Indomethacin-Loaded Solid Lipid Nanoparticles for Ocular Delivery: Development, Characterization, and In Vitro Evaluation

Abstract

Purpose: The goal of this study was to develop and characterize indomethacin-loaded solid lipid nanoparticles (IN-SLNs; 0.1% w/v) for ocular delivery. Methods: Various lipids, homogenization pressures/cycles, Tween 80 fraction in the mixture of surfactants (Poloxamer 188 and Tween 80; total surfactant concentration at 1% w/v), and pH were investigated in the preparation of the IN-SLNs. Compritol Ò 888 ATO was selected as the lipid phase for the IN-SLNs, as indomethacin exhibited a highest distribution coefficient and solubility in this phase. Results: Homogenization at 15,000 psi for 6 cycles resulted in the smallest particle size. Increase in the Poloxamer 188 fraction resulted in decrease in the entrapment efficiency (EE). The mean particle size, polydispersity index, zeta-potential, and EE of the optimized formulation were 140 nm, 0.16, -21 mV, and 72.0%, respectively. INSLNs were physically stable post-sterilization and on storage for a period of 1 month (last timepoint tested). A dramatic increase in the chemical stability and in vitro corneal permeability of indomethacin was observed with the IN-SLN formulation in comparison to the indomethacin solution-(0.1% w/v) and indomethacin hydroxypropyl-beta-cyclodextrin-based formulations (0.1% w/v). Conclusion: Results from this study suggest that topical IN-SLNs could significantly improve ocular bioavailability of indomethacin.

Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: Effect on formulation and characterization parameters

“…The %EE of 51.51 ± 3.09 was found to be highest with Compritol in comparison with other two lipids. This could be attributed to the fact that Compritol being a mixture of mono, di and triglycerides (glyceryl behenate) along with fatty acids of different chain lengths forms less ordered crystals with many lattice defects which helps in accommodating large amount of drug (Hippalgaonkar et al, 2013;Muller et al, 2000). Hence, Compritol was selected as an optimized lipid and further 1% w/w of TPGS and Pol-188 were taken as stabilizers and/or surfactants (Batch no.…”

Effect of Cyclodextrins on Morphology and Barrier Characteristics of Isolated Rabbit Corneas

“…Several studies in the literature, including some from our own laboratory, have used CDs in the receiver solution during in vitro transcorneal permeability evaluation (14)(15)(16)(17)(18)(19)(20). In view of the findings from this study, it is apparent that use of CDs as solubilizers in the receiver solution could significantly impact transcorneal flux.…”

A novel ion-exchange carrier based upon liposome-encapsulated montmorillonite for ophthalmic delivery of betaxolol hydrochloride

“…In recent years, various ophthalmic drug-delivery systems have been developed for ocular carriers, including liposomes (LPs), [6][7][8] nanoparticles, 9,10 microspheres, 11,12 nanostructured lipid carriers, 13,14 in situ gels, 15,16 and contact lenses. 17 Among these, LPs have proved to be a promising formulation for ocular drug transport in the last decade, because they include enclosed vesicles and bilayer structures.…”