Carrier For Transdermal Drug Delivery Research Articles

Skin permeation of d-limonene-based nanoemulsions as a transdermal carrier prepared by ultrasonic emulsification

Nanoemulsions can be used for transporting pharmaceutical phytochemicals in skin-care products because of their stability and rapid permeation properties. However, droplet size may be a critical factor aiding permeation through skin and transdermal delivery efficiency. We prepared d-limonene nanoemulsions with various droplet sizes by ultrasonic emulsification using mixed surfactants of sorbitane trioleate and polyoxyethylene (20) oleyl ether under different hydrophilic–lipophilic balance (HLB) values. Droplet size decreased with increasing HLB value. With HLB 12, the droplet size was 23nm, and the encapsulated ratio peaked at 92.3%. Transmission electron microscopy revealed spherical droplets and the gray parts were d-limonene precipitation incorporated in spherical droplets of the emulsion system. Franz diffusion cell was used to evaluate the permeation of d-limonene nanoemulsion through rat abdominal skin; the permeation rate depended on droplet size. The emulsion with the lowest droplet size (54nm) achieved the maximum permeation rate. The concentration of d-limonene in the skin was 40.11μL/cm2 at the end of 360min. Histopathology revealed no distinct voids or empty spaces in the epidermal region of permeated rat skin, so the d-limonene nanoemulsion may be a safe carrier for transdermal drug delivery.

All-trans retinoic acid-loaded lipid nanoparticles as a transdermal drug delivery carrier

The objective of this study was to investigate the effects of drug amounts (0.1%, 0.2% and 0.3% w/w), amounts of the oil (10%, 15% and 20% w/w of lipid matrix) and types of the oil (soybean oil (S), medium chain triglycerides (M), oleic acids (O) and linoleic acids (L)) in lipid matrix of all-trans retinoic acid (ATRA)-loaded nanostructured lipid carriers (NLCs) for transdermal drug delivery. The ATRA-loaded solid lipid nanoparticles (SLNs) were formulated with 30% w/w cetyl palmitate. All lipid nanoparticles had average sizes between 130 and 241 nm and had negative zeta potentials. The drug loading of all formulations was higher than 95%. The release of drug from all lipid nanoparticles followed zero-order kinetics. The amount of drug released from all the NLCs and SLNs was significantly greater than the drug released from the ATRA suspension. The ATRA flux of the SLNs was higher than the NLCs. The flux of the NLCs containing oleic acid was significantly higher than the other types of oils. The chemical stability at 4 °C, the percentage of ATRA remaining in all the lipid nanoparticles tested was higher than 80%. It can be concluded that both the SLNs and NLCs are promising dermal drug delivery systems for ATRA.

Development of Ketoprofen Microemulsion for Transdermal Drug Delivery

The aim of this study was to prepare microemulsion for transdermal drug delivery of ketoprofen (KP). The physicochemical and chemical properties of microemulsion were evaluated. The microemulsion were composed of isopropyl myristate (IPM) as oil phase, water, PEG40-hydrogenated castor oil (Cremophor® RH40) as surfactant and PEG400 as co-surfactant, and the surfactant: co-surfactant ratio used was 1:1. The viscosity, droplet size, pH, conductivity of microemulsion and skin permeation of KP through shed snake skin were evaluated. The particle size, viscosity and conductivity of microemulsions were in the range of 172-468 nm, 234.82-1067.35 cP and 6.80-20.87µS/cm, respectively. The ratio of IPM and surfactant mixture played an important role on KP loading capacity of microemulsions formulation and skin permeation of KP. While amount of surfactant increased, the loading capacity of KP increased, but the skin permeation of KP decreased. The results suggested that the novel microemulsion system composed of IPM, water, Cremophor® RH40:PEG400 (ratio 1:1) can be applied for using as a transdermal drug delivery carrier.

Cremophor RH40-PEG 400 microemulsions as transdermal drug delivery carrier for ketoprofen

