Solid-state dependent dissolution and oral bioavailability of piroxicam in rats

Lust, Andres; Laidmäe, Ivo; Palo, Mirja; Meos, Andres; Aaltonen, Jaakko; Veski, Peep; Heinämäki, Jyrki; Kogermann, Karin

doi:10.1016/j.ejps.2012.10.005

Cited by 22 publications

(12 citation statements)

References 41 publications

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“…Interestingly, the PRX-loaded polymeric nanofibers exhibited the second (even wider) endotherm ranging from 100°C to 220°C, presumably suggesting that a physical interaction or fusion of PRX into the PCL-PVAc-PEG graft copolymer (Soluplus) had occurred. Recently, Lust et al [38] reported that the dehydration endotherm of amorphous solid dispersions of PRX and PCL-PVAc-PEG graft copolymer (Soluplus) was narrower than that of the respective physical mixtures. The latter was attributed to the increased temperature used to prepare the solid dispersions by melting method [38].…”

Section: Resultsmentioning

confidence: 99%

“…Recently, Lust et al [38] reported that the dehydration endotherm of amorphous solid dispersions of PRX and PCL-PVAc-PEG graft copolymer (Soluplus) was narrower than that of the respective physical mixtures. The latter was attributed to the increased temperature used to prepare the solid dispersions by melting method [38]. They also showed a broad endotherm ranging from 125°C to 185°C with the physical mixtures of PRX and the present carrier polymer, but in contrast to the present results on nanofibers, Lust et al did not observe an endotherm at higher temperatures with the amorphous solid dispersions prepared by melting method.…”

Section: Resultsmentioning

confidence: 99%

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Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

Paaver

Tamm

Laidmäe

et al. 2014

BioMed Research International

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Electrospinning is an effective method in preparing polymeric nanofibrous drug delivery systems (DDSs) for topical wound healing and skin burn therapy applications. The aim of the present study was to investigate a new synthetic graft copolymer (Soluplus) as a hydrophilic carrier polymer in electrospinning of nanofibrous DDSs. Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG)) was applied in the nonwoven nanomats loaded with piroxicam (PRX) as a poorly water-soluble drug. Raman spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy (SEM) were used in the physical characterization of nanofibrous DDSs. According to the SEM results, the drug-loaded PCL-PVAc-PEG nanofibers were circular in cross-section with an average diameter ranging from 500 nm up to 2 µm. Electrospinning stabilized the amorphous state of PRX. In addition, consistent and sustained-release profile was achieved with the present nanofibrous DDSs at the physiologically relevant temperature and pH applicable in wound healing therapy. In conclusion, electrospinning can be used to prepare nanofibrous DDSs of PCL-PVAc-PEG graft copolymer (Soluplus) and to stabilize the amorphous state of a poorly water-soluble PRX. The use of this synthetic graft copolymer can open new options to formulate nanofibrous DDSs for wound healing.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

Paaver

Tamm

Laidmäe

et al. 2014

BioMed Research International

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“…hPlc of PX PX was assayed using HPLC method reported by Lust et al, 19 with slight modification. HPLC instrument (Agilent Technologies-1260 infinity; Agilent Technologies, Santa Clara, CA, USA) supplied with LC reversed-phase C18 column (Kinetex™; 250×4.6 mm, particle size =5 µm, pore size =100 Å), equipped with Security Guard™ ULTRA cartridge system (4.6 mm) (Phenomenex Co., Torrance, CA, USA) was used.…”

Section: Preparation Of Plasma Samplesmentioning

confidence: 99%

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

El-Habashy

Allam

El-Kamel

2016

IJN

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Nanoparticles (NPs) have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs) to modulate the release and reduce ulcerogenicity of piroxicam (PX) after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2), having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours), was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, t max , of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene ® 20 mg capsules ( P ≤0.001). Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats ( P ≤0.05) as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2) had a significant potential of offsetting deleterious side effects common in PX use.

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“…crystallization, wet granulation, drying, pelletization) or during storage may induce the coexistence of distinct hydrate/anhydrate forms of active pharmaceutical ingredients (APIs) and/or excipients [1]. Crystal hydrates have particular physicochemical properties compared with their anhydrate counterparts that may result in varying solubility and dissolution behavior [2][3][4]. Therefore, the drug bioavailability may be seriously affected and may compromise the quality of the final product due to undesirable mixtures of different polymorphs [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

Monitoring of multiple solid-state transformations at tablet surfaces using multi-series near-infrared hyperspectral imaging and multivariate curve resolution

Alexandrino

Khorasani

Amigo

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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Solid-state dependent dissolution and oral bioavailability of piroxicam in rats

Cited by 22 publications

References 41 publications

Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

Soluplus Graft Copolymer: Potential Novel Carrier Polymer in Electrospinning of Nanofibrous Drug Delivery Systems for Wound Therapy

Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

Monitoring of multiple solid-state transformations at tablet surfaces using multi-series near-infrared hyperspectral imaging and multivariate curve resolution

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