Fundamental aspects of solid dispersion technology for poorly soluble drugs

Huang, Yanbin; Dai, Wei

doi:10.1016/j.apsb.2013.11.001

Cited by 475 publications

(301 citation statements)

References 50 publications

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“…Converting the drug into the amorphous state and the drug-carrier interactions are the instrumental factors in the design and performance of the relevant solid dispersion (Graeser et al, 2010;Huang and Dai, 2014). Because of the higher Gibbs free energy of the amorphous form, the energy required to dissolve the drug from amorphous state is far less than that required for the equivalent amount from the crystalline state (Hancock and Zografi, 1997).…”

Section: Discussionmentioning

confidence: 99%

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Khoder

Abdelkader

ElShaer

et al. 2016

International Journal of Pharmaceutics

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Please cite this article as: Khoder, Mouhamad, Abdelkader, Hamdy, ElShaer, Amr, Karam, Ayman, Najlah, Mohammad, Alany, Raid G., Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin.International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2016.11.019 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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Section: Discussionmentioning

confidence: 99%

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Khoder

Abdelkader

ElShaer

et al. 2016

International Journal of Pharmaceutics

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“…Differential scanning calorimetry studies confirmed encapsulation of the drug within the nanoparticles. The decrease in glass t ransition temperature with increased drug loading shown in Table 2 suggests a solid dispersion of digoxin in the polymer matrix [30]. Because the glass transition temperature of the polymeric nanoparticles is below 37°C, the polymers would be in an elastomeric, rubbery state at physiological temperature, rather than in a rigid, glassy state.…”

Section: Nanoparticle Characterizationmentioning

confidence: 99%

Transport of digoxin-loaded Polymeric Nanoparticles Across BeWo cells, an In Vitro Model of Human Placental Trophoblast

et al. 2015

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Background: Fetal arrhythmias can lead to fetal congestive heart failure and hydrops fetalis. Digoxin (the first-line treatment) has low transplacental permeability and high risk of maternal side effects. Biodegradable digoxin-loaded PEGylated poly(lactic-co-glycolic acid) nanoparticles may increase digoxin transport across BeWo b30 cell monolayers (an in vitro model of trophoblast in human placenta) by reducing the drug's interaction with P-gp. Results/methodology: The nanoparticles showed high encapsulation efficiency and sustained release over 48 h. Transport studies revealed significantly increased permeability across BeWo cell layers of digoxin-loaded nanoparticles when compared with free digoxin. P-gp inhibition also increased the permeability of digoxin, but not digoxin-loaded nanoparticles. Conclusion: This represents a novel treatment strategy for fetal cardiovascular disease which may improve maternal and fetal outcomes.

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“…21 EM is practically insoluble moiety belonging to the BCS-II class. Therefore, SDs of EM were prepared by hot melt method, solvent evaporation method and kneading method.…”

Section: Preparation Of Solid Dispersions (Sds)mentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

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Fundamental aspects of solid dispersion technology for poorly soluble drugs

Cited by 475 publications

References 50 publications

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Transport of digoxin-loaded Polymeric Nanoparticles Across BeWo cells, an In Vitro Model of Human Placental Trophoblast

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

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