Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Varshosaz, Jaleh; Khajavinia, Amir; Ghasemlu, M.; Ataei, E.; Golshiri, K.; Khayam, I.

doi:10.14227/dt200313p15

Cited by 12 publications

(11 citation statements)

References 34 publications

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“…[8][9][10] One of the major problems with this drug is it has a very low aqueous solubility (0.023 mg/ml), which results in poor bioavailability after oral administration. 11,12 Hence there is a need to increase the solubility of piroxicam and also to formulate a suitable dosage form in order to increase the bioavailability. For the effective management of arthritis and osteoarthritis especially in the case of…”

Section: Introductionmentioning

confidence: 99%

Fast Dissolving Oral Film of Piroxicam: Solubility Enhancement by forming an Inclusion Complex with β-cyclodextrin, Formulation and Evaluation

Dharmasthala¹,

Shabaraya²,

Andrade³

et al. 2018

JYP

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Objective: Piroxicam is a long-acting potent nonsteroidal anti-inflammatory drug (NSAID) which has a very low solubility in Gastrointesti nal (GI) fluids results in poor bioavailability after oral administration. The present investigation aimed to formulate and evaluate fast dissolving oral films containing piroxicam to overcome solubility and bioavailability problems thereby to facilitate the convenience of pediatric and geriatric patients. Method: The inclusion complexes of piroxicam with β-cyclodextrin were prepared. In vitro dissolution study was performed to fix the ratio with better dissolution rate. The selected inclusion complex was then utilized for the preparation of fast dissolving oral films by solvent casting method using sodium CMC/ chitosan as film-forming agents, sodium starch glycolate/crospovidone as super disintegrating agents. PEG 400 used as a plasticizer. Formulations (F1-F12) were prepared and evaluated for their physicochemical properties. In vitro disintegration, dissolution and permeation studies were also carried out. Results: Formulation F2 showed the minimum in vitro disintegration time (14.94±3.06 s), formulation F9 showed the maximum in vitro disintegration time (36.66±1.05 s). The formulations F6 and F4 showed better drug release of 94.4% and 92.9% respectively. Better drug permeation of 96.65% was obtained from the formulation F6 in 40 s. Conclusion: The study concluded that the fast dissolving films achieved quicker onset of action compared to the conventional preparations. The formulation found promising to obtain better therapeutic efficiency.

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Section: Introductionmentioning

confidence: 99%

Fast Dissolving Oral Film of Piroxicam: Solubility Enhancement by forming an Inclusion Complex with β-cyclodextrin, Formulation and Evaluation

Dharmasthala¹,

Shabaraya²,

Andrade³

et al. 2018

JYP

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“…7,11 This peak disappeared in the DSC thermogram of P188/0.2, which depicted PX transformation into a molecular dispersion in an amorphous form. 31 In case of P188/0.2 thermogram, a sharp endothermic peak occurred at 50.3°C, representative of P188 and indicative of its presence in a crystalline form. 32 Another endothermic peak was reported at 181°C representative of EC melting point.…”

Section: Scanning Electron Microscopymentioning

confidence: 93%

“…It also showed significant stretching bands at 1,630 cm -1 , for the amide carbonyl C=O, and at 1,351 cm -1 , for the S=O stretching. 31 EC IR spectrum showed a band at 3,472 cm -1 , which could be attributed to the OH stretching vibration.…”

mentioning

confidence: 96%

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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“…Therefore, it resulted in the lowering of the surface energy and enthalpy of the system with smaller particle sizes. 19,39…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

<p>Engineering of Naproxen Loaded Polymer Hybrid Enteric Microspheres for Modified Release Tablets: Development, Characterization, in silico Modelling and in vivo Evaluation</p>

Hameed

Khan

Shahid

et al. 2020

DDDT

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Background: Naproxen (NP) is a non-steroidal anti-inflammatory drug with poor aqueous solubility and low oral bioavailability, which may lead to therapeutic failure. NP causes crucial GIT irritation, bleeding, and peptic and duodenal ulcers.Purpose of the study: This study aimed to engineer and characterize polymer hybrid enteric microspheres using an integrated (experimental and molecular modelling) approach with further development to solid dosage form with modified drug release kinetics and improved bioavailability. Materials and methods: NP loaded polymer hybrid enteric microspheres (PHE-Ms) were fabricated by using a modified solvent evaporation technique coupled with molecular modelling (MM) approach. The PHE-Ms were characterized by particle size, distribution, morphology, crystallinity, EE, drug-polymer compatibility, and DSC. The optimized NP loaded PHE-Ms were further subjected to downstream procedures including tablet dosage form development, stability studies and comparative in vitro-in vivo evaluation. Results: The hydrophobic polymer EUD-L100 and hydrophilic polymer HPMC-E5 delayed and modified drug release at intestinal pH while imparting retardation of NP release at gastric pH to diminish the gastric side effects. The crystallinity of the NP loaded PHE-Ms was established through DSC and P (XRD). The particle size for the developed formulations of PEH-Ms (M1-M5) was in the range from 29.06 ±7.3-74.31 ± 17.7 μm with Span index values of 0.491-0.69, respectively. The produced NP hybrid microspheres demonstrated retarded drug release at pH 1.2 and improved dissolution at pH 6.8. The in vitro drug release patterns were fitted to various release kinetic models and the best-followed model was the Higuchi model with a release exponent "n" value > 0.5. Stability studies at different storage conditions confirmed stability of the NP loaded PHE-Ms based tablets (P<0.05). The molecular modelling (MM) study resulted in adequate binding energy of co-polymer complex SLS-Eudragit-HPMC-Naproxen (−3.9 kcal/mol). In contrast to the NP (unprocessed) and marketed formulations, a significant increase in the C max of PHE-MT1 (44.41±4.43) was observed. Conclusion: The current study concludes that developing NP loaded PHE-Ms based tablets could effectively reduce GIT consequences with restored therapeutic effects. The modified release pattern could improve the dissolution rate and enhancement of oral bioavailability. The MM study strengthens the polymer-drug relationship in microspheres.

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Enhancement in Dissolution Rate of Piroxicam by Two Micronization Techniques

Cited by 12 publications

References 34 publications

Fast Dissolving Oral Film of Piroxicam: Solubility Enhancement by forming an Inclusion Complex with β-cyclodextrin, Formulation and Evaluation

Fast Dissolving Oral Film of Piroxicam: Solubility Enhancement by forming an Inclusion Complex with β-cyclodextrin, Formulation and Evaluation

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

<p>Engineering of Naproxen Loaded Polymer Hybrid Enteric Microspheres for Modified Release Tablets: Development, Characterization, in silico Modelling and in vivo Evaluation</p>

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