Role of the charge, carbon chain length, and content of surfactant on the skin penetration of meloxicam-loaded liposomes

Sureewan Duangjit,1,2 Boonnada Pamornpathomkul,1 Praneet Opanasopit,1 Theerasak Rojanarata,1 Yasuko Obata,2 Kozo Takayama,2 Tanasait Ngawhirunpat11Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, Thailand; 2Department of Pharmaceutics, Hoshi University, Shinagawa-ku, Tokyo, JapanAbstract: The objective of this study was to investigate the influence of surfactant charge, surfactant carbon chain length, and surfactant content on the physicochemical characteristics (ie, vesicle size, zeta potential, elasticity, and entrapment efficiency), morphology, stability, and in vitro skin permeability of meloxicam (MX)-loaded liposome. Moreover, the mechanism for the liposome-enhanced skin permeation of MX was determined by Fourier transform infrared spectroscopy and differential scanning calorimetry. The model formulation used in this study was obtained using a response surface method incorporating multivariate spline interpolation (RSM-S). Liposome formulations with varying surfactant charge (anionic, neutral, and cationic), surfactant carbon chain length (C4, C12, and C16), and surfactant content (10%, 20%, and 29%) were prepared. The formulation comprising 29% cationic surfactant with a C16 chain length was found to be the optimal liposome for the transdermal delivery of MX. The skin permeation flux of the optimal formulation was 2.69-fold higher than that of a conventional liposome formulation. Our study revealed that surfactants affected the physicochemical characteristics, stability, and skin permeability of MX-loaded liposomes. These findings provide important fundamental information for the development of liposomes as transdermal drug delivery systems.Keywords: optimal liposome, optimization, transdermal drug delivery, surfactant charge, surfactant carbon chain length, surfactant conten

Potential enhancement and targeting strategies of polymeric and lipid-based nanocarriers in dermal drug delivery

Nanocarriers used for alternative drug-delivery strategies have gained interest due to improved penetration and delivery of drugs into specific regions of the skin in recent years. Dermal drug delivery via polymeric-based nanocarriers (polymeric nanoparticles, micelles, dendrimers) and lipid-based nanocarriers (solid-lipid nanoparticles and nanostructured lipid carriers, vesicular nanocarriers including liposomes, niosomes, transfersomes and ethosomes) has been widely investigated. Although penetration of nanocarriers through the intact skin could be restricted, these carriers are particularly considered as feasible for the treatment of dermatological diseases in which the skin barrier is disrupted and also for follicular delivery of drugs for management of skin disorders such as acne. This review mainly highlights the recent approaches on potential penetration enhancement and targeting mechanisms of these nanocarriers