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1.
AAPS PharmSciTech ; 25(5): 101, 2024 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-38714629

RESUMO

BACKGROUND: Niacin, an established therapeutic for dyslipidemia, is hindered by its propensity to induce significant cutaneous flushing when administered orally in its unmodified state, thereby constraining its clinical utility. OBJECTIVE: This study aimed to fabricate, characterize, and assess the in-vitro and in-vivo effectiveness of niacin-loaded polymeric films (NLPFs) comprised of carboxymethyl tamarind seed polysaccharide. The primary objective was to mitigate the flushing-related side effects associated with oral niacin administration. METHODS: NLPFs were synthesized using the solvent casting method and subsequently subjected to characterization, including assessments of tensile strength, moisture uptake, thickness, and folding endurance. Surface characteristics were analyzed using a surface profiler and scanning electron microscopy (SEM). Potential interactions between niacin and the polysaccharide core were investigated through X-ray diffraction experiments (XRD) and Fourier transform infrared spectroscopy (FTIR). The viscoelastic properties of the films were explored using a Rheometer. In-vitro assessments included drug release studies, swelling behavior assays, and antioxidant assays. In-vivo efficacy was evaluated through skin permeation assays, skin irritation assays, and histopathological analyses. RESULTS: NLPFs exhibited a smooth texture with favorable tensile strength and moisture absorption capabilities. Niacin demonstrated interaction with the polysaccharide core, rendering the films amorphous. The films displayed slow and sustained drug release, exceptional antioxidant properties, optimal swelling behavior, and viscoelastic characteristics. Furthermore, the films exhibited biocompatibility and non-toxicity towards skin cells. CONCLUSION: NLPFs emerged as promising carrier systems for the therapeutic transdermal delivery of niacin, effectively mitigating its flushing-associated adverse effects.


Assuntos
Administração Cutânea , Liberação Controlada de Fármacos , Niacina , Polissacarídeos , Ratos Wistar , Absorção Cutânea , Pele , Animais , Ratos , Niacina/administração & dosagem , Niacina/química , Niacina/farmacologia , Polissacarídeos/química , Polissacarídeos/administração & dosagem , Polissacarídeos/farmacologia , Pele/metabolismo , Pele/efeitos dos fármacos , Absorção Cutânea/efeitos dos fármacos , Rubor/induzido quimicamente , Resistência à Tração , Masculino , Sistemas de Liberação de Medicamentos/métodos , Tamarindus/química , Polímeros/química
2.
Int J Biol Macromol ; 268(Pt 1): 131511, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38615867

RESUMO

This comprehensive review delves into the intricate landscape of glycans and glycoconjugates, unraveling their multifaceted roles across diverse biological dimensions. From influencing fundamental cellular processes such as signaling, recognition, and adhesion to exerting profound effects at the molecular and genetic levels, these complex carbohydrate structures emerge as linchpins in cellular functions and interactions. The structural diversity of glycoconjugates, which can be specifically classified into glycoproteins, glycolipids, and proteoglycans, underscores their importance in shaping the architecture of cells. Beyond their structural roles, these molecules also play key functions in facilitating cellular communication and modulating recognition mechanisms. Further, glycans and glycoconjugates prove invaluable as biomarkers in disease diagnostics, particularly in cancer, where aberrant glycosylation patterns offer critical diagnostic cues. Furthermore, the review explores their promising therapeutic applications, ranging from the development of glycan-based nanomaterials for precise drug delivery to innovative interventions in cancer treatment. This review endeavors to comprehensively explore the intricate functions of glycans and glycoconjugates, with the primary goal of offering valuable insights into their extensive implications in both health and disease. Encompassing a broad spectrum of biological processes, the focus of the review aims to provide a comprehensive understanding of the significant roles played by glycans and glycoconjugates.


Assuntos
Glicoconjugados , Polissacarídeos , Humanos , Polissacarídeos/química , Polissacarídeos/metabolismo , Glicoconjugados/química , Glicoconjugados/metabolismo , Animais , Neoplasias/metabolismo , Glicosilação , Glicoproteínas/química , Glicoproteínas/metabolismo
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