Dual agents loaded PLGA nanoparticles: systematic study of particle size and drug entrapment efficiency.
PLGA nanoparticles simultaneously loaded with vincristine sulfate (VCR) and quercetin (QC) were prepared via O/W emulsion solvent evaporation. Six independent processing parameters and PLGA characteristics were assessed systematically to enhance the incorporation of the dual agents with different properties (VCR and QC, hydrophilic and hydrophobic molecule, respectively) into PLGA nanoparticles and control particle size. Approaches investigated for the enhancement of drug entrapment efficiencies and the controlling of particle size included the influence of the molecular weight (MW) of PLGA and the lactide-to-glycolide (L:G) ratio of PLGA, PLGA concentration, PVA concentration, initial QC content, acetone-to-dichloromethane (A/D) volume ratio, aqueous phase pH and aqueous to organic phase (W/O) volume ratio. The nanoparticles produced by optimal formulation were submicron size (139.5+/-4.3 nm, n=3) with low polydispersity index (0.095+/-0.031, n=3). Nanoparticles observed by transmission electron microscopy (TEM) showed extremely spherical shape. The entrapment efficiencies determined by high performance liquid chromatography (HPLC) by ultracentrifuge method were 92.84+/-3.37% for VCR and 32.66+/-2.92% for QC (n=3). The drug loadings were 0.0037+/-0.0001% for VCR and 1.36+/-0.12% for QC (n=3).
Song
Xiangrong
X
West China School of Pharmacy, Sichuan University, Sichuan, PR China.
Zhao
Yu
Y
Hou
Shixiang
S
Xu
Fangyuan
F
Zhao
Rongli
R
He
Junyao
J
Cai
Zheng
Z
Li
Yuanbo
Y
Chen
Qiuhong
Q
D000096:Acetone / Q000737:chemistry; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D004563:Electrochemistry; D006863:Hydrogen-Ion Concentration; D019344:Lactic Acid; D008752:Methylene Chloride / Q000737:chemistry; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage*; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011794:Quercetin / Q000008:administration & dosage; D014750:Vincristine / Q000008:administration & dosage
D000972:Antineoplastic Agents, Phytogenic; D004364:Pharmaceutical Preparations; D000096:Acetone; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D008752:Methylene Chloride; D014750:Vincristine; D011794:Quercetin