<p>Self-Assembled Lecithin/Chitosan Nanoparticles Based on Phospholipid Complex: A Feasible Strategy to Improve Entrapment Efficiency and Transdermal Delivery of Poorly Lipophilic Drug</p>

Abstract

Lecithin/chitosan nanoparticles have shown great promise in the transdermal delivery of therapeutic agents. Baicalein, a natural bioactive flavonoid, possesses multiple biological activities against dermatosis. However, its topical application is limited due to its inherently poor hydrophilicity and lipophilicity. In this study, the baicalein-phospholipid complex was prepared to enhance the lipophilicity of baicalein and then lecithin/chitosan nanoparticles loaded with the baicalein-phospholipid complex were developed to improve the transdermal retention and permeability of baicalein. Methods: Lecithin/chitosan nanoparticles were prepared by the solvent-injection method and characterized in terms of particle size distribution, zeta potential, and morphology. The in vitro release, the ex vivo and in vivo permeation studies, and safety evaluation of lecithin/ chitosan nanoparticles were performed to evaluate the effectiveness in enhancing transdermal retention and permeability of baicalein. Results: The lecithin/chitosan nanoparticles obtained by the self-assembled interaction of chitosan and lecithin not only efficiently encapsulated the drug with high entrapment efficiency (84.5%) but also provided sustained release of baicalein without initial burst release. Importantly, analysis of the permeation profile ex vivo and in vivo demonstrated that lecithin/chitosan nanoparticles prolonged the retention of baicalein in the skin and efficiently penetrated the barrier of stratum corneum without displaying skin irritation. Conclusion: These results indicate the potential of drug-phospholipid complexes in enhancing the entrapment efficiency and self-assembled lecithin/chitosan nanoparticles based on phospholipid complexes in the design of a rational transdermal delivery platform to improve the efficiency of transdermal therapy by enhancing its percutaneous retention and penetration in the skin.

Comparative colloidal stability, antitumor efficacy, and immunosuppressive effect of commercial paclitaxel nanoformulations

“…The variation in the droplet volume fraction or size was evident as a variation in the light transmission (ΔT) profiles. An unstable formulation was indicated when the variation was > 10% [ 30 , 34 ]. As shown in Fig.…”

“…3 , the variations in the transmission profiles (ΔT) of PTX emulsion and PTX nanoparticle were < 10%, indicating no apparent aggregation or sedimentation upon dispersion of these nanoformulations in dispersion media at 25 °C for 24 or 48 h. On the contrary, flocculation and sedimentation occurred when PTX liposome was dispersed in 5% glucose solution, as evidenced by the greater ΔT (about 50%) value and by their appearance after 24 h. TSI values were calculated from the changes in transmitted light, which were useful to compare the stability in more depth. Higher TSI values indicated lower stability [ 30 , 34 ]. Although the TSI of all nanoformulations increased with time, PTX emulsion and PTX nanoparticle maintained relatively lower TSI values as compared with that of PTX liposome (Fig.…”

Baicalein ameliorates osteoporosis via AKT/FOXO1 signaling

“…BN is one of the most abundant flavonoids in Scutellaria baicalensis and is widely used in Chinese herbal medicine to treat various human diseases for centuries. [ 13 ]. BN promotes osteogenic differentiation and bone formation [ 14 – 16 ], but the molecular mechanisms underlying the beneficial effects of BN on osteoporosis are not clear.…”

Polysaccharide-Based Transdermal Drug Delivery

“…Lecithin/CS nanoparticles (LCNs) were also used to load baicalein-phospholipid complexes to form BPC-LCNs. Phospholipids combined with baicalein to form a complex and enhance the solubility of baicalein, which is encapsulated into lecithin/CS nanoparticles to enhance skin penetration [ 150 ]. Polyunsaturated fatty acids (PUFAs) and the photosensitizer chlorin e6 (Ce6) were self-assembled into nanoassemblies to prepare L-Ce6 NAs and incorporated into fast-dissolving oligo-HA MN patches to prepare L-Ce6 MNs.…”