Background:
Glioblastoma multiforme (GBM) is a belligerent brain tumor constituting
about 67% of primary brain tumours. The current therapy for glioblastoma multiforme
is surgery, radiations and chemotherapy though the success rate is quite limited. Azacitidine
is a hydrophilic anti-cancer agent which acts by demethylation and is used in the
treatment of both acute and chronic myelomonocytic leukaemia along with GBM.
Objective:
Formulation of stable Azacitidine loaded poly-lactide-co-glycolide (PLGA)
nanoparticles (NPs) with tailor-made release profiles.
Methods:
Preparation of Azacitidine loaded PLGA nanoparticles was done by double
emulsion (w/o/w) solvent evaporation technique. PLGA was used in the formulation, as it
is biocompatible and biodegradable. Polyvinyl alcohol worked as an emulsifier while
Span 80 decreased the interfacial tension among two immiscible phases (aqueous and organic),
resulting in increased stability of the formulation.
Results:
Polymer concentration was directly proportional to the entrapment and drug
loading and inversely proportional to particle size. Azacitidine loaded PLGA NPs showed
a biphasic release model. At the first stage, burst release was observed, followed by sustained
release. About 43.93 ± 0.69% drug was released in 1 hour and the remaining drug
was released in 48 hours.
Conclusion:
Dual release behavior first delivered an ample amount of dose which provided
cytotoxic dose, followed by the maintenance dose for sustaining the cytotoxic drug
levels. Future prospective requires In-vitro cell viability evaluation of tailor-made polymeric
nanoparticles along with In-vivo evaluation for therapeutic intervention in a glioblastoma
tumor model.
Preparation and in vitro evaluation of thienorphine-loaded PLGA nanoparticles
