Feasibility of electrospray deposition for rapid screening of the cocrystal formation and single step, continuous production of pharmaceutical nanococrystals

Emami, Shahram; Siahi‐Shadbad, Mohammadreza; Barzegar-Jalali, Mohammad; Adibkia, Khosro

doi:10.1080/03639045.2018.1430821

Cited by 18 publications

(13 citation statements)

References 56 publications

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“…We utilized a single-nozzle electrospray system which has been described in detail elsewhere. 15 Briefly, a metal collector was placed 10 cm below the spraying needle and a 20 kV voltage was applied between them. MDF and ERS were dissolved in a 1:1 mixture of methanol and acetone with drug to polymer ratios of 1:5 and 1:10.…”

Section: Methodsmentioning

confidence: 99%

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Electrosprayed polymeric nanobeads and nanofibers of modafinil: preparation, characterization, and drug release studies

et al. 2019

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Introduction: Modafinil (MDF) is used orally for the treatment of attention-deficit/hyperactivity disorder and narcolepsy. It holds low solubility and high permeability; therefore, improving its dissolution properties by preparing nanoformulations can be a promising approach to enhance its oral absorption. Our aims were to prepare and characterize MDF-Eudragit® RS100 (MDF-ERS) nanoparticles by electrospray technique. Methods: Electrosprayed nanoparticles were fabricated by varying MDF to ERS ratios and concentrations. The formulations were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FTIR). Release studies were performed on nanoparticles, physical mixtures, and raw MDF. The release data were fitted to different models to understand the mechanism of the drug release. Results: Electrospraying of MDF and ERS solution resulted in the preparation of nonobeads or nanofibers, and the particulate characteristics of the obtained products were largely controlled by the polymer amount in the solution. PXRD and thermal analyses showed that MDF was an amorphous phase in the structures of nanoparticles. Using FTIR, no interaction was observed between MDF and ERS in nanoparticles. Nanoparticles showed biphasic release profiles and the order of dissolution rates was: nanofibers>MDF>nanobeads. The well-fitted model was Weibull model, indicating a Fickian diffusion as the main mechanism of release. Conclusion: The results suggest that by optimization of variables such as solution concentration of MDF-ERS nanofibers and nanobeads with higher dissolution rates can be made by electrospray. Electrospray deposition as a simple, continuous, and surfactant free method is an excellent choice for preparation of drug loaded polymeric nanoparticles.

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Section: Methodsmentioning

confidence: 99%

“…13 Furthermore, this method can directly produce surfactant-free and solid nanoparticles and does not need further separation and drying steps. The technique has been utilized to produce the nanocrystals, 14 nanococrystals, 15 and drug encapsulated polymeric nanoparticles. 16-19…”

Section: Introductionmentioning

confidence: 99%

Electrosprayed polymeric nanobeads and nanofibers of modafinil: preparation, characterization, and drug release studies

et al. 2019

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“…By considering that carbamazepine, indomethacin, and furosemide have dissolution limited bioavailability, the improved dissolution rates of NCCs may result in higher bioavailability. Emami et al 117 have reported the formation of NCCs of indomethacin-saccharin by using electrospray deposition technique. NCCs with a mean size of 219 nm displayed a 3-fold higher dissolution rate than the cocrystals prepared by the solvent evaporation method.…”

Section: Using Nanosized Cocrystals For Bioavailability Improvementmentioning

confidence: 99%

Recent advances in improving oral drug bioavailability by cocrystals

et al. 2018

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Introduction: Oral drug delivery is the most favored route of drug administration. However, poor oral bioavailability is one of the leading reasons for insufficient clinical efficacy. Improving oral absorption of drugs with low water solubility and/or low intestinal membrane permeability is an active field of research. Cocrystallization of drugs with appropriate coformers is a promising approach for enhancing oral bioavailability. Methods: In the present review, we have focused on recent advances that have been made in improving oral absorption through cocrystallization. The covered areas include supersaturation and its importance on oral absorption of cocrystals, permeability of cocrystals through membranes, drug-coformer pharmacokinetic (PK) interactions, conducting in vivo-in vitro correlations for cocrystals. Additionally, a discussion has been made on the integration of nanocrystal technology with supramolecular design. Marketed cocrystal products and PK studies in human subjects are also reported. Results: Considering supersaturation and consequent precipitation properties is necessary when evaluating dissolution and bioavailability of cocrystals. Appropriate excipients should be included to control precipitation kinetics and to capture solubility advantage of cocrystals. Beside to solubility, cocrystals may modify membrane permeability of drugs. Therefore, cocrystals can find applications in improving oral bioavailability of poorly permeable drugs. It has been shown that cocrystals may interrupt cellular integrity of cellular monolayers which can raise toxicity concerns. Some of coformers may interact with intestinal absorption of drugs through changing intestinal blood flow, metabolism and inhibiting efflux pumps. Therefore, caution should be taken into account when conducting bioavailability studies. Nanosized cocrystals have shown a high potential towards improving absorption of poorly soluble drugs. Conclusions: Cocrystals have found their way from the proof-of-principle stage to the clinic. Up to now, at least two cocrystal products have gained approval from regulatory bodies. However, there are remaining challenges on safety, predicting in vivo behavior and revealing real potential of cocrystals in the human.

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“…29 After that, a few more studies followed this line of investigation, aiming for pharmaceutical nanococrystal synthesis using bottom-up methods. [30][31][32][33] Simultaneously, top-down methods were also used for pharmaceutical nanococrystal synthesis. For instance, studies regarding wet milling [34][35][36] and high-pressure homogenization 37 can be found in the literature.…”

Section: Introductionmentioning

confidence: 99%