Formulation and characterization of microspheres loaded with imatinib for sustained delivery.

摘要: The aim of this study was the development imatinib-loaded poly(d,l-lactide-co-glycolide) (PLGA) microspheres with high loading efficiency which can afford continuous release imatinib over a prolonged period time. Imatinib mesylate loaded PLGA size 6-20 μm were prepared by double emulsion (W1/O/W2) method using dichloromethane as volatile solvent. It found that spherical non-porous surface; (LE) highly dependent on pH external water phase (W2). By increasing W2 above highest pKa (pKa 8.1), at is mainly uncharged, LE increased from 10% to 90% (pH 5.0 versus 9.0). Conversely, only 4% its counter ion, mesylate, retained in same condition Since soluble, it unlikely partitions into organic phase. We demonstrated, differential scanning calorimetry (DSC), molecularly dispersed polymeric matrix loadings up 8.0%. At higher drug loading, partially crystallized matrix. released their cargo during three months combination diffusion through polymer and erosion. In conclusion, we have formulated LC. Although started obtained contained base These 3-month interest for local treatment cancer.