Solid dispersions of telaprevir with improved solubility prepared by co-milling: formulation, physicochemical characterization, and cytotoxicity evaluation

Xiong, Xiaopeng; Zhang, Man; Hou, Qing; Tang, Peixiao; Suo, Zili; Zhu, Ye; Li, Hui

doi:10.1016/j.msec.2019.110012

Cited by 27 publications

(30 citation statements)

References 34 publications

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“…In addition, the intermolecular interactions are also responsible for physical stability, particularly carbonyl functionality of PVP usually forms hydrogen bonds with weakly basic drugs containing -NH2 and -OH functionalities. The physical stability of Telaprevir-PVP solid dispersion is attributed to the intermolecular hydrogen bonding N-H--O and O-H-O between PVP and Telaprevir (82). Furthermore, the abovementioned stability mechanisms are always supported by higher Tg of PVP ( Fig.…”

Section: Poly Vinyl Pyrrolidone (Pvp)mentioning

confidence: 92%

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

et al. 2020

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Solid dispersion is the preferred technology to prepare efficacious forms of BCS class-II/IV APIs. To prepare solid dispersions, there exist a wide variety of polymeric carriers with interesting physicochemical and thermochemical characteristics available at the disposal of a formulation scientist. Since the advent of the solid dispersion technology in the early 1960s, there have been more than 5000 scientific papers published in the subject area. This review discusses the polymeric carrier properties of most extensively used polymers PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus® in the solid dispersion technology. The literature trends about preparation techniques, dissolution, and stability improvement are analyzed from the Scopus® database to enable a formulator to make an informed choice of polymeric carrier. The stability and extent of dissolution improvement are largely dependent upon the type of polymeric carrier employed to formulate solid dispersions. With the increasing acceptance of transfer dissolution setup in the research community, it is required to evaluate the crystallization/precipitation inhibition potential of polymers under dynamic pH shift conditions. Further, there is a need to develop a regulatory framework which provides definition and complete classification along with necessarily recommended studies to characterize and evaluate solid dispersions.

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Section: Poly Vinyl Pyrrolidone (Pvp)mentioning

confidence: 92%

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

et al. 2020

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“…Xiong et al [ 18 ] prepared telaprevir-containing SDs by the co-grinding technique using hydroxypropyl methylcellulose (HPMC), PVP K30 and polyethylene glycol (PEG) 6000 as polymers. SDs were characterized and their cytotoxicity was evaluated in vitro by the MTT method against HepG2 and normal liver cells (LO2) at drug concentrations between 0.1 and 30 μM.…”

Section: In Vitro Study Of Solid Dispersions In Polymeric Matricesmentioning

confidence: 99%

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

et al. 2020

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This review aims to provide an overview of studies that address the use, in therapeutic applications, of solid dispersions (SDs) with biological activities in vitro and/or in vivo mainly made up of polymeric matrices, as well as to evaluate the bioactive activity of their constituents. This bibliographic survey shows that the development of solid dispersions provides benefits in the physicochemical properties of bioactive compounds, which lead to an increase in their biological potential. However, despite the reports found on solid dispersions, there is still a need for biological assay-based studies, mainly in vivo, to assist in the investigation and to devise new applications. Therefore, studies based on such an approach are of great importance to enhance and extend the use of solid dispersions in the most diverse therapeutic applications.

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“…Analyzing the polymers spectra, HPMC exhibited bands at 3457 cm −1 attributed to the O-H stretching and at 1053 cm −1 corresponding to C-O-C stretching [20]. In the PEG, a broad band at 3477 cm −1 (νO-H) and a peak at 1096 cm −1 (νC-O) were observed, characteristic of ether.…”

Section: Fourier Transform Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

“…In this case, for the elaboration of solid dispersions (SDs), polymers play a prominent role, as they can stabilize SDs due to their ability to retain the drug in an amorphous form in the polymeric matrix during storage [19], and can increase the wettability, dispersibility, and solubility of drugs [20].…”

Section: Introductionmentioning

confidence: 99%

Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity

et al. 2020

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IVS320 (3a,10b-dihydro-1H-cyclopenta[b]naphtho[2,3-d]furan-5,10-dione) is a naphthoquinone that has low solubility in aqueous medium, a physical behavior that limits its biological activities, considering that compounds from this class have several activities. In this work, solid dispersions (SDs) prepared between IVS320 and polymers hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP) were developed using physical mixture (PM), kneading (KN), and rotary evaporation (RE) methods. Dispersions were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetry (TG), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). In addition, in vitro antiparasitic activity in Trypanosoma cruzi Y strains was evaluated. Physical-chemical characterization demonstrated the formation of SDs through the interaction of IVS320 with polymeric matrices. SDs of IVS320-polymer presented a significant potentiation of antichagasic activity, with inhibitory growth around 62% (IVS320-HPMC/RE), 55% (IVS320-PEG/RE), and 85% (IVS320-PVP/RE), while pure IVS320 showed a value of 48% for the highest concentrations evaluated (50 µg/mL).

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Solid dispersions of telaprevir with improved solubility prepared by co-milling: formulation, physicochemical characterization, and cytotoxicity evaluation

Cited by 27 publications

References 34 publications

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

Novel Solid Dispersions of Naphthoquinone Using Different Polymers for Improvement of Antichagasic Activity

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