Sodium taurocholate (STC) is the sodium salt of taurocholic acid, a bile acid consisting of cholic acid and taurine. STC is a detergent useful for the solubilization of lipids and membrane-bound proteins.
Fig.1 Molecular Structure of STC.
The preparation of SLN was performed using the solvent emulsification/evaporation method. STC is often used as a penetration enhancer for several eye preparations studied earlier. Therefore, the excipient is selected as a cosurfactant for preparing lipid nanoparticles, and stearic acid and tristearate are used as lipid carriers. The properties of the optimized SLN-6 meet the prerequisites of ideal ophthalmic preparation, such as submicron size, narrow PDI, high zeta potential, and good encapsulation efficiency. In vivo study confirmed that VAC from SLN-6 had better ocular bioavailability than drug solution. Hence, the study demonstrated the potential of lipid nanocarriers in the efficient ocular delivery of hydrophilic molecules (like VAC).
Fig.2 Ex vivo corneal permeation of VAC formulations. (Kumar, 2017)
ACZ bilosomes were prepared by the thin-film hydration method using Span 60, cholesterol along with various bile salts (sodium cholate, sodium deoxycholate, STC, and sodium tauroglycocholate) at two molar ratios. The developed vesicular formulations possessed relatively high ACZ entrapment efficiency, their diameters were in the nanometric range (350-735 nm) with monodisperse size distribution and zeta potential values <-43.3. ACZ loaded vesicular formulations showed a biphasic release profile characterized by an initial fast release period in the first 30 min followed by a prolonged period up to 8 h. Selected vesicular formulations appeared as spherical shapes under transmission electron microscopy. The optimized ACZ bilosomal formulation improved and sustained intraocular pressure (IOP) lowering capability in contrast to plain ACZ. In addition, the ocular Draize irritancy test confirmed the safety of the optimized bilosomal formulation post ocular instillation. Thus, the developed bilosomal formulation may be considered as a promising nanocarrier for ocular delivery of ACZ for management of elevated IOP.
Fig.3 Percentage decrease in IOP after ocular application of plain ACZ, ACZ loaded vesicular formulations, marketed DRZ eye drops, and oral administration of marketed ACZ tablet. (Mohsen, 2020)
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