Evaluation of Different Thermoanalytical Methods for the Analysis of the Stability of Naproxen-Loaded Amorphous Solid Dispersions

Szabó, Edina; Haraszti, Anna; Záhonyi, Petra; Vadas, Dániel; Csontos, István; Nagy, Zsombor Kristóf; Mooter, Guy Van den; Marosi, György

doi:10.3390/pharmaceutics14112508

Cited by 3 publications

(4 citation statements)

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“…5). The measured T g of the amorphous SPIR was closer to the T g of the PVPVA64 than in the case of the NAP [28], which explains that the T g of SPIR-loaded ASDs also varies within a narrower range. The determined T g values of the pure component were similar to other publications (despite the different parameters of the amorphization or the MDSC measurement) [12,37].…”

Section: Comparison Of T G Changes Of the 'Strongly Interacting' And ...mentioning

confidence: 61%

“…In one of our previous studies, the T g of the NAP-loaded samples containing 10, 20, 30, 40, and 50% API was already investigated with both MDSC and TSDC (Fig. 3, Table 1) [28]. According to those MDSC results, a slight increase in the T g was observed from 20% drug loading compared to the T g calculated by the Gordon-Taylor equation (Eq.…”

Section: Comparison Of T G Changes Of the 'Strongly Interacting' And ...mentioning

confidence: 83%

“…0.5 mm were prepared. During the experiments, the same measuring method and process parameters (annealing temperature, T a = 20 °C, annealing time, t a = 1 min, polarization temperatures, T p = approximately 10-20 °C higher than the T g of the given sample determined by DSC, polarization time, t p = 5 min, field strength, E = 300 V mm −1 , temperature range between 0 (T 0 ) and 150 °C (T f ) cooling rate, r c = 10 °C min −1 , and heating rate, r h = 5 °C min −1 ) were used, which were described in details in one of our previous studies [28].…”

Section: Thermally Stimulated Depolarization Current (Tsdc)mentioning

confidence: 99%

“…The most widely used technique for measuring the T g is the differential scanning calorimetry (DSC) or its upgraded version, the modulated DSC (mDSC) [25,26]. However, there are many other methods for the determination of T g , such as dielectric relaxation spectroscopy (DRS), thermally stimulated depolarization current (TSDC), micro thermal analysis, and dynamic mechanical analysis (DMA) [27][28][29][30]. These techniques are applicable for determining sub-T g transitions as well.…”

Section: Introductionmentioning

confidence: 99%

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Thermal investigation of relaxations of interacting and non-interacting amorphous solid dispersions

Péter-Haraszti,

Záhonyi,

Farkas

et al. 2024

J Therm Anal Calorim

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In the present research, thermal investigation of amorphous solid dispersions (ASDs) was performed in order to compare their relaxation transitions. Two different active pharmaceutical ingredients (APIs), namely naproxen (NAP) and spironolactone (SPIR), were used as model drugs and combined with polyvinylpyrrolidone vinyl acetate (PVPVA64) copolymer to form stable ASDs. The reason for the API selection was their different interacting potentials based on the presence (in the case of NAP) and the lack of H-bond donor group (in the case of SPIR). Determination of both Tg and sub-Tg transitions suggested that ASDs containing NAP and PVPVA64 are ‘interacting’ systems with respect to the H-bonding. Besides, temperature-dependent Raman spectroscopic experiments confirmed that the naphthalene ring of the NAP has a significant role in the sub-Tg relaxations. In contrast, SPIR-PVPVA64 systems proved to be ‘non-interacting’ ASDs according to the MDSC, TSDC, and Raman measurements. This study highlights that the combination of the results of different thermoanalytical investigations with spectroscopic methods helps to understand the molecular background of the relaxations in ASDs and thus contributes to the conscious design of stable amorphous pharmaceuticals in the early stage of development.

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Section: Comparison Of T G Changes Of the 'Strongly Interacting' And ...mentioning

confidence: 61%

Section: Comparison Of T G Changes Of the 'Strongly Interacting' And ...mentioning

confidence: 83%

Section: Thermally Stimulated Depolarization Current (Tsdc)mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Thermal investigation of relaxations of interacting and non-interacting amorphous solid dispersions

Péter-Haraszti,

Záhonyi,

Farkas

et al. 2024

J Therm Anal Calorim

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Role of Crystal Disorder and Mechanoactivation in Solid-State Stability of Pharmaceuticals

Iyer¹,

Brunsteiner²,

Modhave³

et al. 2023

Journal of Pharmaceutical Sciences

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Navigating the Solution to Drug Formulation Problems at Research and Development Stages by Amorphous Solid Dispersion Technology

Tripathi,

B.H,

Sahoo

et al. 2024

RADDF

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Amorphous Solid Dispersions (ASDs) have indeed revolutionized the pharmaceutical industry, particularly in drug solubility enhancement. The amorphous state of a drug, which is a highenergy metastable state, can lead to an increase in the apparent solubility of the drug. This is due to the absence of a long-range molecular order, which results in higher molecular mobility and free volume, and consequently, higher solubility. The success of ASD preparation depends on the selection of appropriate excipients, particularly polymers that play a crucial role in drug solubility and physical stability. However, ASDs face challenges due to their thermodynamic instability or tendency to recrystallize. Measuring the crystallinity of the active pharmaceutical ingredient (API) and drug solubility is a complex process that requires a thorough understanding of drug-polymer miscibility and molecular interactions. Therefore, it is important to monitor drug solids closely during preparation, storage, and application. Techniques such as solid-state nuclear magnetic resonance (ssNMR), attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR), Raman spectroscopy, and dielectric spectroscopy have been successful in understanding the mechanism of drug crystallization. In addition, the continuous downstream processing of drug-loaded ASDs has introduced new automated methods for consistent ASD production. Advanced techniques such as hot melt extrusion, KinetiSol, electro spraying, and electrospinning have gained popularity. This review provides a comprehensive overview of Amorphous Solid Dispersions (ASDs) for oral drug delivery. It highlights the critical challenges faced during formulation, the impact of manufacturing variables, theoretical aspects of drug-polymer interaction, and factors related to drug-polymer miscibility. ASDs have been recognized as a promising strategy to improve the oral bioavailability of poorly water-soluble drugs. However, the successful development of an ASD-based drug product is not straightforward due to the complexity of the ASD systems. The formulation and process parameters can significantly influence the performance of the final product. Understanding the interactions between the drug and polymer in ASDs is crucial for predicting their stability and performance.

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Evaluation of Different Thermoanalytical Methods for the Analysis of the Stability of Naproxen-Loaded Amorphous Solid Dispersions

Cited by 3 publications

References 58 publications

Thermal investigation of relaxations of interacting and non-interacting amorphous solid dispersions

Thermal investigation of relaxations of interacting and non-interacting amorphous solid dispersions

Role of Crystal Disorder and Mechanoactivation in Solid-State Stability of Pharmaceuticals

Navigating the Solution to Drug Formulation Problems at Research and Development Stages by Amorphous Solid Dispersion Technology

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