Preparation and Characterization of Paclitaxel Loaded SF/PLLA-PEG-PLLA Nanoparticles via Solution-Enhanced Dispersion by Supercritical CO2

Zheng Zhao,Yu Zhang,Yi Li

doi:10.1155/2015/913254

Abstract

Paclitaxel loaded silk fibroin/PLLA-PEG-PLLA (PTX-SF/PLLA-PEG-PLLA) nanoparticles with a mean particle size of about 651 nm were fabricated successfully by the SEDS process. Fourier transform infrared (FTIR) spectroscopy analysis indicated that the PTX was encapsulated by SF/PLLA-PEG-PLLA nanoparticles. X-ray powder diffraction (XRPD) analysis supported the results of FTIR analysis and also suggested that the crystalline state of PTX was decreased obviously. Furthermore, the UV-Vis/HPLC analysis showed that drug load (DL) and encapsulation efficiency (EE) were 18.1% and 90.2%, respectively. Thein vitrodrug release experiment suggested that the PTX-SF/PLLA-PEG-PLLA nanoparticles exhibited a sustained release and only 16.1% and 24.5% of paclitaxel were released at pH 7.4 and 6.0, respectively, in one week. The PTX-SF/PLLA-PEG-PLLA nanoparticles drug delivery system with pH-dependent release property has potential application in the field of tumor therapy.

Highlights

Paclitaxel (PTX), a mitotic inhibitor used in cancer chemotherapy, has exhibited its potency against many kinds of cancers, including advanced ovarian, lung, and breast cancers [1, 2]
Nanoparticles exhibit a composite structure with mean particle size of 634 nm and silk fibroin wrapped with PLLAPEG-PLLA triblock polymer [23]
It suggested that the solution-enhanced dispersion by supercritical CO2 (SEDS) process is an effective method to prepare silk fibroin (SF)/PLLAPEG-PLLA and PTX-SF/PLLA-polyethylene glycol (PEG)-PLLA nanoparticles

Summary

Introduction

Paclitaxel (PTX), a mitotic inhibitor used in cancer chemotherapy, has exhibited its potency against many kinds of cancers, including advanced ovarian, lung, and breast cancers [1, 2]. The anticancer mechanism of PTX involves binding to microtubules, forming dysfunctional microtubules, and resulting in cell death [3]. Its poor solubility in water drastically limits its clinical application in its natural form. Paclitaxel is commercially formulated at 6 mg/mL in a vehicle composed of 1 : 1 blend of Cremophor EL and ethanol to make Taxol. The anticancer drug cannot be selectively accumulated into tumors tissues. The nonspecific distribution will reduce bioavailability and therapeutic efficiency of the anticancer drug because the drug spreads randomly during systemic circulation and effects cells (healthy or tumor cells) indiscriminately [6]

Methods

Results

Conclusion