Amorphous formulations for dissolution and bioavailability enhancement of poorly soluble APIs

Kanaujia, Parijat; Poovizhi, P. N.; Ng, Wai Kiong; Tan, Reginald B. H.

doi:10.1016/j.powtec.2015.05.012

Cited by 146 publications

(73 citation statements)

References 87 publications

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“…19 Importantly, the solubility of CM-SF NPs was greatly improved, which was mainly due to size reduction, supersaturation of CM, water solubility of the SF nanoplatform, better dispersibility and wettability of CM, and hydrogen bonds between CM and the SF nanoplatform. 27,28 The intracellular uptake result of CM-SF NPs is in agreement with previous studies. 26,29 In those studies, the introduction of SF improved the retention of loaded drugs in cancer cells, thus leading to a higher anticancer efficacy.…”

supporting

confidence: 91%

“…Our findings are similar to those of previous studies on colon cancer therapy by mucoadhesive CM-containing chitosan NPs. 27,30 Meanwhile, CM-SP NPs showed reduced toxicity on normal human colon mucosal epithelial cells at an effective concentration (~10 μg/mL) in the treatment of colon cancer cells. This phenomenon could be explained by the slow and sustained drug-release potentials of SF nanoplatforms, thereby reducing their cytotoxicity.…”

mentioning

confidence: 99%

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Supercritical carbon dioxide-developed silk fibroin nanoplatform for smart colon cancer therapy

Xie¹,

Fan²,

Li³

et al. 2017

IJN

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Purpose To deliver insoluble natural compounds into colon cancer cells in a controlled fashion. Materials and methods Curcumin (CM)–silk fibroin (SF) nanoparticles (NPs) were prepared by solution-enhanced dispersion by supercritical CO 2 (SEDS) (20 MPa pressure, 1:2 CM:SF ratio, 1% concentration), and their physicochemical properties, intracellular uptake efficiency, in vitro anticancer effect, toxicity, and mechanisms were evaluated and analyzed. Results CM-SF NPs (<100 nm) with controllable particle size were prepared by SEDS. CM-SF NPs had a time-dependent intracellular uptake ability, which led to an improved inhibition effect on colon cancer cells. Interestingly, the anticancer effect of CM-SF NPs was improved, while the side effect on normal human colon mucosal epithelial cells was reduced by a concentration of ~10 μg/mL. The anticancer mechanism involves cell-cycle arrest in the G 0 /G 1 and G 2 /M phases in association with inducing apoptotic cells. Conclusion The natural compound-loaded SF nanoplatform prepared by SEDS indicates promising colon cancer-therapy potential.

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supporting

confidence: 91%

mentioning

confidence: 99%

Supercritical carbon dioxide-developed silk fibroin nanoplatform for smart colon cancer therapy

Xie¹,

Fan²,

Li³

et al. 2017

IJN

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“…It should be noted that amorphous form of a poorly soluble API has higher apparent solubility and improved dissolution rate as compared to its crystalline form since no crystal lattice has to be broken down for dissolution to take place . Though the amorphous form of APIs represents another promising technique to improve the bioavailability of poorly water‐soluble drugs, their stabilization is a major concern . However, in this study, the ibuprofen amorphous particles encapsulated inside the ionic polymer (alginate) hydrogel matrix remain stable for at least 4 months at 25 °C and 60% relative humidity (see the DSC/XRD results in the Supporting Information).…”

Section: Resultsmentioning

confidence: 82%

Low Energy Nanoemulsions as Templates for the Formulation of Hydrophobic Drugs

Badruddoza

Gupta

Myerson

et al. 2018

Advanced Therapeutics

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Most small molecule active pharmaceutical ingredients (APIs) are hydrophobic which poses formulation challenges due to their poor water solubility. Current approaches are energy intensive and involve presenting the API in a nanoparticle form that is then combined with other additives into a stable formulation. Here, a bottom-up and scalable method that formulates nanoparticles (crystalline or amorphous) of poorly water-soluble APIs directly embedded in composite hydrogel beads is presented. Using nanoemulsions prepared from a low energy method as templates, the flexible approach allows to vary the embedded API nanoparticle size from 100 to 500 nm and the hydrogel bead size from 100 to 1200 µm, and subsequently achieve control over the dissolution kinetics. To better understand the dissolution process, a physical model is build that allows to collapse the kinetic data onto a master curve and predict the dependence of release rates on size of both API nanoparticles and hydrogel beads. Lastly, it is demonstrated that the dissolution kinetics of multiple drugs embedded in the same hydrogel matrix can be tuned simultaneously, an attractive property for commercial multi-drug dosage applications. The new approach not only leads to process intensification, but also improved performance.

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“…The crystalline state of the lactose made a great impact on the LCSND. As known to us, crystal structure can maintain stability during storage and the amorphous component can promote dissolution . Then the crystal state of LCSND was crucial for storage stability.…”

Section: Resultsmentioning

confidence: 99%

Optimization and characterization of lambda‐cyhalothrin solid nanodispersion by self‐dispersing method

Wang

Cui

Zhao

et al. 2018

Pest Management Science

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Amorphous formulations for dissolution and bioavailability enhancement of poorly soluble APIs

Cited by 146 publications

References 87 publications

Supercritical carbon dioxide-developed silk fibroin nanoplatform for smart colon cancer therapy

Supercritical carbon dioxide-developed silk fibroin nanoplatform for smart colon cancer therapy

Low Energy Nanoemulsions as Templates for the Formulation of Hydrophobic Drugs

Optimization and characterization of lambda‐cyhalothrin solid nanodispersion by self‐dispersing method

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