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1.
Int J Pharm ; 646: 123443, 2023 Nov 05.
Artículo en Inglés | MEDLINE | ID: mdl-37748633

RESUMEN

The expression of inflammatory markers and vascular endothelial growth factor (VEGF) was found to be upregulated in various posterior ocular disorders, including diabetic retinopathy (DR). Effective delivery of therapeutic agents to the retina poses a significant challenge in ophthalmic drug delivery due to biological ocular barriers. Triamcinolone acetonide (TA) was selected as the model corticosteroid drug targeting cytokines and VEGF in DR. However, despite TA's low molecular weight and hydrophobicity, which enable it to bypass the conjunctival epithelial barrier, it doesn't efficiently exert its effect at the target site. Nanocarriers have emerged as a solution to enhance drug delivery to the retina and improve bioavailability. This study aimed to compare the effects of Triamcinolone-loaded cubic liquid crystalline nanoparticles (TA-cubic LCNPs) and TA-Suspension in an experimental DR model administered via the subconjunctival (SCJ) route. The results demonstrated that TA-cubic LCNPs enhanced TA periocular delivery efficacy by reducing inflammatory and VEGF markers through the advanced glycation end products (AGE)/protein kinase C pathway. They were identified as promising nano-carriers, exhibiting potential for targeted delivery to the retina.

2.
Drug Discov Today ; 27(11): 103357, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36115632

RESUMEN

Multiple sclerosis (MS) is an autoimmune neuroinflammatory disorder attributed to neurodegeneration and demyelination, resulting in neurological impairment. miRNA has a significant role in biological processes in MS. In this review, we focus on the feasibility of delivering miRNAs through nanoformulations for managing MS. We provide a brief discussion of miRNA synthesis and evidence for miRNA dysregulation in MS. We also highlight formulation strategies and resulting technologies for the effective delivery of miRNAs through nanocarrier systems for achieving high therapeutic benefits.

3.
Daru ; 19(4): 249-56, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-22615665

RESUMEN

BACKGROUND AND THE PURPOSE OF THE STUDY: Olanzapine is an antipsychotic used in treatment of schizophrenia. This research was carried out to design oral controlled release matrix pellets of water insoluble drug Olanzapine (OZ), using blend of Sodium Alginate (SA) and Glyceryl Palmito-Stearate (GPS) as matrix polymers, micro crystalline cellulose (MCC) as spheronizer enhancer and Sodium Lauryl Sulphate (SLS) as pore forming agent. METHODS: OZ formulations were developed by the pelletization technique by drug loaded pellets and characterized with regard to the drug content, size distribution, Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and X-ray Diffraction study (XRD). Stability studies were carried out on the optimized formulation for a period of 90 days at 40±2 °C and 75±5% relative humidity. RESULTS AND MAJOR CONCLUSION: The drug content was in the range of 93.34-98.12%. The mean particle size of the drug loaded pellets was in the range 1024 to 1087µm. SEM photographs and calculated sphericity factor confirmed that the prepared formulations were spherical in nature. The compatibility between drug and polymers in the drug loaded pellets was confirmed by DSC and FTIR studies. Stability studies indicated that pellets are stable. XRD patterns revealed the crystalline nature of the pure OZ. Loose surface crystal study indicated that crystalline OZ is present in all formulations and more clear in formulation F5. Drug release was controlled for more than 24 hrs and mechanism of the drug release followed by Fickian diffusion. It may be concluded that F5 is an ideal formulation for once a day administration.

4.
Daru ; 18(3): 200-10, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-22615618

RESUMEN

BACKGROUND AND THE PURPOSE OF THE STUDY: Many drugs which have narrow therapeutic window and are absorbed mainly in stomach have been developed as gastroretentive delivery system. Rosiglitazone maleate, an anti-diabetic, is highly unstable at basic pH and is extensively absorbed from the stomach. Hence there is a need to develop a gastroretentive system. In this study a superporous hydrogel was developed as a gastroretentive drug delivery system. METHODS: Chitosan/poly(vinyl alcohol) interpenetrating polymer network type superporous hydrogels were prepared using a gas foaming method employing glyoxal as the crosslinking agent for Rosiglitazone maleate. Sodium bicarbonate was applied as a foaming agent to introduce the porous structure. Swelling behaviors of superporous hydrogel in acidic solution were studied to investigate their applications for gastric retention device. The optimum preparation condition of superporous hydrogels was obtained from the gelation kinetics. FT-IR, scanning electron microscopy, porosity and swelling ratio studies were used to characterize these polymers. In vitro drug release studies were also carried out. RESULTS: The introduction of a small amount of Poly(Vinyl Alcohol) enhanced the mechanical strength but slightly reduced the swelling ratio. The prepared superporous hydrogels were highly sensitive to pH of swelling media, and showed reversible swelling and de-swelling behaviors maintaining their mechanical stability. The degradation kinetics in simulated gastric fluid showed that it had biodegradability. Swelling was dependent on the amount of chitosan and crosslinker. The drug release from superporous hydrogels was sustained for 6 hrs. MAJOR CONCLUSION: The studies showed that chitosan-based superporous hydrogels could be used as a gastroretentive drug delivery system for rosiglitazone maleate in view of their swelling and prolonged drug release characteristics in acidic pH.

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