Relevance of the theoretical critical pore radius in mesoporous silica for fast crystallizing drugs

Vraníková, Barbora; Niederquell, Andreas; Šklubalová, Zdeňka; Kuentz, Martin

doi:10.1016/j.ijpharm.2020.120019

Cited by 19 publications

(15 citation statements)

References 63 publications

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“…It can also improve the in vitro dissolution rate and apparent solubility compared to their crystalline counterparts and in vivo performance [15,16]. The two mechanisms that have been proposed for the inhibition of drug crystallization in MS include (1) the adsorption of drugs on MS due to the molecular interaction between the surface of MPS and the functional groups of the drug molecules and (2) the nanoconfinement effect of MPS from a smaller pore diameter compare to critical crystalline nuclei, which caused the suppression of crystal growth [17,18]. This showed that the surface area and pore volume of MS could affect the drug encapsulation and crystallization [19,20].…”

Section: Introductionmentioning

confidence: 99%

A Comparative Study of the Pharmaceutical Properties between Amorphous Drugs Loaded-Mesoporous Silica and Pure Amorphous Drugs Prepared by Solvent Evaporation

Budiman

Aulifa

2022

Pharmaceuticals

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The formulation of poorly water-soluble drugs is one of the main challenges in the pharmaceutical industry, especially in the development of oral dosage forms. Meanwhile, there is an increase in the number of poorly soluble drugs that have been discovered as new chemical entities. It was also reported that the physical transformation of a drug from a crystalline form into an amorphous state could be used to increase its solubility. Therefore, this study aims to evaluate the pharmaceutical properties of amorphous drug loaded-mesoporous silica (MPS) and pure amorphous drugs. Ritonavir (RTV) was used as a model of a poorly water-soluble drug due to its low recrystallization tendency. RTV loaded-MPS (RTV/MPS) and RTV amorphous were prepared using the solvent evaporation method. Based on observation, a halo pattern in the powder X-ray diffraction pattern and a single glass transition (Tg) in the modulated differential scanning calorimetry (MDSC) curve was discovered in RTV amorphous, indicating its amorphization. The Tg was not detected in RTV/MPS, which showed that the loading RTV was completed. The solid-state NMR and FT-IR spectroscopy also showed the interaction between RTV and the surface of MPS in the mesopores. The high supersaturation of RTV was not achieved for both RTV/MPS and the amorphous state due to its strong interaction with the surface of MPS and was not properly dispersed in the medium, respectively. In the dissolution test, the molecular dispersion of RTV within MPS caused rapid dissolution at the beginning, while the amorphous showed a low rate due to its agglomeration. The stability examination showed that the loading process significantly improved the physical and chemical stability of RTV amorphous. These results indicated that the pharmaceutical properties of amorphous drugs could be improved by loaded-MPS.

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Section: Introductionmentioning

confidence: 99%

A Comparative Study of the Pharmaceutical Properties between Amorphous Drugs Loaded-Mesoporous Silica and Pure Amorphous Drugs Prepared by Solvent Evaporation

Budiman

Aulifa

2022

Pharmaceuticals

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“…[1][2][3][4] An amorphous drug is formed by dispersing on the surface of silica, which is the wall of the pores. In the pores, a spatial constraint confers good physical stability on a confined drug 5) ; however, the interaction with a silica surface can make the drug chemically unstable. 6,7) By contrast, a crystalline drug in the pores has been recognized, and is called nanocrystalline.…”

Section: Introductionmentioning

confidence: 99%

Low-Field NMR to Characterize the Crystalline State of Ibuprofen Confined in Ordered or Nonordered Mesoporous Silica

Okada

Hayashi

Tsuji

et al. 2022

CHEMICAL & PHARMACEUTICAL BULLETIN

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The crystalline state of ibuprofen (IBU) confined in mesoporous silica was characterized using low-field time-domain nuclear magnetic resonance (TD-NMR). IBU was loaded into ordered (Santa Barbara Amorphous-15 [SBA-15]; SBA) or nonordered mesoporous silica (Sylysia 320; SYL) using a well-known incipient wetness impregnation method. The dissolution profile of IBU from the silica was measured. The IBU-loaded SBA showed a relatively higher drug concentration at 10 and 20 min, which was typical of a supersaturated solution. However, it did not maintain that concentration. By contrast, the IBU-loaded SYL did not show such a dissolution profile in the early stage. To characterize the crystalline state of IBU confined in silica, the T 1 relaxation time of IBU-loaded silica powder was measured and analyzed by curve fitting. Monophasic T 1 relaxation was observed for IBU-loaded SBA. This may indicate that the amorphous phase, which has various molecular mobilities, was close to within the length of 1 H spin diffusion. The TD-NMR technique, even if the sample is powder, can rapidly and easily measure NMR relaxation. Therefore, it can be useful toward fully characterizing the crystalline state of drugs confined in mesopores.

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“…Furthermore, drugs must be temporarily mobilized by either the solvent-free (melt method) or solvent-based methods (incipient wetness impregnation, solvent evaporation method) to ensure encapsulation ( Le et al., 2019 ; Riikonen et al., 2018 ). Moreover, several factors influence drug loading including pore size and volume, surface area and surface functionality of MS, loading method, surface interaction, and drug molecule size ( Ambrogi et al., 2007 ; Le et al., 2019 ; Vraníková et al., 2020 ).…”

Section: Introductionmentioning

confidence: 99%

Encapsulation of drug into mesoporous silica by solvent evaporation: A comparative study of drug characterization in mesoporous silica with various molecular weights

Budiman

Aulifa

2021

Heliyon

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Mesoporous silica (MS) is a promising material as a drug carrier that is used in pharmaceutical applications. It was discovered that the incorporation of drugs into MS has the potential to improve their dissolution and bioavailability due to the large specific surface area. This study aimed to characterize the drugs with various molecular weights in MS as well as to elucidate their impact on the loading amount and the amorphization within MS. The solvent evaporation method was used to encapsulate itraconazole (ITZ), nifedipine (NIF), and nicotinamide (NIC), respectively, into MS. The result shows the absence of glass transition and the melting peak of ITZ, NIF, and SAC within MS signifying the successful encapsulation. A hallo pattern was found in ITZ and NIF within MS indicating the amorphization. The high molecular weight and the interaction between the drug with the silica surface is reportedly contributed to the formation of the amorphous state. Meanwhile, the characteristic diffraction peaks of NIC crystal were observed for NIC within MS. In conclusion, the molecular weight of the drug has a significant effect on the loading amount and the amorphization of the drug within MS.

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Relevance of the theoretical critical pore radius in mesoporous silica for fast crystallizing drugs

Cited by 19 publications

References 63 publications

A Comparative Study of the Pharmaceutical Properties between Amorphous Drugs Loaded-Mesoporous Silica and Pure Amorphous Drugs Prepared by Solvent Evaporation

A Comparative Study of the Pharmaceutical Properties between Amorphous Drugs Loaded-Mesoporous Silica and Pure Amorphous Drugs Prepared by Solvent Evaporation

Low-Field NMR to Characterize the Crystalline State of Ibuprofen Confined in Ordered or Nonordered Mesoporous Silica

Encapsulation of drug into mesoporous silica by solvent evaporation: A comparative study of drug characterization in mesoporous silica with various molecular weights

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