Fabrication and Evaluation of Amitriptyline HCl Loaded Nanostructured Lipid Carriers and In-Vitro Characterization
Abstract
Both liquid and solid lipids make up the 2ndgeneration lipid nanoparticles, also known as nanostructured lipid carriers (NLCs), which are designed to increase medication encapsulation and storage stability. They enhance solubility, stability, and bioavailability. This study aims to develop an aqueous NLC dispersion for Amitriptyline HCl (AMT-HCl) to boost bioavailability while reducing dose frequency, amount, side effects, and toxicity.AMT-NLCs were prepared using the hot-melt high pressure homogenization (HPH) method, which contains Oleic acid as liquid lipid and stearic acid as solid lipids with a combination of Poloxamer 188 and Tween 80 as surfactants.The optimization involved adjusting the solid-to-liquid lipid ratio and surfactant concentrations. NLCs, which are advanced second-generation lipid nanoparticles, consist of both solid and liquid lipids, enabling improved drug encapsulation and reduced leakage during storage.AMT-NLCs evaluated for FTIR (no interaction), entrapment efficiency (77.3% to 84.4%), drug loading (9.9%) zeta potential (-33.7mv), particle size (93.33 nm), PDI (0.196), drug release (91.2%). TEM images showed AMT-HCl loaded NLC are in nano size with spherical in shape. Nanostructured lipid carriers (NLCs) prepared via the HPH method exhibited good entrapment efficiency, and particle size below 100 nm indicates better absorption through intranasal route and delivery of drug to the brain. The formulated batches demonstrated good drug loading and drug release pattern. Zeta potential indicates stable aqueous dispersion. The NLC (6) batch exhibited the most potential of all the produced batches, indicating that NLC may be the most effective approach for transporting medications to the brain through the intranasal route.NLC 6 holds promise for managing oxidative stress-related neurodegenerative diseases, including depression.
Keywords
Amitriptyline HCl; depression; nose-to-brain; NLC; poloxamer 188; stearic acid.