Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning

Marano, Stefania; Barker, S. A.; Raimi-Abraham, Bahijja Tolulope; Missaghi, Shahrzad; Rajabi‐Siahboomi, Ali R.; Craig, Duncan Q.M.

doi:10.1016/j.ejpb.2016.03.021

Cited by 73 publications

(62 citation statements)

References 57 publications

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“…A similar solid dispersion formulation which was prepared using sucrose alone or in combination with other surfactants or polymers has successfully maintained the amorphous state of both drug and the carrier and increased the solubility of the drug. 44,45 Next, the determinant factor of the dissolution performance can be attributed to the impact of sucrose on the dissolution of curcumin. This phenomenon, ie, the presence of sugar molecules increasing the curcumin dissolution profile, very likely occurred through the formation of nanostructured molecular-level of curcumin/sucrose composites during spray-drying.…”

Section: X-ray Diffraction Analysismentioning

confidence: 99%

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

Wijiani¹,

Isadiartuti²,

Rijal³

et al. 2020

IJN

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Introduction: Curcumin faces a major challenge in clinical use due to its poor aqueous solubility, which affects its bioavailability over oral use. The present study was carried out to overcome this problem. Methods: An amorphous micellar curcumin-spray dried powder (MC-SDP) with selfassembled casein was prepared by the addition of sucrose as a protectant. The dry powder of curcumin-loaded micelles was obtained by a spray-drying technique in the presence of sucrose as a protectant. The MC-SDP in the form of dry powder was further developed into tablets to investigate the dissolution profile. The physical properties of preformed powder were characterized by differential thermal analysis (DTA), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Quantitative analysis in the form of solutions was analyzed by high-performance liquid chromatography (HPLC). Results: The physical properties demonstrated that MC-SDP varies from dented to smoother surfaces as a function of sucrose. Furthermore, melting transitions of curcumin in the form of MC-SDP were broadened in all sample mixtures, as observed in the DTA thermogram. The XRD spectra showed that the sharp and very intense peaks of single curcumin crystalline structure no longer existed in all MC-SDP forms, indicating that the mixtures were amorphous. Moreover, a further dissolution study of MC-SDP showed a significant increase of drug dissolved with the presence of sucrose, where >80% of curcumin from MC-SDP was dissolved within 30 min. Conclusion: The study demonstrated the manufacture of micellar spray-dried powder that would contribute to the development of oral delivery of curcumin.

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Section: X-ray Diffraction Analysismentioning

confidence: 99%

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

Wijiani¹,

Isadiartuti²,

Rijal³

et al. 2020

IJN

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show abstract

“…Approximately 75% of new chemical entities are poorly soluble in aqueous medium and many even in the organic medium [1]. Solubility is quantitatively defined as the concentration of solute in a saturated solution at a certain temperature, while qualitatively may be defined as the spontaneous interaction of two or more substances for formation of a homogeneous molecular dispersion [2].…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Lafutidine Nanosuspension for Oral Drug Delivery System

2018

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Objective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combination of polymer with surfactant such as tween 80, three formulations show the effect of stirring speed and three formulations prepare to show the effect of addition of co-surfactant such as tween 20. All these formulations are evaluated for their particle size and entrapment efficiency and in vitro release. The selected one was evaluated for zeta potential, scanning electron microscope, atomic force microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, saturation solubility and stability study.Results: The formulations (F3-F10) were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: polymer: surfactant ratio 1:4:4 and the optimum stirring speed was 1500 rpm. Dramatic effect on the particle size reduction was found by the addition of co-surfactant (tween 20) in formulation F7 that has a particle size 15.89±1.8 nm. The selected formula F7 showed an enhanced dissolution profile (10 min) compared to the pure drug at all-time intervals.Conclusion: The results show that the formulation that contains drug: PVP-K90: tween 80: tween 20 in ratio 1:4:2:2 is the best one and can be utilized to formulate lafutidine nanosuspension.

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“…This literature review found that phosphate buffer solutions, in the range of pH 5.8-8.0, were employed in 32.6% of cases as medium for the shake-flask method (15 of 46 studies) (8,11,19,31,32,37,(41)(42)(43)45,46,48,51,57,58) and in 40.0% as dissolution medium (8 of 20 studies) (10,11,22,24,(51)(52)(53)56). Acetate buffer was used less frequently, in 4 of 46 studies (8.7%) (41,42,45,49) as medium for the shake-flask method and in 2 of 20 studies (10.0%) as dissolution medium (52,56).…”

Section: Buffer Solutionsmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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Development of micro-fibrous solid dispersions of poorly water-soluble drugs in sucrose using temperature-controlled centrifugal spinning

Abstract: Graphical abstract

Cited by 73 publications

References 57 publications

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

Formulation and Characterization of Lafutidine Nanosuspension for Oral Drug Delivery System

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

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