Novel piroxicam-loaded nanospheres generated by the electrospraying technique: physicochemical characterisation and oral bioavailability evaluation

Mustapha, Omer; Din, Fakhar ud; Kim, Dong Wuk; Park, Jong Hyuck; Woo, Kyu Bong; Lim, Soo-Jeong; Youn, Yu Seok; Cho, Kwan Hyung; Rashid, Rehmana; Yousaf, Abid Mehmood; Kim, Jong Oh; Yong, Chul Soon; Choi, Han‐Gon

doi:10.1080/02652048.2016.1185475

Cited by 37 publications

(15 citation statements)

References 46 publications

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“…These systems are also valuable in evading various drawbacks associated with conventional dosage forms like low aqueous solubility, poor bioavailability, poor membrane permeability, variable plasma concentration, undesirable effects, poor patient compliance, and finally poor patient efficacy (Bochot & Fattal, 2012;Zaki Ahmad et al, 2014;Song et al, 2015). From the last few decades, with various novel drug delivery system approaches including solid lipid nanoparticles, dual reverse thermosensitive systems, complexation, electro spraying, solid dispersions, co-solvency and nanosizing (nanoemulsion, nanosuspension, nanoparticles, and nanocrystals) had been proposed to resolve these issues (Ud Din et al, 2015aDin et al, ,b, 2017Rashid et al, 2015aRashid et al, , 2015bAhmad et al, 2016;Mustapha et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

et al. 2017

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Vesicular drug delivery systems have gained wide attention in the field of nanotechnology. Among them proniosomes become the superior over other vesicular carriers. Proniosomes are dry formulations of water soluble nonionic surfactant coated carrier system which immediately forms niosomes upon hydration. They have the capability to overcome the instability problems associated with niosomes and liposomes and have the potential to improve solubility, bioavailability, and absorption of various drugs. Furthermore, they offer versatile drug delivery concept for enormous number of hydrophilic and hydrophobic drugs. They have the potential to deliver drugs effectively through different routes at specific site of action to achieve controlled release action and reduce toxic effects associated with drugs. This review discusses the general preparation techniques of proniosomes and mainly focus on the applications of proniosomes in drug delivery and targeting. Moreover, this review demonstrates critical appraisal of the literature for proniosomes. Additionally, this review extensively explains the potential of proniosomes in delivering drugs via different routes, such as oral, parenteral, dermal and transdermal, ocular, oral mucosal, vaginal, pulmonary, and intranasal. Finally, the comparison of proniosomes with niosomes manifests the clear distinction between them. Moreover, proniosomes need to be explored for proteins and peptide delivery and in the field of nutraceuticals and develop pilot plant scale up studies to investigate them in industrial set up. ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 99%

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

et al. 2017

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“…30,31 Nano-sized solid dispersion is a magnificent drug delivery system to ameliorate dissolution rate and solubility of a poorly water-soluble substance in the aqueous media. 18 with electrospraying is a smart way to fabricate nanoparticulated solid dispersions; 24,35 accordingly, in the present research work we adopted these techniques to obtain bezafibrate-loaded nanoparticulated solid dispersions (nanospheres). The recipe of each formulation is shown in Table 1.…”

