Physicochemical Characterization of Chitosan-Decorated Finasteride Solid Lipid Nanoparticles for Skin Drug Delivery

Abstract

Finasteride is considered the drug of choice for androgenic alopecia and benign prostate hyperplasia. The aim of the study was to formulate nanodrug carriers of finasteride with enhanced retentive properties in the skin. The finasteride was formulated as solid lipid nanoparticles that were decorated with different concentrations of chitosan for improved retentive properties. Solid lipid nanoparticles (SLNs) were synthesized by “high-speed homogenization technique” using stearic acid as a solid lipid while PEG-6000 and Tween-80 were used as surfactants. The SLNs were evaluated for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, and drug release behavior. The mean particle size of SLNs was in the range of 10.10 nm to 144.2 nm. The PDI ranged from 0.244 to 0.412 while zeta potential was in the range of 8.9 mV to 62.6 mV. The drug entrapment efficiency in chitosan undecorated formulations was 48.3% while an increase in drug entrapment was observed in chitosan-decorated formulations (51.1% to 62%). The in vitro drug release studies of SLNs showed an extended drug release for 24 hours after 4 hours of initial burst release. The extended drug release was observed in chitosan-coated SLNs in comparison with uncoated nanoparticles. The permeation and retention study revealed higher retention of drug in the skin and low permeation with chitosan-decorated SLNs that ranged from 39.4 μg/cm2 to 13.2 μg/cm2. TEM images depicted spherical shape of SLNs. The stability study confirmed stable formulations in temperature range of 5°C and 40°C for three months. It is concluded from this study that the SLNs of finasteride were successfully formulated and chitosan decoration enhanced the drug retention in the skin layers. Therefore, these formulations could be used in androgenic alopecia and benign prostate hyperplasia to avoid the side effects, drug degradation, and prolonged use of drug with conventional oral therapy.

Influence of Surface-Modification via PEGylation or Chitosanization of Lipidic Nanocarriers on In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Apixaban

“…The presence of an additional PEG or chitosan layer provided the modified NLC formulations with additional steric stability, which reduced the coagulation of vesicles and eventually led to a reduction in growth rate [ 21 , 25 ]. Moreover, chitosan could increase repulsive forces among the positively charged surfaces of the NLC vesicles [ 78 ].…”

Recent Progress of Lipid Nanoparticles-Based Lipophilic Drug Delivery: Focus on Surface Modifications

“…In addition, chitosan coating can improve the physical stability and extend the storage period of SLNs by over two times at 4 °C. Sohaib et al [ 129 ] confirmed that the drug-loading rate, drug release duration, and skin penetration were improved when finasteride, a lipophilic drug, was delivered to the skin through CS-SLNs in animal experiments.…”

Effects of Lipid Phase Content on the Technological and Sensory Properties of O/W Emulsions Containing Bemotrizinol Loaded Nanostructured Lipid Carriers

“…In the last two decades, UV-filter incorporation into lipid nanoparticles has been proposed as a promising strategy to develop formulations containing lower amounts of organic UV-filters without reducing the sun protection factor (SPF), due to the ability of these nanocarriers to act as physical sunscreens [15][16][17][18][19][20]. The first generation of lipid nanoparticles, namely solid lipid nanoparticles (SLN), consisted of a solid lipid core stabilized by surfactants in aqueous media [21][22][23][24][25][26][27][28]. Due to their drawbacks, such as poor stability and loading capacity, a second generation of lipid nanoparticles (nanostructured lipid carriers, NLC) whose core was made up of mixtures of liquid and solid lipids was developed [29][30][31][32][33][34][35].…”