RESUMEN
Metformin, the primary therapy for type 2 diabetes mellitus (T2DM), showed limitations such as varying absorption, rapid system clearance, required large amount, resistance, longstanding side effects. Use of Nano formulations for pharmaceuticals is emerging as a viable technique to reduce negative consequences of drug, while simultaneously attaining precise release and targeted distribution. This study developed a Polyethylene Glycol conjugated Graphene Oxide Quantum dots (GOQD-PEG) nanocomposite for the sustained release of metformin. Herein, we evaluated the effectiveness of metformin-loaded nanoconjugate in in vitro insulin resistance model. Results demonstrated drug loaded nanoconjugate successfully restored glucose uptake and reversed insulin resistance in in vitro conditions at reduced dosage compared to free metformin.
Asunto(s)
Preparaciones de Acción Retardada , Grafito , Resistencia a la Insulina , Metformina , Nanoconjugados , Polietilenglicoles , Puntos Cuánticos , Grafito/química , Puntos Cuánticos/química , Metformina/administración & dosificación , Metformina/farmacología , Metformina/farmacocinética , Metformina/química , Polietilenglicoles/química , Nanoconjugados/química , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Humanos , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Sistemas de Liberación de Medicamentos , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Glucosa/metabolismo , Glucosa/químicaRESUMEN
The goal of the study was to look into drug-polyelectrolyte complexation between ciprofloxacin (Cipro) and λ-carrageenan (CRG), and to employ the complex as a sustained-release matrix. The maximum binding capacity of the complexation was determined using the dialysis bag method and employed to prepare the complex. In comparison to Cipro, CRG, and their physical mixing, the complex was examined using differential scanning calorimetry, Fourier infrared spectroscopy, powder X-ray diffraction, and scanning electron microscopy. Cipro-CRG matrices, manufactured as direct compression tablets based on the greatest binding capacity, were assessed for swelling, erosion and drug release in 0.1 M HCl, in comparison with those of CRG, Hydroxypropyl methylcellulose (HPMC) and Cipro-HPMC matrices. In vivo absorption study comparing the Cipro-CRG matrix to Cipro immediate-release tablet was also carried out. The greatest binding capacity of Cipro to CRG was 55% (w/w). Multiple interactions, including electrostatic interaction, Vander wall forces, and hydrogen bonding, have been proposed to be involved in complexation with drug amorphization. As a result of the complexation, the swelling and erosion properties of CRG changed, with Cipro-CRG matrix showing substantially less swelling and erosion than Cipro-free CRG matrix. Cipro-CRG matrix exhibited swelling and erosion similar to Cipro-HPMC matrix. However, the former matrix demonstrated Cipro release with significantly less burst impact and a significantly slower release rate. Furthermore, Cipro-CRG matrices in vivo demonstrated slow-prolonged oral drug absorption with consequent significant changes in pharmacokinetic parameters in comparison to those obtained for immediate-release tablets.