Design and Optimization of PLGA-Based Diclofenac Loaded Nanoparticles

Abstract

Drug based nanoparticle (NP) formulations have gained considerable attention over the past decade for their use in various drug formulations. NPs have been shown to increase bioavailability, decrease side effects of highly toxic drugs, and prolong drug release. Nonsteroidal anti-inflammatory drugs such as diclofenac block cyclooxygenase expression and reduce prostaglandin synthesis, which can lead to several side effects such as gastrointestinal bleeding and renal insufficiency. The aim of this study was to formulate and characterize diclofenac entrapped poly(lactide-co-glycolide) (PLGA) based nanoparticles. Nanoparticles were formulated using an emulsion-diffusion-evaporation technique with varying concentrations of poly vinyl alcohol (PVA) (0.1, 0.25, 0.5, or 1%) or didodecyldimethylammonium bromide (DMAB) (0.1, 0.25, 0.5, 0.75, or 1%) stabilizers centrifuged at 8,800 rpm or 12,000 rpm. The resultant nanoparticles were evaluated based on particle size, zeta potential, and entrapment efficacy. DMAB formulated NPs showed the lowest particle size (108±2.1 nm) and highest zeta potential (−27.71±0.6 mV) at 0.1 and 0.25% respectively, after centrifugation at 12,000 rpm. Results of the PVA based NP formulation showed the smallest particle size (92.4±7.6 nm) and highest zeta potential (−11.14±0.5 mV) at 0.25% and 1% w/v, respectively, after centrifugation at 12,000 rpm. Drug entrapment reached 77.3±3.5% and 80.2±1.2% efficiency with DMAB and PVA formulations, respectively. The results of our study indicate the use of DMAB for increased nanoparticle stability during formulation. Our study supports the effective utilization of PLGA based nanoparticle formulation for diclofenac.

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“…However, it has been observed that the size of the nanoparticles was higher than that of the blank nanoparticles. This phenomenon has also been observed in a previous study [15].…”

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“…It is, thus, reckoned that this fact can result on different adsorption efficiency of T-80. Moreover, although different surfactants (DMAB or DDAB) did not influence NPs physical properties, it is believed that due to the greater lipophilicity of DMAB, this surfactant can promote a better emulsification process for the formation of the polymeric condensate [41]. We could only verify small tendencies of improved PDI and ζ potential for this surfactant group.…”

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“…They decreased the surface tension between the organic and aqueous phase that would stabilize an emulsion as well as solubilize the waterinsoluble drug. 2 Thus, an increase in their concentration in the aqueous phase would allow the diffusion and solubilization of more drugs out of the hydrophobic core into the external aqueous phase.…”

“…P188/0.2 and CA25/0.2, which are stabilizers with emulsifying properties, can form molecular micelles through the interaction between their hydrophobic portion and the hydrophobic polymer, which could highly affect the release of drug from the formed NPs, in different patterns for both P188 and CA25, possessing different surface activities. 2 Drug release data were fitted into various kinetics equations, namely zero-order, first-order, Higuchi, Korsmeyer-Peppas, Hixson-Crowell, Baker-Lonsdale, and …”