Dissolution and permeation characteristics of artemether tablets formulated with two gums of different surface activity

Purpose: To evaluate the dissolution and permeation characteristics of artemether tablets formulated with cashew and prosopis gums, and compare with tablets prepared with acacia gum.Methods: Artemether tablets containing varying concentrations (1.0 to 4.0 %w/w) of cashew and prosopis gums or 3 %w/w of acacia (control) gum as binders were formulated by wet granulation method. The tablets were evaluated for crushing strength, friability and disintegration time. Dissolution and permeation characteristics of the formulations were studied using USP methods.Results: Tablets formulated with prosopis gum had higher crushing strength, higher friability and higher disintegration time compared to those of cashew gum at corresponding binder concentrations. Tablets formulated with 3 %w/w cashew gum exhibited complete drug release within 1 h, 95 % drug permeation in 188 min (in simulated gastric fluid [SGF]) and 95 % permeation in 224 min (under simulated intestinal fluid [SIF] condition) while those made with 3 %w/w prosopis gum exhibited 70.7 % drug release in 1 h, 95 % permeation in 135 min (in SGF) and 95 % permeation in 170 min (under SIF condition).Conclusion: Cashew gum is effective as a binder over a relatively wide range of concentrations to achieve fast drug release though with minimal permeation enhancement while prosopis gum is characterized by delayed drug release but enhanced permeation of the released drug.Keywords: Cashew gum, Acacia, Prosopis, Artemether, Drug release, Dissolution, Permeatio

Antimicrobial Peptide Design, Molecular Docking and ADMET Studies Against the Methicillin-Resistant Staphylococcus aureus and Carbapenem-resistant and Carbapenemase-producing Pseudomonas aeruginosa: Prediction of novel anti-MRSA and anti-CRPA AMPs

Carbapenem-resistant and carbapenemase-producing Pseudomonas aeruginosa (CRPA) and methicillin-resistant Staphylococcus aureus (MRSA) are two pathogens that are resistant to currently available antimicrobials. As an alternative to effective medication molecules, antimicrobial peptides (AMPs) have the potential to cure superbug-caused infections effectively. Two new AMPs (ama1 and ama2) were designed utilizing a knowledge-based technique with optimal parameters. First, the PEP-FOLD 3.5 server made a de novo prediction of the AMPs' three-dimensional (3D) structure, which was validated using PROCHECK of SAVES v6.0 by checking the amino acid locations in the Ramachandra plot. Then, protein-peptide docking simulations of the predicted AMPs and reference AMP (Aurein 1.2) for positive control were performed using the HPEPDOCK docking web server, followed by the computation of the AMPs' physicochemical parameters and toxicity profile using the ProtParam and vNN-ADMET web servers, respectively. The sequences for ama1 and ama2 were AWGKIKALR and IKWLRLAKP, respectively. Docking analysis revealed that the antibacterial activity of ama1 and ama2 was superior to that of Aurein 1.2 against CRPA-resistant enzyme (6ew3), respectively. However, ama1, ama2, and Aurein 1.2 inhibited the activity of MRSA-resistant protein (4c12). Both the physicochemical qualities and the toxicity profiles were advantageous. Therefore, the in-silico-derived AMPs could serve as a pharmaceutical candidate for developing multidrug-resistant bacteria-effective antimicrobials. HIGHLIGHTS Two cationic antimicrobial peptides (AMPs) were designed. Molecular docking of the AMPs revealed better antimicrobial activity than the reference. The novel AMPs had net positive charge and optimal hydrophobic amino acids