Nanostructured lipid carriers with exceptional gastrointestinal stability and inhibition of P-gp efflux for improved oral delivery of tilmicosin.

Nanostructured lipid carriers with exceptional gastrointestinal stability and inhibition of P-gp efflux for improved oral delivery of tilmicosin. Colloids Surf B Biointerfaces. 2019 Nov 17;:110649 Authors: Zhang Q, Yang H, Sahito B, Li X, Peng L, Gao X, Ji H, Wang L, Jiang S, Guo D Abstract Tilmicosin (TMS) is widely applied to treat porcine bacterial respiratory diseases in veterinary medicine. However, oral administration of TMS is greatly limited due to its physicochemical properties, such as poor water solubility, gastric acid sensitivity and bitterness. Therefore, nanostructured lipid carriers (NLCs) were developed as an oral delivery system for TMS by the high shear method combined with ultrasonic techniques in this study. The results showed that TMS-NLCs were approximately spherical with a hydrodynamic diameter of 283.03 nm and a zeta potential of -30.04 mV. TMS was almost entirely encapsulated in the NLCs by interacting with the lipid matrix, as characterized by differential scanning calorimetry and fourier transform infrared spectroscopy. Thus, TMS-NLCs had an excellent encapsulation efficiency and loading capacity with values of 93.46% and 9.23%, respectively. TMS-NLCs maintained good stability not only during storage at 4 ℃, 25 ℃ and 40 ℃ for 90 days but also in stimulated gastrointestinal (GI) fluids at 37 ℃ for 7 days. Therefore, TMS-NLCs displayed low and sustained release in vitro without an initial b...
Source: Colloids and Surfaces - Category: Biotechnology Authors: Tags: Colloids Surf B Biointerfaces Source Type: research