Investigation and correlation of drug polymer miscibility and molecular interactions by various approaches for the preparation of amorphous solid dispersions

Meng, Fan; Trivino, Anne; Prasad, Dev; Chauhan, Harsh

doi:10.1016/j.ejps.2015.02.003

Cited by 144 publications

(116 citation statements)

References 37 publications

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“…Some of the reasons given for excipient selection included reliance on previous reports of the use of similar excipients and their historical applicability in ASDs and oral dosage forms (100–125); the physicochemical properties and functions of the excipient, possible interactions between the compound and the excipient, and the miscibility/immiscibility of the compound and excipient (105–108,111,112,114,126–148); the processability or suitability of the excipient for the preparation method (73,105,119,127,149–152); and the possibility of designing a controlled-release profile and/or pH-dependent release of the compound from the amorphous formulation (99,100,107,123,153–156). An attempt to tailor and customize excipients by modifying the functional groups which could be potentially used in ASD formulations has also been reported (157).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

“…These are particularly used as a means to estimate the homogeneity of the mixture at a particular ratio, which is postulated to influence the stability of the resulted amorphous system. Among others, these include the calculation of the Hansen solubility parameters (104,126,146,154,161) and the Flory-Huggins theory (94,150). …”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

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The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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“…As supporting evidence, Tween 20 demonstrated a C=O stretching peak at 1734 cm −1 (pure T20) and at 1730 cm −1 (in PCT5). The prefer- 25) δ=in-plane bending; ν=stretching.…”

Section: )mentioning

confidence: 99%

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Rahma

Munir

Khairurrijal

et al. 2016

Biological & Pharmaceutical Bulletin

141

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An electrospun fiber of polyvinyl(pyrrolidone) (PVP)-Tween 20 (T20) with curcumin as the encapsulated drug has been developed. A study of intermolecular interactions was performed using Raman spectroscopy, Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD).The Raman and FT-IR studies showed that curcumin preferrably interacted with T20 and altered PVP chain packing, as supported by XRD and physical stability data. The hydroxyl stretching band in PVP shifted to a lower wavenumber with higher intenstity in the presence of curcumin and PVP, indicating that hydrogen bond formation is more intense in a curcumin or curcumin-T20 containing fiber. The thermal pattern of the fiber did not indicate phase separation. The conversion of curcumin into an amorphous state was confirmed by XRD analysis. An in vitro release study in phosphate buffer pH 6.8 showed that intermolecular interactions between each material influenced the drug release rate. However, low porosity was found to limit the hydrogen bond-mediated release.Key words curcumin; fiber; electrospinning; interaction; porosity; polymeric drug delivery system Curcumin is the major constituent of turmeric rhizome (Curcuma sp.).1) Curcumin has a number of demonstrated pharmacological effects, such as antioxidant, anti-inflammatory, anticancer, hepatoprotective, 1) antimicrobial, and antiviral. 2)Clinical trials have proven that curcumin is well tolerated by the body, with a maximum dose of 12 g daily.3) Unfortunately, the efficacy of curcumin is limited by its poor solubility in water, as well as its instability under light, heat, and alkaline conditions.1) The solubility of curcumin in aqueous buffer (pH 5) is reported to be 11 ng/mL.3) Moreover, the absorption of curcumin in the gastrointestinal tract is very low, leading to poor bioavailability (in animals and humans).2) Therefore, designing an effective delivery system is necessary in order to address the limitations of curcumin use. 1-3)A wide range of drug delivery systems has been developed to improve the bioavailability of poorly soluble drugs, including fast-dissolving tablets, 4) incorporation into a hydrophilic complex, 1) micellization, and solid dispersion. 5) Electrospinning, a technique of producing thin strands of fiber using high voltage, has opened up opportunities in the development of drug delivery systems. An optimized electrospinning process can produce nano-sized fibers. 6)The high surface area and porosity of these electrospun fibers are advantageous in their use as carriers for poorly water-soluble drugs.5) The high surface area generally increases the dissolution rate of the incorporated drug, thus potentially enhancing its bioavailability. 5)Therefore, the incorporation of curcumin into an electrospun fiber is expected to improve its oral bioavailability.Tailoring a suitable drug-loaded fiber requires careful selection of materials, in addition to an optimized production process and environment. Generally, the drug is mixed with a polymer s...

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“…Additionally in solid state, the formation of a stable drug polymer matrix resulted in the inhibition of drug crystallization (Meng et al, 2015). XRD analysis, combined with the investigation of DSC, demonstrated that when loaded in the PVA4-88 by using the solvent casting method, MH would like to form solid dispersions with the polymer and be amorphous in this polymer matrix.…”

Section: X-ray Diffraction Characterizationmentioning

confidence: 99%

Preparation of an oral thin film containing meclizine hydrochloride: In vitro and in vivo evaluation

Yuan

Quan

Fang

2015

International Journal of Pharmaceutics

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Investigation and correlation of drug polymer miscibility and molecular interactions by various approaches for the preparation of amorphous solid dispersions

Cited by 144 publications

References 37 publications

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Intermolecular Interactions and the Release Pattern of Electrospun Curcumin-Polyvinyl(pyrrolidone) Fiber

Preparation of an oral thin film containing meclizine hydrochloride: In vitro and in vivo evaluation

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