Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Mantas, Athanasios; Mihranyan, Albert

doi:10.3390/pharmaceutics11010037

Cited by 15 publications

(11 citation statements)

References 34 publications

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“…IBU, a typical nonsteroidal anti-inflammatory drug, is broadly exploited to treat pain, fever and inflammation. However, its poor water solubility always limits its fast action for achieving a desired therapeutic effect [46,47,48]. HPMC is commonly utilized as an excipient in oral tablet, eye drops, and capsule formations.…”

Section: Introductionmentioning

confidence: 99%

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Huang

Hou

et al. 2019

Pharmaceutics

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In pharmaceutical nanotechnology, the intentional manipulation of working processes to fabricate nanoproducts with suitable properties for achieving the desired functional performances is highly sought after. The following paper aims to detail how a modified coaxial electrospraying has been developed to create ibuprofen-loaded hydroxypropyl methylcellulose nanoparticles for improving the drug dissolution rate. During the working processes, a key parameter, i.e., the spreading angle of atomization region (θ, °), could provide a linkage among the working process, the property of generated nanoparticles and their functional performance. Compared with the applied voltage (V, kV; D = 2713 − 82V with RθV2 = 0.9623), θ could provide a better correlation with the diameter of resultant nanoparticles (D, nm; D = 1096 − 5θ with RDθ2 = 0.9905), suggesting a usefulness of accurately predicting the nanoparticle diameter. The drug released from the electrosprayed nanoparticles involved both erosion and diffusion mechanisms. A univariate quadratic equation between the time of releasing 95% of the loaded drug (t, min) and D (t = 38.7 + 0.097D − 4.838 × 105D2 with a R2 value of 0.9976) suggests that the nanoparticle diameter has a profound influence on the drug release performance. The clear process-property-performance relationship should be useful for optimizing the electrospraying process, and in turn for achieving the desired medicated nanoparticles.

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Section: Introductionmentioning

confidence: 99%

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Huang

Hou

et al. 2019

Pharmaceutics

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“…The cellulose batches used in this study were identical to those used previously [12,13]. Notably, the pore volume of CLAD was 276 times and the specific surface area of CLAD was about 108 times larger than that for MCC as derived from N 2 gas sorption analysis.…”

Section: Resultsmentioning

confidence: 95%

“…We have previously shown that heat-assisted mixing of poorly soluble drugs from varying pharmacological classes with high surface area nanocellulose results in enhanced solubility and dissolution rate in biorelevant media. In particular, the latter effect was shown for NSAIDs from arylpropionic acid derivatives, e.g., ibuprofen, flurbiprofen, ketoprofen, and naproxen [12], as well as dihydropyridine-type calcium channel blockers, e.g., nifedipine, felodipine [13]. In this article, we extend this strategy and demonstrate improved formulation for a model problem drug featuring both poor solubility and unusually high number of polymorphs.…”

Section: Introductionmentioning

confidence: 83%

Dissolution Behavior of Flufenamic Acid in Heated Mixtures with Nanocellulose

Mantas

Mihranyan

2020

Molecules

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Flufenamic acid (FFA) is a problem drug that has up to eight different polymorphs and shows poor solubility. Variability in bioavailability has been reported in the past resulting in limited use of FFA in the oral solid dosage form. The goal of this article was to investigate the polymorphism and amorphization behavior of FFA in non-heated and heated mixtures with high surface area nanocellulose, i.e., Cladophora cellulose (CLAD). As a benchmark, low surface area microcrystalline cellulose (MCC) was used. The solid-state properties of mixtures were characterized with X-ray diffraction, Fourier-transform infrared spectroscopy, and differential scanning calorimetry. The dissolution behavior of mixtures was studied in three biorelevant media, i.e., fasted state simulated gastric fluid, fasted state simulated intestinal fluid, and fed state simulated intestinal fluid. Additional thermal analysis and dissolution tests were carried out following 4 months of storage at 75% RH and room temperature. Heated mixtures of FFA with CLAD resulted in complete amorphization of the drug, whereas that with MCC produced a mixture of up to four different polymorphs. The amorphous FFA mixture with CLAD exhibited rapid and invariable fasted/fed state dissolution in simulated intestinal fluids, whereas that of MCC mixtures was highly dependent on the biorelevant medium. The storage of the heated FFA-CLAD mixture did not result in recrystallization or changes in dissolution profile, whereas heated FFA-MCC mixture showed polymorphic changes. The straightforward dry powder formulation strategy presented here bears great promise for reformulating a number of problem drugs to enhance their dissolution properties and reduce the fasted/fed state variability.

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“…)-2,6-dimethyl-3,5-dicarbomethoxy-1,4-dihydropyridine (Nifedipine) is a calcium channel blocker drug used for the treatment of angiocardiopathy. Although oral administration is the best convenient route and has better patient compliance, bioavailability of nifedipine has been limited by poor solubility, photo-instability, or short plasma half-life [1]. Nifedipine is a BCS class II agent with a solubility of 5-6 µg/mL in the pH range from 4 to 13 [2], resulting in low bioavailability [3].…”

Section: -(2-mentioning

confidence: 99%

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

et al. 2020

Molecules

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Proliposomes were used to improve the solubility and oral bioavailability of nifedipine. Nifedipine proliposomes were prepared by methanol injection-spray drying method. The response surface method was used to optimize formulation to enhance the encapsulation efficiency (EE%) of nifedipine. The particle size of nifedipine proliposomes after rehydration was 114 nm. Surface morphology of nifedipine proliposomes was observed by a scanning electron microscope (SEM) and interaction of formulation ingredients was assessed by differential scanning calorimetry (DSC). The solubility of nifedipine is improved 24.8 times after forming proliposomes. In vitro release experiment, nifedipine proliposomes had a control release effect, especially in simulated gastric fluid. In vivo, nifedipine proliposomes significantly improved the bioavailability of nifedipine. The area under the concentration-time curve (AUC0–∞) of nifedipine proliposomes was about 10 times than nifedipine after oral administration. The elimination half-life (T1/2β) of nifedipine was increased from 1.6 h to 6.6 h. In conclusion, proliposomes was a promising system to deliver nifedipine through oral route and warranted further investigation.

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Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and Dissolution Rate

Cited by 15 publications

References 34 publications

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

The Process–Property–Performance Relationship of Medicated Nanoparticles Prepared by Modified Coaxial Electrospraying

Dissolution Behavior of Flufenamic Acid in Heated Mixtures with Nanocellulose

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

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