Formulation, optimization and evaluation of vitamin E TPGS emulsified dorzolamide solid lipid nanoparticles
Herein, we designed this research to develop dorzolamide (DRZ) encapsulated solid lipid nanoparticles (SLNs) for ocular administration. The DRZ-SLNs were fabricated by ultrasonic emulsification method and optimized statistically by Box-Behnken design (3 factors at three levels BBD). Glyceryl monostearate (GMS; A), D-a-Tocopherol polyethylene glycol 1000 succinate (TPGS; B), and sonication time (ST; C) were chosen as independent variables while particles size (PS; R1), polydispersity index (PDI; R2), and encapsulation efficiency (EE%; R3) were selected as dependent variables/responses.
The optimized DRZ-SLNs showed the PS, PDI, and EE of 175.38 ± 5.42 nm, 0.19 ± 0.05, and 80.47 ± 3.57%, respectively. The optimized DRZ-SLNs represented initially fast release within 2 h and then a sustained release profile from 2 h to 10 h in simulated tear fluids (STF). DRZ-SLNs revealed 2.87-fold higher trans corneal permeation enhancement compared to DRZ solution. Furthermore, HET-CAM study and the histopathology study revealed that optimized DRZ-SLNs was found to be non-irritant and safe for ocular delivery. Therefore, it was concluded that the DRZ SLNs can be a promising and effective nanoplatform for ocular administration.
Article information: Mohammed Shadab Shahab, Md Rizwanullah, Syed Sarim Imam, Formulation, optimization and evaluation of vitamin E TPGS emulsified dorzolamide solid lipid nanoparticles, Journal of Drug Delivery Science and Technology, Volume 68, 2022. https://doi.org/10.1016/j.jddst.2021.103062.