Modified Nanoprecipitation Method for Preparation of Cytarabine-Loaded PLGA Nanoparticles

Abstract

Abstract. The present investigation was aimed at developing cytarabine-loaded poly(lactide-coglycolide) (PLGA)-based biodegradable nanoparticles by a modified nanoprecipitation which would have sustained release of the drug. Nine batches were prepared as per 3 2 factorial design to optimize volume of the cosolvent (0.22-0.37 ml) and volume of non-solvent (1.7-3.0 ml). A second 3 2 factorial design was used for optimization of drug: polymer ratio (1:5) and stirring time (30 min) based on the two responses, mean particle size (125±2.5 nm), and percentage entrapment efficiency (21.8±2.0%) of the Cyt-PLGA nanoparticles. Optimized formulation showed a zeta potential of −29.7 mV indicating good stability; 50% w/w of sucrose in Cyt-PLGA NP was added successfully as cryoprotectant during lyophilization for freeze-dried NPs and showed good dispersibility with minimum increase in their mean particle sizes. The DSC thermograms concluded that in the prepared PLGA NP, the drug was present in the amorphous phase and may have been homogeneously dispersed in the PLGA matrix. In vitro drug release from the pure drug was complete within 2 h, but was sustained up to 24 h from PLGA nanoparticles with Fickian diffusion. Stability studies showed that the developed PLGA NPs should be stored in the freeze-dried state at 2-8°C where they would remain stable in terms of both mean particle size and drug content for 2 months.

A quality by design approach on polymeric nanocarrier delivery of gefitinib: formulation, in vitro, and in vivo characterization

“…[58][59][60] The actual R 2 value (0.9965) was found to be almost similar to the predicted R 2 value (0.9911). Hence, this is also a supportive evidence for the selected model.…”

“…[58][59][60] The actual R 2 value was more than the predicted R 2 value (0.7628), which also reflects the suitability of the present R2FI model.…”

“…[59][60][61] This actual R 2 value (0.9992) was better than the predicted R 2 value (0.9866). It strongly supports the suitability of the present R2FI model.…”

Formulation and Characterization of Ketorolac Tromethamine Nanoparticle with Eudragit RS-100 and RL-100 by Nano precipitation Method

“…NP were prepared by the nanoprecipitation method with slight modification [13][14][15]. A modified nanoprecipitation method utilizes use of a co-solvent to either increase the entrapment efficiency of the drug in nanoparticles or to reduce the mean particle size of the nanoparticles.Different amount of Eudragit RS 100 or RL 100 and 200 mg of KT were dissolved in 10 ml methanol.…”

Pramipexole Dihydrochloride Loaded Mpegpcl Nanosuspension by Modified Nanoprecipitation: In Vitro and in Vivo Evaluation

“…The preparation of pramipexole dihydrochloride nanosuspension is carried by modified nanoprecipitation method [14,15]. In this method, phosphate buffer with pH 9.0 was used as an external medium instead of aqueous phase.…”