Squarticles as a Lipid Nanocarrier for Delivering Diphencyprone and Minoxidil to Hair Follicles and Human Dermal Papilla Cells
Journal Title: The AAPS Journal - Year 2014, Vol 16, Issue 1
Abstract
Delivery of diphencyprone (DPCP) and minoxidil to hair follicles and related cells is important in the treatment of alopecia. Here we report the development of “squarticles,” nanoparticles formed from sebum-derived lipids such as squalene and fatty esters, for use in achieving targeted drug delivery to the follicles. Two different nanosystems, nanostructured lipid carriers (NLC) and nanoemulsions (NE), were prepared. The physicochemical properties of squarticles, including size, zeta potential, drug encapsulation efficiency, and drug release, were examined. Squarticles were compared to a free control solution with respect to skin absorption, follicular accumulation, and dermal papilla cell targeting. The particle size of the NLC type was 177 nm; that of the NE type was 194 nm. Approximately 80% of DPCP and 60% of minoxidil were entrapped into squarticles. An improved drug deposition in the skin was observed in the in vitro absorption test. Compared to the free control, the squarticles reduced minoxidil penetration through the skin. This may indicate a minimized absorption into systemic circulation. Follicular uptake by squarticles was 2- and 7-fold higher for DPCP and minoxidil respectively compared to the free control. Fluorescence and confocal images of the skin confirmed a great accumulation of squarticles in the follicles and the deeper skin strata. Vascular endothelial growth factor expression in dermal papilla cells was significantly upregulated after the loading of minoxidil into the squarticles. In vitro papilla cell viability and in vivo skin irritancy tests in nude mice suggested a good tolerability of squarticles to skin. Squarticles provide a promising nanocarrier for topical delivery of DPCP and minoxidil.
Authors and Affiliations
Ibrahim A. Aljuffali, Calvin T. Sung, Feng-Ming Shen, Chi-Ting Huang, Jia-You Fang
Keywords
Related Articles
- EP ID EP681050
- DOI 10.1208/s12248-013-9550-y
- Views 54
- Downloads 0
Postexposure management and treatment of anthrax in dogs—Executive councils of the American academy of veterinary pharmacology and therapeutics and the American college of veterinary clinical pharmacology
Dogs are generally at low risk of developing disease following exposure to anthrax. When disease does occur, it appears associated with oral exposure to the bacteria leading to massive swelling of the head, neck, and med...
Interspecies considerations in the evaluation of human food safety for veterinary drugs
Residues are composed of the parent drug and metabolites, and therefore interspecies comparisons must involve a consideration of comparative xenobiotic metabolism. The focus of this article will be the residue studies th...
Mathematical Model Approach to Describe Tumour Response in Mice After Vaccine Administration and its Applicability to Immune-Stimulatory Cytokine-Based Strategies
The online version of this article (doi:10.1208/s12248-013-9483-5) contains supplementary material, which is available to authorized users.
Monoamine oxidase inhibitory properties of some benzazoles: Structure-; Activity relationships
Benzazoles containing two or three nitrogen atoms were screened for their inhibitory activity toward monoamine oxidases MAO-A and MAO-B. In order to clarify the mechanism of interaction of these compounds with the enzyme...
Targeted pharmaceutical nanocarriers for cancer therapy and imaging
The use of various pharmaceutical nanocarriers has become one of the most important areas of nanomedicine. Ideally, such carriers should be specifically delivered (targeted) to the pathological area to provide the maximu...