Section: Resultsmentioning

confidence: 99%

<p>Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate</p>

Sun¹,

Shen²,

Shafique³

et al. 2020

IJN

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Background: Bezafibrate is a BCS class II drug as it presents very low solubility in water; therefore, its bioavailability after oral administration is very poor. The aim of this work was to enhance solubility and dissolution rate of bezafibrate in water in order to enhance its oral bioavailability. Methods: Several formulations were prepared using PVP K30 and Cremophor ELP employing the solvent-evaporation method and the electrospraying technique. Solubility, release rate, bioavailability in male Sprague Dawley rats, and lipid profile attributes in Wistar rats were assessed in comparison with bezafibrate plain powder. Solid-state characterization was carried out using X-ray diffraction (XRD) analysis, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM). Results: All the formulations exerted positive effect towards the desired goal. In particular, the optimized formulation furnished about 14-fold enhanced solubility and 85.48 ± 10.16% drug was released in 10 min as compared with bezafibrate alone (4.06 ± 2.59%). The drug existed in the amorphous state in the prepared sample as confirmed by XRD and DSC, whilst no drug-excipient interactions were observed through FTIR analysis. Moreover, SEM revealed smooth-surfaced spherical particles of the optimized formulation. A 5.5-fold higher oral bioavailability was achieved with the optimized formulation in comparison with bezafibrate plain powder. Also, TG, LDL and TC were decreased, and HDL was increased considerably in HFD-treated rats. Conclusion: The optimized formulation consisting of bezafibrate, PVP K30 and cremophor ELP (1/12/1.5, w/w/w) might be a capable drug delivery system for orally administering poorly water-soluble bezafibrate with improved bioavailability and antihyperlipidemic effects.

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“…The SEGS had a faster time to maximum concentration (T max ) as compared with the SNEDDS; however, there were no significant differences in T max value among all formulations. The enhanced oral bioavailability of the SEGS and SNEDDS results from an increased solubility and dissolution [39,40]. Moreover, SEGS produced by fluid bed granulation gave a higher and faster oral bioavailability of the oily drug than that of the SNEDDS produced by spray-drying.…”

Section: Resultsmentioning

confidence: 99%

Comparison of 1-Palmitoyl-2-Linoleoyl-3-Acetyl-Rac-Glycerol-Loaded Self-Emulsifying Granule and Solid Self-Nanoemulsifying Drug Delivery System: Powder Property, Dissolution and Oral Bioavailability

Kim

Lim

et al. 2019

Pharmaceutics

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The main objective of this study was to compare the powder property, dissolution and bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG)-loaded self-emulsifying granule system (SEGS) and solid self-nanoemulsifying drug delivery system (SNEDDS). Various SEGS formulations were prepared, and the effect of surfactant and binder on the drug solubility in them, leading to selecting sodium lauryl sulphate (SLS) and hydroxyl propyl methyl cellulose (HPMC). The SEGS and SNEDDS were prepared with PLAG/SLS/HPMC/calcium silicate/microcrystalline cellulose at the weight ratio of 1:0.25:0.1:0.5:3 employing the fluid bed granulation and spray-drying technique, respectively. Their powder properties were compared in terms of flow ability, emulsion droplet size, scanning electron microscopy, and powder X-ray diffraction. Furthermore, the solubility, dissolution, and oral bioavailability in rats of the SEGS were assessed in comparison with the SNEDDS. The SEGS and SNEDDS enhanced the solubility of the drug approximately 36- and 32-fold as compared with the drug alone; but they had no differences. The crystalline drug may exist in both the calcium silicate and microcrystalline cellulose (MCC) in the SEGS, but only in the calcium silicate in the SNEDDS. The SEGS had considerably improved the flow ability (Hausner ratio, 1.23 vs. 1.07; Carr index, 19.8 vs. 43.5%) and drug dissolution as compared with the SNEDDS. The SEGS and SNEDDS with double peak profiles, unlike the single peak of drug alone, showed a significantly higher plasma concentration and area under the curve (AUC), as compared with drug alone. Although they were not significantly different, the SEGS gave higher AUC than did the SNEDDS, suggesting its enhanced oral bioavailability of PLAG. Thus, the SEGS could be used as a powerful oral dosage form to improve the flow ability and oral bioavailability of PLAG, an oily drug.

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Novel piroxicam-loaded nanospheres generated by the electrospraying technique: physicochemical characterisation and oral bioavailability evaluation

Cited by 37 publications

References 46 publications

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

<p>Electrosprayed Polymeric Nanospheres for Enhanced Solubility, Dissolution Rate, Oral Bioavailability and Antihyperlipidemic Activity of Bezafibrate</p>

Comparison of 1-Palmitoyl-2-Linoleoyl-3-Acetyl-Rac-Glycerol-Loaded Self-Emulsifying Granule and Solid Self-Nanoemulsifying Drug Delivery System: Powder Property, Dissolution and Oral Bioavailability

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