Current Issue : April-June Volume : 2022 Issue Number : 2 Articles : 5 Articles
In this work, dasatinib (DAS) nanoemulsion and nanocrystal are produced by high-gravity technology that approaches to practical mass production. The drug nanoformulations were systematically characterized and evaluated. At a low high-gravity level ( ) = 47, nanoemulsion droplets were 16.15 0.42 nm with a PDI of 0.122 0.021. The nanoemulsion’s size and active pharmaceutical ingredient (API) content remained stable at long-term (4 months) freeze–thaw and dilution experiments. At a high = 188, the as-prepared nanocrystal was lamellar with a short diameter of about 200 nm and a long diameter of about 750 nm. In vitro performances demonstrated the nanoemulsion displayed higher cytotoxicity on MDA-MB-231 tumor cells, Caco-2 cell permeability and drug release than that of the nanocrystal, indicating that nanoemulsion should be an ideal alternative for dasatinib oral administration....
This study aimed at engineering cytocompatible and injectable antibiotic-laden fibrous microparticles gelatin methacryloyl (GelMA) hydrogels for endodontic infection ablation. Clindamycin (CLIN) or metronidazole (MET) was added to a polymer solution and electrospun into fibrous mats, which were processed via cryomilling to obtain CLIN- or MET-laden fibrous microparticles. Then, GelMA was modified with CLIN- or MET-laden microparticles or by using equal amounts of each set of fibrous microparticles. Morphological characterization of electrospun fibers and cryomilled particles was performed via scanning electron microscopy (SEM). The experimental hydrogels were further examined for swelling, degradation, and toxicity to dental stem cells, as well as antimicrobial action against endodontic pathogens (agar diffusion) and biofilm inhibition, evaluated both quantitatively (CFU/mL) and qualitatively via confocal laser scanning microscopy (CLSM) and SEM. Data were analyzed using ANOVA and Tukey’s test ( = 0.05). The modification of GelMA with antibiotic-laden fibrous microparticles increased the hydrogel swelling ratio and degradation rate. Cell viability was slightly reduced, although without any significant toxicity (cell viability > 50%). All hydrogels containing antibiotic-laden fibrous microparticles displayed antibiofilm effects, with the dentin substrate showing nearly complete elimination of viable bacteria. Altogether, our findings suggest that the engineered injectable antibiotic-laden fibrous microparticles hydrogels hold clinical prospects for endodontic infection ablation....
Annona muricata (Annonaceae) is a tropical plant widely known for its edible fruits. Recent scientific studies have confirmed the folkloric use of its seeds as an antidiarrheal agent. This study sought to formulate capsules and suspensions using the ethanolic extract from Annona muricata seeds. The dried ethanolic extract was formulated into granules and subsequently encapsulated. The suspension formulated was assessed for sedimentation rate, sedimentation volume, viscosity, dissolution, drug content, and flow rate, while pharmacopeia tests such as disintegration, dissolution, uniformity of weight, and drug content were carried out on the formulated capsules. The formulated suspension passed the drug content and in vitro release studies. Annona muricata suspension exhibited pseudoplastic flow with good sedimentation rate and sedimentation volume.Theformulated capsules passed the in vitro dissolution studies, weight uniformity, disintegration, and drug content tests. The ethanolic extract of Annona muricata seeds was appropriately formulated into standardized solid and liquid oral dosage forms....
The main aim of this work is the biopharmaceutical characterization of a new hybrid benzodiazepine-dihydropyridine derivative, JM-20, derived with potent anti-ischemic and neuroprotective effects. In this study, the pKa and the pH-solubility profile were experimentally determined. Additionally, effective intestinal permeability was measured using three in vitro epithelial cell lines (MDCK, MDCK-MDR1 and Caco-2) and an in situ closed-loop intestinal perfusion technique. The results indicate that JM-20 is more soluble at acidic pH (9.18 0.16); however, the Dose number (Do) was greater than 1, suggesting that it is a low-solubility compound. The permeability values obtained with in vitro cell lines as well as with the in situ perfusion method show that JM-20 is a highly permeable compound (Caco-2 value 3.8 105). The presence of an absorption carrier-mediated transport mechanism was also demonstrated, as well as the efflux effect of P-glycoprotein on the permeability values. Finally, JM-20 was provisionally classified as class 2 according to the biopharmaceutical classification system (BCS) due to its high intestinal permeability and low solubility. The potential good oral absorption of this compound could be limited by its solubility....
In this work, the capacity of the mucilage extracted from the cladodes of Opuntia ficusindica (OFI) and aloe vera (AV) leaves as wall material in the microencapsulation of pink guava carotenoids using spray-drying was studied. The stability of the encapsulated carotenoids was quantified using UV–vis and HPLC/MS techniques. Likewise, the antioxidant activity (TEAC), color (CIELab), structural (FTIR) and microstructural (SEM and particle size) properties, as well as the total dietary content, of both types of mucilage microcapsules were determined. Our results show that the use of AV mucilage, compared to OFI mucilage, increased both the retention of _-carotene and the antioxidant capacity of the carotenoid microcapsules by around 14%, as well as the total carotenoid content (TCC) by around 26%, and also favors the formation of spherical-type particles (Ø _= 26 _m) without the apparent damage of a more uniform size and with an attractive red-yellow hue. This type of microcapsules is proposed as a convenient alternative means to incorporate guava carotenoids, a natural colorant with a high antioxidant capacity, and dietary fiber content in the manufacture of functional products, which is a topic of interest for the food, pharmaceutical, and cosmetic industries....
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