Cassia Britto Detoni

Poly(ϵ-caprolactone) microcapsules and nanocapsules in drug delivery

Introduction: Poly(ϵ-caprolactone) (PCL), a biodegradable and biocompatible polymer, is useful to encapsulate a wide range of drugs making it an interesting material for the preparation of carriers with potential applications in therapeutics. Areas covered: The design and development of those carriers to modulate drug release, to improve the drug stability or apparent solubility in aqueous media, as well as to target tissues and organs are discussed. Expert opinion: Microencapsulation is a well-established process in pharmaceutical industry to protect drugs from chemical degradation and to control drug release. In this context, PCL is a useful polymer to prepare microcapsules. Nanoencapsulation, a more recent approach, offers new possibilities in drug delivery. PCL can be used as polymer to prepare different types of nanocapsules presenting diverse flexibility according to the chemical nature of the core. Those nanocapsules are capable of controlling drug release and improving photochemical stability. In addition, they can modulate cutaneous drug penetration/permeation and act as physical sunscreen due to their capability of light scattering. Considering the pharmaceutical point of view, PCL nanocapsules are versatile formulations, once they can be used in the liquid form, as well as incorporated into semi-solid or solid dosage forms.

Photostability and skin penetration of different E-resveratrol-loaded supramolecular structures.

It is desirable and challenging to prevent E‐resveratrol (E‐RSV) from photoisomerizing to its Z‐configuration to preserve its biological and pharmacological activities. The aim of this research was to evaluate the photostability of E‐RSV‐loaded supramolecular structures and the skin penetration profile of chemically and physically stable nanoestructured formulations. Different supramolecular structures were developed to act as carriers for E‐RSV, that is, liposomes, polymeric lipid‐core nanocapsules and nanospheres and solid lipid nanoparticles. The degrees of photostability of these formulations were compared with that of an ethanolic solution of E‐RSV. The skin penetration profiles of the stable formulations were obtained using vertical diffusion cells (protected from light and under UVA radiation) with porcine skin as the membrane, followed by tape stripping and separation of the viable epidermis and dermis in a heated water bath. Photoisomerization was significantly delayed by the association of resveratrol with the nanocarriers independently of the supramolecular structure. Liposomes were the particles capable of maintaining E‐RSV concentration for the longest time. On the other hand, E‐RSV‐loaded liposomes reduced in size showing low physical stability under UVA radiation. In the dark, the skin penetration profiles were very similar, but under UVA radiation the E‐RSV‐loaded nanocarriers showed increasing amounts in the total epidermis.

Hyaluronate nanoparticles included in polymer films for the prolonged release of vitamin E for the management of skin wounds

Lecithin and hyaluronic acid were used for the preparation of polysaccharide decorated nanoparticles loaded with vitamin E using the cationic lipid dioctadecyldimethylammonium bromide (DODMA). Nanoparticles showed mean particle size in the range 130-350 nm and narrow size distribution. Vitamin E encapsulation efficiency was higher than 99%. These nanoparticles were incorporated in polymeric films containing Aloe vera extract, hyaluronic acid, sodium alginate, polyethyleneoxide (PEO) and polyvinylalcohol (PVA) as an innovative treatment in skin wounds. Films were thin, flexible, resistant and suitable for application on burn wounds. Additionally, in vitro occlusion study highlighted the dependence of the occlusive effect on the presence of nanoparticles. The results obtained show that the bioadhesive films containing vitamin E acetate and Aloe vera could be an innovative therapeutic system for the treatment of skin wounds, such as burns. The controlled release of the vitamin along with a reduction in water loss through damaged skin provided by the nanoparticle-loaded polymer film are considered important features for an improvement in wound healing and skin regeneration.

UVA-UVB Photoprotective Activity of Topical Formulations Containing Morinda citrifolia Extract

Exposure to solar radiation, particularly its ultraviolet (UV) component, has a variety of harmful effects on human health. Some of these effects include sunburn cell formations, basal and squamous cell cancers, melanoma, cataracts, photoaging of the skin, and immune suppression. The beneficial photoprotective effects of topical formulations with the extract, Morinda citrifolia, have not been investigated. This present study aims to investigate the potential benefits of M. citrifolia topical application on the dorsal skin of mice, exposed to UVA-UVB light. Using 7 days of treatment, [before (baseline values) and 20 h after UV exposure], the thickness, skin barrier damage (TEWL), erythema, and histological alterations were evaluated. The results showed that the formulations containing the extract protected the skin against UV-induced damage.

Determination of in vitro usnic acid delivery into porcine skin using a HPLC method.

Usnic acid, a lichen metabolite, has been proposed as a potential topical treatment for microbial skin lesions, burn wounds as well as a sunscreen. An isocratic HPLC method was validated according to FDAs Guidance for Industry: Bioanalytical Method Validation to determine skin penetration and permeation of usnic acid. The penetration and permeation of usnic acid was evaluated using Franz cells and porcine skin. The method was valid according to selectivity, linearity, precision, accuracy and stability. Usnic acid was quantified in the skin surface (6.13 µg cm(2)), stratum corneum (34.4 µg cm(2)), viable epidermis (5.6 µg cm(2)), dermis (28.2 µg cm(2)) and receptor compartment (3.2 µg cm(2)). These results help us to understand the penetration profile of usnic acid and plan topical therapeutic approaches as well as new topical delivery systems to modulate this penetration profile.

Polymeric Nanocapsules for Topical Delivery

Polymeric nanocapsules represent an interesting carrier system for cutaneous applications. The possibilities of modulating skin penetration/permeation by altering the design of the formulation and the range of applicability are the main subjects under study. With this in mind, this chapter will address methods of nanocapsule preparation and the influence of the polymeric wall, the surface functionalization, and the vehicle on the skin penetration/permeation profile of active substances loaded in polymeric nanocapsules. Additionally, therapeutic and cosmetic applications of nanocapsules will also be discussed.

Nanosized and Nanoencapsulated Sunscreens

Nanotechnology represents an important complement to traditional chromophore-based UV filters. Nanosized metal oxides are widely used due to their broad protection spectrum and reduced skin irritation. These particles are already present in most commercial sunscreen lotions even though their photoreactivity has been highlighted as a potential cause of cytotoxic effects in human skin cells (e.g. fibroblasts, epithelial cells). However, this cytotoxicity is not likely to represent a significant health risk to consumers as several skin penetration assays have shown that the photoreactive particles penetrate at most to the stratum spinosum of the epidermis. Nanoencapsulation of traditional organic UV filters is a more recent approach to improve skin retention, photostability and the UV blocking ability of the free molecules. All of these improvements have been confirmed with different scientific assays for different particles, especially polymeric nanocapsules and solid lipid nanoparticles. These technological advantages offered by nanometric particles for sun protection formulations have made them commercially important. In inventories from non-governmental organizations there are approximately 30 commercial sunscreen products listed as containing nanoparticles.