Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems

Gupta, Shweta; Kesarla, Rajesh; Omri, Abdelwahab

doi:10.1155/2013/848043

Cited by 219 publications

(188 citation statements)

References 87 publications

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“…Compared to low drug loading, zeta potential values decreased by increasing experimental drug loading which might be drug loading at the micellar cavities to promote destabilization of the system. 32 The negative relationship between volume of the …”

Section: Zeta Potential Of Liposomesmentioning

confidence: 99%

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

Zidan

Ahmed

Aljaeid

2016

IJN

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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.

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Section: Zeta Potential Of Liposomesmentioning

confidence: 99%

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

Zidan

Ahmed

Aljaeid

2016

IJN

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“…This may in turn bring about more bioavailability due to enhanced in vivo release as only solubilised particles can be absorbed through lipophilic cellular membranes. [16] These nanostructured systems might be able to potentiate required action of herbal extracts, reducing the necessary dosage, side effects and improved activity. Nanosystems can distribute the bioactive component at adequate concentration throughout the whole treatment period, directing it to the preferred site of action.…”

Section: Particle Size Analysis and Morphological Characterisationmentioning

confidence: 99%

Formulation and characterisation of nanosuspension of herbal extracts for enhanced antiradical potential

Jahan

Aslam

Rahman

et al. 2015

Journal of Experimental Nanoscience

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Nanotechnology is a promising technique to increase the bioavailability of herbal medicines. This paper presents the nanosuspension approach for increasing the aqueous solubility and thereby bioactivity of important herbal extracts. Nanosuspensions of the seeds of three plants extract (Silybum marianum, Elettaria cardamomum and Coriandrum sativum) were prepared by using polyvinyl alcohol (1.5% w/v) as a stabiliser. Prepared nanoparticles were characterised by scanning electron microscope. Activity of nanosuspension formulation was assessed by using four in vitro antioxidant assays. S. marianum, E. cardamomum and C. sativum particle size was observed to fall in range of 446.1 § 112.6, 456.63 § 339.2 and 432.1 § 172.8 nm, respectively, most of the particles were having spherical shape and smooth topology. These synthesised nanoparticles were found to be more effective against quenching free radical than their crude extracts and standards [butylated hydroxyl toluene and ascorbic acid]. C. sativum nanosuspension showed most free radical scavenging potential against 2,2-diphenyl-1-picrylhdrazyl (DPPH) and superoxide free radical scavenging assays (IC 50 0.59 § 0.01 and 0.81 § 0.11 mg/ml). S. marianum nanosuspension was found to be most effective against DPPH radicals scavenging (IC 50 0.34 § 0.02 mg/ml). It was concluded that nanosuspension of herbal medicines potentiates the antioxidant potential.

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“…The small-sized droplets of SMEDDS offer an increase in dissolution rate and bioavailability of drugs [13,14] . Other important advantages of SMEDDS include ease of manufacturing and scale-up [15] .…”

Section: Research Papermentioning

confidence: 99%

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

Pattewar¹,

Kasture²,

Pande³

et al. 2018

pharmaceutical-sciences

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The aim of present study was to formulate and evaluate self-microemulsifying drug delivery system containing piroxicam and to use the ability of porous magnesium alumina metasilicate as a solid carrier for self-microemulsifying drug delivery system. It was developed to resolve the problems of piroxicam such as low water solubility, low bioavailability and gastrointestinal irritation. Self-microemulsifying drug delivery system containing varying proportions of Capmul MCM, Cremophor EL and Transcutol-P were prepared and optimized using response surface methodology of Design-Expert ® software version 10. Liquid selfmicroemulsifying drug delivery systems were subjected to in vitro evaluation, including self-emulsification efficiency study, droplet size, zeta potential measurement and in vitro drug release studies. Solid selfmicroemulsifying drug delivery system was prepared by adding liquid self-microemulsifying drug delivery system with Neusilin US2 and filled in hard gelatin capsule. The optimized formulation consists of 28.26 % of Capmul MCM, 44.16 % of Cremophor EL and 27.58 % of Transcutol-P. The results showed that the drug release profile of piroxicam from the self-microemulsifying drug delivery formulations was higher than the pure piroxicam powder. The release of piroxicam was rapid and complete. Solid self-microemulsifying drug delivery systems after filled in hard gelatin capsule, predicted to be a promising technique to deliver a liquid formulation in solid dosage form.

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Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems

Cited by 219 publications

References 87 publications

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

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

Formulation and characterisation of nanosuspension of herbal extracts for enhanced antiradical potential

Development and Optimization of Piroxicam-loaded Solid Self-micro emulsifying Drug Delivery System

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