Preparation and Evaluation of Solid-Self-Emulsifying Drug Delivery System Containing Paclitaxel for Lymphatic Delivery

Abstract

Solid-self-emulsifying drug delivery system (S-SEDDS) of paclitaxel (Ptx) was developed by the spray drying method with the purpose of improving the low bioavailability (BA) of Ptx. 10% oil (ethyl oleate), 80% surfactant mixture (Tween 80 : Carbitol, 90 : 10, w/w), and 10% cosolvent (PEG 400) were chosen according to their solubilizing capacity. The mean droplet size, zeta potential, and encapsulation efficiency of the prepared S-SEDDS were 16.9 ± 1.53 nm, 12.5 ± 1.66 mV, and 56.2 ± 8.1%, respectively. In the S-SEDDS, Ptx presents in the form of molecular dispersion in the emulsions or is distributed in an amorphous state or crystalline with very small size. The prepared S-SEDDS formulation showed 70 and 75% dissolution in 60 and 30 min in dissolution medium pH 1.2 and 6.8, respectively. Significant increase (P≤0.05) in the peak concentration (Cmax), the area under the curve (AUC0–∞), and the lymphatic targeting efficiency of Ptx was observed after the oral administration of the Ptx-loaded S-SEDDS to rats (20 mg/kg as Ptx). Our research suggests the prepared Ptx-loaded S-SEDDS can be a good candidate for the enhancement of BA and targeting drug delivery to the lymphatic system of Ptx.