Direct incorporation of nano graphene oxide (nGO) into hydrophobic drug crystals for enhanced aqueous dissolution

Islam, Mohammad Saiful; Renner, Faradae; Azizighannad, Samar; Mitra, Somenath

doi:10.1016/j.colsurfb.2020.110827

Cited by 21 publications

(9 citation statements)

References 35 publications

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“…The hydrodynamic Z average intensity weighted nGO particle size was confirmed to be an average of 131.4 nm ( Figure 1 a) on Zetasizer (nGO water solutions 1, 2 and 3 refer to three different nGO dilutions to prepare drug samples). Additionally, Atomic Force Microscopy (AFM) measurements have shown nGO particle thickness to be 1–3 nm [ 52 ]. The dynamic light scattering percent intensity distribution for MA and MA-nGO particle analysis data suggest that before (pure MA) and after antisolvent coprecipitation (MA-nGO composites) produce uniform drug composite crystallites.…”

Section: Resultsmentioning

confidence: 99%

“…Unaltered crystalline structure will maintain active ingredients polymorphism properties. Micron-sized graphene oxide was also incorporated and was found to wrap the crystal, making the composite insoluble [ 52 ].…”

Section: Resultsmentioning

confidence: 99%

“…An antisolvent technique was used for drug composite synthesis based on a published procedure [ 52 ]. Different amounts of nanographene oxide (2.6 mg, 4.0 mg, and 6.0 mg) were used during the incorporation process to prepare the MA sample solution.…”

Section: Methodsmentioning

confidence: 99%

“…Additionally, chemical surface morphology and inner structure was observed through JEM-F200, Transmission Electron Microscope (TEM) (JOEL, Tokyo, Japan). Alternatively, particle thickness was characterized previously using Bruker Dimension icon Scan Asyst, AFM instrument (Billerica, MA, USA) [ 52 ]. The crystalline and chemical functional structure of the prepared MA-nGO composites were analyzed through Raman spectroscopy, which was carried out using a ThermoFisher Scientific DXR Raman Microscope (Madison, WI, USA) with 532 nm wavelength laser and filter.…”

Section: Methodsmentioning

confidence: 99%

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Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate

et al. 2021

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The aim of this work is to present an approach to enhance the dissolution of progestin medication, megestrol acetate (also known as MEGACE), for improving the dissolution rate and kinetic solubility by incorporating nano graphene oxide (nGO). An antisolvent precipitation process was investigated for nGO-drug composite preparation, where prepared composites showed crystalline properties that were similar to the pure drug but enhanced aqueous dispersibility and colloidal stability. To validate the efficient release profile of composite, in vitro dissolution testing was carried out using United States Pharmacopeia, USP-42 paddle method, with gastric pH (1.4) and intestinal pH (6.5) solutions to mimic in vivo conditions. Pure MA is practically insoluble (2 µg/mL at 37 °C). With the incorporation of nGO, it was possible to dissolve nearly 100% in the assay. With the incorporation of 1.0% of nGO, the time required to dissolve 50% and 80% of drug, namely T50 and T80, decreased from 138.0 min to 27.0 min, and the drug did not dissolve for 97.0 min in gastric media, respectively. Additionally, studies done in intestinal media have revealed T50 did not dissolve for 92.0 min. This work shows promise in incorporating functionalized nanoparticles into the crystal lattice of poorly soluble drugs to improve dissolution rate.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Hydrophilic and Functionalized Nanographene Oxide Incorporated Faster Dissolving Megestrol Acetate

et al. 2021

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“…Crystallization technology is one of the most widely applied processes in pharmaceutical purification. [ 1–4 ] It can improve the particle size, crystal habit and product purity of the API crystals. These factors can significantly influence a drug's efficacy, physiological activity and stability.…”

Section: Introductionmentioning

confidence: 99%

The Agglomeration of Niacin Crystals in the Cooling Crystallization Process

Wang

2021

Crystal Research and Technology

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Crystal agglomeration is an important factor that can affect the purity and crystal habit of crystalline products. Agglomeration of niacin crystals in its cooling crystallization and its mechanism is investigated using both experimental and molecular dynamics simulation methods. The magnitude of the interaction energy which is mainly contributed by the hydrogen bond and π–π stacking between the (0 1 1) crystal face and (1 1 −1) crystal face that have both the pyridine and carboxyl groups is the main factor determining the extent of agglomeration of niacin crystal. Besides, the interaction energy increases with the crystallization temperature and the supersaturation of the solution, and hence the agglomeration is more severe. The change of solvent species has minimal effect on the agglomeration of crystals. Besides, the agglomeration situation of carbamazepine and acetaminophen that with similar structures to niacin is also verified using molecular dynamics simulations. The findings in this work can be used to predict, control the agglomeration phenomenon, and optimize the crystallization process of niacin and other substances with similar chemical structure.

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