Surface modified nanostructured lipid carrier for improved ocular delivery: In vitro and ex-vivo study

Chandrashekhar Mahadeo Chakole, Pravat Kumar Sahoo, Pankaj Kumar Sharma, MeenakshiKanwarChauhan*

Delhi Institute of Pharmaceutical Sciences and Research, DPSR-University, New Delhi, India

ABSTRACT

Nano structured lipid carrier (NLC) is a new generation Nano particulate system that offers several advantages over polymeric nanoparticles. However, NLC possesses less muco-adhesiveness in the eye due to its anionic nature. Therefore, the present study aimed to modify the surface of NLC with cationic compounds to improve corneal permeability. The objective of the present study was to prepare and optimize Dexamethasone NLC, surface modification of NLC with carboxymethyl chitosan, and comparative evaluation of both with the marketed formulation. A combined melt emulsification and ultrasonication method was used to prepare NLC. The optimized NLC formulations shown particle size (64±2.3 nm), polydispersity in Dexamethasone (0.270±0.008), zeta potential (-12±3.42 mV), and entrapment efficiency (96.66±0.41%). Carboxymethyl chitosan modified dexamethasone loaded NLC showed particle size (260.73±4.66 nm) and dexamethasone (10.8±6.0 mV). It exhibited sustained drug release than NLC and marketed eye drop. In the ex vivo study, surface modified NLC had a permeability coefficient of 228.88 cm h-1, which is 2.60-and 1.61-times greater than eye drop and NLC, respectively. Surface-modified NLC has shown comparatively sustained release with plain NLC and commercial eye drops. The surface-modified form can adhere firmly with mucin and shown improved trans corneal permeability. Therefore, CNLC would be the potential nanocarrier for dexamethasone to minimize dose requirement and overcome systemic adverse events.

Keywords:

Cationic NLC, Ocular drug delivery, Ocular permeability, Dexamethasone