Formulation, characterization and pulmonary deposition of nebulized celecoxib encapsulated nanostructured lipid carriers

Abstract

The aim of the current study was to encapsulate celecoxib (Cxb) in the Nanostructured Lipid Carrier (Cxb-NLC) nanoparticles and evaluate the lung disposition of nanoparticles following nebulization in Balb/c mice. Cxb-NLC nanoparticles were prepared with Cxb, Compritol, Miglyol and sodium taurocholate using high-pressure homogenization. Cxb-NLC nanoparticles were characterized for physical and aerosol properties. In-vitro cytotoxicity studies were performed with A549 cells. The lung deposition and pharmacokinetic parameters of Cxb-NLC and Cxb solution (Cxb-Soln) formulations were determined using Inexpose™ system and Pari LC star jet nebulizer. The particle size and entrapment efficiency of Cxb-NLC formulation were 217 ± 20 nm and > 90%, respectively. The Cxb-NLC released the drug in controlled fashion, and in vitro aersolization of Cxb-NLC formulation showed FPF of 75.6 ± 4.6 %, MMAD of 1.6 ±0.13 μm and GSD of 1.2 ± 0.21. Cxb-NLC showed dose and time dependent cytotoxicity against A549 cells. Nebulization of Cxb-NLC demonstrated 4 fold higher AUC t/ D in lung tissues compared to Cxb-Soln. The systemic clearance of Cxb-NLC was slower (0.93 L/h) compared to Cxb-Soln (20.03 L/h). Cxb encapsulated NLC were found to be stable and aerodynamic properties were within the respirable limits. Aerosolization of Cxb-NLC improved the Cxb pulmonary bioavailability compared to solution formulation which will potentially lead to better patient compliance with minimal dosing intervals.

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

“…Our results are in contrast to the observations of Wang et al (2009) who demonstrated the highest release of drug/prodrug tested from SLN, followed by the NLC and lipid emulsion (LE). Regarding the release kinetics of MFA from SLN and NLC, a biphasic pattern with burst drug release at the initial stage and sustained drug release subsequently was found in contrast to the observations of Patlolla et al (2010). They observed zero order release pattern for celecoxib (Cxb) from Cxb-NLC.…”

Optimization, formulation, and characterization of multiflavonoids-loaded flavanosome by bulk or sequential technique

“…Entrapment efficiency (EE) of the optimal formulation was determined using vivaspin ® centrifuge filters (Sartorius AG, Goettingen, Germany) as described previously 26 with slight modification. Briefly, 1 mL of the flavonosome was loaded on the top compartment of the vivaspin centrifuge filter membrane (MWCO -10 kDa) and centrifuged at 3,500 rpm for 15 minutes.…”

“…Subsequently, equivalent solvent comprising the mixture of Q:K:A:PC was prepared at a ratio similar to that of the same concentration used during the flavonosome formulation and undergone the abovementioned vivaspin protocol to determine the total drug. Thus, the % of EE was determined using the following formula: 26 …”

The Impact of Variables on Particle Size of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers; A Comparative Literature Review

“…All of these drawbacks suggest that these colloidal drug delivery systems are not ideal for use as drug carriers. 8 Nanolipid carriers have gained much interest in pharmaceutical sciences for several delivery routes, e.g., dermal, 11,12 oral, 13 parenteral, 14 pulmonary, [15][16][17][18] and ocular. 19,20 Solid lipid nanoparticles (SLNs) were introduced in the early 1990s as drug carriers.…”