Preparation, characterization and optimization of sildenafil citrate loaded PLGA nanoparticles by statistical factorial design

Abstract

Background and the aim of the studyThe objective of the present study was to formulate and optimize nanoparticles (NPs) of sildenafil-loaded poly (lactic-co-glycolic acid) (PLGA) by double emulsion solvent evaporation (DESE) method. The relationship between design factors and experimental data was evaluated using response surface methodology.MethodA Box-Behnken design was made considering the mass ratio of drug to polymer (D/P), the volumetric proportion of the water to oil phase (W/O) and the concentration of polyvinyl alcohol (PVA) as the independent agents. PLGA-NPs were successfully prepared and the size (nm), entrapment efficiency (EE), drug loading (DL) and cumulative release of drug from NPs post 1 and 8 hrs were assessed as the responses.ResultsThe NPs were prepared in a spherical shape and the sizes range of 240 to 316 nm. The polydispersity index of size was lower than 0.5 and the EE (%) and DL (%) varied between 14-62% and 2-6%, respectively. The optimized formulation with a desirability factor of 0.9 was selected and characterized. This formulation demonstrated the particle size of 270 nm, EE of 55%, DL of 3.9% and cumulative drug release of 79% after 12 hrs. In vitro release studies showed a burst release at the initial stage followed by a sustained release of sildenafil from NPs up to 12 hrs. The release kinetic of the optimized formulation was fitted to Higuchi model.ConclusionsSildenafil citrate NPs with small particle size, lipophilic feature, high entrapment efficiency and good loading capacity is produced by this method. Characterization of optimum formulation, provided by an evaluation of experimental data, showed no significant difference between calculated and measured data.

Follicular delivery of spironolactone via nanostructured lipid carriers for management of alopecia

“…This model explains the time-dependent release of drug from an insoluble matrix based on Fickian diffusion. 35 Similar results were reported by Ghasemian et al 36 TeM microscopy TEM images of the optimized SL-NLC 2 confirmed that the particles were nonaggregated and spherical in shape with narrow size distribution (Figure 4). It was observed from different frames that only single colloidal species were present throughout the investigated sample.…”

PLGA Microparticles Entrapping Chitosan-Based Nanoparticles for the Ocular Delivery of Ranibizumab

“…The resultant primary emulsion was added to 3 mL of secondary continuous phase composed of 1% w/v PVA plus 0.5% w/v of empty chitosan-based nanoparticles, prepared as outlined in Section 2.4. To avoid creating a concentration gradient which would act as driving force for diffusion, affecting the drug entrapment efficiency and release (37) a similar concentration of nanoparticles was used in the primary phase and continuous phase for all of the preparations. The mixture was homogenised for a further 2 minutes.…”

Inhaled sildenafil nanocomposites: lung accumulation and pulmonary pharmacokinetics

“…As previously reported, SC-loaded PLGA nanoparticles were prepared using the DESE method and the formulation parameters were then optimized 21 . In the optimum condition, approximately, 0.8 mL of aqueous drug solution (3 mg/mL) was emulsified in 1.2 mL methylene chloride containing 40 mg of PLGA.…”

“…The capsule shells, inhaler body and impinger throat, stages 1 and 2 were washed separately with water and the volume of each sample was adjusted with the same solvent. SC was extracted from nanoparticles and the concentration of drug was analyzed for each sample by the HPLC method 21 .…”

“…In our previous report, SC-loaded PLGA nanoparticles were prepared by the method of double emulsion solvent evaporation (DESE) 21 . In this study, microstructures containing these nanoparticles were prepared and evaluated for the effects of carrier type, presence of leucine and the rate of spraying on the characteristics of resulting particles.…”