The aim of this study was to prepare novel microemulsion for transdermal drug delivery of ketoprofen (KP). The microemulsion composed of ketoprofen as model drug, isopropyl myristate (IPM) as oil phase, surfactant mixture consisting of polyoxyl 40 hydrogenated castor oil (Cremophor RH40) as surfactant and polyethylene glycol 400 (PEG400) as co-surfactant at the ratio 1:1, and water were prepared. The viscosity, droplet size, pH, conductivity of microemulsions, and skin permeation of KP through shed snake skin were evaluated. The particle size, pH, viscosity and conductivity of microemulsions were in the range of 114–210 nm, 6.3–6.8, 124–799 cPs and 1–45 µS/cm, respectively. The ratio of IPM, and surfactant mixture played the important role in the skin permeation of KP microemulsions. As the amount of surfactant mixture and IPM increased, the skin permeation of KP decreased. The formulation composed of 30% IPM, 45% surfactant mixture and 25% water showed the highest skin permeation flux. The incorporation of terpenes in the 2.5% KP microemulsions resulted in significant enhancement in skin permeation of KP. The rank order of enhancement ratio for skin permeation enhancement of terpenes was α-pinene > limonene > menthone. The results suggested that the novel microemulsion system containing IPM, water, Cremophor RH40:PEG400 and terpenes can be applied for using as a transdermal drug delivery carrier.

Charged liposomes as carriers to enhance the permeation through the skin

Introduction: In recent years, there has been increased interest in developing charged liposomes as carriers for transdermal drug delivery. It is necessary to modify the basic composition of the liposomes in order to enhance the penetration properties of the vesicles through the skin. Charged liposomes offer several advantages compared with previous drug delivery systems.Areas covered: This paper provides a brief overview of the different drug delivery systems that exist which aim to improve the permeation of drugs through the skin, focusing on the use of charged liposomes for transdermal delivery. We propose a classification of such liposomes based on the origin of the charge given to the vesicles.Expert opinion: Despite the advances that are occurring in the design of charged liposomes for transdermal drug delivery, the long-term stability continues to be a drawback in such systems. The presence of charge on the surface of the vesicles favors the electrostatic repulsion among them, creating a ζ potential positive or negative that prevents their aggregation and flocculation. However, there is loss of the encapsulated drug, which limits the in vivo use of these systems. It should be emphasized that charged liposomes are indeed a promising candidate for use in gene therapy and vaccine targeting, in a great diversity of diseases, for which drugs are administered by the percutaneous route.

Preparation and characterization of marine sponge collagen nanoparticles and employment for the transdermal delivery of 17β-estradiol-hemihydrate

Background: Transdermal administration of estradiol offers advantages over oral estrogens for hormone replacement therapy regarding side effects by bypassing the hepatic presystemic metabolism. Aim: The objective of this study was to develop nanoparticles of Chondrosia reniformis sponge collagen as penetration enhancers for the transdermal drug delivery of 17β-estradiol-hemihydrate in hormone replacement therapy. Method: Collagen nanoparticles were prepared by controlled alkaline hydrolysis and characterized using atomic force microscopy and photon correlation spectroscopy. Estradiol-hemihydrate was loaded to the nanoparticles by adsorption to their surface, whereupon a drug loading up to 13.1% of sponge collagen particle mass was found. After incorporation of drug-loaded nanoparticles in a hydrogel, the estradiol transdermal delivery from the gel was compared with that from a commercial gel that did not contain nanoparticles. Results: Saliva samples in postmenopausal patients showed significantly higher estradiol levels after application of the gel with nanoparticles. The area under the curve (AUC) for estradiol time–concentration curves over 24 hours was 2.3- to 3.4-fold higher and estradiol levels 24 hours after administration of estradiol were at least twofold higher with the nanoparticle gel. Conclusions: The hydrogel with estradiol-loaded collagen nanoparticles enabled a prolonged estradiol release compared to a commercial gel and yielded a considerably enhanced estradiol absorption. Consequently, sponge collagen nanoparticles represent promising carriers for transdermal drug delivery.

Methoxy poly(ethylene glycol)‐block‐poly(D,L‐lactic acid) copolymer nanoparticles as carriers for transdermal drug delivery

AbstractThis work evaluates the transdermal drug delivery properties of amphiphilic copolymer self‐assembled nanoparticles by skin penetration experiments in vitro. Paclitaxel‐loaded methoxy poly(ethylene glycol)‐block‐poly(D,L‐lactic acid) diblock copolymer nanoparticles (PNPs) were prepared by a solid dispersion technique and were applied to the surface of excised full‐thickness rat skin in Franz diffusion cells. HPLC, transmission electron microscopy, Fourier transform infrared spectroscopy and 1H NMR were used to assay the receptor fluid. The results show that the amphiphilic copolymer nanoparticles with the entrapped paclitaxel are able to penetrate rat skin. Ethanol can improve the delivery of PNPs and increase the cumulative amount of paclitaxel in the receptor fluid by 3 times. Fluorescence microscopy measurements indicate that the PNPs can penetrate the skin not only via appendage routes including sweat ducts and hair follicles but also via epidermal routes. Copyright © 2007 Society of Chemical Industry