Pharmaceutical Applications of Solid Dispersion Systems

Chiou, Win L.; Riegelman, Sidney

doi:10.1002/jps.2600600902

Cited by 1,550 publications

(881 citation statements)

References 61 publications

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“…Furthermore, the disappearance of thermal features of curcumin ( Figure 1d) suggests some interaction between curcumin and gelatin, most likely due to the formation of an amorphous solid dispersion, a known condition for increasing drug dissolution. 19 On the other hand, the hydrogen bonding between curcumin and gelatin, verified by Fourier transform infrared spectroscopy (Figure 1e), would inhibit curcumin crystallization and let the compound precipitate out in the amorphous form, resulting in increased curcumin solubility. Hence, it is likely to be that gelatin inhibited the association of curcumin molecules to form crystal nuclei and subsequent crystal growth in the nanofibers during the electrospinning process.…”

Section: Discussionmentioning

confidence: 99%

Nano-formulated curcumin accelerates acute wound healing through Dkk-1-mediated fibroblast mobilization and MCP-1-mediated anti-inflammation

et al. 2017

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Turmeric, a product of Curcuma longa, has a very long history of being used for the treatment of wounds in many Asian countries. Curcumin, the principal curcuminoid of turmeric, has recently been identified as a main mediator of turmeric's medicinal properties. However, the inherent limitations of the compound itself, such as hydrophobicity, instability, poor absorption and rapid systemic elimination, pose big hurdles for translation to wider clinical application. We present here an approach for engineering curcumin/gelatin-blended nanofibrous mats (NMs) by electrospinning to adequately enhance the bioavailability of the hydrophobic curcumin for wound repair. Curcumin was successfully formulated as an amorphous nanosolid dispersion and favorably released from gelatin-based biomimetic NMs that could be easily applied topically to experimental wounds. We show synergistic signaling by the released curcumin during the healing process: (i) mobilization of wound site fibroblasts by activating the Wnt signaling pathway, partly mediated through Dickkopf-related protein-1, and (ii) persistent inhibition of the inflammatory response through decreased expression of monocyte chemoattractant protein-1 by fibroblasts. With a combination of these effects, the curcumin/gelatin-blended NMs enhanced the regenerative process in a rat model of acute wounds, providing a method for translating this ancient medicine for use in modern wound therapy.

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Section: Discussionmentioning

confidence: 99%

Nano-formulated curcumin accelerates acute wound healing through Dkk-1-mediated fibroblast mobilization and MCP-1-mediated anti-inflammation

et al. 2017

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“…Exhaustive research has been carried out on dissolution enhancement of drugs using water-insoluble polymers such as crospovidone (14,15) and enteric polymers such as hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, Eudragit® L100 and S100 (16), and Eudragit® E (17,18). As a rule, inclusion of water-soluble carriers results in a fast release of the drug from the matrix, and a poorly soluble or insoluble carrier leads to a slower release of the drug from the matrix (19,20). On a similar line, the use of MC along with PVP K30 may nullify the drawback associated with PVP.…”

Section: Introductionmentioning

confidence: 99%

Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

et al. 2013

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Abstract. The effect of ternary solid dispersions of poor water-soluble NSAID meloxicam with moringa coagulant (obtained by salt extraction of moringa seeds) and polyvinylpyrrolidone on the in vitro dissolution properties has been investigated. Binary (meloxicam-moringa and meloxicam-polyvinylpyrrolidone (PVP)) and ternary (meloxicam-moringa-PVP) systems were prepared by physical kneading and ball milling and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry. The in vitro dissolution behavior of meloxicam from the different products was evaluated by means of United States Pharmacopeia type II dissolution apparatus. The results of solid-state studies indicated the presence of strong interactions between meloxicam, moringa, and PVP which were of totally amorphous nature. All ternary combinations were significantly more effective than the corresponding binary systems in improving the dissolution rate of meloxicam. The best performance in this respect was given by the ternary combination employing meloxicam-moringa-PVP ratio of [1:(3:1)] prepared by ball milling, with about six times increase in percent dissolution rate, whereas meloxicam-moringa (1:3) and meloxicam-PVP (1:4) prepared by ball milling improved dissolution of meloxicam by almost 3-and 2.5-folds, respectively. The achieved excellent dissolution enhancement of meloxicam in the ternary systems was attributed to the combined effects of impartation of hydrophilic characteristic by PVP, as well as to the synergistic interaction between moringa and PVP.

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“…The matrix can be either crystalline or amorphous. The drug can be dispersed molecularly, in amorphous particles (clusters) or in crystalline particles 34 . Chiou and Riegelman, in their classic review, defined these systems as 'the dispersion of one or more active ingredients in an inert carrier matrix at solid-state prepared by the melting (fusion), solvent or melting-solvent method, while Corrigan suggested the definition as being a 'product formed by converting a fluid drug-carrier combination to the solid state' 35 .…”

Section: Extension To Bcs: (Bcs Containing Six Classes)mentioning

confidence: 99%

“…Because of the greater stability, smaller bulk, accurate dosage and easy production, solid dosage forms have many advantages over other types of oral dosage forms. Therefore, most of the new chemical entities under development these days are intended to be used as a solid dosage form that originate an effective reproducible in vivo plasma concentration after oral administration 3,4 . In fact, most new chemical entities are poorly soluble drugs, not wellabsorbed after oral administration 4,5 , which can distract from the drug's inherent efficacy [6][7][8] .…”

Section: Introductionmentioning

confidence: 99%

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2010

IJPSR

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The solubility behavior of drugs remains one of the most challenging aspects in the formulation development. Although there was a great interest in solid dispersion systems during the past four decades to increase solubility by improving dissolution rate and bioavailability of poorly soluble drugs; there commercial use has been very limited, primarily because of manufacturing difficulties and various stability problems. It can be carried out by reducing drug particle size to the absolute minimum, and hence improving drug wet-ability, bioavailability may be significantly improved. Solid dispersion of drugs was generally produced by melt or solvent evaporation methods. Recently, surfactants have been included to stabilize the formulations, thus avoiding drug recrystallization and potentiating their solubility. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the eminent approach to improve the solubility or the dissolution rate and recent revival has been discussed.

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Pharmaceutical Applications of Solid Dispersion Systems

Cited by 1,550 publications

References 61 publications

Nano-formulated curcumin accelerates acute wound healing through Dkk-1-mediated fibroblast mobilization and MCP-1-mediated anti-inflammation

Nano-formulated curcumin accelerates acute wound healing through Dkk-1-mediated fibroblast mobilization and MCP-1-mediated anti-inflammation

Solid-State Characterization and Dissolution Properties of Meloxicam–Moringa Coagulant–PVP Ternary Solid Dispersions

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