Tyrosine kinase inhibitor loaded PCL microspheres prepared by S/O/W technique using ethanol as pretreatment agent.
A new tyrosine kinase inhibitor (denoted as CH331) and its poly(epsilon-caprolactone) (PCL) microspheres were studied. The CH331 particles were pretreated with ethanol and then used to prepare CH331 loaded PCL microspheres by S/O/W solvent evaporation technique. Solubility values of CH331 in several organic and aqueous media were measured. The amount of ethanol and CH331 solubility play a significant role in drug loading, encapsulation efficiency, mean diameter and morphology of the microspheres, crystallinity and in vitro drug release. The treatment with a suitable amount of ethanol leads to more uniform sizes, better appearance and higher encapsulation efficiency for the microspheres. Compared with 0.5% PVA phosphate buffer solution (pH 7.4), 0.5% PVA aqueous solution as outer aqueous phase lowers encapsulation efficiency of microspheres, however, improves the drug release behavior.
Zhang
Yanting
Y
School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
Zhang
Yaqiong
Y
Guo
Shengrong
S
Huang
Wenlin
W
D002626:Chemistry, Pharmaceutical / Q000379:methods; D003460:Crystallization; D000431:Ethanol / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D047428:Protein Kinase Inhibitors / Q000737:chemistry*; D011799:Quinazolines / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry
C541773:CH 331; D011091:Polyesters; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D012997:Solvents; C016240:polycaprolactone; D000431:Ethanol