Design and Evaluation of Voriconazole Loaded Solid Lipid Nanoparticles for Ophthalmic Application

Abstract

Voriconazole is a second-generation antifungal agent with excellent broad spectrum of antifungal activity commercially available for oral and intravenous administration. Systemic administration of voriconazole is associated with side effects including visual and hepatic abnormalities. This study assessed the feasibility of using solid lipid nanoparticles for ocular delivery of voriconazole adopting stearic acid as lipidic material, tween 80 as a stabilizer, and Carbopol 934 as controlled release agent and for increasing the precorneal residence time in eye. The systems were prepared using two different methods, that is, ultrasonication method and microemulsion technique. The results indicated that the larger particle size of SLNs was found with microemulsion technique (308 ± 3.52 nm to 343 ± 3.51) compared to SLN prepared with ultrasonication method (234 ± 3.52 nm to 288 ± 4.58 nm). The polydispersity index values were less than 0.3 for all formulations and zeta potential of the prepared formulations by these two methods varied from −22.71 ± 0.63 mV to −28.86 ± 0.58 mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug. The in vitro release study and the SLN formulations prepared with ultrasonication method demonstrated sustained release up to 12 hours. This study demonstrated that SLN prepared by ultrasonication method is more suitable than microemulsion technique without causing any significant effect on corneal hydration level.

An approach to revolutionize cataract treatment by enhancing drug probing through intraocular cell line

“…Khare et al [18] and Huang et al [30] described a simple protocol of lyophilization of nanoparticles which was followed with suitable modifications. 2.5% w/v mannitol was mixed as a cryoprotectant to the above prepared dispersion followed by lyophilization executed for 24 h to check physical stability and redispersibility of the mix.…”

“…This was carried out by a protocol described by Khare et al [18]. Entrapment efficiency is described as the percentage of the actual drug mass captured in the polymeric carrier, comparative to the original amount of drug loaded, and was calculated using the following equation: …”

“…The whole corneal planning technique was adopted from Khare et al [18] with suitable modifications and had to be completed within 1 h of the goat sacrifice. Proper institute ethical clearance for large animals was obtained for the studies.…”

“…Nano-biotechnology in clinical research has led to abundant pathbreaking therapeutics. The unique possibilities of nanoparticles like reducing toxicity of a drug and biocompatibility make them excellent nanocarriers for therapeutic purposes [18]. Nanoparticulates also help in achieving the most important feature of ocular drug delivery that is equal bioavailability due to their reduced size [19].…”

“…It was approximated from various studies that size of 10–400 nm will allow better passage of nanoparticulates into the deeper layers of ocular structure for prevention of cataract [17,18]. The preparation technique of the SLN-NAC will ensure that the nanoparticles will be transformed from lipophilic to hydrophilic and also may reduce the irritation of the eye.…”