This research aimed to design, optimize, and evaluate berberine-laden nanostructured lipid carriers overlaid with chitosan (BER-CTS-NLCs) for efficient brain delivery via the intranasal route. The nanostructured lipid carriers containing berberine (BER-NLCs) were formulated via hot homogenization and ultrasonication strategy and optimized for the influence of a variety of causal variables, including the amount of glycerol monostearate (solid lipid), poloxamer 407 (surfactant) concentration, and oleic acid (liquid lipid) amount, on size of the particles, entrapment, and the total drug release after 24 h. The optimal BER-NLCs formulation was then coated with chitosan. Their diameter, in vitro release, surface charge, morphology, ex vivo permeability, pH, histological, and in vivo (pharmacokinetics and brain uptake) parameters were estimated. BER-CTS-NLCs had a size of 180.9 ± 4.3 nm, sustained-release properties, positive surface charge of 36.8 mV, and augmented ex-vivo permeation via nasal mucosa. The histopathological assessment revealed that the BER-CTS-NLCs system is safe for nasal delivery. Pharmacokinetic and brain accumulation experiments showed that animals treated intranasally with BER-CTS-NLCs had substantially greater drug levels in the brain. The ratios of BER brain/blood levels at 30 min, AUCbrain/AUCblood, drug transport percentage, and drug targeting efficiency for BER-CTS-NLCs (IN) were higher compared to BER solution (IN), suggesting enhanced brain targeting. The optimized nanoparticulate system is speculated to be a successful approach for boosting the effect of BER in treating CNS diseases, such as Alzheimer’s disease, through intranasal therapy.
Rs-SNEDDS is a promising drug delivery system for improving the drug solubility and antihyperlipidemic effect using natural oils as (olive oil and garlic oil).
The aim of this study was to develop a novel double-layer bi-medicated prolonged release mucoadhesive buccal film (MBF) containing lidocaine hydrochloride (LC) and diclofenac potassium (DK). The ultimate goal of the prepared system is the treatment of radiation-induced oral mucositis pain with improved patient acceptance. MBFs were prepared using 3 × 2 randomized full factorial design for film optimization. Nanoemulsion system (NES) was used to mask DK bitter taste. The prepared films were characterized, viz thickness, mass uniformity, surface pH, folding endurance, swelling studies, ex vivo bioadhesive strength, in vitro drug release, and ex vivo permeation. The in vivo evaluation was carried out by testing the anti-inflammatory and analgesic activities on rats followed by a clinical study on patients to prove their acceptance. The optimized MBF composed of 10% w/w HPMC-4KM, 50 mg LC, and 50 mg DK-NES was selected due to prolonged in vitro drug release pattern and ex vivo permeability (95.24 ± 2.14 and 93.48 ± 3.24% in 6 h, respectively). MBF exposed a strong anti-inflammatory effect from 61 to 87% inhibition with a strong analgesic effect when compared to DK® and LC®, respectively. The clinical study revealed that films were accepted by the patients, and the presence of LC on the outer side helped in pain feeling reduction while DK-NES in the inner side facilitated in rapidly relieving the inflammation effect.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.