Background:
Treatment of glioma with conventional approaches remains a far-reaching
target to provide the desired outcome. This study aimed to develop and optimize Gemcitabine hydrochloride-
loaded PLGA nanoparticles (GNPs) using the Box-Behnken design methodology. The
independent variables chosen for this study included the quantity of Polymer (PLGA) (X1), Tween
80 (X2), and Sonication time (X3), whereas the dependent variables were Particle size (Y1) EE %
(Y2) and PDI (Y3). The optimized biodegradable nanoparticles are investigated for their anti-cancer
effectiveness in U87MG human glioblastoma cells in vitro.
Method:
The formulation process involved two steps. Initially, emulsification was carried out by
combining the organic polymer solution with the aqueous surfactant solution. Subsequently, in the
second step, the organic solvent was evaporated, resulting in the precipitation of the polymer and
the formation of nanoparticles. The quantity of PLGA, Tween 80, and PVA (at a constant concentration)
was adjusted based on the experimental trial approach. Subsequently, the PLGA-based nanoparticles
underwent characterization, wherein their particle size, encapsulation efficiency, polydispersity
index (PDI), and cumulative release were assessed. The optimal formulation composition
was determined as 200 mg of PLGA, 4 ml of Tween 80, and 2 mg of PVA. Further, the optimized
GNPs were evaluated for their anti-cancer effectiveness on U87 MG cells by MTT and apoptosis
assay.
Results:
The results demonstrated that the gemcitabine hydrochloride loaded PLGA nanoparticles
in the optimal formulation exhibited an encapsulation efficiency of 81.66 %, a particle size of 140.1
nm, and a PDI of 0.37. The morphology of the Opt-GNP-PLGA-NP was observed to be spherical
through transmission electron microscopy (TEM).
Conclusion:
The Apoptosis study further confirmed the observations of MTT assay as the Opt-
GNP-PLGA-NP significantly enhanced the apoptosis in U-87 MG cells than the Standard marketed
formulation.
other:
The in vitro cell line study was performed to ensure brain targeting