A pre formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Tetracaine TTC is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers NLC may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4 TTC. Structural properties and encapsulation efficiency EE amp; 8201; gt; amp; 8201;63 guided the selection of three pre formulations of different lipid composition, through a 23 factorial design of experiments DOE . DLS and TEM analyses revealed average sizes 193 220 nm , polydispersity lt; amp; 8201;0.2 , zeta potential amp; 8722; amp; 8201;21.8 to amp; 8722; amp; 8201;30.1 mV and spherical shape of the nanoparticles, while FTIR ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre formulation CP TRANS TTC showed phase separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid cetyl palmitate and liquid Transcutol lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach DOE and biophysical techniques two optimized pre formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic gt; amp; 8201;48 h and reducing TTC cytotoxicity against Balb c 3T3 cell