Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles

Abstract

The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.

Surface-Decorated Nanocarrier as a Targeted Drug Delivery Cargo to Folate Receptor-Overexpressing Cells for Enhancing Anti-cancer and Anti-inflammatory Activity

“…In addition, when PVA concentration increases, residual PVA molecules can deposit on the surface of the NPs and the coalescence of NPs may be enhanced, increasing PS [62]. Similar results were reported earlier in the literature [58]. As shown in Table 1, PS was significantly (p<0.001) increased upon surface modification with FA-CS conjugate (F10 and F11) compared to the selected uncoated formulation (F2), which could be assigned to the electrostatic interaction and hydrogen bonding between the protonated amino groups of CS and negatively charged carboxylate groups of PLGA, confirming efficient surface functionalization of FA-CS on NPs surface, depending on adsorption mechanism [2].…”

“…Noteworthy, PS was gradually increased as the polymer concentration increased, at both drug-polymer weight ratios (1:5 or 1:10) or fixed drug amounts (F1 vs F5 and F2 vs F6), which might have been caused by an increase in the viscosity of the organic phase, leading to a reduction in net shear stress and the formation of larger particles [28,52]. Moreover, the dispersion rate of PLGA solution in the aqueous phase might have decelerated as the viscosity of the organic phase increased, forming larger droplets, and generating larger NPs as the organic solvent is eliminated [57][58][59]. Moreover, PS slightly decreased as drug amount increased (F4 vs F1, F5 vs F2, and F6 vs F3) at maintained polymer concentration, which could be related to the fact that at higher drug amount, drug-polymer interaction increases [54]; henceforth, polymerpolymer and polymer-solvent interaction diminish and so does the PS as such polymer related interactions impart significant increment in the PS [57].…”

Redox-Sensitive Poly(lactic-co-glycolic acid) Nanoparticles of Palbociclib: Development, Ultrasound/Photoacoustic Imaging, and Smart Breast Cancer Therapy

“…DCM was removed from the synthesized PLGA-NPs under magnetic stirring. 25 Similarly, PLB-entrapped redox-sensitive PLGA-NPs were prepared with a slight modification. Briefly, PLGA (20 mg) and PLB (3 mg) were dissolved in 2 mL of DCM.…”

“…The organic solvent was removed from the synthesized PLGA-NPs under magnetic stirring. 25 Further, Coumarin 6 (C6) or ICG-loaded PLGA-NPs were prepared as per the above method by replacement of PLB with 0.3 mg of C6 or ICG. The developed NPs were centrifuged, and the obtained pellets were washed with DW and redispersed in the normal saline.…”

Development and Evaluation of Amlodipine-Polymer Nanocomposites Using Response Surface Methodology

“…There are many recent studies in which nanotechnology has been used to deliver amlodipine; for example, Alawdi investigated the loading of amlodipine on nanodiamond particles [15]. The emulsion solvent evaporation method was employed successfully to produce the amlodipine-PLGA nanoparticles [16]. The transdermal system containing amlodipine-pluronic was investigated and enhanced transdermal permeation of the poorly water-soluble drug via transdermal films [17].…”