Eco-Friendly Route for Encapsulation of 5-Fluorouracil Into Polycaprolactone Nanoparticles

Abstract

T HE MAIN objective of this study was to allocate and evaluate the most optimum conditions to prepare the 5-Fluorouracil (5-FU) entrapped polycaprolactone (PCL) nanoparticles (5-FU-PCNs) by eco-friendly route. The inner aqueous phase (W 1 ) was added to solution containing PCL with homogenization to form primary emulsion (W 1 /O) which was emulsified with the outer aqueous phase (W 2 ) containing polyvinyl alcohol (PVA) as stabilizer to attain the double emulsion (W 1 /O/W 2 ). The different parameters were investigated to reach the most successful formulation for 5-FU-PCNs, such as polymer concentration, effect of stabilizer concentration ratio(0.5%, 1% and 3%) on drug encapsulation efficiency, etc. The encapsulation efficiency of PCNs was in the range of 14-65.6%. The prepared nanoparticles showed the spherical shape having an average size of 183-944nm.The prepared systems were elucidated by fourier transform infrared spectroscopy (FTIR), UV-spectroscopy, photon correlation spectroscopy (PCS), X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA),scanning electron (SEM) and atomic-force microscopy (AFM). The optimized ratios of the different parameters of double emulsion process were founded. SEM and AFM confirmed the complicated morphology and the formation of the spherical micro-and nanocapsules.

Preparation, Characterization and In vitro Biological activity of 5-Fluorouracil Loaded onto poly (D, L-lactic-co-glycolic acid) Nanoparticles

“…Preparation of PVA solution To be used as emulsion stabilizer in outer aqueous phase where PVA is the most widely used stabilizer due to its low toxicity, good water solubility, and availability in a wide range of molecular weights [28,29]. Three different concentration PVA stock solutions (0.5, 1 and 2 wt.…”

“…Three different concentration PVA stock solutions (0.5, 1 and 2 wt. % stocks A, B and C) were prepared by slowly adding 2.5, 5 and 7.5 mg PVA, respectively, into 500 mL distilled water with stirring and heating at 60 °C for 40 min to obtain a clear 0.5, 1 and 2% PVA solution, respectively [29].…”

“…of 5-FU as 10, 15, 20 and 25 mg of 5-FU was dissolved in 1 ml of 0.5% Acetic acid in order to aid the dissolution of 5-FU and then 5 ml PLGA solution was added at constant (drug: polymer; 1:10). This mixture was properly homogenized using digital high speed homogenizer (T-10; model) at 20,000 rpm for 5 min using to have the first emulsion (W1/O) [29].…”