Methods: The TQ-PLGA NPs were prepared and characterized for size, zeta potential, encapsulation efficiency, and release profile.
Results: The particle size was 147.2 nm, with 22.1 positive zeta potential and 96.8% encapsulation efficiency. The NPs released 45.6% of the encapsulated TQ within 3 h followed by characteristic sustained release over 7 days with a total of 69.7% cumulative release. TQ-PLGA NPs were taken up effectively by the cells in a time-dependent manner up to 24 h. Higher cell toxicity was determined within the first 24 h in melanoma cells due to the rapid release of TQ from the NPs and its low stability in the cell culture media.
Conclusion: TQ-PLGA NPs is a potential anticancer agent taking advantage of the sustained release and tailored size that allows accumulation in the cancer tissue by the enhanced permeability and retention effect. However, stability problems of the active ingredient were address in this study and requires further investigation.
METHODS: The paracetamol was encapsulated in beads, which were prepared mainly from alginate and chitosan through electrospray technique. The paracetamol beads were sprinkled on the instant jelly prepared from glycine, ι-carrageenan and calcium lactate gluconate. The paracetamol instant jelly characteristics, in terms of physical appearance, texture, rheology, in vitro drug release and palatability were assessed on a human volunteer.
RESULTS: The paracetamol instant jelly was easily reconstituted in 20 mL of water within 2 min to form jelly with acceptable consistency and texture. The jelly must be ingested within 30 min after reconstitution to avoid the bitter taste. The palatability assessment carried out on 12 human subjects established the similar palatability and texture of the paracetamol instant jelly dosage comparable to the commercial paracetamol suspension and was found to be even better in overcoming the aftertaste of paracetamol.
CONCLUSION: Such findings indicate that paracetamol instant jelly will compensate for the use of sweetening and flavoring agents as well as develop pediatric dosage forms with limited undesired excipients.
METHODS: MTT and trypan blue exclusion tests were conducted to determine the 50% inhibitory concentration (IC50) and cell proliferation. FITC Annexin and Guava® reagent were used to study the cell apoptosis and examine the cell cycle phases, respectively. The expression of JAK/STAT-negative regulator genes, SOCS-1, SOCS-3, and SHP-1, was investigated using reverse transcriptase- quantitative PCR (RT-qPCR).
RESULTS: TQ demonstrated a potential inhibition of HL60 cell proliferation and a significant increase in apoptotic cells in dose and time-dependent manner. TQ significantly induced cycle arrest at G0-G1 phase (P < 0.001) and enhanced the re-expression of JAK/STAT-negative regulator genes.
CONCLUSION: TQ potentially inhibited HL60 cell proliferation and significantly increased apoptosis with re-expression of JAK/STAT-negative regulator genes suggesting that TQ could be a new therapeutic candidate for leukemia therapy.
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Aim: This research aimed to optimize electrospray-operating parameters in producing alginate-RJ microbeads.
Materials and Methods: Optimization of alginate-RJ microbeads electrospray parameters was carried out using 24 factorial design with three center points (19 runs). The studied parameters were flow rate, high voltage, nozzle size, and tip-to-collector distance, whereas the responses were particle size, particle size distribution, and sphericity factor. The responses of each run were analyzed using Design-Expert software.
Results: Nozzle size is a significant parameter that influences the particle size. Flow rate is a significant parameter influencing the sphericity factor.
Conclusion: Screening of the electrospray-operating parameters paves the way in determining the significant parameters and their design space to produce consistent alginate-RJ microbeads.