Parkinson's disease (PD) is a debilitating neurodegenerative disorder characterized by motor and non-motor symptoms, with limited effective treatment options. This study proposes a novel approach utilizing intranasal delivery of carbenoxolone (CBX) via chitosan-coated solid lipid nanoparticles (CS-coated SLNs) to manage PD symptoms by enhancing CBX delivery and brain targeting. Formulated CS-coated SLNs exhibited favorable quality attributes including particle size (164 ± 0.12 nm), surface charge (18 ± 0.89 mV), high entrapment efficiency (97.98 ± 0.98 %), and sustained drug release profile. In vivo evaluations in a rotenone-induced rat model of PD involved intranasal administration of CBX suspension and CBX-loaded CS-coated SLN (equivalent to 20 mg/kg/day) over four weeks. The CBX nano-formulation group showed significant improvements in motor function, coordination, and balance, as well as modulation of neurotransmitter levels, with increased dopamine and decreased α-synuclein levels compared to the control group. Moreover, the CBX nano-formulation exhibited superior efficacy in reducing neuroinflammation, oxidative stress, and apoptosis markers. Histological examination revealed restored neuronal architecture, suggesting potential neuroprotective effects. In conclusion, mucoadhesive chitosan-coated SLNs offer a promising nasal delivery system overcoming brain drug delivery obstacles facing CBX therapy in PD, paving the way to the development of novel treatments and improved quality of life for PD patients.
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http://dx.doi.org/10.1016/j.ijpharm.2025.125197 | DOI Listing |
Int J Pharm
January 2025
Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour 22511, Egypt. Electronic address:
Parkinson's disease (PD) is a debilitating neurodegenerative disorder characterized by motor and non-motor symptoms, with limited effective treatment options. This study proposes a novel approach utilizing intranasal delivery of carbenoxolone (CBX) via chitosan-coated solid lipid nanoparticles (CS-coated SLNs) to manage PD symptoms by enhancing CBX delivery and brain targeting. Formulated CS-coated SLNs exhibited favorable quality attributes including particle size (164 ± 0.
View Article and Find Full Text PDFACS Nano
December 2024
Key Laboratory of Smart Drug Delivery, Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China.
Brain metastasis contributes substantially to the morbidity and mortality of various malignancies and is characterized by high chemoresistance. Intracellular communication between carcinoma cells and astrocytes through gap junctions, which are assembled mainly by the connexin 43 protein, has been shown to play a vital role in this process. However, effectively blocking the gap junctions between the two cell types remains extremely challenging because of insufficient drug delivery to the target site.
View Article and Find Full Text PDFAdv Sci (Weinh)
November 2024
Key Laboratory of Zoonosis, Chinese Ministry of Education, College of Basic Medical Sciences, Jilin University, Changchun, Jilin, 130021, China.
Reversing the hepatic inflammatory and immunosuppressive microenvironment caused by gut microbiota-derived lipopolysaccharides (LPS), accumulating to the liver through the gut-liver axis, is crucial for suppressing hepatocellular carcinoma (HCC) and metastasis. However, synergistically manipulating LPS-induced inflammation and gut microbiota remains a daunting task. Herein, a Trojan-horse strategy is proposed using an oral dextran-carbenoxolone (DEX-CBX) conjugate, which combines prebiotic and glycyrrhetinic acid (GA) homologs, to targeted delivery GA to HCC through the gut-liver axis for simultaneous modulation of hepatic inflammation and gut microbiota.
View Article and Find Full Text PDFJ Recept Signal Transduct Res
April 2024
Department of Pharmacology & Toxicology, College of Veterinary Science and Animal Husbandry, Orissa University of Agriculture and Technology, Bhubaneswar, India.
Preeclampsia, a gestational associated hypertension, has been reported in 6-8% of pregnant women worldwide leading to premature delivery and low birth weight of newborn due to reduced blood flow to placenta. Although several vasodilators (Methyl dopa, hydralazine, β-blockers and diuretics) are currently in use to treat preeclampsia, still there is a search for safer drugs with better efficacy. Lately, antihypertensive vasodilators from natural sources are gaining importance in treating preeclampsia.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
June 2021
Amity Institute of Biotechnology, Amity University, Uttar Pradesh, Sector-125, Noida, 201313, India. Electronic address:
Carbenoxolone (CBX) is a semi-synthetic plant derivative with pleiotropic pharmacological properties like anti-microbial and anti-inflammatory activities. Though approved for treatment of gastric ulcers, its use is limited due to adverse effects such as cytotoxicity. Bovine serum albumin (BSA) is a natural, non-toxic protein with high water-solubility and low immunogenicity, and is widely used as a nanocarrier for targeted drug delivery.
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