemulgovanjem SLM, omogućavaju produženo oslobađanje i poboljšanu penetraciju vitamina C u kožu svinja (40).…”