Present study explores native L-asparaginase encapsulated long-acting cross-linker-free PLGA-nanoformulation in an Ehrlich ascites tumor model. L-asparaginase-PLGA nanoparticles for tumor were prepared using a double emulsion solvent evaporation technique, optimized and validated by Box-Behnken Design. L-ASN-PNs showed a particle size of 195 nm ± 0.2 nm and a PDI of 0.2. Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM) techniques revealed its smooth morphology and elicited an in-vitro release of 80% of the drug, following the Higuchi drug release model. In-vivo studies of L-ASN-PNs on an Ehrlich ascites tumor (EAT) model were completed and compared with the standard medication of 5-fluorouracil (5-FU) treatment. L-ASN-PN treated mice showed a 51.15% decrease in tumor volume and 100% survival rate with no reduction in body weight, no haemotoxicity and no hepatotoxicity, as evident from the hematological parameters, and liver enzyme parameters that were well within the prescribed limits. Chemotherapy has severe side effects and restricted therapeutic success. Henceforth, the purported L-Asparaginase PLGA nanoparticles are a suitable entity for better tumor regression, intra-tumor accumulation and no hematological side-effects.

本研究探索了在Ehrlich腹水肿瘤模型中天然L-天冬酰胺酶封装的长效无交联剂PLGA纳米配方。使用双重乳液溶剂蒸发技术制备了用于肿瘤的L-天冬酰胺酶-PLGA纳米粒子，并通过Box-Behnken Design优化和验证。L-ASN-PNs的粒径为195 nm±0.2 nm，PDI为0.2。遵循Higuchi药物释放模型，扫描电子显微镜（SEM）和透射电子显微镜（TEM）技术揭示了其光滑的形态，并引发了80％的药物体外释放。体内已完成对艾氏腹水肿瘤（EAT）模型的L-ASN-PNs的研究，并将其与5-氟尿嘧啶（5-FU）治疗的标准药物进行了比较。L-ASN-PN治疗的小鼠的血液学参数和肝酶参数均在规定范围内，显示肿瘤体积减少51.15％，存活率100％，且体重未降低，无血液毒性和肝毒性限制。化学疗法具有严重的副作用并且限制了治疗的成功。今后，声称的L-天冬酰胺酶PLGA纳米颗粒是用于更好的肿瘤消退，肿瘤内积累且没有血液学副作用的合适实体。