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.
Highlights
Paclitaxel (Ptx) is an anticancer drug that has a diterpenoid pseudoalkaloid structure and is extracted from the bark of Western yew, Taxus brevifolia [1, 2]
We evaluated the pharmacokinetic characteristics and lymphatic targeting efficiency of the prepared Solid-self-emulsifying drug delivery system (S-Self-emulsifying drug delivery system (SEDDS)) in rats
The oil represents one of the most important excipients in the SEDDS formulation because it can solubilize considerable amount of the lipophilic drug and increase the fraction of the drug transported via the intestinal lymphatic system
Summary
Paclitaxel (Ptx) is an anticancer drug that has a diterpenoid pseudoalkaloid structure and is extracted from the bark of Western yew, Taxus brevifolia [1, 2]. It is active in metastatic breast cancer and is under evaluation for the adjuvant and neoadjuvant treatment of early breast cancer [3, 4]. Ptx is practically insoluble in water with a very low aqueous solubility [2, 8, 9] It is soluble in a mixture of Cremophor EL and anhydrous ethanol (50 : 50, v/v) [2, 10]. Cremophor EL has been associated with serious side effects and leads to hypersensitivity, nephrotoxicity, and neurotoxicity in many patients [2, 11]
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