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1.
Curr Drug Metab ; 22(4): 280-286, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32964821

RESUMEN

BACKGROUND: Human immunodeficiency virus (HIV)/AIDS is one of the principal concerns contributing to the global burden and the accompanying deleterious outcomes could not be left unattended. Despite significant advances and innovative research being conducted throughout the globe in order to improve the therapeutic profile of conventionally available antiretroviral (ARV) drugs in the eradication of HIV virus reservoirs, its penetration across the blood-brain barrier (BBB) is still a formidable mission. This makes the central nervous system a dominant and vulnerable site for virus propagation, which ultimately affects the therapeutic potential of the drug administered. Therefore there is an upsurge in the prerequisite of novel technologies to come into play, paving the way for nanotechnology. METHODS: This review primarily provides a comprehensive outline and emphasizes on the nanotechnological techniques employed for the delivery of ARV drugs and their stupendous advantages in overcoming the hurdles associated with the same. RESULTS: The nanotechnological approach bears the potential of site-specific delivery across the BBB via targeting explicit transport processes and provides a sustained release mechanism. Furthermore, different routes of administration explored have also yielded beneficial outcomes for the delivery of ARV drugs. CONCLUSION: The futuristic holistic nanotechnology methods, however, should focus on increasing drug trafficking and permeability across the BBB to ameliorate the therapeutic effect of ARV drugs. Additionally, the domain warrants clinical studies to be undertaken to make the technology commercially viable and a success to deal with the problems of the treatment strategy.


Asunto(s)
Síndrome de Inmunodeficiencia Adquirida/tratamiento farmacológico , Fármacos Anti-VIH/administración & dosificación , Barrera Hematoencefálica/efectos de los fármacos , Enfermedades Virales del Sistema Nervioso Central/tratamiento farmacológico , Sistema de Administración de Fármacos con Nanopartículas/farmacología , Síndrome de Inmunodeficiencia Adquirida/complicaciones , Síndrome de Inmunodeficiencia Adquirida/inmunología , Síndrome de Inmunodeficiencia Adquirida/virología , Fármacos Anti-VIH/farmacocinética , Barrera Hematoencefálica/metabolismo , Enfermedades Virales del Sistema Nervioso Central/inmunología , Enfermedades Virales del Sistema Nervioso Central/virología , VIH-1/efectos de los fármacos , VIH-1/inmunología , Humanos , Sistema de Administración de Fármacos con Nanopartículas/química , Nanomedicina Teranóstica/métodos , Nanomedicina Teranóstica/tendencias , Distribución Tisular , Resultado del Tratamiento
2.
Int J Biol Macromol ; 167: 605-619, 2021 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-33278450

RESUMEN

The research presented aims at developing Ropinirole hydrochloride (RHCl) nanoemulsion (NE) with nigella oil for Parkinson's disease (PD). In silico study was done to explore interactions of ropinirole and thymoquinone at receptor site (TNF-α and NFK-ß). Ropinirole and Thymoquinone forms a hydrogen bond with residue Arginine 201 and residue Arginine 253 with a bond length of 1.89 Å and 2.30 Å at the NF-κß receptor. NE was optimized using Central Composite Rotatable Design (CCRD). The globule size of chitosan coated NE, Polydispersity index (PDI) and zeta potential were 183.7 ± 5.2 nm, 0.263 ± 0.005, and 24.9 mV respectively. NE exhibited 85.28% transmittance showing the formulation was clear and transparent. TEM showed that NE had spherical globules with no aggregation. The formulation had a stable pH value of 5.8 ± 0.18. In vitro release and permeation studies exhibited 2 folds and 3.4 folds enhancement when compared with the drug suspension. Neurobehavioral activity and biochemical parameters corroborated well with the pharmacokinetic results. Histopathological study and immunohistochemical analysis were performed to get better picture of 6-OHDA induced toxicity and reversal of PD symptoms. Thus, the NE tailored is a promising synergistic approach yielding enticing outcomes for better management of PD related symptoms.


Asunto(s)
Quitosano/química , Indoles/administración & dosificación , FN-kappa B/metabolismo , Nigella/química , Enfermedad de Parkinson/metabolismo , Aceites de Plantas/administración & dosificación , Factor de Necrosis Tumoral alfa/metabolismo , Animales , Benzoquinonas/farmacología , Modelos Animales de Enfermedad , Estabilidad de Medicamentos , Sinergismo Farmacológico , Emulsiones , Femenino , Humanos , Indoles/química , Indoles/farmacocinética , Masculino , Simulación del Acoplamiento Molecular , FN-kappa B/química , Nanopartículas , Oxidopamina/efectos adversos , Enfermedad de Parkinson/tratamiento farmacológico , Enfermedad de Parkinson/etiología , Aceites de Plantas/química , Aceites de Plantas/farmacocinética , Ratas , Factor de Necrosis Tumoral alfa/química
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