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Nicotinamide polymeric nanoemulsified systems: a quality-by-design case study for a sustained antimicrobial activity.

Zidan AS, Ahmed OA, Aljaeid BM - Int J Nanomedicine (2016)

Bottom Line: EC, EE, particle size, polydispersity index, zeta potential, and percentage release in 24 hours were found to be in the range of 33.5%-68.8%, 53.1%-67.1%, 43.3-243.3 nm, 0.08-0.28, 9.5-53.3 mV, and 5.8%-22.4%, respectively.One-way analysis of variance and Pareto charts revealed that the experimental loadings of 2-hydroxypropyl-β-cyclodextrin and Eudragit(®) S100 were the most significant for their effects on nicotinamide EC and EE.In conclusion, the study demonstrated the potential of polymeric nanoemulsified system to sustain the release and antibacterial activity of nicotinamide.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

ABSTRACT
Nicotinamide, the amide form of vitamin B3, was demonstrated to combat some of the antibiotic-resistant infections that are increasingly common around the world. The objective of this study was to thoroughly understand the formulation and process variabilities affecting the preparation of nicotinamide-loaded polymeric nanoemulsified particles. The quality target product profile and critical quality attributes of the proposed product were presented. Plackett-Burman screening design was employed to screen eight variables for their influences on the formulation's critical characteristics. The formulations were prepared by an oil-in-water emulsification followed by solvent replacement. The prepared systems were characterized by entrapment capacity (EC), entrapment efficiency (EE), particle size, polydispersity index, zeta potential, transmission electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, in vitro drug release, and their antibacterial activity against bacterial scrums. EC, EE, particle size, polydispersity index, zeta potential, and percentage release in 24 hours were found to be in the range of 33.5%-68.8%, 53.1%-67.1%, 43.3-243.3 nm, 0.08-0.28, 9.5-53.3 mV, and 5.8%-22.4%, respectively. One-way analysis of variance and Pareto charts revealed that the experimental loadings of 2-hydroxypropyl-β-cyclodextrin and Eudragit(®) S100 were the most significant for their effects on nicotinamide EC and EE. Moreover, the polymeric nanoemulsified particles demonstrated a sustained release profile for nicotinamide. The Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction demonstrated a significant interaction between the drug and 2-hydroxypropyl-β-cyclodextrin that might modulate the sustained release behavior. Furthermore, the formulations provided a sustained antibacterial activity that depended on nicotinamide-loading concentration, release rate, and incubation time. In conclusion, the study demonstrated the potential of polymeric nanoemulsified system to sustain the release and antibacterial activity of nicotinamide.

No MeSH data available.


Related in: MedlinePlus

In vitro nicotinamide release from 12 formulations of Plackett–Burman design (n=3).Notes: (A) Cumulative percentage of nicotinamide released in linear time scale. (B) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with Higuchi model. (C) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with transient-boundary model.
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f5-ijn-11-1501: In vitro nicotinamide release from 12 formulations of Plackett–Burman design (n=3).Notes: (A) Cumulative percentage of nicotinamide released in linear time scale. (B) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with Higuchi model. (C) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with transient-boundary model.

Mentions: Figure 5 shows that the release data exhibited sustained release profiles, that is, an initial burst effect followed by subsequent slower release (Figure 5). At the initial stage, the burst release is usually ascribed to the free nicotinamide associated with the interface of the nanoemulsion’s hydrophobic core and/or hydrophilic corona, or even within the micelle corona compartment, hence facilitating the passive diffusion of the drug.33 The obtained release data fitted to a logarithmic time-dependent release better than Higuchi diffusion release (Figure 5). This behavior would be explained by the expanding transient boundary at the interface of either the polymer surface or HP-β-CD-adsorbed layer and the aqueous medium.19 The following is the logarithmic equation to predict the drug release rate, where Qti is percentage drug released after time t to the receptor medium and K is the release constant or the slope of plotting Qti versus log10t divided by 2.303.Qti=(2.303×log10(ti)×K)+Qti−1(6)


Nicotinamide polymeric nanoemulsified systems: a quality-by-design case study for a sustained antimicrobial activity.

