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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

Compatibility analysis of nicotinamide with the investigated excipients.Notes: (A) FTIR, (B) DSC, and (C) XRD data for the nicotinamide-loaded polymeric nanoemulsified particles (batch F3) and raw materials.Abbreviations: FTIR, Fourier transform infrared spectroscopy; DSC, differential scanning calorimetry; XRD, X-ray diffraction; HP-β-CD, 2-hydroxypropyl-β-cyclodextrin.
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f6-ijn-11-1501: Compatibility analysis of nicotinamide with the investigated excipients.Notes: (A) FTIR, (B) DSC, and (C) XRD data for the nicotinamide-loaded polymeric nanoemulsified particles (batch F3) and raw materials.Abbreviations: FTIR, Fourier transform infrared spectroscopy; DSC, differential scanning calorimetry; XRD, X-ray diffraction; HP-β-CD, 2-hydroxypropyl-β-cyclodextrin.

Mentions: Solid-state analysis of the prepared polymeric nanoemulsified particle was done not only to understand the effect of process parameters on physical characteristics of nicotinamide but also to mine any interaction that occurred between the drug and the employed excipients. Figure 6 demonstrates DSC thermograms of nicotinamide, individual additives, and formulation F3 of highest EE and EC. The heat of fusion involved during DSC analysis was dependent on the employed powder weight. Hence, all thermograms were overlaid with normalization to 1 mg weight. Nicotinamide thermogram showed a sharp thermal transition at 130°C corresponding to its melting peak.19 DSC thermogram of Eudragit S100 showed a wide endothermic transition at 50°C–118°C, which attributed to the evaporation of the adsorbed moisture (ΔH =63.87 J/g). The glass thermal transition of Eudragit S100 was not detected which probably was covered by the adsorbed moisture evaporation. In general, glass transition temperature of Eudragit S100 is~120°C. The DSC thermogram of HP-β-CD showed a broad endothermic transition at 60°C–150°C due to evaporation of water that had been absorbed by HP-β-CD. In the DSC curve of formulation F3 of polymeric nanoemulsified particles, the melting peak of nicotinamide disappeared, owing to the amorphous transformation of the drug or its inclusion and/or interaction with either HP-β-CD or Eudragit S100, respectively.34 Hence, further solid-state characterization was done by FTIR and XRD to strengthen this hypothesis.


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)

Compatibility analysis of nicotinamide with the investigated excipients.Notes: (A) FTIR, (B) DSC, and (C) XRD data for the nicotinamide-loaded polymeric nanoemulsified particles (batch F3) and raw materials.Abbreviations: FTIR, Fourier transform infrared spectroscopy; DSC, differential scanning calorimetry; XRD, X-ray diffraction; HP-β-CD, 2-hydroxypropyl-β-cyclodextrin.
© Copyright Policy
Related In: Results  -  Collection

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

f6-ijn-11-1501: Compatibility analysis of nicotinamide with the investigated excipients.Notes: (A) FTIR, (B) DSC, and (C) XRD data for the nicotinamide-loaded polymeric nanoemulsified particles (batch F3) and raw materials.Abbreviations: FTIR, Fourier transform infrared spectroscopy; DSC, differential scanning calorimetry; XRD, X-ray diffraction; HP-β-CD, 2-hydroxypropyl-β-cyclodextrin.
Mentions: Solid-state analysis of the prepared polymeric nanoemulsified particle was done not only to understand the effect of process parameters on physical characteristics of nicotinamide but also to mine any interaction that occurred between the drug and the employed excipients. Figure 6 demonstrates DSC thermograms of nicotinamide, individual additives, and formulation F3 of highest EE and EC. The heat of fusion involved during DSC analysis was dependent on the employed powder weight. Hence, all thermograms were overlaid with normalization to 1 mg weight. Nicotinamide thermogram showed a sharp thermal transition at 130°C corresponding to its melting peak.19 DSC thermogram of Eudragit S100 showed a wide endothermic transition at 50°C–118°C, which attributed to the evaporation of the adsorbed moisture (ΔH =63.87 J/g). The glass thermal transition of Eudragit S100 was not detected which probably was covered by the adsorbed moisture evaporation. In general, glass transition temperature of Eudragit S100 is~120°C. The DSC thermogram of HP-β-CD showed a broad endothermic transition at 60°C–150°C due to evaporation of water that had been absorbed by HP-β-CD. In the DSC curve of formulation F3 of polymeric nanoemulsified particles, the melting peak of nicotinamide disappeared, owing to the amorphous transformation of the drug or its inclusion and/or interaction with either HP-β-CD or Eudragit S100, respectively.34 Hence, further solid-state characterization was done by FTIR and XRD to strengthen this hypothesis.

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