Pluronic F127 as a suitable carrier for preparing the imatinib base solid dispersions and its potential in development of a modified release dosage forms

Karolewicz, Bożena; Gajda, Maciej; Gòrniak, Agata; Owczarek, Artur

doi:10.1007/s10973-017-6139-1

Cited by 54 publications

(27 citation statements)

References 11 publications

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“…In this study, PL works by forming eutectic mixture with APG in all SDs as indicated by DSC thermograms of different SDs. DSC thermograms of SDs prepared by kneaded, melted and microwave technology showed two peaks (one at around 50 0 C) and second at around 345 0 C, suggesting formation of eutectic mixture between PL and APG in all SDs (Karolewicz et al, 2017). The melting temperature of APG was recorded as 366.36 ° C by Huang et al (2016).…”

Section: Resultsmentioning

confidence: 99%

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Alshehri

Shakeel

Ibrahim

et al. 2019

Saudi Pharmaceutical Journal

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Apigenin (APG) is a poorly soluble bioactive compound/nutraceutical which shows poor bioavailability upon oral administration. Hence, the objective of this research work was to develop APG solid dispersions (SDs) using different techniques with the expectation to obtain improvement in its in vitro dissolution rate and in vivo bioavailability upon oral administration. Different SDs of APG were prepared by microwave, melted and kneaded technology using pluronic-F127 (PL) as a carrier. Prepared SDs were characterized using “thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) spectrometer, powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM)”. After characterization, prepared SDs of APG were studied for in vitro drug release/dissolution profile and in vivo pharmacokinetic studies. The results of TGA, DSC, FTIR, PXRD and SEM indicated successful formation of APG SDs. In vitro dissolution experiments suggested significant release of APG from all SDs (67.39–84.13%) in comparison with control (32.74%). Optimized SD of APG from each technology was subjected to in vivo pharmacokinetic study in rats. The results indicated significant improvement in oral absorption of APG from SD prepared using microwave and melted technology in comparison with pure drug and commercial capsule. The enhancement in oral bioavailability of APG from microwave SD (319.19%) was 3.19 fold as compared with marketed capsule (100.00%). Significant enhancement in the dissolution rate and oral absorption of APG from SD suggested that developed SD systems can be successfully used for oral drug delivery system of APG.

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Section: Resultsmentioning

confidence: 99%

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Alshehri

Shakeel

Ibrahim

et al. 2019

Saudi Pharmaceutical Journal

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“…Pure CLT showed a distinct N=N stretching peak of tetrazole at 1666 cm −1 and a C=C stretching band at 1504 cm −1 [ 35 ]. POX exhibited a characteristic peak at 1103 cm −1 , ascribed to the stretching vibration of C-O-C [ 36 ]. Meanwhile, SLS exhibited a characteristic peak of –OSO 3 - stretching at 1229 cm −1 [ 37 ].…”

Section: Resultsmentioning

confidence: 99%

Role of Surfactant Micellization for Enhanced Dissolution of Poorly Water-Soluble Cilostazol Using Poloxamer 407-Based Solid Dispersion via the Anti-Solvent Method

et al. 2021

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This study aimed to investigate the role of micellization of sodium lauryl sulfate (SLS) in poloxamer 407 (POX)-based solid dispersions (POX-based SDs) using the anti-solvent method in enhancing the dissolution rate of practically water-insoluble cilostazol (CLT). Herein, SLS was incorporated into CLT-loaded SDs, at a weight ratio of 50:50:10 of CLT, POX, and SLS by three different methods: anti-solvent, fusion (60 °C), and solvent (ethanol) evaporation. The SDs containing micellar SLS in the anti-solvent method were superior in the transformation of the crystalline form of the drug into a partial amorphous state. It was notable that there was an existence of a hydrophobic interaction between the surfactant and the hydrophobic regions of polymer chain via non-covalent bonding and the adsorption of micellar SLS to the POX-based SDs matrix. Moreover, SLS micellization via the anti-solvent method was effectively interleaved in SDs and adhered by the dissolved CLT, which precluded drug particles from aggregation and recrystallization, resulting in improved SD wettability (lower contact angle) and reduced particle size and dissolution rate. In contrast, SDs without micellar SLS prepared by the solvent method exerted drug recrystallization and an increase of particle size, resulting in decreased dissolution. Incorporation of surfactant below or above critical micellar concentration (CMC) in SDs using the anti-solvent method should be considered in advance. Dissolution results showed that the pre-added incorporation of micellar SLS into POX-based SDs using the anti-solvent method could provide a way of a solubilization mechanism to enhance the dissolution rate of poorly water-soluble drugs.

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“…), and insoluble in THF, ethyl ether, and chloroform. The FT-IR spectrum of Plx-g-CMP (Figure 3c) shows both the specific absorption bands of CMP and Plx (2890 cm −1 (C-H stretching aliphatic), 1385 cm −1 (in-plane O-H bend) and 1112 cm −1 (C-O-stretch) [58]) (see Figure 3d). In addition, a shift of the ester absorption band from 1735 to 1739 cm −1 is observed, as well as the appearance of absorption bands specific to the amide bond (1635 cm −1 (C=O, amide I), 1554 cm −1 (coupling NH and CN, amide II) and 1450 cm −1 (C-N stretch, amide III)), which demonstrates the coupling of poloxamer to the carboxymethyl pullulan chain through an amide bond.…”

Section: Ds (%) =mentioning

confidence: 99%

Thermosensitive Poloxamer-graft-Carboxymethyl Pullulan: A Potential Injectable Hydrogel for Drug Delivery

Constantin¹,

Cosman²,

Bercea³

et al. 2021

Polymers

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A thermosensitive copolymer composed of amphiphilic triblock copolymer, poloxamer 407, grafted on hydrophilic pullulan with pendant carboxymethyl groups (CMP) was prepared and characterized. The structure of the new copolymer was assessed by Fourier transform infrared (FT-IR) and 1H nuclear magnetic resonance (1H NMR) spectroscopy. The content of the poloxamer in the grafted copolymer was 83.8% (w/w). The effect of the copolymer concentration on the gelation behavior was analyzed by the vertical method and rheological tests; the gel phase of the copolymer occurred at a lower concentration (11%, w/v) as compared with poloxamer (18%, w/v). The starting gelation time under the simulated physiological conditions (phosphate buffer with a pH of 7.4, at 37 °C) was sensitive on the rest temperature before the test, this being 990 s and 280 s after 24 h rest at 4 °C and 20 °C, respectively. The rheological tests evidenced a high elasticity and excellent ability of the copolymer to recover the initial structure after the removal of the applied force or external stimuli. Moreover, the hydrogel has proved a sustained release of amoxicillin (taken as a model drug) over 168 h. Taken together, the results clearly indicate that this copolymer can be used as an injectable hydrogel.

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Pluronic F127 as a suitable carrier for preparing the imatinib base solid dispersions and its potential in development of a modified release dosage forms

Cited by 54 publications

References 11 publications

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Role of Surfactant Micellization for Enhanced Dissolution of Poorly Water-Soluble Cilostazol Using Poloxamer 407-Based Solid Dispersion via the Anti-Solvent Method

Thermosensitive Poloxamer-graft-Carboxymethyl Pullulan: A Potential Injectable Hydrogel for Drug Delivery

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