Zidan AS, Ahmed OA, Aljaeid BM - Int J Nanomedicine (2016)

In vitro nicotinamide release from 12 formulations of Plackett–Burman design (n=3).Notes: (A) Cumulative percentage of nicotinamide released in linear time scale. (B) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with Higuchi model. (C) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with transient-boundary model.
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4835127&req=5

f5-ijn-11-1501: In vitro nicotinamide release from 12 formulations of Plackett–Burman design (n=3).Notes: (A) Cumulative percentage of nicotinamide released in linear time scale. (B) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with Higuchi model. (C) Cumulative percentage of nicotinamide released from representative formulations F3 and F8 fitted with transient-boundary model.
Mentions: Figure 5 shows that the release data exhibited sustained release profiles, that is, an initial burst effect followed by subsequent slower release (Figure 5). At the initial stage, the burst release is usually ascribed to the free nicotinamide associated with the interface of the nanoemulsion’s hydrophobic core and/or hydrophilic corona, or even within the micelle corona compartment, hence facilitating the passive diffusion of the drug.33 The obtained release data fitted to a logarithmic time-dependent release better than Higuchi diffusion release (Figure 5). This behavior would be explained by the expanding transient boundary at the interface of either the polymer surface or HP-β-CD-adsorbed layer and the aqueous medium.19 The following is the logarithmic equation to predict the drug release rate, where Qti is percentage drug released after time t to the receptor medium and K is the release constant or the slope of plotting Qti versus log10t divided by 2.303.Qti=(2.303×log10(ti)×K)+Qti−1(6)

Bottom Line: EC, EE, particle size, polydispersity index, zeta potential, and percentage release in 24 hours were found to be in the range of 33.5%-68.8%, 53.1%-67.1%, 43.3-243.3 nm, 0.08-0.28, 9.5-53.3 mV, and 5.8%-22.4%, respectively.One-way analysis of variance and Pareto charts revealed that the experimental loadings of 2-hydroxypropyl-β-cyclodextrin and Eudragit(®) S100 were the most significant for their effects on nicotinamide EC and EE.In conclusion, the study demonstrated the potential of polymeric nanoemulsified system to sustain the release and antibacterial activity of nicotinamide.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

ABSTRACT
Nicotinamide, the amide form of vitamin B3, was demonstrated to combat some of the antibiotic-resistant infections that are increasingly common around the world. The objective of this study was to thoroughly understand the formulation and process variabilities affecting the preparation of nicotinamide-loaded polymeric nanoemulsified particles. The quality target product profile and critical quality attributes of the proposed product were presented. Plackett-Burman screening design was employed to screen eight variables for their influences on the formulation's critical characteristics. The formulations were prepared by an oil-in-water emulsification followed by solvent replacement. The prepared systems were characterized by entrapment capacity (EC), entrapment efficiency (EE), particle size, polydispersity index, zeta potential, transmission electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, in vitro drug release, and their antibacterial activity against bacterial scrums. EC, EE, particle size, polydispersity index, zeta potential, and percentage release in 24 hours were found to be in the range of 33.5%-68.8%, 53.1%-67.1%, 43.3-243.3 nm, 0.08-0.28, 9.5-53.3 mV, and 5.8%-22.4%, respectively. One-way analysis of variance and Pareto charts revealed that the experimental loadings of 2-hydroxypropyl-β-cyclodextrin and Eudragit(®) S100 were the most significant for their effects on nicotinamide EC and EE. Moreover, the polymeric nanoemulsified particles demonstrated a sustained release profile for nicotinamide. The Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction demonstrated a significant interaction between the drug and 2-hydroxypropyl-β-cyclodextrin that might modulate the sustained release behavior. Furthermore, the formulations provided a sustained antibacterial activity that depended on nicotinamide-loading concentration, release rate, and incubation time. In conclusion, the study demonstrated the potential of polymeric nanoemulsified system to sustain the release and antibacterial activity of nicotinamide.

No MeSH data available.


Related in: MedlinePlus