Iqra Khan , Rabia Arshad , Waqar Aman , Kashif Barkat , Abdul Malik , Tanveer A. Tabish , Nikhat J. Siddiqi
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引用次数: 0
Abstract
The aim of this study was to improve the therapeutic efficacy, drug delivery and physicochemical features of antimicrobial peptides (AMPs) L-Lysine, for chronic obstructive pulmonary disease (COPD) by developing a glycosylated self-nanoemulsifying drug delivery system (SNEDDS). Roflumilast (Rof) a phosphodiesterase 4 (PDE4) inhibitor, was entrapped within the SNEDDS system (Glucolysinated Rof SNEDDS) for targeted COPD treatment. The Glucolysinated Rof SNEDDS were successfully formulated and characterized in terms of physicochemical properties, in vitro as well as in vivo efficacy. Conjugation chemistry was confirmed using FTIR spectroscopy, mean droplet size of SNEDDS was 222 ± 0.46 nm, with 0.42 ± 0.11 PDI and −24.3 ± 1.20 mV zeta potential. The formulation demonstrated outstanding mucoadhesion capabilities, with a 95 % improvement in drug entrapment efficiency and 80 % sustained drug release over 12 h. Toxicity assessments were conducted by Pharmacokinetics approaches, which confirmed the formulation's safety. Strong antibacterial action was revealed against Pseudomonas aeruginosa, which disrupt bacterial membrane integrity as demonstrated with SEM imaging. PDE4 inhibition was confirmed by strong binding energy in docking analysis. Serum biochemistry analysis remained constant throughout treatment, and histopathological investigations indicated the shielding effect of excipients used. These results presented, highlight the potential of Glucolysinated Rof SNEDDS as a novel and effective drug delivery system for targeted COPD therapy, synergizing therapeutic efficacy with biocompatibility.
期刊介绍:
The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.