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Formulation, development and in vivo characterization of selegiline hydrochloride nanostructured lipid nanocarrier
Anuradha Patil1, Amarjitsing Rajput1, Praveen Subbappa2
1Department of Pharmaceutics, Bharti Vidyapeeth Deemed to be University, Poona College of Pharmacy, Erandwane, Pune 411038, Maharashtra, India.
Abstract:
Depression is a common mental condition causing depressed mood and loss of pleasure. The primary treatment approach for the management of depression consists of the use of selegiline (MAO-B) inhibitor compound. The present work aimed to develop and optimize selegiline-loaded nanostructured lipid carriers for transdermal application, utilizing a 23 full factorial design approach. The optimized nanostructured lipid carriers formulation (Batch B7) demonstrated a particle size of 158.71 ± 0.56 nm, a narrow size distribution (0.266 ± 0.006), high entrapment efficiency (59.60 ± 0.34 %), and a zeta potential of -23.2 ± 2.21 mV. Furthermore, x-ray diffraction and differential scanning calorimetry studies revealed the amorphous transformation of selegiline within the nanostructured lipid carrier. Transmission Electron Microscopy study has shown that nanostructured lipid carrier particles had a spherical shape with a smooth surface. These optimized nanostructured lipid carriers were then incorporated into a microneedle array patch for transdermal delivery. The selegiline-loaded nanostructured lipid carrier microneedle array patch exhibited no skin irritation in a rabbit model. It enhanced drug diffusion ex vivo (1.13-fold compared to pure selegiline-loaded microneedle array patch) with 90 % drug release in 12 h. The pharmacokinetic study demonstrated a steady and controlled release profile with a half-life of 29.9 ± 0.14 h and AUC0-t (26.57 ± 0.51 μg/ml*h) of selegiline loaded nanostructured lipid carrier microneedle array patch. On the contrary, a pure selegiline-loaded microneedle array patch showed a short half-life of 6.5 ± 0.26 h and AUC0-t (20.90 ± 0.31 μg/ml*h). The sustained release profile and prolonged half-life in plasma and the brain suggest improved therapeutic efficacy. Histopathology analysis revealed no significant toxicity to vital organs. Thus, a selegiline nanostructured lipid carrier-loaded microneedle array patch can increase brain bioavailability compared to a pure selegiline-loaded microneedle array patch for managing depression.
