Crystallization of Amorphous Solid Dispersions of Resveratrol during Preparation and Storage—Impact of Different Polymers

Wegiel, Lindsay A.; Mauer, Lisa J.; Edgar, Kevin J.; Taylor, Lynne S.

doi:10.1002/jps.23358

Cited by 164 publications

(132 citation statements)

References 34 publications

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“…All the polymers (with both incorporation methods) inhibited crystallisation 41 of the amorphous IND. The SDs were better than the predissolved polymer solutions at inhibiting 42 crystallisation. The SDs were also better at maintaining drug supersaturation.…”

mentioning

confidence: 91%

Polymer incorporation method affects the physical stability of amorphous indomethacin in aqueous suspension

Surwase

Itkonen

Aaltonen

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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mentioning

confidence: 91%

Polymer incorporation method affects the physical stability of amorphous indomethacin in aqueous suspension

Surwase

Itkonen

Aaltonen

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…Besides these, it undergoes rapid first-pass metabolism by CYP3A4 in the liver and suffers enterohepatic recirculation (Marier et al, 2002;, leading eventually to marked reduction in the drug oral bioavailable fraction (almost zero) in humans and animals like rats (Amri et al, 2012). Under the aforementioned circumstances, various formulation approaches of t-RVT have been reported, such as liposome (Hung et al, 2006), solid dispersions (Wegiel et al, 2013), b-cyclodextrins inclusion complex (TrochePesqueira et al, 2013), microspheres (Nam et al, 2005), suspensions, but all with limited fruition.…”

Section: Introductionmentioning

confidence: 99%

Trans-resveratrol self-nano-emulsifying drug delivery system (SNEDDS) with enhanced bioavailability potential: optimization, pharmacokinetics andin situsingle pass intestinal perfusion (SPIP) studies

2014

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Trans-resveratrol (t-RVT) is a potent antioxidant. By virtue of extensive pre-systemic metabolism and existence of enterohepatic recirculation, t-RVT bioavailability is almost zero. The current study aimed to develop self-nanoemulsifying drug delivery systems (SNEDDS) using long-chain triglycerides (LCTs) of t-RVT in an attempt to circumvent such obstacles. Equilibrium solubility studies indicated the choice of Lauroglycol FCC as lipid, and of Labrasol and Transcutol P as surfactants, for formulating the SNEDDS. Ternary phase diagrams were constructed to select the areas of nanoemulsions, and the amounts of lipid (X 1 ) and surfactant (X 2 ) as the critical factor variables. The SNEDDS were optimized using 3 2 central composite design (CCD) and the optimized formulation (OPT) located using overlay plot. The nanometer size range and high negative values of zeta potential depicted non-coalescent nature of the SNEDDS. Optimized formulation indicated marked improvement in drug release profile vis-à-vis pure drug. Cloud point determination and accelerated stability studies ascertained the stability of OPT. Augmentation in the values of K a (3.29-fold) and AUC (4.31-fold) indicated significant enhancement in the rate and extent of bioavailability by the OPT compared with pure drug. In situ perfusion (SPIP) studies in Wistar rats construed remarkable enhancement in the absorptivity and permeability parameters of SNEDDS vis-à-vis the pure drug. Successful establishment of level A of in vitro/in vivo correlation substantiated the judicious choice of the in vitro dissolution milieu for simulating the in vivo conditions. The present study, therefore, reports the successful development of SNEDDS with distinctly enhanced bioavailability of t-RVT. KeywordsBioavailability, central composite design, in situ single pass intestinal perfusion, pharmacokinetic study, self-nanoemulsifying drug-delivery system History

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“…BMV was examined in solution (0.4% w/w in ethanol) and in the solid state (crystalline, as provided by the supplier, and amorphous forms). An amorphous film of BMV was formed by depositing a drop of an ethanolic solution onto a cleaned glass slide [23,24].…”

Section: Raman Microscopymentioning

confidence: 99%

Biophysical elucidation of the mechanism of enhanced drug release and topical delivery from polymeric film-forming systems

Garvie-Cook

Frederiksen

Petersson

et al. 2015

Journal of Controlled Release

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The effect of incorporating the lipidic medium-chain triglyceride (MCT) into polymeric film-forming systems (FFS) for topical drug delivery has been evaluated. First, the in vitro release of betamethasone-17-valerate (BMV), a representative dermatological drug, was determined from FFS comprising either hydrophobic polyacrylate co-polymers, or hydrophilic hydroxypropyl cellulose, with and without MCT. Release was enhanced from both polymers in the presence of MCT. Atomic force microscopy imaging and nanoindentation of FFS with MCT revealed two-phase structured films with softer inclusions (0.5 to 4μm in diameter) surrounded by a more rigid structure. Chemical mapping with Raman micro-spectroscopy showed that MCT was primarily confined to the inclusions within the polymer, which predominated in the surrounding film. BMV was distributed throughout the film but was more concentrated outside the inclusions. Furthermore, while BMV dissolved better into the hydrophobic films, it was more soluble in the MCT inclusions in hydrophilic films, suggesting its increased availability for diffusion from these softer regions of the polymer and explaining the release enhancement observed. Second, ex vivo skin penetration studies clearly revealed that uptake of BMV was higher from hydrophobic FFS than that from the more hydrophilic polymer due, at least in part, to the superior anti-nucleation efficiency of the former. Drug was quickly taken up into the SC from which it then diffused continuously over a sustained period into the lower, viable skin layers. In the presence of MCT, the overall uptake of BMV was increased and provides the basis for further optimisation of FFS as simple, convenient and sustained formulations for topical therapy.

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Crystallization of Amorphous Solid Dispersions of Resveratrol during Preparation and Storage—Impact of Different Polymers

Cited by 164 publications

References 34 publications

Polymer incorporation method affects the physical stability of amorphous indomethacin in aqueous suspension

Polymer incorporation method affects the physical stability of amorphous indomethacin in aqueous suspension

Trans-resveratrol self-nano-emulsifying drug delivery system (SNEDDS) with enhanced bioavailability potential: optimization, pharmacokinetics andin situsingle pass intestinal perfusion (SPIP) studies

Biophysical elucidation of the mechanism of enhanced drug release and topical delivery from polymeric film-forming systems

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