Amorphous solid dispersion (ASD) has emerged to be an outstanding strategy among multiple options available for improving solubility and consequently biological activity. Interestingly several binary SD systems continue to exhibit insufficient solubility over time. Therefore, the goal of current research was to design ternary amorphous solid dispersions (ASDs) of hydrophobic model drug curcumin (CUR) to enhance the solubility and dissolution rate in turn, presenting enhanced anti-bacterial, antioxidant and anti-inflammatory activity. For this purpose several ternary solid dispersions (TSDs) consisting of Soluplus®, Syloid® XDP 3150, Syloid® 244 and Poloxamer® 188 in combination with HPMC E5 (binary carrier) were prepared using solvent evaporation method. Both solubility and dissolution testing of prepared solid dispersion were performed to determine the increase in solubility and dissolution. Solid state investigation was carried out utilizing infrared spectroscopy, also known as Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM),Differential scanning calorimetry (DSC) and X-ray diffraction (XRD).Optimized formulations were also tested for their biological effectiveness including anti-bacterial, anti-oxidant and anti-inflammatory activity. Amid all Ternary formulations F3 entailing 20 % soluplus® remarkably improved the solubility (186 μg/ml ± 3.95) and consequently dissolution (91 % ± 3.89 %) of curcumin by 3100 and 9 fold respectively. These finding were also supported by FTIR, SEM, XRD and DSC. In-vitro antibacterial investigation of F3 also demonstrated significant improvement in antibacterial activity against both gram positive ( and gram negative (, bacteria. Among all the tested strains was found to be most susceptible with a zone of inhibition of 24 mm ± 2.87. Antioxidant activity of F3 was also notably enhanced (93 % ± 5.30) in contrast to CUR (69 % ± 4.79). In vitro anti-inflammatory assessment also exhibited that F3 markedly protected BSA (bovine serum albumin) from denaturation with percent BSA inhibition of 80 % ± 3.16 in comparison to CUR (49 % ± 2.91). Hence, F3 could be an effective solid dispersion system for the delivery of model hydrophobic drug curcumin.
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http://dx.doi.org/10.1016/j.heliyon.2024.e34636 | DOI Listing |
J Hazard Mater
December 2024
School of Environmental Science and Engineering, Shanghai Jiao Tong University, Shanghai 200240, PR China; Shanghai Institute of Pollution Control and Ecological Security, Shanghai 200092, PR China. Electronic address:
Wet-crushing with aqueous media protection is considered safer and more efficient than common inert-gas protected dry-crushing in preprocessing spent lithium-ion batteries (LIBs). However, it is also accompanied with the releasement and transformation of hazardous electrolyte, while the mechanisms and pollution impact yet remain unknown. Based on a self-built wet-crushing system, this topic was systematically investigated here.
View Article and Find Full Text PDFInt J Pharm
January 2025
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009 PR China. Electronic address:
Micronization is frequently employed to increase the dissolution of poorly soluble drugs, but it easily led to powder aggregation and difficult to mix well on the micro level with poor content uniformity and erratic dissolution behavior. Mannitol is the most commonly used pharmaceutical excipient, and its β form (β-mannitol) is commercially available and extensively investigated, whereas form α (α-mannitol) remain poorly understood. Here, this study demonstrated that α-mannitol could significantly eliminate aggregation phenomena of micronized drugs (i.
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January 2025
Real Jardín Botánico (RJB-CSIC), C/ Moyano 1, 28014, Madrid, Spain.
ACS Omega
December 2024
Department of Pharmaceutical Technology, Gazi University, Ankara 06560, Turkey.
Lidocaine (LID), frequently used in dermal applications, is a nonpolar local anesthetic agent that is practically insoluble in water. The main aim of this study is to develop the nanosuspension formulation of LID using the design of experiments (DoE). The improved solubility and dissolution rate provided by nanosizing are expected to result in enhanced dermal bioavailability.
View Article and Find Full Text PDFFront Vet Sci
December 2024
Guangdong Key Laboratory for Veterinary Drug Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University (SCAU), Guangzhou, China.
Albendazole (ABZ), classified as a class II basic drug under the Biopharmaceutics Classification System (BCS), is widely recognized for its therapeutic efficacy in treating and preventing trichuriasis. However, despite its clinical relevance, ABZ's oral administration presents challenges due to its poor solubility and pH sensitivity, which diminish its therapeutic effectiveness. Additionally, high dosing regimens of ABZ pose risks of developmental toxicity in animal models.
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